Raghupathi Kandarapu - Academia.edu (original) (raw)
Papers by Raghupathi Kandarapu
Using furosemide (FU) as a model drug, we examined the wet granulation method as a way to improve... more Using furosemide (FU) as a model drug, we examined the wet granulation method as a way to improve the taste masking and physical characteristics of orally disintegrating tablets (ODTs). In the wet granulation method, yogurt powder (YO) was used as a corrective and maltitol (MA) was used as a binding agent. The taste masked FU tablets were prepared using the direct compression method. Microcrystalline cellulose (AvicelPH-302) and mannitol were added as excipients at a mixing ratio of 1/1 by weight. Based on the results of sensory test on taste, the prepared granules markedly improved the taste of FU, and a su‹cient masking eŠect was obtained at the YO/FU ratio of 1 or more. Furthermore, it was found that the masking eŠect achieved by YO granules made with the wet granulation method was similar to or better than that produced by the granules made with dry granulation method. All types of tablets displayed su‹cient hardness (over 3.5×10-2 kN), and rapidly disintegrating tablets were obtained with YO granules produced at a mixing ratio of FU/YO＝1/1, which disintegrated within 20 s. Disintegration time lengthened as the mixing ratio of YO to FU increased. In the mixing ratio of FU/YO＝1/1, the hardness of tablets with granules made by the wet granulation method exceeded that of tablets with granules made by the dry granulation method, with minimal diŠerences in disintegration time. The hardness and disintegration time of the tablets with granules made by the wet granulation method could be controlled by varying the compression force. In conclusion, YO was found to be a useful additive for masking unpleasant tastes. FU ODTs with improved taste, rapid disintegration and greater hardness could be prepared with YOcontaining granules made by the wet granulation method using MA as a binding agent.
YAKUGAKU ZASSHI, 2010
Using furosemide (FU) as a model drug, we examined the wet granulation method as a way to improve... more Using furosemide (FU) as a model drug, we examined the wet granulation method as a way to improve the taste masking and physical characteristics of orally disintegrating tablets (ODTs). In the wet granulation method, yogurt powder (YO) was used as a corrective and maltitol (MA) was used as a binding agent. The taste masked FU tablets were prepared using the direct compression method. Microcrystalline cellulose (AvicelPH-302) and mannitol were added as excipients at a mixing ratio of 1/1 by weight. Based on the results of sensory test on taste, the prepared granules markedly improved the taste of FU, and a su‹cient masking eŠect was obtained at the YO/FU ratio of 1 or more. Furthermore, it was found that the masking eŠect achieved by YO granules made with the wet granulation method was similar to or better than that produced by the granules made with dry granulation method. All types of tablets displayed su‹cient hardness (over 3.5×10-2 kN), and rapidly disintegrating tablets were obtained with YO granules produced at a mixing ratio of FU/YO＝1/1, which disintegrated within 20 s. Disintegration time lengthened as the mixing ratio of YO to FU increased. In the mixing ratio of FU/YO＝1/1, the hardness of tablets with granules made by the wet granulation method exceeded that of tablets with granules made by the dry granulation method, with minimal diŠerences in disintegration time. The hardness and disintegration time of the tablets with granules made by the wet granulation method could be controlled by varying the compression force. In conclusion, YO was found to be a useful additive for masking unpleasant tastes. FU ODTs with improved taste, rapid disintegration and greater hardness could be prepared with YOcontaining granules made by the wet granulation method using MA as a binding agent.
Research Journal of Pharmacy and Technology, 2020
Journal of Pharmaceutical Research International, 2021
Aim: The aim of the present study was to develop silybin liposome by incorporating phosphatidyl c... more Aim: The aim of the present study was to develop silybin liposome by incorporating phosphatidyl choline & cholesterol so as to increase its oral bioavailability and liver targeted enhanced hepatoprotection. Methodology: Thin film hydration technique was used for the development of liposomes by using phosphatidyl choline, cholesterol and drug. Liposomes were evaluated for vesicle size, zeta potential, PDI, encapsulation efficiency, surface morphology and in vitro drug release study. Further the optimized formulation was evaluated for APAP-induced alterations in liver and kidney function tests in rats and histopathological studies. Results: The results were promising with a sustained drug release of 80% within 20hrs, optimized vesicle size of 276nm and 89% encapsulation efficiency. The animal studies demonstrated superior hepatoprotective effect compared to silybin solution. Conclusion: The silybin liposomes showed better in-vitro release & in-vivo hepatoprotection along with better a...
L'invention concerne des compositions pharmaceutiques comprenant une pluralite de particules ... more L'invention concerne des compositions pharmaceutiques comprenant une pluralite de particules formulees contenant au moins un ingredient actif et au moins un excipient pharmaceutiquement acceptable, granulees avec une composition de granulation contenant au moins un excipient pharmaceutique.
La presente invention concerne une composition pharmaceutique comprenant le fingolimod, un sel ph... more La presente invention concerne une composition pharmaceutique comprenant le fingolimod, un sel pharmaceutiquement acceptable de celui-ci ou un derive de phosphate dont la concentration en impuretes I (w/w) est inferieure a environ 0,5 % au bout de six mois d'etude de stabilite a 40 °C et pour 75 % d'humidite relative (RH).
L'invention concerne des compositions pharmaceutiques comportant des polymeres qui liberent l... more L'invention concerne des compositions pharmaceutiques comportant des polymeres qui liberent la paroxetine de maniere controlee, pendant une periode prolongee ou de maniere progressive. Une forme de realisation de l'invention concerne des compositions pharmaceutiques a liberation controlee, dont la biodisponibilite est amelioree et qui comprennent la paroxetine ou des sels pharmaceutiquement acceptables de celle-ci, ces compositions permettant de reduire la dose administree par voie orale.
Stp Pharma Sciences, 2001
The assessment of potential incompatibilities between an active drug substance and excipients is ... more The assessment of potential incompatibilities between an active drug substance and excipients is an important exercise in the early stages of formulation development to ensure essential product stability Differential scanning calorimetry (DSC) and high performance liquid chromatography (HPLC) were successfully employed to evaluate the compatibility of ketorolac tromethamine (KTM) with various polymers and common tablet excipients in the process of developing a controlled release delivery system. The results of DSC and HPLC were combined in order to assess the incompatibility. Among the excipients tested, sodium carboxymethylcellulose and chitosan exhibited potential signs of chemical interaction with the drug. A physical type of drug-excipient interaction was found with magnesium stearate. Overall, a good correlation was observed between DSC and HPLC results in the assessment of compatibility.
In the last few years, STDs and AIDS have taken heavy toll on global economy and human resources.... more In the last few years, STDs and AIDS have taken heavy toll on global economy and human resources. STDs also increase risk of HIV transmission. Heterosexual transmission is the major route of transmission of STDs includingAIDS. Although the present day therapy can cure some STDs; but fails to prevent their transmission. In the absence of AIDS vaccine, barrier contraceptive techniques such as "microbicides" are being looked upon as promising candidates for reducing or eliminating incidences of STDs. Microbicides are novel agents/formulations applied to the areas involved in sexual contact and can prevent transmission of infective pathogens even during unprotected sex. Concurrent use of condoms and behavioural modifications reduces the risk of STD transmission significantly. Presently, though none available in the market, more than 60 different compounds and formulations are in the various stages of preclinical and clinical development. This review discusses vaginal microbicides for successful intervention of STDs, their essential features, mechanism of action, and regulatory considerations in the development of such products.
Drug Discovery Today, 2001
Pharmaceutical technology, 2003
Résumé/Abstract Optimization techniques are being explored extensively in pharmaceutical research... more Résumé/Abstract Optimization techniques are being explored extensively in pharmaceutical research as a tool to achieve the optimum composition of a delivery system. The design and development of novel drug delivery systems (NDDS) involve careful selection and ...
AIDS Patient Care and STDs, 2003
In recent years, AIDS and sexually transmitted diseases (STDs) have become a burgeoning problem a... more In recent years, AIDS and sexually transmitted diseases (STDs) have become a burgeoning problem and are spreading at an alarming rate. Microbicides are being developed as a new therapeutic category for prevention of transmission of sexually transmitted infections (STIs) and HIV. Many of the microbicide formulations (MF) may fail to elicit a protective response either because of a lack of efficacy or inadequate formulation. Manufacturing a stable, efficacious, safe, and optimal product is the main objective of formulation development programs. Preformulation parameters (PP), as discussed in Part I of this series, influence formulation development significantly and should be considered carefully before designing a formulation strategy. Initially, based on PP and market research, a target product profile (TPP) is generated, which defines product attributes that can be normally classified as "essential" and "desirable." A complex and dynamic process begins thereafter that takes into consideration myriad factors starting from selection of delivery system, selection of excipients, compatibility study, prototype composition, selection of process and optimization, stability testing, scale up, manufacturing under good manufacturing practices (GMP), and packaging development. Prototype formulations are evaluated for several performance characteristics (e.g., dispersion behavior, bioadhesion, retention, spreading, rheology). These compositions are also subjected to biologic evaluation by various in vitro and in vivo models. Such a well-planned, well-coordinated, and well-implemented formulation development program not only accelerates overall development but also minimizes failures in subsequent clinical development studies. The objective of this review is to highlight the importance of formulation science, outline the steps involved in this process, and explore how these can be exploited for achieving optimal MF.
International journal of …, 2002
Résumé/Abstract The vagina is a potential site for the local and systemic delivery of drugs. Pres... more Résumé/Abstract The vagina is a potential site for the local and systemic delivery of drugs. Presently, significant attention is given to the development of vaginal formulations ('microbicides') that prevent sexual acquisition of acquired immunodeficiency syndrome ( ...
Using furosemide (FU) as a model drug, we examined the wet granulation method as a way to improve... more Using furosemide (FU) as a model drug, we examined the wet granulation method as a way to improve the taste masking and physical characteristics of orally disintegrating tablets (ODTs). In the wet granulation method, yogurt powder (YO) was used as a corrective and maltitol (MA) was used as a binding agent. The taste masked FU tablets were prepared using the direct compression method. Microcrystalline cellulose (AvicelPH-302) and mannitol were added as excipients at a mixing ratio of 1/1 by weight. Based on the results of sensory test on taste, the prepared granules markedly improved the taste of FU, and a su‹cient masking eŠect was obtained at the YO/FU ratio of 1 or more. Furthermore, it was found that the masking eŠect achieved by YO granules made with the wet granulation method was similar to or better than that produced by the granules made with dry granulation method. All types of tablets displayed su‹cient hardness (over 3.5×10-2 kN), and rapidly disintegrating tablets were obtained with YO granules produced at a mixing ratio of FU/YO＝1/1, which disintegrated within 20 s. Disintegration time lengthened as the mixing ratio of YO to FU increased. In the mixing ratio of FU/YO＝1/1, the hardness of tablets with granules made by the wet granulation method exceeded that of tablets with granules made by the dry granulation method, with minimal diŠerences in disintegration time. The hardness and disintegration time of the tablets with granules made by the wet granulation method could be controlled by varying the compression force. In conclusion, YO was found to be a useful additive for masking unpleasant tastes. FU ODTs with improved taste, rapid disintegration and greater hardness could be prepared with YOcontaining granules made by the wet granulation method using MA as a binding agent.
YAKUGAKU ZASSHI, 2010
Using furosemide (FU) as a model drug, we examined the wet granulation method as a way to improve... more Using furosemide (FU) as a model drug, we examined the wet granulation method as a way to improve the taste masking and physical characteristics of orally disintegrating tablets (ODTs). In the wet granulation method, yogurt powder (YO) was used as a corrective and maltitol (MA) was used as a binding agent. The taste masked FU tablets were prepared using the direct compression method. Microcrystalline cellulose (AvicelPH-302) and mannitol were added as excipients at a mixing ratio of 1/1 by weight. Based on the results of sensory test on taste, the prepared granules markedly improved the taste of FU, and a su‹cient masking eŠect was obtained at the YO/FU ratio of 1 or more. Furthermore, it was found that the masking eŠect achieved by YO granules made with the wet granulation method was similar to or better than that produced by the granules made with dry granulation method. All types of tablets displayed su‹cient hardness (over 3.5×10-2 kN), and rapidly disintegrating tablets were obtained with YO granules produced at a mixing ratio of FU/YO＝1/1, which disintegrated within 20 s. Disintegration time lengthened as the mixing ratio of YO to FU increased. In the mixing ratio of FU/YO＝1/1, the hardness of tablets with granules made by the wet granulation method exceeded that of tablets with granules made by the dry granulation method, with minimal diŠerences in disintegration time. The hardness and disintegration time of the tablets with granules made by the wet granulation method could be controlled by varying the compression force. In conclusion, YO was found to be a useful additive for masking unpleasant tastes. FU ODTs with improved taste, rapid disintegration and greater hardness could be prepared with YOcontaining granules made by the wet granulation method using MA as a binding agent.
Research Journal of Pharmacy and Technology, 2020
Journal of Pharmaceutical Research International, 2021
Aim: The aim of the present study was to develop silybin liposome by incorporating phosphatidyl c... more Aim: The aim of the present study was to develop silybin liposome by incorporating phosphatidyl choline & cholesterol so as to increase its oral bioavailability and liver targeted enhanced hepatoprotection. Methodology: Thin film hydration technique was used for the development of liposomes by using phosphatidyl choline, cholesterol and drug. Liposomes were evaluated for vesicle size, zeta potential, PDI, encapsulation efficiency, surface morphology and in vitro drug release study. Further the optimized formulation was evaluated for APAP-induced alterations in liver and kidney function tests in rats and histopathological studies. Results: The results were promising with a sustained drug release of 80% within 20hrs, optimized vesicle size of 276nm and 89% encapsulation efficiency. The animal studies demonstrated superior hepatoprotective effect compared to silybin solution. Conclusion: The silybin liposomes showed better in-vitro release & in-vivo hepatoprotection along with better a...
L'invention concerne des compositions pharmaceutiques comprenant une pluralite de particules ... more L'invention concerne des compositions pharmaceutiques comprenant une pluralite de particules formulees contenant au moins un ingredient actif et au moins un excipient pharmaceutiquement acceptable, granulees avec une composition de granulation contenant au moins un excipient pharmaceutique.
La presente invention concerne une composition pharmaceutique comprenant le fingolimod, un sel ph... more La presente invention concerne une composition pharmaceutique comprenant le fingolimod, un sel pharmaceutiquement acceptable de celui-ci ou un derive de phosphate dont la concentration en impuretes I (w/w) est inferieure a environ 0,5 % au bout de six mois d'etude de stabilite a 40 °C et pour 75 % d'humidite relative (RH).
L'invention concerne des compositions pharmaceutiques comportant des polymeres qui liberent l... more L'invention concerne des compositions pharmaceutiques comportant des polymeres qui liberent la paroxetine de maniere controlee, pendant une periode prolongee ou de maniere progressive. Une forme de realisation de l'invention concerne des compositions pharmaceutiques a liberation controlee, dont la biodisponibilite est amelioree et qui comprennent la paroxetine ou des sels pharmaceutiquement acceptables de celle-ci, ces compositions permettant de reduire la dose administree par voie orale.
Stp Pharma Sciences, 2001
The assessment of potential incompatibilities between an active drug substance and excipients is ... more The assessment of potential incompatibilities between an active drug substance and excipients is an important exercise in the early stages of formulation development to ensure essential product stability Differential scanning calorimetry (DSC) and high performance liquid chromatography (HPLC) were successfully employed to evaluate the compatibility of ketorolac tromethamine (KTM) with various polymers and common tablet excipients in the process of developing a controlled release delivery system. The results of DSC and HPLC were combined in order to assess the incompatibility. Among the excipients tested, sodium carboxymethylcellulose and chitosan exhibited potential signs of chemical interaction with the drug. A physical type of drug-excipient interaction was found with magnesium stearate. Overall, a good correlation was observed between DSC and HPLC results in the assessment of compatibility.
In the last few years, STDs and AIDS have taken heavy toll on global economy and human resources.... more In the last few years, STDs and AIDS have taken heavy toll on global economy and human resources. STDs also increase risk of HIV transmission. Heterosexual transmission is the major route of transmission of STDs includingAIDS. Although the present day therapy can cure some STDs; but fails to prevent their transmission. In the absence of AIDS vaccine, barrier contraceptive techniques such as "microbicides" are being looked upon as promising candidates for reducing or eliminating incidences of STDs. Microbicides are novel agents/formulations applied to the areas involved in sexual contact and can prevent transmission of infective pathogens even during unprotected sex. Concurrent use of condoms and behavioural modifications reduces the risk of STD transmission significantly. Presently, though none available in the market, more than 60 different compounds and formulations are in the various stages of preclinical and clinical development. This review discusses vaginal microbicides for successful intervention of STDs, their essential features, mechanism of action, and regulatory considerations in the development of such products.
Drug Discovery Today, 2001
Pharmaceutical technology, 2003
Résumé/Abstract Optimization techniques are being explored extensively in pharmaceutical research... more Résumé/Abstract Optimization techniques are being explored extensively in pharmaceutical research as a tool to achieve the optimum composition of a delivery system. The design and development of novel drug delivery systems (NDDS) involve careful selection and ...
AIDS Patient Care and STDs, 2003
In recent years, AIDS and sexually transmitted diseases (STDs) have become a burgeoning problem a... more In recent years, AIDS and sexually transmitted diseases (STDs) have become a burgeoning problem and are spreading at an alarming rate. Microbicides are being developed as a new therapeutic category for prevention of transmission of sexually transmitted infections (STIs) and HIV. Many of the microbicide formulations (MF) may fail to elicit a protective response either because of a lack of efficacy or inadequate formulation. Manufacturing a stable, efficacious, safe, and optimal product is the main objective of formulation development programs. Preformulation parameters (PP), as discussed in Part I of this series, influence formulation development significantly and should be considered carefully before designing a formulation strategy. Initially, based on PP and market research, a target product profile (TPP) is generated, which defines product attributes that can be normally classified as "essential" and "desirable." A complex and dynamic process begins thereafter that takes into consideration myriad factors starting from selection of delivery system, selection of excipients, compatibility study, prototype composition, selection of process and optimization, stability testing, scale up, manufacturing under good manufacturing practices (GMP), and packaging development. Prototype formulations are evaluated for several performance characteristics (e.g., dispersion behavior, bioadhesion, retention, spreading, rheology). These compositions are also subjected to biologic evaluation by various in vitro and in vivo models. Such a well-planned, well-coordinated, and well-implemented formulation development program not only accelerates overall development but also minimizes failures in subsequent clinical development studies. The objective of this review is to highlight the importance of formulation science, outline the steps involved in this process, and explore how these can be exploited for achieving optimal MF.
International journal of …, 2002
Résumé/Abstract The vagina is a potential site for the local and systemic delivery of drugs. Pres... more Résumé/Abstract The vagina is a potential site for the local and systemic delivery of drugs. Presently, significant attention is given to the development of vaginal formulations ('microbicides') that prevent sexual acquisition of acquired immunodeficiency syndrome ( ...