A series of novel 2-(4-substituted-piperazinyl-methyl)-3-(N-isonicotinamide-yl)-quinazoline- 4-on... more A series of novel 2-(4-substituted-piperazinyl-methyl)-3-(N-isonicotinamide-yl)-quinazoline- 4-one 4a-l were designed, synthesized, characterized and evaluated for in vitro antitubercular, antibacterial and antifungal activity. Compounds 4f , 4h and 4l exhibited excellent antitubercular activity against mycobacterium tuberculosis H 37 Rv .
A facile synthesis of 3-[(4-chloro-3-methylphenoxy)methyl]-6-aryl-5,6-dihydro-[1,2,4]triazolo[3,4... more A facile synthesis of 3-[(4-chloro-3-methylphenoxy)methyl]-6-aryl-5,6-dihydro-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles 3a-n has been achieved by microwave promoted condensation of 3-mercapto-4-amino-5-[(4-chloro-3-methylphenoxy)methyl]-4H-1,2,4-triazole 1 with various aromatic aldehydes 2a-n in presence of catalytic amount of p-TsOH (para-toluenesulphonic acid). The structures of 3a-n are supported by IR and 1 H and 13 C NMR spectral data.
Phosphorus Sulfur and Silicon and The Related Elements, Jan 5, 2012
Using an environmentally benign procedure under microwave irradiation, a variety of 4-methyl-N-(4... more Using an environmentally benign procedure under microwave irradiation, a variety of 4-methyl-N-(4-(2-oxo-2H-chromen-3-yl)thiazol-2-yl)-2-substituted phenyl-2,3-dihydrobenzo [b][1,4]thiazepine-3-carboxamide compounds were synthesized from 2-arylidene-3-oxo-N-(4-(2-oxo-2H-chromen-3-yl)thiazol-2-yl)butanamide. Structures of these compounds were confirmed by IR, NMR (H & C), and mass spectral analyses. Also, a considerable increase in the reaction rate has been observed with better yield in the microwave technique. The newly synthesized compounds were evaluated for antimicrobial activity against a variety of bacterial strains, and some of these compounds have shown significant antibacterial and antifungal activities.Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements for the following free supplemental resource: Biological Activity.
Abstract Carbon nanotubes (CNTs) possess excellent properties in terms of their unique physicoche... more Abstract Carbon nanotubes (CNTs) possess excellent properties in terms of their unique physicochemical properties and excellent architecture which make these as an alternative carrier for the delivery of various pharmaceutical ingredients. This chapter focuses on description of CNTs in terms of their types, methods for preparation, applications and recent progress in the field of drug delivery. Chapter has been divided into two sections, first section covers several types of carbon nanotubes, different properties of the carbon nanotubes, methods for the preparation of CNTs and applications thereof. Later section of the chapter contains potential use of CNTs in the drug delivery systems and the current progress in their research fields.
Abstract The unique properties of nanocomposites have attracted research interest, especially in ... more Abstract The unique properties of nanocomposites have attracted research interest, especially in tissue engineering applications owing to their properties. Nano-hydroxyapatite is a widely used bioceramic material for bone graft substitute owing to its biocompatibility and osteoconductive properties. The different types of hydroxyapatite nanocomposites—ceramics, metals, and polymers have allowed their use in biomedical fields such as bone tissue engineering. This enables a wide range of properties to be incorporated into nanocomposite materials and also into drug delivery system. The aim of this chapter is to focus on the main applications on tissue repair and regeneration. The first part discusses the classification of nanocomposites and thereafter the applications related to that specific area of research is mentioned.
Applications of Nanocomposite Materials in Drug Delivery, 2018
Abstract Carbon nanotubes (CNTs) possess excellent properties in terms of their unique physicoche... more Abstract Carbon nanotubes (CNTs) possess excellent properties in terms of their unique physicochemical properties and excellent architecture which make these as an alternative carrier for the delivery of various pharmaceutical ingredients. This chapter focuses on description of CNTs in terms of their types, methods for preparation, applications and recent progress in the field of drug delivery. Chapter has been divided into two sections, first section covers several types of carbon nanotubes, different properties of the carbon nanotubes, methods for the preparation of CNTs and applications thereof. Later section of the chapter contains potential use of CNTs in the drug delivery systems and the current progress in their research fields.
International Journal of Pharmaceutical Sciences and Nanotechnology, 2012
Designing and evaluating a multiparticulate controlled release dosage form, to increase the effic... more Designing and evaluating a multiparticulate controlled release dosage form, to increase the efficacy of acyclovir (a selective antiherpes agent). Spray drying technique for microsphere production is compared with novel solvent evaporation-matrix erosion technique for variable drug loading in different concentration of ethyl cellulose. The microspheres were characterized for physicochemical properties. The microspheres sizes were ranged from 7-25 μm. The spray dried microspheres had better encapsulation efficiency (up to 91%) compared to that of novel solvent evaporation-matrix erosion technique microspheres. Scanning electron microscopy confirmed spherical geometry due to high cross-linking density. Differential scanning calorimetry, Fourier-transform infrared spectroscopy and x-ray diffraction studies showed chemical stability and intactness of entrapped drug in the microspheres. In vitro release of acyclovir from spray dried microspheres continued for longer period compared to nov...
Expeditious greener approach for the synthesis of aryl thioamide derivatives is reported. The syn... more Expeditious greener approach for the synthesis of aryl thioamide derivatives is reported. The synthetic strategy involves the reaction of aromatic carboxylic acids and thiourea in presence of Ammonium cerric nitrate as a catalyst with or without the help of ultrasound. A comparative study was done between both the synthetic methodologies. It was found that the high yield of the product in shorter reaction time was achieved in ultrasound technique.
Page 1. Vol.3 Issue 2, April‐June 2010 ISSN 0974‐2441 Asian Journal of Pharmaceutical and Clinica... more Page 1. Vol.3 Issue 2, April‐June 2010 ISSN 0974‐2441 Asian Journal of Pharmaceutical and Clinical Research Page 80 REVIEW ON THE PHARMACEUTICAL APPLICATIONS OF HOT MELT EXTRUDER Pradip S Patel*, Jignesh P Raval, Hemul V Patel ...
The unique properties of nanocomposites have attracted research interest, especially in tissue en... more The unique properties of nanocomposites have attracted research interest, especially in tissue engineering applications owing to their properties. Nano-hydroxyapatite is a widely used bioceramic material for bone graft substitute owing to its biocompatibility and osteoconductive properties. The different types of hydroxyapatite nanocomposites—ceramics, metals, and polymers have allowed their use in biomedical fields such as bone tissue engineering. This enables a wide range of properties to be incorporated into nanocomposite materials and also into drug delivery system. The aim of this chapter is to focus on the main applications on tissue repair and regeneration. The first part discusses the classification of nanocomposites and thereafter the applications related to that specific area of research is mentioned.
The aim of the present research was to prepare orodispersible tablets of Lamotrigine for applicat... more The aim of the present research was to prepare orodispersible tablets of Lamotrigine for applications in epilepsy and convulsion related problems. Fast action onset is highly desirable in the control of this type of disease condition. All tablets were prepared by solid dispersion method using mannitol and synthetic superdisintegrants like Explotab, Cross Povidone and Micro Crystalline Cellulose. The different powder blends were evaluated for pre-formulation parameters. Effect of superdisintegrants on wetting, disintegration and dissolution parameters was studied. The tablets were evaluated for various parameters like wetting time, hardness, friability, drug content, disintegration and in vitro dissolution. Tablets with Explotab have shown good disintegrating features, also the dispersion not showing any bitter taste; indicate the capability of Vanilla used, as taste masking agents. Almost more than 99% of drug was released from the formulation(F4) within 27 min. Tablets have shown n...
Doxycycline hyclate (DH), one of the bacteriostatic drugs is an effective ingredient against many... more Doxycycline hyclate (DH), one of the bacteriostatic drugs is an effective ingredient against many bacteria. It is used to treat bacterial infections such as urinary tract infection, upper respiratory tract infection, acne, gonorrhea, chlamydia and anthrax, etc. DH generally works by stopping protein synthesis of the particular bacteria as well as protozoans. Presently, several drug delivery systems based on micro particulates/nano particulates systems are available. In this chapter, pharmacotherapeutics of DH and current drug delivery systems are discussed in details. Further, chapter also demonstrates how in situ gelling systems can make drug therapy so facile with special reference to the drug. The key advantage of in situ gelling systems is the possibility of administering accurate and reproducible quantities of drug molecule in contrast to already gelled formulations as well as that of micro/nano particulate systems.
Journal of Pharmaceutical Sciences & Emerging Drugs, 2014
Release Kinetics of Cellulosic Nano particulate Formulation forOral Administration of anAntiviral... more Release Kinetics of Cellulosic Nano particulate Formulation forOral Administration of anAntiviral Drug: Effect of Process and Formulation variables Recently, researchers have increasing interest in cellulosic polymers for optimizing the efficiency of existing drugs utilizing better-designed drug delivery systems. In the present research nanoparticles were prepared using cellulose esters to obtain a drug product with a good oral bioavailability and biological half life. Acyclovir (ACY) was formulated by combining the modified solvent evaporation/extraction technique, sonicator and high pressure homogenization approaches. Various formulation parameters such as sonication-time, concentration of cellulose esters and surfactants were studied. Nanoparticles were obtained with enhanced encapsulation efficiency, negatively charged, defined shape, size and with homogeneous size distribution.
Novel biobased polyurethanes from soyabean oil-derived polyols, soyabean oil phosphate ester poly... more Novel biobased polyurethanes from soyabean oil-derived polyols, soyabean oil phosphate ester polyol (SOPE), blending of SOPE with monoglyceride of soyabean oil (SOPESG) and blending of SOPE with polyethylene glycol 400 mol. wt (SOPEP14) using aromatic isocynate adduct(TDI-TMP) were prepared and their dynamic mechanical properties were investigated after casting sheets on glass plate. The results showed that the damping ability gets enhanced through the introduction of monoglyceride and PEG-400 in to the base resin system.
Page 1. Asian J. Research Chem. 2(2): April.-June, 2009 , 171 ISSN 0974-4169 www.ajrconline.org R... more Page 1. Asian J. Research Chem. 2(2): April.-June, 2009 , 171 ISSN 0974-4169 www.ajrconline.org RESEARCH ARTICLE A Rapid, Convenient Microwave assisted and Conventional Synthesis of novel azetidin-2-one derivatives as Potent Antimicrobial agents ...
Formazans 5a-m have been prepared by the condensation of Schiff base 3 and diazonium salt of subs... more Formazans 5a-m have been prepared by the condensation of Schiff base 3 and diazonium salt of substituted aromatic amines, 4a-m. The intermediate Schiffbase, 3 was itself synthesized by condensation of isonicotinic acid hydrazide, 1 with p-methoxybenzaldehyde, 2. The structures of the compound have been confirmed by elemental analysis and spectral analysis. The antibacterial activity of the compounds has also been screened.
A series of spiro[pyrrolidin-2,3 0-oxindoles] has been synthesized by exo-selective 1,3-dipolar c... more A series of spiro[pyrrolidin-2,3 0-oxindoles] has been synthesized by exo-selective 1,3-dipolar cycloaddition reaction of a stabilized azomethine ylide, generated in situ by thermal [1,5]-prototropy, across various (E)-3-arylidene-1-phenyl-pyrrolidine-2,5-diones. The stereochemistry of these N-heterocycles has been confirmed using an X-ray diffraction study. To rationalize the observed regio-and stereoselectivity, DFT calculations at the B3LYP/6-31G(d,p) level were employed. It was found that this reaction preferentially affords the kinetic product. The compounds have been screened for their in vitro antibacterial, antifungal, antimalarial and antitubercular activities. Several compounds exhibited good activities comparable to those of established standard drugs.
A series of novel 2-(4-substituted-piperazinyl-methyl)-3-(N-isonicotinamide-yl)-quinazoline- 4-on... more A series of novel 2-(4-substituted-piperazinyl-methyl)-3-(N-isonicotinamide-yl)-quinazoline- 4-one 4a-l were designed, synthesized, characterized and evaluated for in vitro antitubercular, antibacterial and antifungal activity. Compounds 4f , 4h and 4l exhibited excellent antitubercular activity against mycobacterium tuberculosis H 37 Rv .
A facile synthesis of 3-[(4-chloro-3-methylphenoxy)methyl]-6-aryl-5,6-dihydro-[1,2,4]triazolo[3,4... more A facile synthesis of 3-[(4-chloro-3-methylphenoxy)methyl]-6-aryl-5,6-dihydro-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles 3a-n has been achieved by microwave promoted condensation of 3-mercapto-4-amino-5-[(4-chloro-3-methylphenoxy)methyl]-4H-1,2,4-triazole 1 with various aromatic aldehydes 2a-n in presence of catalytic amount of p-TsOH (para-toluenesulphonic acid). The structures of 3a-n are supported by IR and 1 H and 13 C NMR spectral data.
Phosphorus Sulfur and Silicon and The Related Elements, Jan 5, 2012
Using an environmentally benign procedure under microwave irradiation, a variety of 4-methyl-N-(4... more Using an environmentally benign procedure under microwave irradiation, a variety of 4-methyl-N-(4-(2-oxo-2H-chromen-3-yl)thiazol-2-yl)-2-substituted phenyl-2,3-dihydrobenzo [b][1,4]thiazepine-3-carboxamide compounds were synthesized from 2-arylidene-3-oxo-N-(4-(2-oxo-2H-chromen-3-yl)thiazol-2-yl)butanamide. Structures of these compounds were confirmed by IR, NMR (H & C), and mass spectral analyses. Also, a considerable increase in the reaction rate has been observed with better yield in the microwave technique. The newly synthesized compounds were evaluated for antimicrobial activity against a variety of bacterial strains, and some of these compounds have shown significant antibacterial and antifungal activities.Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements for the following free supplemental resource: Biological Activity.
Abstract Carbon nanotubes (CNTs) possess excellent properties in terms of their unique physicoche... more Abstract Carbon nanotubes (CNTs) possess excellent properties in terms of their unique physicochemical properties and excellent architecture which make these as an alternative carrier for the delivery of various pharmaceutical ingredients. This chapter focuses on description of CNTs in terms of their types, methods for preparation, applications and recent progress in the field of drug delivery. Chapter has been divided into two sections, first section covers several types of carbon nanotubes, different properties of the carbon nanotubes, methods for the preparation of CNTs and applications thereof. Later section of the chapter contains potential use of CNTs in the drug delivery systems and the current progress in their research fields.
Abstract The unique properties of nanocomposites have attracted research interest, especially in ... more Abstract The unique properties of nanocomposites have attracted research interest, especially in tissue engineering applications owing to their properties. Nano-hydroxyapatite is a widely used bioceramic material for bone graft substitute owing to its biocompatibility and osteoconductive properties. The different types of hydroxyapatite nanocomposites—ceramics, metals, and polymers have allowed their use in biomedical fields such as bone tissue engineering. This enables a wide range of properties to be incorporated into nanocomposite materials and also into drug delivery system. The aim of this chapter is to focus on the main applications on tissue repair and regeneration. The first part discusses the classification of nanocomposites and thereafter the applications related to that specific area of research is mentioned.
Applications of Nanocomposite Materials in Drug Delivery, 2018
Abstract Carbon nanotubes (CNTs) possess excellent properties in terms of their unique physicoche... more Abstract Carbon nanotubes (CNTs) possess excellent properties in terms of their unique physicochemical properties and excellent architecture which make these as an alternative carrier for the delivery of various pharmaceutical ingredients. This chapter focuses on description of CNTs in terms of their types, methods for preparation, applications and recent progress in the field of drug delivery. Chapter has been divided into two sections, first section covers several types of carbon nanotubes, different properties of the carbon nanotubes, methods for the preparation of CNTs and applications thereof. Later section of the chapter contains potential use of CNTs in the drug delivery systems and the current progress in their research fields.
International Journal of Pharmaceutical Sciences and Nanotechnology, 2012
Designing and evaluating a multiparticulate controlled release dosage form, to increase the effic... more Designing and evaluating a multiparticulate controlled release dosage form, to increase the efficacy of acyclovir (a selective antiherpes agent). Spray drying technique for microsphere production is compared with novel solvent evaporation-matrix erosion technique for variable drug loading in different concentration of ethyl cellulose. The microspheres were characterized for physicochemical properties. The microspheres sizes were ranged from 7-25 μm. The spray dried microspheres had better encapsulation efficiency (up to 91%) compared to that of novel solvent evaporation-matrix erosion technique microspheres. Scanning electron microscopy confirmed spherical geometry due to high cross-linking density. Differential scanning calorimetry, Fourier-transform infrared spectroscopy and x-ray diffraction studies showed chemical stability and intactness of entrapped drug in the microspheres. In vitro release of acyclovir from spray dried microspheres continued for longer period compared to nov...
Expeditious greener approach for the synthesis of aryl thioamide derivatives is reported. The syn... more Expeditious greener approach for the synthesis of aryl thioamide derivatives is reported. The synthetic strategy involves the reaction of aromatic carboxylic acids and thiourea in presence of Ammonium cerric nitrate as a catalyst with or without the help of ultrasound. A comparative study was done between both the synthetic methodologies. It was found that the high yield of the product in shorter reaction time was achieved in ultrasound technique.
Page 1. Vol.3 Issue 2, April‐June 2010 ISSN 0974‐2441 Asian Journal of Pharmaceutical and Clinica... more Page 1. Vol.3 Issue 2, April‐June 2010 ISSN 0974‐2441 Asian Journal of Pharmaceutical and Clinical Research Page 80 REVIEW ON THE PHARMACEUTICAL APPLICATIONS OF HOT MELT EXTRUDER Pradip S Patel*, Jignesh P Raval, Hemul V Patel ...
The unique properties of nanocomposites have attracted research interest, especially in tissue en... more The unique properties of nanocomposites have attracted research interest, especially in tissue engineering applications owing to their properties. Nano-hydroxyapatite is a widely used bioceramic material for bone graft substitute owing to its biocompatibility and osteoconductive properties. The different types of hydroxyapatite nanocomposites—ceramics, metals, and polymers have allowed their use in biomedical fields such as bone tissue engineering. This enables a wide range of properties to be incorporated into nanocomposite materials and also into drug delivery system. The aim of this chapter is to focus on the main applications on tissue repair and regeneration. The first part discusses the classification of nanocomposites and thereafter the applications related to that specific area of research is mentioned.
The aim of the present research was to prepare orodispersible tablets of Lamotrigine for applicat... more The aim of the present research was to prepare orodispersible tablets of Lamotrigine for applications in epilepsy and convulsion related problems. Fast action onset is highly desirable in the control of this type of disease condition. All tablets were prepared by solid dispersion method using mannitol and synthetic superdisintegrants like Explotab, Cross Povidone and Micro Crystalline Cellulose. The different powder blends were evaluated for pre-formulation parameters. Effect of superdisintegrants on wetting, disintegration and dissolution parameters was studied. The tablets were evaluated for various parameters like wetting time, hardness, friability, drug content, disintegration and in vitro dissolution. Tablets with Explotab have shown good disintegrating features, also the dispersion not showing any bitter taste; indicate the capability of Vanilla used, as taste masking agents. Almost more than 99% of drug was released from the formulation(F4) within 27 min. Tablets have shown n...
Doxycycline hyclate (DH), one of the bacteriostatic drugs is an effective ingredient against many... more Doxycycline hyclate (DH), one of the bacteriostatic drugs is an effective ingredient against many bacteria. It is used to treat bacterial infections such as urinary tract infection, upper respiratory tract infection, acne, gonorrhea, chlamydia and anthrax, etc. DH generally works by stopping protein synthesis of the particular bacteria as well as protozoans. Presently, several drug delivery systems based on micro particulates/nano particulates systems are available. In this chapter, pharmacotherapeutics of DH and current drug delivery systems are discussed in details. Further, chapter also demonstrates how in situ gelling systems can make drug therapy so facile with special reference to the drug. The key advantage of in situ gelling systems is the possibility of administering accurate and reproducible quantities of drug molecule in contrast to already gelled formulations as well as that of micro/nano particulate systems.
Journal of Pharmaceutical Sciences & Emerging Drugs, 2014
Release Kinetics of Cellulosic Nano particulate Formulation forOral Administration of anAntiviral... more Release Kinetics of Cellulosic Nano particulate Formulation forOral Administration of anAntiviral Drug: Effect of Process and Formulation variables Recently, researchers have increasing interest in cellulosic polymers for optimizing the efficiency of existing drugs utilizing better-designed drug delivery systems. In the present research nanoparticles were prepared using cellulose esters to obtain a drug product with a good oral bioavailability and biological half life. Acyclovir (ACY) was formulated by combining the modified solvent evaporation/extraction technique, sonicator and high pressure homogenization approaches. Various formulation parameters such as sonication-time, concentration of cellulose esters and surfactants were studied. Nanoparticles were obtained with enhanced encapsulation efficiency, negatively charged, defined shape, size and with homogeneous size distribution.
Novel biobased polyurethanes from soyabean oil-derived polyols, soyabean oil phosphate ester poly... more Novel biobased polyurethanes from soyabean oil-derived polyols, soyabean oil phosphate ester polyol (SOPE), blending of SOPE with monoglyceride of soyabean oil (SOPESG) and blending of SOPE with polyethylene glycol 400 mol. wt (SOPEP14) using aromatic isocynate adduct(TDI-TMP) were prepared and their dynamic mechanical properties were investigated after casting sheets on glass plate. The results showed that the damping ability gets enhanced through the introduction of monoglyceride and PEG-400 in to the base resin system.
Page 1. Asian J. Research Chem. 2(2): April.-June, 2009 , 171 ISSN 0974-4169 www.ajrconline.org R... more Page 1. Asian J. Research Chem. 2(2): April.-June, 2009 , 171 ISSN 0974-4169 www.ajrconline.org RESEARCH ARTICLE A Rapid, Convenient Microwave assisted and Conventional Synthesis of novel azetidin-2-one derivatives as Potent Antimicrobial agents ...
Formazans 5a-m have been prepared by the condensation of Schiff base 3 and diazonium salt of subs... more Formazans 5a-m have been prepared by the condensation of Schiff base 3 and diazonium salt of substituted aromatic amines, 4a-m. The intermediate Schiffbase, 3 was itself synthesized by condensation of isonicotinic acid hydrazide, 1 with p-methoxybenzaldehyde, 2. The structures of the compound have been confirmed by elemental analysis and spectral analysis. The antibacterial activity of the compounds has also been screened.
A series of spiro[pyrrolidin-2,3 0-oxindoles] has been synthesized by exo-selective 1,3-dipolar c... more A series of spiro[pyrrolidin-2,3 0-oxindoles] has been synthesized by exo-selective 1,3-dipolar cycloaddition reaction of a stabilized azomethine ylide, generated in situ by thermal [1,5]-prototropy, across various (E)-3-arylidene-1-phenyl-pyrrolidine-2,5-diones. The stereochemistry of these N-heterocycles has been confirmed using an X-ray diffraction study. To rationalize the observed regio-and stereoselectivity, DFT calculations at the B3LYP/6-31G(d,p) level were employed. It was found that this reaction preferentially affords the kinetic product. The compounds have been screened for their in vitro antibacterial, antifungal, antimalarial and antitubercular activities. Several compounds exhibited good activities comparable to those of established standard drugs.
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