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Yonni E Apeji

Ahmadu Bello University, Nigeria, Department of Pharmaceutics and Pharmaceutical Microbiology, Faculty Member

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Dr Apeji is a lecturer/researcher at the Department of Pharmaceutics, Ahmadu Bello University, Zaria. My research interests include excipient development for direct compression, compaction studies, micro-/nanoparticulate drug delivery systems, co-processing, hot melt extrusion.
Supervisors: Prof. A. R. Oyi, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Ahmadu Bello University, Zaria, email: [email protected] , Prof. G. A. Alebiowu, Department of Pharmaceutics, Faculty of Pharmacy, Obafemi Awolowo University, Ile-Ife, Osun state, Nigeria, email: [email protected], and Prof. A. K. Bansal, Department of Pharmaceutics, National Institute for Pharmaceutical Education and Research (NIPER), Sector 67, SAS Nagar, Mohali, 160 062, India
Phone: +234(0)8052622947
Address: Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Ahmadu Bello University, Zaria, Kaduna, Nigeria

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sandesh somnache

Ahmadu Bello University, Nigeria

RAJESWARI ALETI

University of Nigeria Nsukka Enugu State Nigeria

Philomena Entsie

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Papers by Yonni E Apeji

Direct Compression Properties of Co-Processed Excipient Containing Cow Bone Powder, Khaya Gum and Maize Starch

Malaysian Journal of Pharmaceutical Sciences

The aim of this study was to evaluate the direct compression properties of a novel coprocessed ex... more The aim of this study was to evaluate the direct compression properties of a novel coprocessed excipient (CPE) generated by processing cow bone powder (CBP), maize starch (MS) and Khaya gum (KG) together to form a single composite excipient. Design of experiments (DoE) was employed to optimise the formulation of CPE. CPE was prepared by wet granulation using the optimised formulation of CBP (40%), MS (40%) and KG (20%) as recommended by DoE. Assessment of the organoleptic properties of CPE revealed an odourless, tasteless and coarse texture with a neutral pH of 7.3. CPE was found to be partly crystalline and partly amorphous and demonstrated compatibility between the three components of the formulation. The material in terms of flowability compared well with the flow parameters of StarLac, a reference co-processed excipient. Tablets of diclofenac produced by direct compression using CPE as the directly compressible excipient compared well with the hardness and disintegration time of...

Functionality evaluation of co-processed excipients as diluents in tablets manufactured by wet granulation

European Pharmaceutical Journal, 2020

Diluents are essential components of a tablet formulation. The type of diluent used in a formulat... more Diluents are essential components of a tablet formulation. The type of diluent used in a formulation influences the quality of tablets produced from that formulation. The aim of this study was to evaluate the tableting properties of co-processed excipients (C-PEs) incorporated as diluents in tablet formulation by wet granulation. Metronidazole tablets were prepared by wet granulation incorporating different diluents that were either single component excipients (SCEs) (lactose and microcrystalline cellulose) or C-PEs (Ludipress®, StarLac®, Prosolv® and AVICEL®HFE). The granules obtained for each formulation were evaluated for particle size analysis, flow properties and compression properties. Tablets weighing 500 mg were compressed from the metronidazole granules on a Single Station Tablet Press using a 12 mm punch and die tooling system. The tablets were kept for 24 h post-production, and the properties of weight uniformity, thickness, tensile strength, friability, disintegration ti...

Quantifying the effect of glidant on the compaction and tableting properties of paracetamol granules

Journal of Research in Pharmacy, 2020

Glidants play a vital role in tablet formulation. This study aimed to examine the impact of glida... more Glidants play a vital role in tablet formulation. This study aimed to examine the impact of glidants on the compaction and tableting properties of paracetamol granules prepared by wet granulation. Three formulations of paracetamol granules were prepared to consist of either talc, colloidal silicon dioxide (CSD) or a combination of both in equal proportion (1:1) as glidants added extragranularly. The granules were characterised by measuring the particle size, angle of repose, bulk and tapped densities, true densities, and moisture content. Compaction studies on the granules were carried out using the Heckel, Kawakita, Walker, and compressibility-tabletability-compactibility (CTC) models. Tablets were prepared from the granules for each formulation and evaluated according to USP requirements. The results of the granule analysis revealed that granule properties were similar across the formulations irrespective of the type of glidant used. Compaction studies revealed that talc granules exhibited a greater degree of plasticity and compressibility compared to the other formulations. However, CSD granules and granules containing the two glidants in equal proportion were found to have better compactibility and tabletability, resulting in tablets with relatively better properties. This study has underscored the impact of glidants on the compaction and tableting properties of paracetamol granules.

Effect of mode of superdisintegrant incorporation on tableting properties of metronidazole granules

Pharmaceutical Sciences Asia, 2019

Superdisintegrants are a special class of excipients used in a tablet formulation to aid disinteg... more Superdisintegrants are a special class of excipients used in a tablet formulation to aid disintegration and possibly enhance the release kinetics of a drug. The intragranular and extragranular effect of sodium starch glycolate (SSG) or croscarmellose sodium (CCM) as superdisintegrants on tableting properties of metronidazole granules were investigated. The granules were characterized for particle size analysis, angle of repose, bulk and tapped densities as well as Carr's index (CI) and Hausner's ratio (HR). Tablets were prepared from each batch of granules weighing 500 mg on a single punch tablet press using 12 mm flat-faced punches and compressed at 57.5 MPa. The tablets were kept at 25 ± 2 °C/75 % RH for 24 h to allow for elastic recovery and the properties of weight variation, content uniformity, thickness, crushing strength (CS), disintegration time (DT), and drug-release were evaluated. The results showed that all the batches of granules exhibited good flow based on angle of repose < 30° , CI < 20 %, and HR ≤ 1.2. The evaluated tablet properties demonstrated that intragranular addition of either SSG or CCM lowered the CS and DT when compared to the extragranular effect. This indicates that the incorporation mode of superdisintegrant in a tablet formulation exerts an influence on tablet properties.

Development and Characterization of a Microcrystalline Cellulose-based co-Processed Excipient using Design of Experiment Approach

Jordan Journal of Pharmaceutical Sciences

The study aims to develop a co-processed excipient (CPE) containing microcrystalline cellulose (M... more The study aims to develop a co-processed excipient (CPE) containing microcrystalline cellulose (MCC) and crospovidone (CPV) using the wet massing technique. Preformulation studies were carried out on CPE to characterize its physicochemical properties. Optimization of the formulation of CPE was carried out using a mixture of experimental designs. The optimization study suggested a composite excipient containing MCC (99 %) and CPV (1 %). Solid state characterization of CPE revealed a material that is predominantly crystalline in nature. The particle size of CPE increased in comparison to starting material. FT-IR confirmed the compatibility of MCC and CPV when co-processed together to yield a single composite excipient. There was a decrease in moisture content and moisture sorption capacity of CPE when compared to MCC. Powder characterization revealed an improvement in bulk flow properties of CPE relative to MCC. In summary, the physicochemical properties obtained suggest that CPE will...

Optimization of the Extragranular Excipient Composition of Paracetamol Tablet formulation using the Quality by Design Approach

Brazilian Journal of Pharmaceutical Sciences, 2022

The purpose of this study is to optimize the composition of extragranular excipients (EGE) and mi... more The purpose of this study is to optimize the composition of extragranular excipients (EGE) and mixing time of granules with EGE of paracetamol tablet formulation using Design of Experiments (DoE) approach. The effect of the composition of EGE and the mixing time of granules with EGE on granule and tableting properties of paracetamol tablet formulation was investigated using a combined model of mixture and process factors (Design-Expert 12). A total of 18 tablet formulations were manufactured by wet granulation using varying compositions of EGE and varying mixing time. Granule and tablet properties of each formulation were evaluated as response variables for the design, data generated were fitted into models and analysed to generate a design space that was used for optimization studies. The proposed EGE composition as predicted by the design was confirmed and validated after preparation and evaluation of the granule and tablet properties. The optimized composition for the EGE that yielded granules and tablets of desirable characteristics was found to be maize starch (5 %), talc (4.9 %) and magnesium stearate (0.1 %) with a mixing time of 2 min. The tablets produced with the optimized composition had better mechanical strength and disintegration time than the formulation prepared using an existing formula of maize starch (7.8 %), talc (2 %) and magnesium stearate (0.2 %) that were obtained using the One Variable at a Time (OVAT) approach. This study confirmed the relevance of quality by design in development of pharmaceutical formulations.

Formulation and Evaluation of Ascorbic acid Tablets by Direct Compression using Microcrystalline Starch as a Direct Compression Excipient

International Journal of Health Research, 2011

PURPOSE: To evaluate the tableting properties of microcrys talline starch (MCS) used as a direct ... more PURPOSE: To evaluate the tableting properties of microcrys talline starch (MCS) used as a direct compression excipient in the formulation of ascorbic acid tablets and to compare with the properties of tablets produced using microcrystalline cellulose (MCC). METHODS: MCS was obtained by partial hydrolysis of cassava ( Manihot esculenta Crantz) starch using the enzyme, α-amylase. The hydrolysis was allowed to proceed for 5 hr under controlled temper ature and pH (56 °C, 6). The derived MCS was recovered by filtration after pr ecipitation with ethanol (95% v /v). Powder properties were investigated and tablets of ascorbic acid were formulated using MCS and MCC as direct compression excipients. RESULTS: Mechanical properties of tablets formulated with M CS were comparable to those of MCC. Tablets formulated with MCS disintegrated within 15 min and gave a 100% release of ascorbic a cid within 30 min compared to MCC which disintegrated after 60 min. CONCLUSION: MCS can be incorporated as ...

Tableting Performance of Maize and Potato Starches used in Combination as Binder/Disintegrant in Metronidazole Tablet Formulation

Turkish Journal of Pharmaceutical Sciences, 2021

The aim of this study was to characterize the tableting performance of maize and potato starches ... more The aim of this study was to characterize the tableting performance of maize and potato starches when used in combination either as a disintegrant or binder in solid dosage form development. Wet granulation was used to process metronidazole granules incorporating either maize starch, potato starch or a combination of the two starches as binder or disintegrant at 10 % w /w. Granule analysis was carried out on the various formulations and subsequently compressed into tablets weighing approximately 500 mg following the addition of extragranular excipients. Tablet properties were assessed after 24 h of storage. Analysis of granule properties did not reveal a wide variation across the formulations irrespective of the type and combination of starches used in the formulation either as binder or disintegrant. It was observed, however that there were slight differences in particle size, bulk and tapped densities of granule formulations containing the combined starch as excipients when compared to granule formulations containing an individual starch as excipient. Tablets prepared using the combined starches as binder had lower tensile strength and disintegration time when compared to other formulations incorporating the individual starches as binders. However, when evaluated as disintegrant, the tablet formulation containing the combined starches produced tablets with relatively lower disintegration time when compared to formulations containing the individual starches as disintegrant. Hence, the combination of maize and potato starches as excipients in tablet formulation influenced the outcome of granule and tablet properties.

Comparative analysis of co-processed starches prepared by three different methods

by Yonni E Apeji and Sophie Nock-Anyebe

Co-processing is currently of interest in the generation of high-functionality excipients for tab... more Co-processing is currently of interest in the generation of high-functionality excipients for tablet formulation. In the present study, comparative analysis of the powder and tableting properties of three co-processed starches prepared by three different methods was carried out. The co-processed excipients consisting of maize starch (90%), acacia gum (7.5%) and colloidal silicon dioxide (2.5%) were prepared by co-dispersion (SAS-CD), co-fusion (SAS-CF) and co-granulation (SAS-CG). Powder properties of each co-processed excipient were characterized by measuring particle size, flow indices, particle density, dilution potential and lubricant sensitivity ratio. Heckel and Walker models were used to evaluate the compaction behaviour of the three co-processed starches. Tablets were produced with paracetamol as the model drug by direct compression on an eccentric Tablet Press fitted with 12 mm flat-faced punches and compressed at 216 MPa. The tablets were stored at room temperature for 24 ...

Evaluation of the Antibacterial Activity of Adansonia digitata L. Seed oil gotten from Zaria, Kaduna State, Nigeria, on some strains of bacteria

The use of essential oils as antibacterial agents have become popular over the years, this is in ... more The use of essential oils as antibacterial agents have become popular over the years, this is in a bid to search for alternative ways of dealing with strains of bacteria that have become resistant to conventional antibiotics. This study was carried out to evaluate the antibacterial potentials of Adansonia digitata seed oil from Zaria, Kaduna state, Nigeria, on the clinical isolates of some bacteria ( Bacillus subtilis, Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli ). The oil was extracted from the seeds using the soxhlet extraction method with n-hexane as the solvent. Well diffusion method was used to test susceptibility of the strains of bacteria to the oil, using Gentamycin and Streptomycin as standard positive controls. Experiments were carried out in duplicates. Data obtained from the experiment was analysed using one way analysis of variance (ANOVA) and Duncan Multiple Range Test (DMRT), with P A. digitata oil was unable to create any inhibition zones in th...

Design and Development of a Starch-Based Multifunctional Excipient (Stargelasil) for Tablet Formulation

A THESIS SUBMITTED TO THE SCHOOL OF POSTGRADUATE STUDIES, AHMADU BELLO UNIVERSITY IN PARTIAL FULF... more A THESIS SUBMITTED TO THE SCHOOL OF POSTGRADUATE STUDIES, AHMADU BELLO UNIVERSITY IN PARTIAL FULFILMENT OF THE REQUIREMENTS FOR THE AWARD OF THE DOCTOR OF PHILOSOPHY DEGREE IN PHARMACEUTICS DEPARTMENT OF PHARMACEUTICS AND PHARMACEUTICAL MICROBIOLOGY, FACULTY OF PHARMACEUTICAL SCIENCES, AHMADU BELLO UNIVERSITY, ZARIA

Performance Evaluation of Maize Starch as a Multifunctional Excipient in Metronidazole Tablet Formulation

espanolObjetivo: El objetivo de este estudio fue evaluar el rendimiento del almidon de maiz como ... more espanolObjetivo: El objetivo de este estudio fue evaluar el rendimiento del almidon de maiz como excipiente multifuncional en la formulacion de comprimidos de metronidazol. Metodos: Metronidazol Tabletas En Honorario preparado por granulacion humeda que contiene almidon de maiz como diluyente (40%), desintegrante (10%) y aglutinante (5%) y en comparacion con una formulacion de referencia que contiene lactosa como diluyente (40%), almidon de maiz como desintegrante (10%) y Acacia como aglutinante (5%). Los granulos se analizaron para el tamano de particula, propiedades de flujo, compresibilidad y contenido de humedad. Las tabletas con un peso de 500 mg fueron comprimidas para ambas formulaciones en una simple Punch Tablet Press usando un punzon de 12 mm de cara plana en 57,5 MPa. Los comprimidos se mantuvieron durante 24 h para permitir la recuperacion elastica y evaluar el peso y el contenido uniformidad, espesor, resistencia a la trituracion, friabilidad, tiempo de desintegracion y...

Compaction and tableting properties of composite particles of microcrystalline cellulose and crospovidone engineered for direct compression

Future Journal of Pharmaceutical Sciences

Background Excipients with improved functionality have continued to be developed by the particle ... more Background Excipients with improved functionality have continued to be developed by the particle engineering strategy of co-processing. The aim of this study was to evaluate the compaction and tableting properties of composite particles of microcrystalline cellulose (MCC) and crospovidone (CPV) engineered by co-processing. Results Heckel analysis of the compaction behavior revealed a decrease in plasticity of co-processed excipient (CPE) when compared to MCC due to an increase in Heckel yield pressure from 144 to 172 MPa. The compressibility-tabletability-compactibility (CTC) profile revealed a decrease in individual parameters for CPE when compared to MCC. CPE was found to be more sensitive to the lubricant effect of sodium stearyl fumarate (SSF) when compared to MCC and less sensitive to magnesium stearate (MST) when compared to MCC. A higher dilution potential was obtained for MCC (60%) compared to 44% for CPE when metronidazole was used as model drug. Tableting properties reveal...

Evaluation of the Powder and Compaction Properties of Microcrystalline Starch (MCS) Derived from Cassava (Manihot Esculenta Crantz) Starch by Enzymatic Hydrolysis

The aim of this study was to investigate and determine the powder and compaction properties of mi... more The aim of this study was to investigate and determine the powder and compaction properties of microcrystalline starch (MCS) and compare with the properties of a well known direct compression filler-binder, microcrystalline cellulose (MCC). Cassava starch was extracted from the freshly harvested tubers of Manihot esculenta Crantz and subjected to 5hours of enzymatic hydrolysis to yield microcrystalline starch. The powder and compaction properties were evaluated and compared with MCC 101, a commercial brand of microcrystalline cellulose. Results of the powder properties of MCS revealed differences in the particle size, angle of repose, flow rate, bulk density, tapped density, true density, Hausner’s ratio, Carr’s index and powder porosity when compared to MCC. The compaction studies of both materials revealed that MCS had a faster onset of deformation and a greater extent of deformation in comparison to MCC. These results suggest that MCS has the potential of being used as a filler-b...

Formulation and Evaluation of Cyperus esculentus (Tiger Nut) Starch-Alginate Microbeads in the Oral Delivery of Ibuprofen

Journal of Pharmaceutical Innovation

Microencapsulation is a technique employed in the development of controlled drug delivery systems... more Microencapsulation is a technique employed in the development of controlled drug delivery systems. It is beneficial in reducing dosing frequency, ensuring targeted drug delivery, and improving drug bioavailability. The objective of this study was to evaluate the effectiveness of Cyperus esculentus starch and its derivative in the development of microbeads for sustained delivery of ibuprofen. Ibuprofen-loaded microbeads were prepared by ionotropic gelation using Cyperus esculentus starch and its derivative in combination with sodium alginate at concentrations of 1:1, 1:2, and 2:1 and calcium chloride solution as cross-linker. Morphology of the microbeads by scanning electron microscopy (SEM), Fourier transform infrared (FT-IR), and differential scanning calorimetry (DSC) were investigated. Entrapment efficiency, swelling capacity, mucoadhesion, and in vitro drug release were also evaluated. SEM showed that the microbeads were spherical to irregular in shape, FT-IR returned prominent peaks specific for ibuprofen and absence of new peaks, DSC revealed evidence of entrapment of ibuprofen in the microbeads, and entrapment efficiency ranged between 46.05 and 89.86%. Microbeads prepared with native and cross-linked starches showed better mucoadhesion, and those prepared with cross-linked starch blend exhibited highest swelling capacity. In vitro release was pH dependent, and increasing the concentration of cross-linked starch in the blend caused greater retardation of drug release (45.19%) than the formulations containing native starch-alginate blend or sodium alginate alone. The blend of cross-linked Cyperus esculentus starch and sodium alginate shows propensity to sustain ibuprofen release and could be exploited for targeted delivery especially to the lower GIT.

Design and characterization of the material attributes of a co-processed excipient developed for direct compression tableting

ACTA Pharmaceutica Sciencia, 2019

The objective of the study was to characterize the material attributes of a co-processed excipien... more The objective of the study was to characterize the material attributes of a co-processed excipient and determine its suitability for tableting applications. A single composite excipient named SGS consisting of tapioca starch (TS), gelatin (GEL) and colloidal silicon dioxide (CSD) was developed by co-processing using the method of co-fusion and its solid-state, powder and mechanical properties evaluated. Particle morphology revealed spherical shaped particles of SGS with slightly rough surfaces. PXRD was characterized by a halo diffraction pattern consistent with amorphous materials. FT-IR studies demonstrated drug-excipient compatibility. Flow properties of SGS improved in relation to its physical mixture (SGS-PM) and the mechanical properties of SGS was enhanced as a result of co-processing. The outcome of the study demonstrates the suitability of SGS as a tableting excipient.

Evaluación del rendimiento del almidón de maíz como excipiente multifuncional en la formulación de comprimidos de metronidazol

Ars Pharmaceutica (Internet)

Objetivo: El objetivo de este estudio fue evaluar el rendimiento del almidón de maíz como excipie... more Objetivo: El objetivo de este estudio fue evaluar el rendimiento del almidón de maíz como excipiente multifuncional en la formulación de comprimidos de metronidazol. Métodos: Metronidazol Tabletas En Honorario preparado por granulación húmeda que contiene almidón de maíz como diluyente (40%), desintegrante (10%) y aglutinante (5%) y en comparación con una formulación de referencia que contiene lactosa como diluyente (40%), almidón de maíz como desintegrante (10%) y Acacia como aglutinante (5%). Los gránulos se analizaron para el tamaño de partícula, propiedades de flujo, compresibilidad y contenido de humedad. Las tabletas con un peso de 500 mg fueron comprimidas para ambas formulaciones en una simple Punch Tablet Press usando un punzón de 12 mm de cara plana en 57,5 MPa. Los comprimidos se mantuvieron durante 24 h para permitir la recuperación elástica y evaluar el peso y el contenido uniformidad, espesor, resistencia a la trituración, friabilidad, tiempo de desintegración y in vit...

Comparative Analysis of Co-Processed Starches prepared by Three Different Methods

British Journal of Pharmacy

Summary Co-processing is currently of interest in the generation of high-functionality excipients... more Summary Co-processing is currently of interest in the generation of high-functionality excipients for tablet formulation. In the present study, comparative analysis of the powder and tableting properties of three co-processed starches prepared by three different methods was carried out. The co-processed excipients consisting of maize starch (90%), acacia gum (7.5%) and colloidal silicon dioxide (2.5%) were prepared by co-dispersion (SAS-CD), co-fusion (SAS-CF) and co-granulation (SAS-CG). Powder properties of each co-processed excipient were characterized by measuring particle size, flow indices, particle density, dilution potential and lubricant sensitivity ratio. Heckel and Walker models were used to evaluate the compaction behaviour of the three co-processed starches. Tablets were produced with paracetamol as the model drug by direct compression on an eccentric Tablet Press fitted with 12 mm flat-faced punches and compressed at 216 MPa. The tablets were stored at room temperature...

[Effect of EUDRAGIT® RS on the release behaviour of theophylline solid dispersions]

Ceska a Slovenska farmacie : casopis Ceske farmaceuticke spolecnosti a Slovenske farmaceuticke spolecnosti

The purpose of this study was to extend the release of theophylline using Eudragit® RS 100 and Eu... more The purpose of this study was to extend the release of theophylline using Eudragit® RS 100 and Eudragit® RSPO as carriers. Solid dispersions of theophylline were prepared by the solvent evaporation technique using Eudragit® RS 100, Eudragit® RSPO and their blend in various drug : polymer ratios. The prepared solid dispersions were characterized with respect to entrapment efficiency, solubility and recovery yield. In vitro drug release of theophylline from the solid dispersions was evaluated in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) without enzymes. Solubility studies demonstrated a decrease in the solubility of the drug from the solid dispersions. The solubilities of pure drug and solid dispersions were lowered in SGF compared to SIF. Solid dispersions prepared with Eudragit® RS 100 entrapped a greater amount of theophylline in comparison to those with Eudragit® RSPO or the polymer blends and were able to extend the release of theophylline over 24 hrs. Fo...

Development and Optimization of a Starch-Based Co-processed Excipient for Direct Compression Using Mixture Design

AAPS PharmSciTech, Jan 16, 2017

The development of novel excipients with enhanced functionality has been explored using particle ... more The development of novel excipients with enhanced functionality has been explored using particle engineering by co-processing. The aim of this study was to improve the functionality of tapioca starch (TS) for direct compression by co-processing with gelatin (GEL) and colloidal silicon dioxide (CSD) in optimized proportions. Design of Experiment (DoE) was employed to optimize the composition of the co-processed excipient using the desirability function and other supporting studies as a basis for selecting the optimized formulation. The co-processed excipient (SGS) was thereafter developed by the method of co-fusion. Flow and compaction studies of SGS were carried out in comparison to its parent component (TS) and physical mixture (SGS-PM). Tablets were prepared by direct compression (DC) containing ibuprofen (200 mg) as a model for poor compressibility using SGS, Prosolv®, and StarLac® as multifunctional excipients. The optimized composition of SGS corresponded to TS (90%), GEL (7.5%...

Direct Compression Properties of Co-Processed Excipient Containing Cow Bone Powder, Khaya Gum and Maize Starch

Malaysian Journal of Pharmaceutical Sciences

The aim of this study was to evaluate the direct compression properties of a novel coprocessed ex... more The aim of this study was to evaluate the direct compression properties of a novel coprocessed excipient (CPE) generated by processing cow bone powder (CBP), maize starch (MS) and Khaya gum (KG) together to form a single composite excipient. Design of experiments (DoE) was employed to optimise the formulation of CPE. CPE was prepared by wet granulation using the optimised formulation of CBP (40%), MS (40%) and KG (20%) as recommended by DoE. Assessment of the organoleptic properties of CPE revealed an odourless, tasteless and coarse texture with a neutral pH of 7.3. CPE was found to be partly crystalline and partly amorphous and demonstrated compatibility between the three components of the formulation. The material in terms of flowability compared well with the flow parameters of StarLac, a reference co-processed excipient. Tablets of diclofenac produced by direct compression using CPE as the directly compressible excipient compared well with the hardness and disintegration time of...

Functionality evaluation of co-processed excipients as diluents in tablets manufactured by wet granulation

European Pharmaceutical Journal, 2020

Diluents are essential components of a tablet formulation. The type of diluent used in a formulat... more Diluents are essential components of a tablet formulation. The type of diluent used in a formulation influences the quality of tablets produced from that formulation. The aim of this study was to evaluate the tableting properties of co-processed excipients (C-PEs) incorporated as diluents in tablet formulation by wet granulation. Metronidazole tablets were prepared by wet granulation incorporating different diluents that were either single component excipients (SCEs) (lactose and microcrystalline cellulose) or C-PEs (Ludipress®, StarLac®, Prosolv® and AVICEL®HFE). The granules obtained for each formulation were evaluated for particle size analysis, flow properties and compression properties. Tablets weighing 500 mg were compressed from the metronidazole granules on a Single Station Tablet Press using a 12 mm punch and die tooling system. The tablets were kept for 24 h post-production, and the properties of weight uniformity, thickness, tensile strength, friability, disintegration ti...

Quantifying the effect of glidant on the compaction and tableting properties of paracetamol granules

Journal of Research in Pharmacy, 2020

Glidants play a vital role in tablet formulation. This study aimed to examine the impact of glida... more Glidants play a vital role in tablet formulation. This study aimed to examine the impact of glidants on the compaction and tableting properties of paracetamol granules prepared by wet granulation. Three formulations of paracetamol granules were prepared to consist of either talc, colloidal silicon dioxide (CSD) or a combination of both in equal proportion (1:1) as glidants added extragranularly. The granules were characterised by measuring the particle size, angle of repose, bulk and tapped densities, true densities, and moisture content. Compaction studies on the granules were carried out using the Heckel, Kawakita, Walker, and compressibility-tabletability-compactibility (CTC) models. Tablets were prepared from the granules for each formulation and evaluated according to USP requirements. The results of the granule analysis revealed that granule properties were similar across the formulations irrespective of the type of glidant used. Compaction studies revealed that talc granules exhibited a greater degree of plasticity and compressibility compared to the other formulations. However, CSD granules and granules containing the two glidants in equal proportion were found to have better compactibility and tabletability, resulting in tablets with relatively better properties. This study has underscored the impact of glidants on the compaction and tableting properties of paracetamol granules.

Effect of mode of superdisintegrant incorporation on tableting properties of metronidazole granules

Pharmaceutical Sciences Asia, 2019

Superdisintegrants are a special class of excipients used in a tablet formulation to aid disinteg... more Superdisintegrants are a special class of excipients used in a tablet formulation to aid disintegration and possibly enhance the release kinetics of a drug. The intragranular and extragranular effect of sodium starch glycolate (SSG) or croscarmellose sodium (CCM) as superdisintegrants on tableting properties of metronidazole granules were investigated. The granules were characterized for particle size analysis, angle of repose, bulk and tapped densities as well as Carr's index (CI) and Hausner's ratio (HR). Tablets were prepared from each batch of granules weighing 500 mg on a single punch tablet press using 12 mm flat-faced punches and compressed at 57.5 MPa. The tablets were kept at 25 ± 2 °C/75 % RH for 24 h to allow for elastic recovery and the properties of weight variation, content uniformity, thickness, crushing strength (CS), disintegration time (DT), and drug-release were evaluated. The results showed that all the batches of granules exhibited good flow based on angle of repose < 30° , CI < 20 %, and HR ≤ 1.2. The evaluated tablet properties demonstrated that intragranular addition of either SSG or CCM lowered the CS and DT when compared to the extragranular effect. This indicates that the incorporation mode of superdisintegrant in a tablet formulation exerts an influence on tablet properties.

Development and Characterization of a Microcrystalline Cellulose-based co-Processed Excipient using Design of Experiment Approach

Jordan Journal of Pharmaceutical Sciences

The study aims to develop a co-processed excipient (CPE) containing microcrystalline cellulose (M... more The study aims to develop a co-processed excipient (CPE) containing microcrystalline cellulose (MCC) and crospovidone (CPV) using the wet massing technique. Preformulation studies were carried out on CPE to characterize its physicochemical properties. Optimization of the formulation of CPE was carried out using a mixture of experimental designs. The optimization study suggested a composite excipient containing MCC (99 %) and CPV (1 %). Solid state characterization of CPE revealed a material that is predominantly crystalline in nature. The particle size of CPE increased in comparison to starting material. FT-IR confirmed the compatibility of MCC and CPV when co-processed together to yield a single composite excipient. There was a decrease in moisture content and moisture sorption capacity of CPE when compared to MCC. Powder characterization revealed an improvement in bulk flow properties of CPE relative to MCC. In summary, the physicochemical properties obtained suggest that CPE will...

Optimization of the Extragranular Excipient Composition of Paracetamol Tablet formulation using the Quality by Design Approach

Brazilian Journal of Pharmaceutical Sciences, 2022

The purpose of this study is to optimize the composition of extragranular excipients (EGE) and mi... more The purpose of this study is to optimize the composition of extragranular excipients (EGE) and mixing time of granules with EGE of paracetamol tablet formulation using Design of Experiments (DoE) approach. The effect of the composition of EGE and the mixing time of granules with EGE on granule and tableting properties of paracetamol tablet formulation was investigated using a combined model of mixture and process factors (Design-Expert 12). A total of 18 tablet formulations were manufactured by wet granulation using varying compositions of EGE and varying mixing time. Granule and tablet properties of each formulation were evaluated as response variables for the design, data generated were fitted into models and analysed to generate a design space that was used for optimization studies. The proposed EGE composition as predicted by the design was confirmed and validated after preparation and evaluation of the granule and tablet properties. The optimized composition for the EGE that yielded granules and tablets of desirable characteristics was found to be maize starch (5 %), talc (4.9 %) and magnesium stearate (0.1 %) with a mixing time of 2 min. The tablets produced with the optimized composition had better mechanical strength and disintegration time than the formulation prepared using an existing formula of maize starch (7.8 %), talc (2 %) and magnesium stearate (0.2 %) that were obtained using the One Variable at a Time (OVAT) approach. This study confirmed the relevance of quality by design in development of pharmaceutical formulations.

Formulation and Evaluation of Ascorbic acid Tablets by Direct Compression using Microcrystalline Starch as a Direct Compression Excipient

International Journal of Health Research, 2011

PURPOSE: To evaluate the tableting properties of microcrys talline starch (MCS) used as a direct ... more PURPOSE: To evaluate the tableting properties of microcrys talline starch (MCS) used as a direct compression excipient in the formulation of ascorbic acid tablets and to compare with the properties of tablets produced using microcrystalline cellulose (MCC). METHODS: MCS was obtained by partial hydrolysis of cassava ( Manihot esculenta Crantz) starch using the enzyme, α-amylase. The hydrolysis was allowed to proceed for 5 hr under controlled temper ature and pH (56 °C, 6). The derived MCS was recovered by filtration after pr ecipitation with ethanol (95% v /v). Powder properties were investigated and tablets of ascorbic acid were formulated using MCS and MCC as direct compression excipients. RESULTS: Mechanical properties of tablets formulated with M CS were comparable to those of MCC. Tablets formulated with MCS disintegrated within 15 min and gave a 100% release of ascorbic a cid within 30 min compared to MCC which disintegrated after 60 min. CONCLUSION: MCS can be incorporated as ...

Tableting Performance of Maize and Potato Starches used in Combination as Binder/Disintegrant in Metronidazole Tablet Formulation

Turkish Journal of Pharmaceutical Sciences, 2021

The aim of this study was to characterize the tableting performance of maize and potato starches ... more The aim of this study was to characterize the tableting performance of maize and potato starches when used in combination either as a disintegrant or binder in solid dosage form development. Wet granulation was used to process metronidazole granules incorporating either maize starch, potato starch or a combination of the two starches as binder or disintegrant at 10 % w /w. Granule analysis was carried out on the various formulations and subsequently compressed into tablets weighing approximately 500 mg following the addition of extragranular excipients. Tablet properties were assessed after 24 h of storage. Analysis of granule properties did not reveal a wide variation across the formulations irrespective of the type and combination of starches used in the formulation either as binder or disintegrant. It was observed, however that there were slight differences in particle size, bulk and tapped densities of granule formulations containing the combined starch as excipients when compared to granule formulations containing an individual starch as excipient. Tablets prepared using the combined starches as binder had lower tensile strength and disintegration time when compared to other formulations incorporating the individual starches as binders. However, when evaluated as disintegrant, the tablet formulation containing the combined starches produced tablets with relatively lower disintegration time when compared to formulations containing the individual starches as disintegrant. Hence, the combination of maize and potato starches as excipients in tablet formulation influenced the outcome of granule and tablet properties.

Comparative analysis of co-processed starches prepared by three different methods

by Yonni E Apeji and Sophie Nock-Anyebe

Co-processing is currently of interest in the generation of high-functionality excipients for tab... more Co-processing is currently of interest in the generation of high-functionality excipients for tablet formulation. In the present study, comparative analysis of the powder and tableting properties of three co-processed starches prepared by three different methods was carried out. The co-processed excipients consisting of maize starch (90%), acacia gum (7.5%) and colloidal silicon dioxide (2.5%) were prepared by co-dispersion (SAS-CD), co-fusion (SAS-CF) and co-granulation (SAS-CG). Powder properties of each co-processed excipient were characterized by measuring particle size, flow indices, particle density, dilution potential and lubricant sensitivity ratio. Heckel and Walker models were used to evaluate the compaction behaviour of the three co-processed starches. Tablets were produced with paracetamol as the model drug by direct compression on an eccentric Tablet Press fitted with 12 mm flat-faced punches and compressed at 216 MPa. The tablets were stored at room temperature for 24 ...

Evaluation of the Antibacterial Activity of Adansonia digitata L. Seed oil gotten from Zaria, Kaduna State, Nigeria, on some strains of bacteria

The use of essential oils as antibacterial agents have become popular over the years, this is in ... more The use of essential oils as antibacterial agents have become popular over the years, this is in a bid to search for alternative ways of dealing with strains of bacteria that have become resistant to conventional antibiotics. This study was carried out to evaluate the antibacterial potentials of Adansonia digitata seed oil from Zaria, Kaduna state, Nigeria, on the clinical isolates of some bacteria ( Bacillus subtilis, Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli ). The oil was extracted from the seeds using the soxhlet extraction method with n-hexane as the solvent. Well diffusion method was used to test susceptibility of the strains of bacteria to the oil, using Gentamycin and Streptomycin as standard positive controls. Experiments were carried out in duplicates. Data obtained from the experiment was analysed using one way analysis of variance (ANOVA) and Duncan Multiple Range Test (DMRT), with P A. digitata oil was unable to create any inhibition zones in th...

Design and Development of a Starch-Based Multifunctional Excipient (Stargelasil) for Tablet Formulation

A THESIS SUBMITTED TO THE SCHOOL OF POSTGRADUATE STUDIES, AHMADU BELLO UNIVERSITY IN PARTIAL FULF... more A THESIS SUBMITTED TO THE SCHOOL OF POSTGRADUATE STUDIES, AHMADU BELLO UNIVERSITY IN PARTIAL FULFILMENT OF THE REQUIREMENTS FOR THE AWARD OF THE DOCTOR OF PHILOSOPHY DEGREE IN PHARMACEUTICS DEPARTMENT OF PHARMACEUTICS AND PHARMACEUTICAL MICROBIOLOGY, FACULTY OF PHARMACEUTICAL SCIENCES, AHMADU BELLO UNIVERSITY, ZARIA

Performance Evaluation of Maize Starch as a Multifunctional Excipient in Metronidazole Tablet Formulation

espanolObjetivo: El objetivo de este estudio fue evaluar el rendimiento del almidon de maiz como ... more espanolObjetivo: El objetivo de este estudio fue evaluar el rendimiento del almidon de maiz como excipiente multifuncional en la formulacion de comprimidos de metronidazol. Metodos: Metronidazol Tabletas En Honorario preparado por granulacion humeda que contiene almidon de maiz como diluyente (40%), desintegrante (10%) y aglutinante (5%) y en comparacion con una formulacion de referencia que contiene lactosa como diluyente (40%), almidon de maiz como desintegrante (10%) y Acacia como aglutinante (5%). Los granulos se analizaron para el tamano de particula, propiedades de flujo, compresibilidad y contenido de humedad. Las tabletas con un peso de 500 mg fueron comprimidas para ambas formulaciones en una simple Punch Tablet Press usando un punzon de 12 mm de cara plana en 57,5 MPa. Los comprimidos se mantuvieron durante 24 h para permitir la recuperacion elastica y evaluar el peso y el contenido uniformidad, espesor, resistencia a la trituracion, friabilidad, tiempo de desintegracion y...

Compaction and tableting properties of composite particles of microcrystalline cellulose and crospovidone engineered for direct compression

Future Journal of Pharmaceutical Sciences

Background Excipients with improved functionality have continued to be developed by the particle ... more Background Excipients with improved functionality have continued to be developed by the particle engineering strategy of co-processing. The aim of this study was to evaluate the compaction and tableting properties of composite particles of microcrystalline cellulose (MCC) and crospovidone (CPV) engineered by co-processing. Results Heckel analysis of the compaction behavior revealed a decrease in plasticity of co-processed excipient (CPE) when compared to MCC due to an increase in Heckel yield pressure from 144 to 172 MPa. The compressibility-tabletability-compactibility (CTC) profile revealed a decrease in individual parameters for CPE when compared to MCC. CPE was found to be more sensitive to the lubricant effect of sodium stearyl fumarate (SSF) when compared to MCC and less sensitive to magnesium stearate (MST) when compared to MCC. A higher dilution potential was obtained for MCC (60%) compared to 44% for CPE when metronidazole was used as model drug. Tableting properties reveal...

Evaluation of the Powder and Compaction Properties of Microcrystalline Starch (MCS) Derived from Cassava (Manihot Esculenta Crantz) Starch by Enzymatic Hydrolysis

The aim of this study was to investigate and determine the powder and compaction properties of mi... more The aim of this study was to investigate and determine the powder and compaction properties of microcrystalline starch (MCS) and compare with the properties of a well known direct compression filler-binder, microcrystalline cellulose (MCC). Cassava starch was extracted from the freshly harvested tubers of Manihot esculenta Crantz and subjected to 5hours of enzymatic hydrolysis to yield microcrystalline starch. The powder and compaction properties were evaluated and compared with MCC 101, a commercial brand of microcrystalline cellulose. Results of the powder properties of MCS revealed differences in the particle size, angle of repose, flow rate, bulk density, tapped density, true density, Hausner’s ratio, Carr’s index and powder porosity when compared to MCC. The compaction studies of both materials revealed that MCS had a faster onset of deformation and a greater extent of deformation in comparison to MCC. These results suggest that MCS has the potential of being used as a filler-b...

Formulation and Evaluation of Cyperus esculentus (Tiger Nut) Starch-Alginate Microbeads in the Oral Delivery of Ibuprofen

Journal of Pharmaceutical Innovation

Microencapsulation is a technique employed in the development of controlled drug delivery systems... more Microencapsulation is a technique employed in the development of controlled drug delivery systems. It is beneficial in reducing dosing frequency, ensuring targeted drug delivery, and improving drug bioavailability. The objective of this study was to evaluate the effectiveness of Cyperus esculentus starch and its derivative in the development of microbeads for sustained delivery of ibuprofen. Ibuprofen-loaded microbeads were prepared by ionotropic gelation using Cyperus esculentus starch and its derivative in combination with sodium alginate at concentrations of 1:1, 1:2, and 2:1 and calcium chloride solution as cross-linker. Morphology of the microbeads by scanning electron microscopy (SEM), Fourier transform infrared (FT-IR), and differential scanning calorimetry (DSC) were investigated. Entrapment efficiency, swelling capacity, mucoadhesion, and in vitro drug release were also evaluated. SEM showed that the microbeads were spherical to irregular in shape, FT-IR returned prominent peaks specific for ibuprofen and absence of new peaks, DSC revealed evidence of entrapment of ibuprofen in the microbeads, and entrapment efficiency ranged between 46.05 and 89.86%. Microbeads prepared with native and cross-linked starches showed better mucoadhesion, and those prepared with cross-linked starch blend exhibited highest swelling capacity. In vitro release was pH dependent, and increasing the concentration of cross-linked starch in the blend caused greater retardation of drug release (45.19%) than the formulations containing native starch-alginate blend or sodium alginate alone. The blend of cross-linked Cyperus esculentus starch and sodium alginate shows propensity to sustain ibuprofen release and could be exploited for targeted delivery especially to the lower GIT.

Design and characterization of the material attributes of a co-processed excipient developed for direct compression tableting

ACTA Pharmaceutica Sciencia, 2019

The objective of the study was to characterize the material attributes of a co-processed excipien... more The objective of the study was to characterize the material attributes of a co-processed excipient and determine its suitability for tableting applications. A single composite excipient named SGS consisting of tapioca starch (TS), gelatin (GEL) and colloidal silicon dioxide (CSD) was developed by co-processing using the method of co-fusion and its solid-state, powder and mechanical properties evaluated. Particle morphology revealed spherical shaped particles of SGS with slightly rough surfaces. PXRD was characterized by a halo diffraction pattern consistent with amorphous materials. FT-IR studies demonstrated drug-excipient compatibility. Flow properties of SGS improved in relation to its physical mixture (SGS-PM) and the mechanical properties of SGS was enhanced as a result of co-processing. The outcome of the study demonstrates the suitability of SGS as a tableting excipient.

Evaluación del rendimiento del almidón de maíz como excipiente multifuncional en la formulación de comprimidos de metronidazol

Ars Pharmaceutica (Internet)

Objetivo: El objetivo de este estudio fue evaluar el rendimiento del almidón de maíz como excipie... more Objetivo: El objetivo de este estudio fue evaluar el rendimiento del almidón de maíz como excipiente multifuncional en la formulación de comprimidos de metronidazol. Métodos: Metronidazol Tabletas En Honorario preparado por granulación húmeda que contiene almidón de maíz como diluyente (40%), desintegrante (10%) y aglutinante (5%) y en comparación con una formulación de referencia que contiene lactosa como diluyente (40%), almidón de maíz como desintegrante (10%) y Acacia como aglutinante (5%). Los gránulos se analizaron para el tamaño de partícula, propiedades de flujo, compresibilidad y contenido de humedad. Las tabletas con un peso de 500 mg fueron comprimidas para ambas formulaciones en una simple Punch Tablet Press usando un punzón de 12 mm de cara plana en 57,5 MPa. Los comprimidos se mantuvieron durante 24 h para permitir la recuperación elástica y evaluar el peso y el contenido uniformidad, espesor, resistencia a la trituración, friabilidad, tiempo de desintegración y in vit...

Comparative Analysis of Co-Processed Starches prepared by Three Different Methods

British Journal of Pharmacy

Summary Co-processing is currently of interest in the generation of high-functionality excipients... more Summary Co-processing is currently of interest in the generation of high-functionality excipients for tablet formulation. In the present study, comparative analysis of the powder and tableting properties of three co-processed starches prepared by three different methods was carried out. The co-processed excipients consisting of maize starch (90%), acacia gum (7.5%) and colloidal silicon dioxide (2.5%) were prepared by co-dispersion (SAS-CD), co-fusion (SAS-CF) and co-granulation (SAS-CG). Powder properties of each co-processed excipient were characterized by measuring particle size, flow indices, particle density, dilution potential and lubricant sensitivity ratio. Heckel and Walker models were used to evaluate the compaction behaviour of the three co-processed starches. Tablets were produced with paracetamol as the model drug by direct compression on an eccentric Tablet Press fitted with 12 mm flat-faced punches and compressed at 216 MPa. The tablets were stored at room temperature...

[Effect of EUDRAGIT® RS on the release behaviour of theophylline solid dispersions]

Ceska a Slovenska farmacie : casopis Ceske farmaceuticke spolecnosti a Slovenske farmaceuticke spolecnosti

The purpose of this study was to extend the release of theophylline using Eudragit® RS 100 and Eu... more The purpose of this study was to extend the release of theophylline using Eudragit® RS 100 and Eudragit® RSPO as carriers. Solid dispersions of theophylline were prepared by the solvent evaporation technique using Eudragit® RS 100, Eudragit® RSPO and their blend in various drug : polymer ratios. The prepared solid dispersions were characterized with respect to entrapment efficiency, solubility and recovery yield. In vitro drug release of theophylline from the solid dispersions was evaluated in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) without enzymes. Solubility studies demonstrated a decrease in the solubility of the drug from the solid dispersions. The solubilities of pure drug and solid dispersions were lowered in SGF compared to SIF. Solid dispersions prepared with Eudragit® RS 100 entrapped a greater amount of theophylline in comparison to those with Eudragit® RSPO or the polymer blends and were able to extend the release of theophylline over 24 hrs. Fo...

Development and Optimization of a Starch-Based Co-processed Excipient for Direct Compression Using Mixture Design

AAPS PharmSciTech, Jan 16, 2017

The development of novel excipients with enhanced functionality has been explored using particle ... more The development of novel excipients with enhanced functionality has been explored using particle engineering by co-processing. The aim of this study was to improve the functionality of tapioca starch (TS) for direct compression by co-processing with gelatin (GEL) and colloidal silicon dioxide (CSD) in optimized proportions. Design of Experiment (DoE) was employed to optimize the composition of the co-processed excipient using the desirability function and other supporting studies as a basis for selecting the optimized formulation. The co-processed excipient (SGS) was thereafter developed by the method of co-fusion. Flow and compaction studies of SGS were carried out in comparison to its parent component (TS) and physical mixture (SGS-PM). Tablets were prepared by direct compression (DC) containing ibuprofen (200 mg) as a model for poor compressibility using SGS, Prosolv®, and StarLac® as multifunctional excipients. The optimized composition of SGS corresponded to TS (90%), GEL (7.5%...