Vinay Rao - Academia.edu (original) (raw)

Papers by Vinay Rao

In the present study, Valacyclovir tablets were formulated using different formulation parameters... more In the present study, Valacyclovir tablets were formulated using different formulation parameters and their effects on the dissolution rate of these tablets were evaluated. The binding agent used in this study was Povidone. Tablets were prepared by wet granulation method and were evaluated for various parameters like weight variation, hardness, friability, disintegration time, drug content and in vitro dissolution studies. This Process validation report for Valacyclovir Hydrochloride Tablets 500mg & 1gram common blend is based on the observations/data collected during manufacturing of three consecutive batches, which were manufactured as per Batch Manufacturing record for Export Market at Aurobindo Pharma Ltd. Unit-VII, Jadcherla. Samples were collected and analysed as per Process validation protocol. The data & test results of blend at various in-process phases were complied with the specified limits and final blend sample analysis results found to be complying within specifications. This study and results obtained assures that the manufacturing process is reproducible, yielding consistent product, which meets specification.

Aaps Pharmscitech, Dec 14, 2021

In order to be at pace with the market requirements of solid dosage forms and regulatory standard... more In order to be at pace with the market requirements of solid dosage forms and regulatory standards, a transformation towards systematic processing using continuous manufacturing (CM) and automated model-based control is being thought through for its fundamental advantages over conventional batch manufacturing. CM eliminates the key gaps through the integration of various processes while preserving quality attributes via the use of process analytical technology (PAT). The twin screw extruder (TSE) is one such equipment adopted by the pharmaceutical industry as a substitute for the traditional batch granulation process. Various types of granulation techniques using twin screw extrusion technology have been explored in the article. Furthermore, individual components of a TSE and their conjugation with PAT tools and the advancements and applications in the field of nutraceuticals and nanotechnology have also been discussed. Thus, the future of granulation lies on the shoulders of continuous TSE, where it can be coupled with computational mathematical studies to mitigate its complications.

This is an Open Access article distributed under the terms of the Creative Commons Attribution Li... more This is an Open Access article distributed under the terms of the Creative Commons Attribution License

A novel stability-indicating reverse phase Ultra performance liquid chromatography method was dev... more A novel stability-indicating reverse phase Ultra performance liquid chromatography method was developed and validated for the determination of lacosamide (LCM) and its related substances in bulk and pharmaceutical formulations. The separation of impurities from lacosamide was accomplished on HSS C18 Column using (100 x 2.1mm, 1.8μm) 0.01 M mono basic potassium phosphates for adjusting the pH to 2.0 with ortho phosphoric acid: Acetonitrile (85:15, v/v) as mobile phase. The flow rate was 0.7 mL/min and the detection was carried out at 210 nm with run time of 5 minutes. The developed isocratic UPLC method was consequently validated for specificity, linearity, range, accuracy, precision and robustness and shown equivalency with the API Vendor method.

Objective: The current work focuses on the development and optimization of Naproxen 800mg sustain... more Objective: The current work focuses on the development and optimization of Naproxen 800mg sustained release tablets using surface response methodology. Methods: The drug release was controlled by formulating it into a sustained release tablet. The formulae was developed using various individual concentrations and viscosity grades of HPMC polymers for Naproxen SR tablets. The compatibility of polymers along with pure drug Naproxen was evaluated using FTIR and DSC studies. The tablets were prepared and Pre-and Post-compressional parameters, In-vitro dissolution testing, release rate kinetics and stability studies were evaluated. Results: The FT-IR and DSC spectras confirms the absence of chemical interaction between drug and polymers. All the Pre-compressional and Postcompressional parameters were found to be in limits. From the dissolution testing of all these formulations the low and high level of polymer concentrations which were within the range of Target product profile was determined. The design space as defined by the above experiments is within 21.3 to 22.8 range of the total polymer concentration. The data for stability studies revealed that no considerable differences in drug content and dissolution rates for a period of 6 months as per ICH guidelines. Conclusion: Based on the above results, a design space for all the three polymers was successfully developed within which when the tablets are fabricated, the target product profile will always be achieved.

Zenodo (CERN European Organization for Nuclear Research), May 21, 2015

Even though a number of non-steroidal anti-inflammatory drugs (NSAIDS) are available with differe... more Even though a number of non-steroidal anti-inflammatory drugs (NSAIDS) are available with different chemistries, they share a common solubility characteristic that is they are relatively more soluble in alkaline environment and practically insoluble in acidic environment. This work deals with developing a wax matrix drug delivery platform for controlled delivery of three model NSAIDS, Diclofenac sodium (DNa), Mefenamic acid (MA) and Naproxen (NPX) using the melt granulation technique. The aim of developing the platform was to have a general understanding on how an erodible matrix system modulates drug delivery rate and extent and how it can be optimized to give a delivery system which shall release the drug as per a common target product profile (TPP). Commonly used waxes like Cetostearyl alcohol and stearic acid were used singly an in combination to achieve a TPP of not 15 to 35% in 1 hour and not less than 80% Q in 24 hours. Full factorial design of experiments was followed for optimization of the formulation.

American Journal of Advanced Drug Delivery, Jun 30, 2013

The effect of three different viscosity grades on the in vitro dissolution profile of Aripiprazol... more The effect of three different viscosity grades on the in vitro dissolution profile of Aripiprazole controlled release tablets was studied. The study was carried out using full factorial design of experiments. The release rate of 5 to 6 mg%/ hour was targeted and the effect of the polymers on drug release over 24 hours was evaluated at the total polymer level between 30% and 45%. The DOE experiments have shown that when the combination of polymer is used, the total polymer concentration should be in a narrow range of 32.4% w/w to 37.5% w/w in order to achieve the target dissolution profile.

American Journal of Advanced Drug Delivery, Jun 30, 2013

The objective of the study was to formulate bilayer tablets consisting of Paracetamol (PM) and Ac... more The objective of the study was to formulate bilayer tablets consisting of Paracetamol (PM) and Aceclofenac (AC). 100% of the dose of PM and 50% of the dose of AC was formulated as a fast disintegrating and rapidly dissolving layer which was overlaid with a controlled release layer containing the balance 50% of the dose of AC. The IRlayer was designed in a way to achieve complete release of the dose within a 30 min and SR-layer was designed to deliver the dose at a constant rate of 4 to 5 mg % /hour. To optimize the composition of the IR layer the level of Croscarmellose sodium (CCS) in the formulation was optimized. For optimizing the SR layer, HPMC K4M, K15M and K100M at different levels were evaluated and the type and concentration of HPMC was finalized. These results indicated that release of the drug from the tablet was influenced by content of super disintegrant and polymer grade and concentration. Formulation containing 1.5 % w/w of CCS in IR-layer and 6 % w/w of HPMC K100M in SR-layer showed desired drug release. Thus bilayer tablets could be a potential dosage form for delivering Paracetamol as immediate release and Aceclofenac in a controlled release manner.

American Journal of Advanced Drug Delivery, Aug 30, 2013

Zolpidem tartarate (ZT) is indicated for the short-term treatment of insomnia characterized by di... more Zolpidem tartarate (ZT) is indicated for the short-term treatment of insomnia characterized by difficulties with sleep initiation. The objective of this research was to prepare oral dissolving films (ODF) containing ZT. Different combinations of polymers and plasticizers were evaluated for optimizing the physical properties and the in vitro drug release. Films were prepared and subjected to various physicochemical evaluations and in vitro dissolution studies. The film prepared using HPMC E15 (F4) with 1:1 ratio of drug and polymer with glycerol as plasticizer were considered to have acceptable physical properties, disintegration time of below 60 seconds and > 85% of drug release within 5 minutes and hence were considered as optimum.

American Journal of Advanced Drug Delivery, Dec 31, 2015

Objective: The variable aqueous solubility of Hydrochlorthiazide (HCTZ) is the major factor limit... more Objective: The variable aqueous solubility of Hydrochlorthiazide (HCTZ) is the major factor limiting its oral bioavailability. The objective of the study is to enhance of the solubility of HCTZ by using solid dispersion technique. Methods: The polymers used were PVP K30, PVP S630, HPMC & PEG 6000 and solid dispersions were prepared by solvent evaporation method in different ratios of 1:0.5, 1:1, 1:3, 1:5 respectively. The prepared solid dispersions were characterized by DSC and FTIR. The equilibrium solubility was determined in water to study the effect of polymers on solubility of HCTZ. In vitro dissolution studies were conducted in distilled water from solid dispersions equivalent to 12.5 mg of HCTZ. How the solid dispersions affect the permeation of the drug across membranes was evaluated by measuring the In vitro permeation of Drug PVP and Drug HPMC across cellophane membrane using the vertical Franz diffusion cell. Results: Successful conversion of the crystalline Hydrochlorthiazide to amorphous solid dispersion was achieved at 1:1, 1:3 & 1:5 levels of drug to HPMC E 15 & drug to PVP and with PVP S630 it was achieved at 1:3 & 1:5 level. Amorphous conversion was not observed in case of PEG 6000 at any level. The solid dispersion prepared with HPMC E 15 & PVP K30 at 1:5 level showed a 98% and 66.3% drug release at 5min respectively. The enhancements in case of 1:5 Plasdone s630 and PEG 6000 were not significant. The results of equilibrium solubility studies indicates that the solvent evaporated solid dispersions of HPMC E 15 & PVP K30 were the best Permeation studies indicate that a 3 to 4 fold increase in the solubility of the drug results in 10 fold increase in permeation. Thus enhancement in solubility also results in enhancement in the permeation across artificial membranes. Conclusion: The above study shows that solid dispersion of HCTZ

The aim of developing the platform was to have a general understanding on how an erodible matrix ... more The aim of developing the platform was to have a general understanding on how an erodible matrix system modulates drug delivery rate and extent and how it can be optimized to give a delivery system which shall release the drug as per a common target product profile (TPP). Mefenamic Acid (one of the NSAID’s) is prepared by using Melt Granulation Process. Commonly used waxes like Cetostearyl alcohol and stearic acid were used singly an in combination to achieve a TPP of not 15 to 35 % in 1 hour and not less than 80 % Q in 24hours. Full factorial design of experiments was followed for optimization of the formulation. Dissolution profile of the NSAID is taken and recorded. Market available brands of the same NSAID is taken for dissolution profile. The results are recorded. The two recorded results are then compared and verified with the USP standards.

Drug Development and Industrial Pharmacy, 1994

Materials PF was purchased from Clariant Corp. (Muttentz, Switzerland). Stearic acid (SA) was obt... more Materials PF was purchased from Clariant Corp. (Muttentz, Switzerland). Stearic acid (SA) was obtained from Kanto Chemical Co., Ltd. (Tokyo, Japan). Acetonitrile, ethanol, methanol, oleic acid (OA), sodium dodecyl sulfate (SDS), propylene glycol (PG), isopropyl myristate (IPM), L(Ϫ)-menthol (MEN), D(ϩ)-limonene (LIM) and phosphoric acid were purchased from Wako Pure Chemical Industries, Ltd. (Osaka, Japan) as the purest grade available. Macrogol 400 (MG) was of Japanese Pharmacopoeia (JP) grade. Sucrose fatty acid esters were obtained from Mitsubishi-Kagaku Foods Corporation (Tokyo, Japan). We used four kinds of sucrose fatty acid esters (L595, L1695, O1570 and S1570). L, O and S indicate lauric acid, oleic acid and stearic acid, respectively. The hydrophilic lipophilic balance (HLB) values of L595, L1695, O1570 and S1570 were 5, 16, 15 and 15, respectively. All other chemicals were obtained commercially as the purest grade available. Animals Male Sprague-Dawley rats weighing approximately 200-220 g were purchased from Tokyo Laboratory Animals Science Co., Ltd. (Tokyo, Japan). The experimental protocol was approved by the Ethics Review Committee for Animal Experimentation of Hoshi University. The guidelines for animal experimentation at Hoshi University conform to the basic guidelines published by the Ministry of Education, Culture, Sports, Science and Technology of Japan. In Vitro Transdermal Permeation Experiments After sacrifice using ether, the abdominal hair was removed using an electric clipper, and the abdominal skin was excised and mounted on flow-through Franz diffusion cells. 18) The exposed skin area was 0.785 cm 2 and test solutions (0.5 ml)

American Journal of Advanced Drug Delivery, 2014

The aim of developing the platform was to have a general understanding on how an erodible matrix ... more The aim of developing the platform was to have a general understanding on how an erodible matrix system modulates drug delivery rate and extent and how it can be optimized to give a delivery system which shall release the drug as per a common target product profile (TPP). Mefenamic Acid (one of the NSAID’s) is prepared by using Melt Granulation Process. Commonly used waxes like Cetostearyl alcohol and stearic acid were used singly an in combination to achieve a TPP of not 15 to 35% in 1 hour and not less than 80% Q in 24hours. Full factorial design of experiments was followed for optimization of the formulation. Dissolution profile of the NSAID is taken and recorded. Market available brands of the same NSAID is taken for dissolution profile. The results are recorded. The two recorded results are then compared and verified with the USP standards.

American Journal of Advanced Drug Delivery, 2013

The effect of 3 different categories of permeation enhancers on the in vitro permeation of Lamotr... more The effect of 3 different categories of permeation enhancers on the in vitro permeation of Lamotrigine across cellophane membrane were evaluated using vertical type Franz Diffusion Cell. This work was conducted as a permeation enhancer screening study for development of Lamotrigine Transdermal Drug Delivery System. Dimethyl Sulfoxide (DMSO) at 5% v/v and Tween 80 at 0.1% v/v gave a 6 and 7 folds enhancement in permeation values respectively. SLS and Peppermint Oil did not show any enhancement in the penetration.

Aim of present study was to develop solid self micro emulsifying drug delivery system (S-SEDDS) w... more Aim of present study was to develop solid self micro emulsifying drug delivery system (S-SEDDS) with Aerosil 200 for enhancement of dissolution rate of model drug Glibenclamide (GBM). SEDDS was prepared using Capmul MCM C8 TM , Cremophor RH 40 TM , and Transcutol P TM as oil, surfactant and cosurfactant respectively. For formulation of stable SEDDS, micro emulsion region was identified by constructing pseudo ternary phase diagram containing different proportion of surfactant: co-surfactant (1:1, 2:1 and 3:1), oil and water. Prepared SEDDS was evaluated for turbidity measurement, globule size and zeta potential, viscosity determination and % transmittance. S-SEDDS was prepared by adsorption technique using Aerosil 200 as solid carrier. Prepared S-SEDDS was evaluated for flow properties, drug content, FTIR, SEM, DSC and in-vitro dissolution study. Results showed that prepared liquid SEDDS passed all evaluation tests. Globule size was found to be 142.8 nm with polydispersity index 0.396. S-SEDDS showed good flow property and drug content. From the experiment, it is clear thateven after conversion of the liquid SEDDS into the solid one there was no significant alteration in the properties of solid SEDDS.in-vitro dissolution studies showed that there was enhancement of dissolution rate of GBM as compared with that of plain drug and marketed formulation. From the results it is concluded that, Aerosil 200 can be used to develop S-SEDDS by adsorption technique to enhance dissolution rate of poorly water soluble model drug GBM

A simple, sensitive, and precise RP-High Performance Liquid Chromatography (HPLC) method for the ... more A simple, sensitive, and precise RP-High Performance Liquid Chromatography (HPLC) method for the simultaneous estimation of Aliskiren (ALS), Amlodipine (AML) and Hydrochlorothiazide (HCTZ) combined dosage form has been developed and validated. The components were well separated using Hypersil BDS, 250 x 4.6 mm, 5 column using Acetonitrile:1ml TEA in 1000 potassium phosphate buffer 0.01M (40:60% v/v) as mobile phase at a flow rate of 1.0 mL/min. The eluents were detected at 228 nm using UV detector. The retention time of HCTZ 3.3 min, ALS was found to be 5.9 min and that of AML was 8.0 min. The linearity was observed between 6.25-37.5µg/mL, 75-450µg/mL and 2.5-15µg/mL for HCTZ, ALS and AML respectively. The marketed dosage form was analysed by using the developed method. The mean recoveries were 100±2% for three compounds. The method was validated for system suitability, specificity, linearity, accuracy, precision, ruggedness and robustness as per ICH guidelines and the results were...

A novel simple, sensitive, accurate and precise RP-High Performance Liquid Chromatography (HPLC) ... more A novel simple, sensitive, accurate and precise RP-High Performance Liquid Chromatography (HPLC) method for the simultaneous estimation of Phenylephrine (PHE), Acetaminophen (ACE), Guaifenesin (GUA) and Dextromethorphan (DEX) combined dosage form has been developed and validated. The components were well separated using Altima, 150 x 4.6 mm, 5m column with 1ml of Conc. Orthophosphoric acid in a 1000ml of water as Solvent A and Acetonitrile as Solvent B at a flow rate of 1.0 mL/min by using gradient programme. The eluents were detected at 272 nm using UV detector. The retention time of PHE, ACE, GUA and DEX found to be 2.5, 6.1, 8.3 and 9.0 min respectively. The linearity was observed between 2.0-7.0μg/mL,130-455μg/mL, 50-300μg/mL and 2.5-15 μg/mL for Phenylephrine, Acetaminophen, Guaifenesin and Dextromethorphan respectively. The method was validated for system suitability, specificity, linearity, accuracy, precision, ruggedness and robustness as per ICH guidelines and the results w...

Diclofenac sodium tablets are available as delayed release tablets in the market. Delayed release... more Diclofenac sodium tablets are available as delayed release tablets in the market. Delayed release tablets are typically produced by coating the tablet with enteric coating polymers. These polymers provide the resistance of drug release in acidic environment of stomach and allow the drug to be released in alkaline environment of the intestine. A large number of enteric polymers are available which provide excellent protection to drug release in acidic environment. However, each polymer dissolves at different alkaline pH. For e.g. Eudragit L-100 dissolves at pH 6 and above while Eudragit S-100 dissolves at pH 6.5 and above. HPMC Phthalate P5.5 dissolves at pH 5.5 and above while HPMC Phthalate P dissolves at pH 6 and above. Hence, for the same drug the bioavailability can subtly but significantly change based on which enteric polymer is used to provide the delayed release. The aim of the current work was to comparatively evaluate five brands of Diclofenac sodium enteric coated tablets...

In the present study, Valacyclovir tablets were formulated using different formulation parameters... more In the present study, Valacyclovir tablets were formulated using different formulation parameters and their effects on the dissolution rate of these tablets were evaluated. The binding agent used in this study was Povidone. Tablets were prepared by wet granulation method and were evaluated for various parameters like weight variation, hardness, friability, disintegration time, drug content and in vitro dissolution studies. This Process validation report for Valacyclovir Hydrochloride Tablets 500mg & 1gram common blend is based on the observations/data collected during manufacturing of three consecutive batches, which were manufactured as per Batch Manufacturing record for Export Market at Aurobindo Pharma Ltd. Unit-VII, Jadcherla. Samples were collected and analysed as per Process validation protocol. The data & test results of blend at various in-process phases were complied with the specified limits and final blend sample analysis results found to be complying within specifications. This study and results obtained assures that the manufacturing process is reproducible, yielding consistent product, which meets specification.

Aaps Pharmscitech, Dec 14, 2021

In order to be at pace with the market requirements of solid dosage forms and regulatory standard... more In order to be at pace with the market requirements of solid dosage forms and regulatory standards, a transformation towards systematic processing using continuous manufacturing (CM) and automated model-based control is being thought through for its fundamental advantages over conventional batch manufacturing. CM eliminates the key gaps through the integration of various processes while preserving quality attributes via the use of process analytical technology (PAT). The twin screw extruder (TSE) is one such equipment adopted by the pharmaceutical industry as a substitute for the traditional batch granulation process. Various types of granulation techniques using twin screw extrusion technology have been explored in the article. Furthermore, individual components of a TSE and their conjugation with PAT tools and the advancements and applications in the field of nutraceuticals and nanotechnology have also been discussed. Thus, the future of granulation lies on the shoulders of continuous TSE, where it can be coupled with computational mathematical studies to mitigate its complications.

This is an Open Access article distributed under the terms of the Creative Commons Attribution Li... more This is an Open Access article distributed under the terms of the Creative Commons Attribution License

A novel stability-indicating reverse phase Ultra performance liquid chromatography method was dev... more A novel stability-indicating reverse phase Ultra performance liquid chromatography method was developed and validated for the determination of lacosamide (LCM) and its related substances in bulk and pharmaceutical formulations. The separation of impurities from lacosamide was accomplished on HSS C18 Column using (100 x 2.1mm, 1.8μm) 0.01 M mono basic potassium phosphates for adjusting the pH to 2.0 with ortho phosphoric acid: Acetonitrile (85:15, v/v) as mobile phase. The flow rate was 0.7 mL/min and the detection was carried out at 210 nm with run time of 5 minutes. The developed isocratic UPLC method was consequently validated for specificity, linearity, range, accuracy, precision and robustness and shown equivalency with the API Vendor method.

Objective: The current work focuses on the development and optimization of Naproxen 800mg sustain... more Objective: The current work focuses on the development and optimization of Naproxen 800mg sustained release tablets using surface response methodology. Methods: The drug release was controlled by formulating it into a sustained release tablet. The formulae was developed using various individual concentrations and viscosity grades of HPMC polymers for Naproxen SR tablets. The compatibility of polymers along with pure drug Naproxen was evaluated using FTIR and DSC studies. The tablets were prepared and Pre-and Post-compressional parameters, In-vitro dissolution testing, release rate kinetics and stability studies were evaluated. Results: The FT-IR and DSC spectras confirms the absence of chemical interaction between drug and polymers. All the Pre-compressional and Postcompressional parameters were found to be in limits. From the dissolution testing of all these formulations the low and high level of polymer concentrations which were within the range of Target product profile was determined. The design space as defined by the above experiments is within 21.3 to 22.8 range of the total polymer concentration. The data for stability studies revealed that no considerable differences in drug content and dissolution rates for a period of 6 months as per ICH guidelines. Conclusion: Based on the above results, a design space for all the three polymers was successfully developed within which when the tablets are fabricated, the target product profile will always be achieved.

Zenodo (CERN European Organization for Nuclear Research), May 21, 2015

Even though a number of non-steroidal anti-inflammatory drugs (NSAIDS) are available with differe... more Even though a number of non-steroidal anti-inflammatory drugs (NSAIDS) are available with different chemistries, they share a common solubility characteristic that is they are relatively more soluble in alkaline environment and practically insoluble in acidic environment. This work deals with developing a wax matrix drug delivery platform for controlled delivery of three model NSAIDS, Diclofenac sodium (DNa), Mefenamic acid (MA) and Naproxen (NPX) using the melt granulation technique. The aim of developing the platform was to have a general understanding on how an erodible matrix system modulates drug delivery rate and extent and how it can be optimized to give a delivery system which shall release the drug as per a common target product profile (TPP). Commonly used waxes like Cetostearyl alcohol and stearic acid were used singly an in combination to achieve a TPP of not 15 to 35% in 1 hour and not less than 80% Q in 24 hours. Full factorial design of experiments was followed for optimization of the formulation.

American Journal of Advanced Drug Delivery, Jun 30, 2013

The effect of three different viscosity grades on the in vitro dissolution profile of Aripiprazol... more The effect of three different viscosity grades on the in vitro dissolution profile of Aripiprazole controlled release tablets was studied. The study was carried out using full factorial design of experiments. The release rate of 5 to 6 mg%/ hour was targeted and the effect of the polymers on drug release over 24 hours was evaluated at the total polymer level between 30% and 45%. The DOE experiments have shown that when the combination of polymer is used, the total polymer concentration should be in a narrow range of 32.4% w/w to 37.5% w/w in order to achieve the target dissolution profile.

American Journal of Advanced Drug Delivery, Jun 30, 2013

The objective of the study was to formulate bilayer tablets consisting of Paracetamol (PM) and Ac... more The objective of the study was to formulate bilayer tablets consisting of Paracetamol (PM) and Aceclofenac (AC). 100% of the dose of PM and 50% of the dose of AC was formulated as a fast disintegrating and rapidly dissolving layer which was overlaid with a controlled release layer containing the balance 50% of the dose of AC. The IRlayer was designed in a way to achieve complete release of the dose within a 30 min and SR-layer was designed to deliver the dose at a constant rate of 4 to 5 mg % /hour. To optimize the composition of the IR layer the level of Croscarmellose sodium (CCS) in the formulation was optimized. For optimizing the SR layer, HPMC K4M, K15M and K100M at different levels were evaluated and the type and concentration of HPMC was finalized. These results indicated that release of the drug from the tablet was influenced by content of super disintegrant and polymer grade and concentration. Formulation containing 1.5 % w/w of CCS in IR-layer and 6 % w/w of HPMC K100M in SR-layer showed desired drug release. Thus bilayer tablets could be a potential dosage form for delivering Paracetamol as immediate release and Aceclofenac in a controlled release manner.

American Journal of Advanced Drug Delivery, Aug 30, 2013

Zolpidem tartarate (ZT) is indicated for the short-term treatment of insomnia characterized by di... more Zolpidem tartarate (ZT) is indicated for the short-term treatment of insomnia characterized by difficulties with sleep initiation. The objective of this research was to prepare oral dissolving films (ODF) containing ZT. Different combinations of polymers and plasticizers were evaluated for optimizing the physical properties and the in vitro drug release. Films were prepared and subjected to various physicochemical evaluations and in vitro dissolution studies. The film prepared using HPMC E15 (F4) with 1:1 ratio of drug and polymer with glycerol as plasticizer were considered to have acceptable physical properties, disintegration time of below 60 seconds and > 85% of drug release within 5 minutes and hence were considered as optimum.

American Journal of Advanced Drug Delivery, Dec 31, 2015

Objective: The variable aqueous solubility of Hydrochlorthiazide (HCTZ) is the major factor limit... more Objective: The variable aqueous solubility of Hydrochlorthiazide (HCTZ) is the major factor limiting its oral bioavailability. The objective of the study is to enhance of the solubility of HCTZ by using solid dispersion technique. Methods: The polymers used were PVP K30, PVP S630, HPMC & PEG 6000 and solid dispersions were prepared by solvent evaporation method in different ratios of 1:0.5, 1:1, 1:3, 1:5 respectively. The prepared solid dispersions were characterized by DSC and FTIR. The equilibrium solubility was determined in water to study the effect of polymers on solubility of HCTZ. In vitro dissolution studies were conducted in distilled water from solid dispersions equivalent to 12.5 mg of HCTZ. How the solid dispersions affect the permeation of the drug across membranes was evaluated by measuring the In vitro permeation of Drug PVP and Drug HPMC across cellophane membrane using the vertical Franz diffusion cell. Results: Successful conversion of the crystalline Hydrochlorthiazide to amorphous solid dispersion was achieved at 1:1, 1:3 & 1:5 levels of drug to HPMC E 15 & drug to PVP and with PVP S630 it was achieved at 1:3 & 1:5 level. Amorphous conversion was not observed in case of PEG 6000 at any level. The solid dispersion prepared with HPMC E 15 & PVP K30 at 1:5 level showed a 98% and 66.3% drug release at 5min respectively. The enhancements in case of 1:5 Plasdone s630 and PEG 6000 were not significant. The results of equilibrium solubility studies indicates that the solvent evaporated solid dispersions of HPMC E 15 & PVP K30 were the best Permeation studies indicate that a 3 to 4 fold increase in the solubility of the drug results in 10 fold increase in permeation. Thus enhancement in solubility also results in enhancement in the permeation across artificial membranes. Conclusion: The above study shows that solid dispersion of HCTZ

The aim of developing the platform was to have a general understanding on how an erodible matrix ... more The aim of developing the platform was to have a general understanding on how an erodible matrix system modulates drug delivery rate and extent and how it can be optimized to give a delivery system which shall release the drug as per a common target product profile (TPP). Mefenamic Acid (one of the NSAID’s) is prepared by using Melt Granulation Process. Commonly used waxes like Cetostearyl alcohol and stearic acid were used singly an in combination to achieve a TPP of not 15 to 35 % in 1 hour and not less than 80 % Q in 24hours. Full factorial design of experiments was followed for optimization of the formulation. Dissolution profile of the NSAID is taken and recorded. Market available brands of the same NSAID is taken for dissolution profile. The results are recorded. The two recorded results are then compared and verified with the USP standards.

Drug Development and Industrial Pharmacy, 1994

Materials PF was purchased from Clariant Corp. (Muttentz, Switzerland). Stearic acid (SA) was obt... more Materials PF was purchased from Clariant Corp. (Muttentz, Switzerland). Stearic acid (SA) was obtained from Kanto Chemical Co., Ltd. (Tokyo, Japan). Acetonitrile, ethanol, methanol, oleic acid (OA), sodium dodecyl sulfate (SDS), propylene glycol (PG), isopropyl myristate (IPM), L(Ϫ)-menthol (MEN), D(ϩ)-limonene (LIM) and phosphoric acid were purchased from Wako Pure Chemical Industries, Ltd. (Osaka, Japan) as the purest grade available. Macrogol 400 (MG) was of Japanese Pharmacopoeia (JP) grade. Sucrose fatty acid esters were obtained from Mitsubishi-Kagaku Foods Corporation (Tokyo, Japan). We used four kinds of sucrose fatty acid esters (L595, L1695, O1570 and S1570). L, O and S indicate lauric acid, oleic acid and stearic acid, respectively. The hydrophilic lipophilic balance (HLB) values of L595, L1695, O1570 and S1570 were 5, 16, 15 and 15, respectively. All other chemicals were obtained commercially as the purest grade available. Animals Male Sprague-Dawley rats weighing approximately 200-220 g were purchased from Tokyo Laboratory Animals Science Co., Ltd. (Tokyo, Japan). The experimental protocol was approved by the Ethics Review Committee for Animal Experimentation of Hoshi University. The guidelines for animal experimentation at Hoshi University conform to the basic guidelines published by the Ministry of Education, Culture, Sports, Science and Technology of Japan. In Vitro Transdermal Permeation Experiments After sacrifice using ether, the abdominal hair was removed using an electric clipper, and the abdominal skin was excised and mounted on flow-through Franz diffusion cells. 18) The exposed skin area was 0.785 cm 2 and test solutions (0.5 ml)

American Journal of Advanced Drug Delivery, 2014

The aim of developing the platform was to have a general understanding on how an erodible matrix ... more The aim of developing the platform was to have a general understanding on how an erodible matrix system modulates drug delivery rate and extent and how it can be optimized to give a delivery system which shall release the drug as per a common target product profile (TPP). Mefenamic Acid (one of the NSAID’s) is prepared by using Melt Granulation Process. Commonly used waxes like Cetostearyl alcohol and stearic acid were used singly an in combination to achieve a TPP of not 15 to 35% in 1 hour and not less than 80% Q in 24hours. Full factorial design of experiments was followed for optimization of the formulation. Dissolution profile of the NSAID is taken and recorded. Market available brands of the same NSAID is taken for dissolution profile. The results are recorded. The two recorded results are then compared and verified with the USP standards.

American Journal of Advanced Drug Delivery, 2013

The effect of 3 different categories of permeation enhancers on the in vitro permeation of Lamotr... more The effect of 3 different categories of permeation enhancers on the in vitro permeation of Lamotrigine across cellophane membrane were evaluated using vertical type Franz Diffusion Cell. This work was conducted as a permeation enhancer screening study for development of Lamotrigine Transdermal Drug Delivery System. Dimethyl Sulfoxide (DMSO) at 5% v/v and Tween 80 at 0.1% v/v gave a 6 and 7 folds enhancement in permeation values respectively. SLS and Peppermint Oil did not show any enhancement in the penetration.

Aim of present study was to develop solid self micro emulsifying drug delivery system (S-SEDDS) w... more Aim of present study was to develop solid self micro emulsifying drug delivery system (S-SEDDS) with Aerosil 200 for enhancement of dissolution rate of model drug Glibenclamide (GBM). SEDDS was prepared using Capmul MCM C8 TM , Cremophor RH 40 TM , and Transcutol P TM as oil, surfactant and cosurfactant respectively. For formulation of stable SEDDS, micro emulsion region was identified by constructing pseudo ternary phase diagram containing different proportion of surfactant: co-surfactant (1:1, 2:1 and 3:1), oil and water. Prepared SEDDS was evaluated for turbidity measurement, globule size and zeta potential, viscosity determination and % transmittance. S-SEDDS was prepared by adsorption technique using Aerosil 200 as solid carrier. Prepared S-SEDDS was evaluated for flow properties, drug content, FTIR, SEM, DSC and in-vitro dissolution study. Results showed that prepared liquid SEDDS passed all evaluation tests. Globule size was found to be 142.8 nm with polydispersity index 0.396. S-SEDDS showed good flow property and drug content. From the experiment, it is clear thateven after conversion of the liquid SEDDS into the solid one there was no significant alteration in the properties of solid SEDDS.in-vitro dissolution studies showed that there was enhancement of dissolution rate of GBM as compared with that of plain drug and marketed formulation. From the results it is concluded that, Aerosil 200 can be used to develop S-SEDDS by adsorption technique to enhance dissolution rate of poorly water soluble model drug GBM

A simple, sensitive, and precise RP-High Performance Liquid Chromatography (HPLC) method for the ... more A simple, sensitive, and precise RP-High Performance Liquid Chromatography (HPLC) method for the simultaneous estimation of Aliskiren (ALS), Amlodipine (AML) and Hydrochlorothiazide (HCTZ) combined dosage form has been developed and validated. The components were well separated using Hypersil BDS, 250 x 4.6 mm, 5 column using Acetonitrile:1ml TEA in 1000 potassium phosphate buffer 0.01M (40:60% v/v) as mobile phase at a flow rate of 1.0 mL/min. The eluents were detected at 228 nm using UV detector. The retention time of HCTZ 3.3 min, ALS was found to be 5.9 min and that of AML was 8.0 min. The linearity was observed between 6.25-37.5µg/mL, 75-450µg/mL and 2.5-15µg/mL for HCTZ, ALS and AML respectively. The marketed dosage form was analysed by using the developed method. The mean recoveries were 100±2% for three compounds. The method was validated for system suitability, specificity, linearity, accuracy, precision, ruggedness and robustness as per ICH guidelines and the results were...

A novel simple, sensitive, accurate and precise RP-High Performance Liquid Chromatography (HPLC) ... more A novel simple, sensitive, accurate and precise RP-High Performance Liquid Chromatography (HPLC) method for the simultaneous estimation of Phenylephrine (PHE), Acetaminophen (ACE), Guaifenesin (GUA) and Dextromethorphan (DEX) combined dosage form has been developed and validated. The components were well separated using Altima, 150 x 4.6 mm, 5m column with 1ml of Conc. Orthophosphoric acid in a 1000ml of water as Solvent A and Acetonitrile as Solvent B at a flow rate of 1.0 mL/min by using gradient programme. The eluents were detected at 272 nm using UV detector. The retention time of PHE, ACE, GUA and DEX found to be 2.5, 6.1, 8.3 and 9.0 min respectively. The linearity was observed between 2.0-7.0μg/mL,130-455μg/mL, 50-300μg/mL and 2.5-15 μg/mL for Phenylephrine, Acetaminophen, Guaifenesin and Dextromethorphan respectively. The method was validated for system suitability, specificity, linearity, accuracy, precision, ruggedness and robustness as per ICH guidelines and the results w...

Diclofenac sodium tablets are available as delayed release tablets in the market. Delayed release... more Diclofenac sodium tablets are available as delayed release tablets in the market. Delayed release tablets are typically produced by coating the tablet with enteric coating polymers. These polymers provide the resistance of drug release in acidic environment of stomach and allow the drug to be released in alkaline environment of the intestine. A large number of enteric polymers are available which provide excellent protection to drug release in acidic environment. However, each polymer dissolves at different alkaline pH. For e.g. Eudragit L-100 dissolves at pH 6 and above while Eudragit S-100 dissolves at pH 6.5 and above. HPMC Phthalate P5.5 dissolves at pH 5.5 and above while HPMC Phthalate P dissolves at pH 6 and above. Hence, for the same drug the bioavailability can subtly but significantly change based on which enteric polymer is used to provide the delayed release. The aim of the current work was to comparatively evaluate five brands of Diclofenac sodium enteric coated tablets...