International Journal of Applied Pharmaceutics, Nov 7, 2022
Objective: Development of pharmaceutical co-crystals is an interesting area of research as co-cry... more Objective: Development of pharmaceutical co-crystals is an interesting area of research as co-crystals are unique because they have the advantages of maintaining drug's intrinsic properties along with improvement in its physicochemical attributes. Objective of this research was to improvise solubility of a Biopharmaceutics Classification System (BCS) class II drug (Ezetimibe) along with better dissolution profile using cocrystallization technique. Methods: In the present study, pharmaceutical cocrystals of a BCS class II drug, Ezetimibe, were prepared using glycine as coformer using neat grinding method. Prepared cocrystals were characterized using Hot Stage Microscopy (HSM), Differential Scanning Calorimetry (DSC), Fourier Transform Infrared (FTIR) and Powder X-Ray Diffract meter (PXRD). In addition, solubility and dissolution studies were also performed. Results: HSM study and DSC study represented melting at Ezetimibe (166 °C), Glycine (233 °C) and cocrystals (174 °C), respectively. Melting point of cocrystal is between API and coformer, indicating towards interaction. During XRD studies, a new peak was observed at 14.7193 and 23.3211 at position 2θ in comparison to parent peaks of
Chapter-4. Synthesis, antimicrobial evaluation and QSAR studies of gallic acid derivatives Develo... more Chapter-4. Synthesis, antimicrobial evaluation and QSAR studies of gallic acid derivatives Development and evaluation of novel preservatives from simple organic acids 55 4. Synthesis, antimicrobial evaluation and QSAR studies of gallic acid derivatives 4.1 Experimental All reagents and solvents used in study were of analytical grade and procured locally. The progress of the reaction was monitored by TLC and products were purified through recrystallization and purity of the compounds was checked by thin layer chromatography (TLC) performed on silica gel G coated plate. The spectral studies, IR and 1 H NMR were determined by standard methods. Infra red (IR) spectra were recorded on FTIR Bruker ATR instrument and was recorded in cm-1. 1 H and 13 C nuclear magnetic resonance (1 H and 13 C NMR) spectra were determined using a Bruker Avance II 400 NMR spectrometer in appropriate deuterated solvents and are expressed in parts per million (δ, ppm) downfield from the internal standard TMS. NMR data are provided with multiplicity (s, singlet; d, doublet; t, triplet; m, multiplet) and number of protons. Mass spectra were taken on Bruker Compass Data Analysis 4.0 Mass spectrometer. 4.1.1. General procedure for the synthesis of 3,4,5-trihydroxybenzoyl chloride Thionyl chloride (0.3 mol) was added gradually to gallic acid (0.25 mol) in a round bottom flask. After addition of thionyl chloride, the mixture was stirred for 4 h and heated to 80 0 C for 30 min in water bath. The excess of thionyl chloride was removed by distillation. 4.1.2. General procedure for the synthesis of amides/anilides of gallic acid The solution of corresponding amine /aniline (0.1 mol) in ether (50mL) was added dropwise to a solution of 3,4,5-trihydroxybenzoyl chloride (0.1 mol, synthesized in previous step) in ether (50 mL) maintained at 0-10 0 C (Scheme 1). The solution was stirred for 30 min and the precipitated amide/anilide was separated by filtration. The crude amide was recrystallized with alcohol. In case of anilides, the precipitated crude anilide was treated with 5% hydrochloric acid, 4% sodium carbonate and water to remove residual aniline and the resultant anilide was recrystallized with alcohol. 4.1.3. Procedure for the synthesis of esters of gallic acid (3
The volatile oil of Cinnamomum zeylanicum Blume, commonly known as cinnamon oil and Ocimum kilima... more The volatile oil of Cinnamomum zeylanicum Blume, commonly known as cinnamon oil and Ocimum kilimandscharicum Baker ex Gurke, commonly known as kapur tulsi oil were subjected to Gas chromatography-Mass spectroscopy (GC-MS) analysis to study their chemical composition. Total eight components of cinnamon oil and eight components of kapur tulsi oil were identified. The major component of cinnamon oil was found to be cinnamaldehyde (91.82%). Minor compounds were found to be 1-8 cineole, muurolene, selinene, geraniol, E-cinnamic acid, vinyl trans-cinnamate. The major component of kapur tulsi oil was found to be camphor (46.14%). Other components were found to be eugenol, 1-8 cineole, limonene, αpinene, camphene, βmyrecene and αterpineol.
A shampoo is a cleaning aid for the hair and is counted among the foremost beauty products. Today... more A shampoo is a cleaning aid for the hair and is counted among the foremost beauty products. Today's shampoo formulations are beyond the stage of pure cleaning of the hair. Additional benefits are expected, e.g, conditioning, smoothing of the hair surface, good health of hair, i.e, hair free of dandruff, dirt, grease and lice and, above all, its safety benefits are expected. As the scalp is one of the most absorbent part of the body, products applied to the scalp go directly to the blood, without being filtered in any way. So it is very important to know and understand the effects of ingredients used in shampoo formulations. In the present review the shampoos based on synthetic ingredients and herbal ingredients are compared for their effectiveness and safety.
In this study, a combination of statistical and analytical approach have been used in the formula... more In this study, a combination of statistical and analytical approach have been used in the formulation development and optimisation guided by “formulation by design” (FbD) for air entrapped microcarriers of alginate of glipizide. Microcarriers of glipizide were prepared by ionotropic-gelation technique, taking concentrations of sodium alginate (SA) and calcium carbonate (CC) as independent variables. The effects of the polymers were evaluated on dependent variables that is drug release (DR), entrapment efficiency (EE), bioadhesive strength (BS), microcarrier size (MS) and total floating time (TFT). Various batches exhibited rough, spherical microcarriers with nominal size variation having sufficient drug EE, very short lag time, while the microcarriers shows the buoyancy over a period of 6–18 hours based on the formulation variables. The DR from the microcarriers was also sustained for more than 10 hours, in 0.1N HCl (pH 1.2). Higuchi’s and the first order kinetic modelling indicated...
Even though experimental designs are becoming popular especially for conventional dosage forms, l... more Even though experimental designs are becoming popular especially for conventional dosage forms, limited studies have been performed to optimize formulations of orally disintegrating films (ODFs). This study aimed to evaluate sildenafil citrate-loaded ODFs for a controlled release with hydroxypropyl methylcellulose as a film-forming polymer. A factorial design was utilized for optimization with three control factors: ethanol ratio, plasticizer ratio, and the type of plasticizer. Tensile strength, disintegration time, water contact angle, and thickness were chosen as responses. For optimization, water contact angle, disintegration time, and thickness were minimized, while the tensile strength was maximized. Based on the conditions, optimal formulations were achieved for each type of plasticizer. Evaluation of desirability indicated that the response values were close to the target. When these optimal formulations were validated, the optimal solutions and target values were similar with small biases. The formulations were characterized using scanning electron microscopy, differential scanning calorimetry, Fourier transform infrared spectroscopy, surface pH, in vitro dissolution, and drug release simulation with a mathematical modeling. After the drug was homogenously dispersed throughout the film, the crystalline form of the drug provided strong hydrogen bonds between the drug and the film components. Moreover, it showed a controlled drug release profiles that were well matched with simulated results. This study suggests that the optimized films may present a better alternative to conventional tablets for the treatment of male erectile dysfunction.
Chapter-3. Synthesis and antimicrobial evaluation of ferulic acid derivatives Development and eva... more Chapter-3. Synthesis and antimicrobial evaluation of ferulic acid derivatives Development and evaluation of novel preservatives from simple organic acids 42 3. Synthesis and antimicrobial evaluation of ferulic acid derivatives 3.1 Experimental All reagents and solvents used in study were of analytical grade and procured locally. The progress of the reaction was monitored by TLC and products were purified through recrystallization and purity of the compounds was checked by thin layer chromatography (TLC) performed on silica gel G coated plate. The spectral studies, IR and 1 H NMR were determined by standard methods. Infra red (IR) spectra were recorded on FTIR Bruker ATR instrument in cm-1. 1 H and 13 C nuclear magnetic resonance (1 H and 13 C NMR) spectra were determined using a Bruker Avance II 400 NMR spectrometer in appropriate deuterated solvents and are expressed in parts per million (δ, ppm) downfield from the internal standard TMS. NMR data are provided with multiplicity (s, singlet; d, doublet; t, triplet; m, multiplet) and number of protons. Mass spectra were taken on Bruker Compass Data Analysis 4.0 Mass spectrometer. 3.1.1 Procedure for the synthesis of 8-hydroxy quinoline esters of ferulic acid
Aim : The present investigation evaluated the antimicrobial potential of methanolic extract of Ci... more Aim : The present investigation evaluated the antimicrobial potential of methanolic extract of Citrus sinensis Linn. (Rutaceae) fruit peel. There is a basis for the traditional use of this plant for local health remedies. Materials and Methods: The antimicrobial activity of methanolic extract of C. sinensis fruit peel was tested against three bacterial and two fungal strains. Turbidimetric or tube dilution method and paper disc diffusion method were followed. Results are expressed as mean ± standard deviation. Results: The C. sinensis fruit peel methanolic extract exhibited antibacterial activity against Escherichia coli with minimum inhibitory concentration of 0.78 μg/ ml and minimum bactericidal concentration of 6.25 μg/ml, and appreciable antifungal activity with minimum inhibitory concentration of 12.5 μg/ml. The phytochemistry of C. sinensis fruit peel methanolic extract revealed the presence of carbohydrates (reducing sugars, hexose sugars, non-reducing polysaccharides, gums, and mucilages), flavonoid glycosides, coumarin glycosides, volatile oils, organic acids, fats and fixed oils. Conclusion: Most of the organic chemical constituents reported are aromatic phenolic compounds, which are known for their wide spectra of antimicrobial activity. Therefore, the bacteriostatic and fungistatic action of the tested extract may be attributed to the presence of polyphenolic compounds. In short, C. sinensis fruit peel methanolic extract is a potential source of natural antimicrobials.
A series of p-coumaric acid derivatives (1-36) was synthesized and characterized by physicochemic... more A series of p-coumaric acid derivatives (1-36) was synthesized and characterized by physicochemical as well as spectral means. The synthesized compounds were evaluated in vitro for their antimicrobial activity against different Gram positive and Gram negative bacterial and fungal strains by the tube dilution method. Results of antimicrobial screening indicated that compound 17 was the most active antimicrobial agent (pMIC am = 1.73 lM/mL). The results of QSAR studies demonstrated that antibacterial, antifungal and overall antimicrobial activities of synthesized p-coumaric acid derivatives were governed by the electronic parameter, electronic energy (Ee) and topological parameters first order molecular connectivity index (1 v) and Wiener index (W).
This study was designed to examine the chemical composition and in vitro antimicrobial potential ... more This study was designed to examine the chemical composition and in vitro antimicrobial potential of methanolic extract of Psidium guajava Linn (Myrtaceae). The inhibitory effect of methanolic extract of P. guajava was tested against three bacterial and two fungal strains by using the paper disc diffusion method. The methanolic extract exhibited antibacterial activity against E. coli with minimum inhibitory concentration, 0.78 μg/ml, minimum bactericidal concentration of 50 μg/ml, and appreciable antifungal activity with minimum inhibitory concentration of 12.5 μg/ml. Preliminary phytochemical analysis of methanolic extract revealed the presence of antimicrobial compounds such as flavonoids, steroids, and tannins, which may contribute for the antimicrobial action of P. guajava. The extract was found to be bacteriostatic and fungistatic in action.
Standardisation of herbal formulation is essential in order to assess the quality of drugs, based... more Standardisation of herbal formulation is essential in order to assess the quality of drugs, based on the concentration of their active principles. The present paper reports on standardisation of Panchsakar churna, a polyherbal ayurvedic medicine used as remedy for promoting the elimination of toxins, supporting intestinal immunity and balancing tridosha. It is a combination of simple and routine use herbs, even then their combined effect is great in managing constipation, haemorrhoids and pain in abdomen, flatulence, assimilatory disorder and rheumatic conditions. Panchsakar churna was prepared as per Ayurveda Sarsangrah. In-house preparation and three marketed preparations have been standardised on the basis of organoleptic, physical and physicochemical characteristics. Fluorescence analysis, extractive values and ash values along with sodium content determination and bulk density, tap density, angle of repose, Hausner ratio and Carr's index were calculated. The parameters used to evaluate the churna can be used as reference standards for the quality assessment in laboratory.
Plan: The aim of present study is to find out new preservatives synthesized from natural sources,... more Plan: The aim of present study is to find out new preservatives synthesized from natural sources, which may have better efficiency and stability than the existing synthetic preservatives. The derivatives of naturally occurring gallic, p-coumaric and ferulic acids were subjected to pharmaceutical product for their stability study. Their preservative efficiency was evaluated and compared with the standard parabens. Preface: Deterioration of pharmaceutical preparations due to growth of microorganisms is a great challenge and need of preservation becomes very important. Literature reports about various problems associated with the existing synthetic preservatives such as lack of stability, development of microbial resistance (in due course of time) and several serious side effects. Methodology: The selected amide, anilide and ester derivatives of gallic, p-coumaric and ferulic acids were subjected to stability testing in an official antacid preparation, (aluminium hydroxide gel-USP) against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Candida albicans and Aspergillus niger as representative challenging microorganisms as per ICH guidelines. Outcome: The selected derivatives were found to be effective against all selected strains and showed preservative efficacy comparable to that of standard. The 8-hydroxy quinoline ester derivative of gallic, p-coumaric and ferulic acids showed better stability than other derivatives and may be used as an alternative to existing preservatives in the pharmaceutical preparations.
The objective of the present research work was to establish the various pharmacognostical paramet... more The objective of the present research work was to establish the various pharmacognostical parameters for the Marrubium vulgare Linn (FamilyLamiaceae) collected from the Pulwama district of Jammu and Kashmir region of India. The evaluation of organoleptic, microscopical features (root, stem and leaf) and leaf constant such as vein islet number, vein termination number, stomatal index and palisade ratio aids in detection of adulteration and allied species of the plant. The study of various physicochemical parameters helps in determining the quality of the herb. The higher alcohol soluble extractive value (8.66 ± 1.2%) suggests that most of the constituents of the plant were soluble in alcohol. The total ash acid insoluble ash and water soluble ash was found to be 10.7 ± 0.46, 1.73 ± 0.61, 8.9 ± 0.65 % respectively. The moisture content and total fibre content of the drug was 17.2 ± 0.35 % and 9.5 ± 0.88 % respectively. The plant was also extracted by percolation and microwave assisted...
Cardiovascular & Hematological Agents in Medicinal Chemistry
: Preventing the development of cardiovascular problems is a key objective of antihypertensive dr... more : Preventing the development of cardiovascular problems is a key objective of antihypertensive drugs. Many of the non-pressure related coronary risk factors for hypertension are thought to be connected to an increase in sympathetic activity. The sympathetic systems have N-type calcium channels at the nerve terminals that control neurotransmitter release. Cilnidipine is a unique fourth-generation calcium channel blocker with blocking action on both L-/N- type calcium channels. Several L-type calcium channel blockers (Nilvadipine, amlodipine, azelnidipine, nifedipine, etc.) have been used to treat hypertensive patients. Cilnidipine is a novel drug that exerts a hypotensive effect through vasodilation action via blocking L-type calcium channels and potent anti-sympathetic activity via blocking N-type calcium channels. Inhibiting N-type calcium channels might be a new approach to treating cardiovascular disorders. Therefore, it is expected that cilnidipine may respond well to complicated hypertension. The present review aims to describe the management mechanism of hypertension, and other pharmacological and physicochemical properties of cilnidipine. Cilnidipine has various other beneficial effects such as lipid-lowering effect, reduced white coat effect, improves insulin sensitivity in essential hypertensive patients, ameliorates osteoporosis in ovariectomized hypertensive rats, reduced arterial stiffness, reduced the risk of pedal edema, antinociceptive effects, neuroprotective and renal protective effect, probably through inhibition of N-type calcium channels. Cilnidipine distinguishes itself from other calcium channel blockers due to its wide range of beneficial pharmacological effects. In conclusion, cilnidipine may be more advantageous than dihydropyridines, such as nisoldipine, amlodipine, azelnidipine, and other antihypertensive drugs.
Journal of medical pharmaceutical and allied sciences
Crystallization is a very promising approach to design solid-state properties with desired physic... more Crystallization is a very promising approach to design solid-state properties with desired physicochemical properties. The objective of the present research work was to design, formulate and evaluate Ezetimibe cocrystals. In the present study, Cocrystals of Biopharmaceutics Classification System (BCS) Class II drug, Ezetimibe using 3-pyridine carboxamide as coformer were prepared. 3-pyridine carboxamide was selected as suitable coformer from initial screening. Cocrystals of Ezetimibe with 3-pyridine carboxamide were obtained in 1:1 ratio by solution crystallization method. Hot stage microscopy indicated interaction among drug and coformer. Differential scanning calorimetry spectra of formulated cocrystals reflected shift in endotherm corresponding to melting point in comparison to Ezetimibe, coformer and physical mixture. Fourier transform infrared (FTIR) spectra indicated towards shifting in specific bands characteristic of Ezetimibe. X-Ray Powder Diffraction pattern pointed toward...
Applied Clinical Research, Clinical Trials and Regulatory Affairs, 2020
Background:: Protection of Intellectual Property Rights is a clear incentive to innovations; yet,... more Background:: Protection of Intellectual Property Rights is a clear incentive to innovations; yet, several countries have provided further incentives to patents in pharmaceuticals because the full patent term of 20 years is largely exhausted, before marketing authorization. Objective:: The purpose of this article is to describe the various incentives to patents in the form of financial support, data exclusivity and most importantly extended market exclusivities and comparison of various incentives to patents in the United States of America, European Union and India. Methodology:: The detail of incentives is collected from various articles, latest topics, books, and newspapers. Result:: These incentives create a positive surrounding to encourage the drug development process, strengthen economic growth and improve a balance between new pharmaceuticals in the market and access of that medicine to general public at a reasonable price. Conclusion:: European Union and the United States of ...
International Journal of Applied Pharmaceutics, Nov 7, 2022
Objective: Development of pharmaceutical co-crystals is an interesting area of research as co-cry... more Objective: Development of pharmaceutical co-crystals is an interesting area of research as co-crystals are unique because they have the advantages of maintaining drug's intrinsic properties along with improvement in its physicochemical attributes. Objective of this research was to improvise solubility of a Biopharmaceutics Classification System (BCS) class II drug (Ezetimibe) along with better dissolution profile using cocrystallization technique. Methods: In the present study, pharmaceutical cocrystals of a BCS class II drug, Ezetimibe, were prepared using glycine as coformer using neat grinding method. Prepared cocrystals were characterized using Hot Stage Microscopy (HSM), Differential Scanning Calorimetry (DSC), Fourier Transform Infrared (FTIR) and Powder X-Ray Diffract meter (PXRD). In addition, solubility and dissolution studies were also performed. Results: HSM study and DSC study represented melting at Ezetimibe (166 °C), Glycine (233 °C) and cocrystals (174 °C), respectively. Melting point of cocrystal is between API and coformer, indicating towards interaction. During XRD studies, a new peak was observed at 14.7193 and 23.3211 at position 2θ in comparison to parent peaks of
Purpose: To develop bioadhesive tablets of diltiazem hydrochloride with a unique combination of b... more Purpose: To develop bioadhesive tablets of diltiazem hydrochloride with a unique combination of bioadhesion and drug release. Method: Tablets were prepared by physical blending of diltiazem hydrochloride with two polymers, viz., carbopol and hydroxylpropyl methyl cellulose in different ratio along with other excipients. A 3 2 central composite design was employed to optimize the formulations on the basis of phycochemical properties, bioadhesive strength (measured as force of detachment from gastric mucosa) and in vitro drug release. HPMC K 4M and Carbopol 934P were taken as the independent variables. Contour plots were drawn and optimum formulations were selected by feasibility and grid searches. Results: The tablets showed excellent bioadhesive strength which varied from 7.6 to 21 g. Both polymers had effect on the bioadhesive strength of the tablets and maximum bioadhesion was observed at the highest level of both the polymers. The drug release from the formulation varied from 79.74 to 94.54 % in 12 h. The diffusion exponent (n) of Korsmeyer-Peppas model ranged from 0.491 to 0.658 which indicates the mechanism of drug release was anomalous transport; the diffusion exponent (n) increased with increase in the amount of either polymer in the bioadhesive tablet. Conclusion: Floating bioadhesive tablets of diltiazem hydrochloride with good bioadhesion and controlled release characteristics is feasible.
International Journal of Applied Pharmaceutics, Nov 7, 2022
Objective: Development of pharmaceutical co-crystals is an interesting area of research as co-cry... more Objective: Development of pharmaceutical co-crystals is an interesting area of research as co-crystals are unique because they have the advantages of maintaining drug's intrinsic properties along with improvement in its physicochemical attributes. Objective of this research was to improvise solubility of a Biopharmaceutics Classification System (BCS) class II drug (Ezetimibe) along with better dissolution profile using cocrystallization technique. Methods: In the present study, pharmaceutical cocrystals of a BCS class II drug, Ezetimibe, were prepared using glycine as coformer using neat grinding method. Prepared cocrystals were characterized using Hot Stage Microscopy (HSM), Differential Scanning Calorimetry (DSC), Fourier Transform Infrared (FTIR) and Powder X-Ray Diffract meter (PXRD). In addition, solubility and dissolution studies were also performed. Results: HSM study and DSC study represented melting at Ezetimibe (166 °C), Glycine (233 °C) and cocrystals (174 °C), respectively. Melting point of cocrystal is between API and coformer, indicating towards interaction. During XRD studies, a new peak was observed at 14.7193 and 23.3211 at position 2θ in comparison to parent peaks of
Chapter-4. Synthesis, antimicrobial evaluation and QSAR studies of gallic acid derivatives Develo... more Chapter-4. Synthesis, antimicrobial evaluation and QSAR studies of gallic acid derivatives Development and evaluation of novel preservatives from simple organic acids 55 4. Synthesis, antimicrobial evaluation and QSAR studies of gallic acid derivatives 4.1 Experimental All reagents and solvents used in study were of analytical grade and procured locally. The progress of the reaction was monitored by TLC and products were purified through recrystallization and purity of the compounds was checked by thin layer chromatography (TLC) performed on silica gel G coated plate. The spectral studies, IR and 1 H NMR were determined by standard methods. Infra red (IR) spectra were recorded on FTIR Bruker ATR instrument and was recorded in cm-1. 1 H and 13 C nuclear magnetic resonance (1 H and 13 C NMR) spectra were determined using a Bruker Avance II 400 NMR spectrometer in appropriate deuterated solvents and are expressed in parts per million (δ, ppm) downfield from the internal standard TMS. NMR data are provided with multiplicity (s, singlet; d, doublet; t, triplet; m, multiplet) and number of protons. Mass spectra were taken on Bruker Compass Data Analysis 4.0 Mass spectrometer. 4.1.1. General procedure for the synthesis of 3,4,5-trihydroxybenzoyl chloride Thionyl chloride (0.3 mol) was added gradually to gallic acid (0.25 mol) in a round bottom flask. After addition of thionyl chloride, the mixture was stirred for 4 h and heated to 80 0 C for 30 min in water bath. The excess of thionyl chloride was removed by distillation. 4.1.2. General procedure for the synthesis of amides/anilides of gallic acid The solution of corresponding amine /aniline (0.1 mol) in ether (50mL) was added dropwise to a solution of 3,4,5-trihydroxybenzoyl chloride (0.1 mol, synthesized in previous step) in ether (50 mL) maintained at 0-10 0 C (Scheme 1). The solution was stirred for 30 min and the precipitated amide/anilide was separated by filtration. The crude amide was recrystallized with alcohol. In case of anilides, the precipitated crude anilide was treated with 5% hydrochloric acid, 4% sodium carbonate and water to remove residual aniline and the resultant anilide was recrystallized with alcohol. 4.1.3. Procedure for the synthesis of esters of gallic acid (3
The volatile oil of Cinnamomum zeylanicum Blume, commonly known as cinnamon oil and Ocimum kilima... more The volatile oil of Cinnamomum zeylanicum Blume, commonly known as cinnamon oil and Ocimum kilimandscharicum Baker ex Gurke, commonly known as kapur tulsi oil were subjected to Gas chromatography-Mass spectroscopy (GC-MS) analysis to study their chemical composition. Total eight components of cinnamon oil and eight components of kapur tulsi oil were identified. The major component of cinnamon oil was found to be cinnamaldehyde (91.82%). Minor compounds were found to be 1-8 cineole, muurolene, selinene, geraniol, E-cinnamic acid, vinyl trans-cinnamate. The major component of kapur tulsi oil was found to be camphor (46.14%). Other components were found to be eugenol, 1-8 cineole, limonene, αpinene, camphene, βmyrecene and αterpineol.
A shampoo is a cleaning aid for the hair and is counted among the foremost beauty products. Today... more A shampoo is a cleaning aid for the hair and is counted among the foremost beauty products. Today's shampoo formulations are beyond the stage of pure cleaning of the hair. Additional benefits are expected, e.g, conditioning, smoothing of the hair surface, good health of hair, i.e, hair free of dandruff, dirt, grease and lice and, above all, its safety benefits are expected. As the scalp is one of the most absorbent part of the body, products applied to the scalp go directly to the blood, without being filtered in any way. So it is very important to know and understand the effects of ingredients used in shampoo formulations. In the present review the shampoos based on synthetic ingredients and herbal ingredients are compared for their effectiveness and safety.
In this study, a combination of statistical and analytical approach have been used in the formula... more In this study, a combination of statistical and analytical approach have been used in the formulation development and optimisation guided by “formulation by design” (FbD) for air entrapped microcarriers of alginate of glipizide. Microcarriers of glipizide were prepared by ionotropic-gelation technique, taking concentrations of sodium alginate (SA) and calcium carbonate (CC) as independent variables. The effects of the polymers were evaluated on dependent variables that is drug release (DR), entrapment efficiency (EE), bioadhesive strength (BS), microcarrier size (MS) and total floating time (TFT). Various batches exhibited rough, spherical microcarriers with nominal size variation having sufficient drug EE, very short lag time, while the microcarriers shows the buoyancy over a period of 6–18 hours based on the formulation variables. The DR from the microcarriers was also sustained for more than 10 hours, in 0.1N HCl (pH 1.2). Higuchi’s and the first order kinetic modelling indicated...
Even though experimental designs are becoming popular especially for conventional dosage forms, l... more Even though experimental designs are becoming popular especially for conventional dosage forms, limited studies have been performed to optimize formulations of orally disintegrating films (ODFs). This study aimed to evaluate sildenafil citrate-loaded ODFs for a controlled release with hydroxypropyl methylcellulose as a film-forming polymer. A factorial design was utilized for optimization with three control factors: ethanol ratio, plasticizer ratio, and the type of plasticizer. Tensile strength, disintegration time, water contact angle, and thickness were chosen as responses. For optimization, water contact angle, disintegration time, and thickness were minimized, while the tensile strength was maximized. Based on the conditions, optimal formulations were achieved for each type of plasticizer. Evaluation of desirability indicated that the response values were close to the target. When these optimal formulations were validated, the optimal solutions and target values were similar with small biases. The formulations were characterized using scanning electron microscopy, differential scanning calorimetry, Fourier transform infrared spectroscopy, surface pH, in vitro dissolution, and drug release simulation with a mathematical modeling. After the drug was homogenously dispersed throughout the film, the crystalline form of the drug provided strong hydrogen bonds between the drug and the film components. Moreover, it showed a controlled drug release profiles that were well matched with simulated results. This study suggests that the optimized films may present a better alternative to conventional tablets for the treatment of male erectile dysfunction.
Chapter-3. Synthesis and antimicrobial evaluation of ferulic acid derivatives Development and eva... more Chapter-3. Synthesis and antimicrobial evaluation of ferulic acid derivatives Development and evaluation of novel preservatives from simple organic acids 42 3. Synthesis and antimicrobial evaluation of ferulic acid derivatives 3.1 Experimental All reagents and solvents used in study were of analytical grade and procured locally. The progress of the reaction was monitored by TLC and products were purified through recrystallization and purity of the compounds was checked by thin layer chromatography (TLC) performed on silica gel G coated plate. The spectral studies, IR and 1 H NMR were determined by standard methods. Infra red (IR) spectra were recorded on FTIR Bruker ATR instrument in cm-1. 1 H and 13 C nuclear magnetic resonance (1 H and 13 C NMR) spectra were determined using a Bruker Avance II 400 NMR spectrometer in appropriate deuterated solvents and are expressed in parts per million (δ, ppm) downfield from the internal standard TMS. NMR data are provided with multiplicity (s, singlet; d, doublet; t, triplet; m, multiplet) and number of protons. Mass spectra were taken on Bruker Compass Data Analysis 4.0 Mass spectrometer. 3.1.1 Procedure for the synthesis of 8-hydroxy quinoline esters of ferulic acid
Aim : The present investigation evaluated the antimicrobial potential of methanolic extract of Ci... more Aim : The present investigation evaluated the antimicrobial potential of methanolic extract of Citrus sinensis Linn. (Rutaceae) fruit peel. There is a basis for the traditional use of this plant for local health remedies. Materials and Methods: The antimicrobial activity of methanolic extract of C. sinensis fruit peel was tested against three bacterial and two fungal strains. Turbidimetric or tube dilution method and paper disc diffusion method were followed. Results are expressed as mean ± standard deviation. Results: The C. sinensis fruit peel methanolic extract exhibited antibacterial activity against Escherichia coli with minimum inhibitory concentration of 0.78 μg/ ml and minimum bactericidal concentration of 6.25 μg/ml, and appreciable antifungal activity with minimum inhibitory concentration of 12.5 μg/ml. The phytochemistry of C. sinensis fruit peel methanolic extract revealed the presence of carbohydrates (reducing sugars, hexose sugars, non-reducing polysaccharides, gums, and mucilages), flavonoid glycosides, coumarin glycosides, volatile oils, organic acids, fats and fixed oils. Conclusion: Most of the organic chemical constituents reported are aromatic phenolic compounds, which are known for their wide spectra of antimicrobial activity. Therefore, the bacteriostatic and fungistatic action of the tested extract may be attributed to the presence of polyphenolic compounds. In short, C. sinensis fruit peel methanolic extract is a potential source of natural antimicrobials.
A series of p-coumaric acid derivatives (1-36) was synthesized and characterized by physicochemic... more A series of p-coumaric acid derivatives (1-36) was synthesized and characterized by physicochemical as well as spectral means. The synthesized compounds were evaluated in vitro for their antimicrobial activity against different Gram positive and Gram negative bacterial and fungal strains by the tube dilution method. Results of antimicrobial screening indicated that compound 17 was the most active antimicrobial agent (pMIC am = 1.73 lM/mL). The results of QSAR studies demonstrated that antibacterial, antifungal and overall antimicrobial activities of synthesized p-coumaric acid derivatives were governed by the electronic parameter, electronic energy (Ee) and topological parameters first order molecular connectivity index (1 v) and Wiener index (W).
This study was designed to examine the chemical composition and in vitro antimicrobial potential ... more This study was designed to examine the chemical composition and in vitro antimicrobial potential of methanolic extract of Psidium guajava Linn (Myrtaceae). The inhibitory effect of methanolic extract of P. guajava was tested against three bacterial and two fungal strains by using the paper disc diffusion method. The methanolic extract exhibited antibacterial activity against E. coli with minimum inhibitory concentration, 0.78 μg/ml, minimum bactericidal concentration of 50 μg/ml, and appreciable antifungal activity with minimum inhibitory concentration of 12.5 μg/ml. Preliminary phytochemical analysis of methanolic extract revealed the presence of antimicrobial compounds such as flavonoids, steroids, and tannins, which may contribute for the antimicrobial action of P. guajava. The extract was found to be bacteriostatic and fungistatic in action.
Standardisation of herbal formulation is essential in order to assess the quality of drugs, based... more Standardisation of herbal formulation is essential in order to assess the quality of drugs, based on the concentration of their active principles. The present paper reports on standardisation of Panchsakar churna, a polyherbal ayurvedic medicine used as remedy for promoting the elimination of toxins, supporting intestinal immunity and balancing tridosha. It is a combination of simple and routine use herbs, even then their combined effect is great in managing constipation, haemorrhoids and pain in abdomen, flatulence, assimilatory disorder and rheumatic conditions. Panchsakar churna was prepared as per Ayurveda Sarsangrah. In-house preparation and three marketed preparations have been standardised on the basis of organoleptic, physical and physicochemical characteristics. Fluorescence analysis, extractive values and ash values along with sodium content determination and bulk density, tap density, angle of repose, Hausner ratio and Carr's index were calculated. The parameters used to evaluate the churna can be used as reference standards for the quality assessment in laboratory.
Plan: The aim of present study is to find out new preservatives synthesized from natural sources,... more Plan: The aim of present study is to find out new preservatives synthesized from natural sources, which may have better efficiency and stability than the existing synthetic preservatives. The derivatives of naturally occurring gallic, p-coumaric and ferulic acids were subjected to pharmaceutical product for their stability study. Their preservative efficiency was evaluated and compared with the standard parabens. Preface: Deterioration of pharmaceutical preparations due to growth of microorganisms is a great challenge and need of preservation becomes very important. Literature reports about various problems associated with the existing synthetic preservatives such as lack of stability, development of microbial resistance (in due course of time) and several serious side effects. Methodology: The selected amide, anilide and ester derivatives of gallic, p-coumaric and ferulic acids were subjected to stability testing in an official antacid preparation, (aluminium hydroxide gel-USP) against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Candida albicans and Aspergillus niger as representative challenging microorganisms as per ICH guidelines. Outcome: The selected derivatives were found to be effective against all selected strains and showed preservative efficacy comparable to that of standard. The 8-hydroxy quinoline ester derivative of gallic, p-coumaric and ferulic acids showed better stability than other derivatives and may be used as an alternative to existing preservatives in the pharmaceutical preparations.
The objective of the present research work was to establish the various pharmacognostical paramet... more The objective of the present research work was to establish the various pharmacognostical parameters for the Marrubium vulgare Linn (FamilyLamiaceae) collected from the Pulwama district of Jammu and Kashmir region of India. The evaluation of organoleptic, microscopical features (root, stem and leaf) and leaf constant such as vein islet number, vein termination number, stomatal index and palisade ratio aids in detection of adulteration and allied species of the plant. The study of various physicochemical parameters helps in determining the quality of the herb. The higher alcohol soluble extractive value (8.66 ± 1.2%) suggests that most of the constituents of the plant were soluble in alcohol. The total ash acid insoluble ash and water soluble ash was found to be 10.7 ± 0.46, 1.73 ± 0.61, 8.9 ± 0.65 % respectively. The moisture content and total fibre content of the drug was 17.2 ± 0.35 % and 9.5 ± 0.88 % respectively. The plant was also extracted by percolation and microwave assisted...
Cardiovascular & Hematological Agents in Medicinal Chemistry
: Preventing the development of cardiovascular problems is a key objective of antihypertensive dr... more : Preventing the development of cardiovascular problems is a key objective of antihypertensive drugs. Many of the non-pressure related coronary risk factors for hypertension are thought to be connected to an increase in sympathetic activity. The sympathetic systems have N-type calcium channels at the nerve terminals that control neurotransmitter release. Cilnidipine is a unique fourth-generation calcium channel blocker with blocking action on both L-/N- type calcium channels. Several L-type calcium channel blockers (Nilvadipine, amlodipine, azelnidipine, nifedipine, etc.) have been used to treat hypertensive patients. Cilnidipine is a novel drug that exerts a hypotensive effect through vasodilation action via blocking L-type calcium channels and potent anti-sympathetic activity via blocking N-type calcium channels. Inhibiting N-type calcium channels might be a new approach to treating cardiovascular disorders. Therefore, it is expected that cilnidipine may respond well to complicated hypertension. The present review aims to describe the management mechanism of hypertension, and other pharmacological and physicochemical properties of cilnidipine. Cilnidipine has various other beneficial effects such as lipid-lowering effect, reduced white coat effect, improves insulin sensitivity in essential hypertensive patients, ameliorates osteoporosis in ovariectomized hypertensive rats, reduced arterial stiffness, reduced the risk of pedal edema, antinociceptive effects, neuroprotective and renal protective effect, probably through inhibition of N-type calcium channels. Cilnidipine distinguishes itself from other calcium channel blockers due to its wide range of beneficial pharmacological effects. In conclusion, cilnidipine may be more advantageous than dihydropyridines, such as nisoldipine, amlodipine, azelnidipine, and other antihypertensive drugs.
Journal of medical pharmaceutical and allied sciences
Crystallization is a very promising approach to design solid-state properties with desired physic... more Crystallization is a very promising approach to design solid-state properties with desired physicochemical properties. The objective of the present research work was to design, formulate and evaluate Ezetimibe cocrystals. In the present study, Cocrystals of Biopharmaceutics Classification System (BCS) Class II drug, Ezetimibe using 3-pyridine carboxamide as coformer were prepared. 3-pyridine carboxamide was selected as suitable coformer from initial screening. Cocrystals of Ezetimibe with 3-pyridine carboxamide were obtained in 1:1 ratio by solution crystallization method. Hot stage microscopy indicated interaction among drug and coformer. Differential scanning calorimetry spectra of formulated cocrystals reflected shift in endotherm corresponding to melting point in comparison to Ezetimibe, coformer and physical mixture. Fourier transform infrared (FTIR) spectra indicated towards shifting in specific bands characteristic of Ezetimibe. X-Ray Powder Diffraction pattern pointed toward...
Applied Clinical Research, Clinical Trials and Regulatory Affairs, 2020
Background:: Protection of Intellectual Property Rights is a clear incentive to innovations; yet,... more Background:: Protection of Intellectual Property Rights is a clear incentive to innovations; yet, several countries have provided further incentives to patents in pharmaceuticals because the full patent term of 20 years is largely exhausted, before marketing authorization. Objective:: The purpose of this article is to describe the various incentives to patents in the form of financial support, data exclusivity and most importantly extended market exclusivities and comparison of various incentives to patents in the United States of America, European Union and India. Methodology:: The detail of incentives is collected from various articles, latest topics, books, and newspapers. Result:: These incentives create a positive surrounding to encourage the drug development process, strengthen economic growth and improve a balance between new pharmaceuticals in the market and access of that medicine to general public at a reasonable price. Conclusion:: European Union and the United States of ...
International Journal of Applied Pharmaceutics, Nov 7, 2022
Objective: Development of pharmaceutical co-crystals is an interesting area of research as co-cry... more Objective: Development of pharmaceutical co-crystals is an interesting area of research as co-crystals are unique because they have the advantages of maintaining drug's intrinsic properties along with improvement in its physicochemical attributes. Objective of this research was to improvise solubility of a Biopharmaceutics Classification System (BCS) class II drug (Ezetimibe) along with better dissolution profile using cocrystallization technique. Methods: In the present study, pharmaceutical cocrystals of a BCS class II drug, Ezetimibe, were prepared using glycine as coformer using neat grinding method. Prepared cocrystals were characterized using Hot Stage Microscopy (HSM), Differential Scanning Calorimetry (DSC), Fourier Transform Infrared (FTIR) and Powder X-Ray Diffract meter (PXRD). In addition, solubility and dissolution studies were also performed. Results: HSM study and DSC study represented melting at Ezetimibe (166 °C), Glycine (233 °C) and cocrystals (174 °C), respectively. Melting point of cocrystal is between API and coformer, indicating towards interaction. During XRD studies, a new peak was observed at 14.7193 and 23.3211 at position 2θ in comparison to parent peaks of
Purpose: To develop bioadhesive tablets of diltiazem hydrochloride with a unique combination of b... more Purpose: To develop bioadhesive tablets of diltiazem hydrochloride with a unique combination of bioadhesion and drug release. Method: Tablets were prepared by physical blending of diltiazem hydrochloride with two polymers, viz., carbopol and hydroxylpropyl methyl cellulose in different ratio along with other excipients. A 3 2 central composite design was employed to optimize the formulations on the basis of phycochemical properties, bioadhesive strength (measured as force of detachment from gastric mucosa) and in vitro drug release. HPMC K 4M and Carbopol 934P were taken as the independent variables. Contour plots were drawn and optimum formulations were selected by feasibility and grid searches. Results: The tablets showed excellent bioadhesive strength which varied from 7.6 to 21 g. Both polymers had effect on the bioadhesive strength of the tablets and maximum bioadhesion was observed at the highest level of both the polymers. The drug release from the formulation varied from 79.74 to 94.54 % in 12 h. The diffusion exponent (n) of Korsmeyer-Peppas model ranged from 0.491 to 0.658 which indicates the mechanism of drug release was anomalous transport; the diffusion exponent (n) increased with increase in the amount of either polymer in the bioadhesive tablet. Conclusion: Floating bioadhesive tablets of diltiazem hydrochloride with good bioadhesion and controlled release characteristics is feasible.
Uploads
Papers by Arun Nanda