Norfloxacin (NF) is a synthetic fluoro-quinolone molecule that is used for the treatment of urina... more Norfloxacin (NF) is a synthetic fluoro-quinolone molecule that is used for the treatment of urinary tract infections. However, due to its poor aqueous solubility, it has low oral bioavailability. The aim of the present study was to improve the aqueous solubility and dissolution profile of NF by formulating its mixed-solvency based solid dispersions (SDs). The NF-loaded SDs were prepared by a solvent evaporation technique using urea, sodium benzoate and a niacinamide hydrotropic mixture. The prepared SDs were evaluated regarding their solubility, mean particle size, in-vitro drug release and oral bioavailability. The optimized batch showed a high percentage yield of 99.04% , with a mean particle size of 132.91 m. Optimized SDs Exhibit 96.48% drug release. The oral bioavailabilities of NF from the optimized SDs, drug alone and marketed formulation were evaluated in Wistar rats at a dose of 20.0 mg/kg. In comparison to the drug alone, approximately 6.90-and 5.0-fold increases in AUC and C max , respectively, were observed for NF from mixed-solvency based SDs. The superior dissolution rate due to its reduced particle size may have contributed to the increased oral bioavailability. This study demonstrated that mixed-solvency may be an alternative approach for poorly soluble drugs to improve their solubility and oral bioavailability.
International Journal of Pharmacy and Pharmaceutical Sciences, May 21, 2015
Objective: The present study was design with an objective of developing a simple and rapid high p... more Objective: The present study was design with an objective of developing a simple and rapid high performance liquid chromatography (HPLC) method for the determination of Efavirenz (EFA) in rat plasma. Methods: Chromatographic separation was achieved on C18 column using acetonitrile-50 mM potassium phosphate (55:45 v/v) as mobile phase at a flow rate of 1 ml/min and UV detection at 250 nm. Results: The retention time of EFA was found to be 13.2 min. The developed method was validated for linearity, limit of quantification (LOQ), limit of detection (LOD), Stability and selectivity. Linearity studies were found to be acceptable over the range of 5-50 μg/ml. Conclusion: The present analytical method was found to be specific, sensitive, accurate and precise for quantification of EFA in rat plasma. It can be successively applied for pharmacokinetics studies also.
The aim of the present work was to design gellan gum and calcium carbonate based floating in situ... more The aim of the present work was to design gellan gum and calcium carbonate based floating in situ gel as an efficient anti-ulcer formulation using andrographolide (AG) as a model drug.
Self-emulsifying drug delivery system (SEDDS) is the isotropic and thermodynamically stable mixtu... more Self-emulsifying drug delivery system (SEDDS) is the isotropic and thermodynamically stable mixture of oil, surfactant, co-solvent/surfactant, and drug. It emulsifies spontaneously when introduced into an aqueous phase under a mild agitation. The current study was aimed to prepare SNEDDS to augment solubility, release rate, and oral bioavailability of BCS class II drug, efavirenz (EFV). A series of oil, surfactant, and co-surfactant was screened out by a ternary phase diagram to locate a better homogenous mixture. The prepared SNEDDS was evaluated regarding its appearance, mean droplet size, phase separation, in vitro drug release, and oral bioavailability. Among the screened oil, surfactant, and co-surfactant, Labrafil M 2125 CS, Tween 80, and Transcutol®P mixture exhibited superior solubilizing capacity, respectively. Optimized SNEDDS exhibits 98.39% drug release. SNEDDS dissolution behavior was attributed to oil/surfactant ratios and properties of the surfactant phase. It also de...
The present work reports preparation of irbesartan (IBS) loaded nanofibre mats using electrospinn... more The present work reports preparation of irbesartan (IBS) loaded nanofibre mats using electrospinning technique. The prepared nanofibres were characterized by scanning electron microscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction analysis, in vitro diffusion and ex vivo skin permeation studies. FTIR studies revealed chemical compatibility of IBS and polyvinyl pyrrolidine (PVP K-30). SEM images confirmed formation of nanofibres wherein IBS existed in amorphous form as revealed by DSC and
The purpose of this study was to achieve incorporation of a higher amount of wax during the prepa... more The purpose of this study was to achieve incorporation of a higher amount of wax during the preparation of ibuprofen beads by a melt solidification technique for better integrity and prolonged drug release by using a combination of waxes. A mixture of cetyl alcohol (CA) and ...
Norfloxacin (NF) is a synthetic fluoro-quinolone molecule that is used for the treatment of urina... more Norfloxacin (NF) is a synthetic fluoro-quinolone molecule that is used for the treatment of urinary tract infections. However, due to its poor aqueous solubility, it has low oral bioavailability. The aim of the present study was to improve the aqueous solubility and dissolution profile of NF by formulating its mixed-solvency based solid dispersions (SDs). The NF-loaded SDs were prepared by a solvent evaporation technique using urea, sodium benzoate and a niacinamide hydrotropic mixture. The prepared SDs were evaluated regarding their solubility, mean particle size, in-vitro drug release and oral bioavailability. The optimized batch showed a high percentage yield of 99.04% , with a mean particle size of 132.91 m. Optimized SDs Exhibit 96.48% drug release. The oral bioavailabilities of NF from the optimized SDs, drug alone and marketed formulation were evaluated in Wistar rats at a dose of 20.0 mg/kg. In comparison to the drug alone, approximately 6.90-and 5.0-fold increases in AUC and C max , respectively, were observed for NF from mixed-solvency based SDs. The superior dissolution rate due to its reduced particle size may have contributed to the increased oral bioavailability. This study demonstrated that mixed-solvency may be an alternative approach for poorly soluble drugs to improve their solubility and oral bioavailability.
International Journal of Pharmacy and Pharmaceutical Sciences, May 21, 2015
Objective: The present study was design with an objective of developing a simple and rapid high p... more Objective: The present study was design with an objective of developing a simple and rapid high performance liquid chromatography (HPLC) method for the determination of Efavirenz (EFA) in rat plasma. Methods: Chromatographic separation was achieved on C18 column using acetonitrile-50 mM potassium phosphate (55:45 v/v) as mobile phase at a flow rate of 1 ml/min and UV detection at 250 nm. Results: The retention time of EFA was found to be 13.2 min. The developed method was validated for linearity, limit of quantification (LOQ), limit of detection (LOD), Stability and selectivity. Linearity studies were found to be acceptable over the range of 5-50 μg/ml. Conclusion: The present analytical method was found to be specific, sensitive, accurate and precise for quantification of EFA in rat plasma. It can be successively applied for pharmacokinetics studies also.
The aim of the present work was to design gellan gum and calcium carbonate based floating in situ... more The aim of the present work was to design gellan gum and calcium carbonate based floating in situ gel as an efficient anti-ulcer formulation using andrographolide (AG) as a model drug.
Self-emulsifying drug delivery system (SEDDS) is the isotropic and thermodynamically stable mixtu... more Self-emulsifying drug delivery system (SEDDS) is the isotropic and thermodynamically stable mixture of oil, surfactant, co-solvent/surfactant, and drug. It emulsifies spontaneously when introduced into an aqueous phase under a mild agitation. The current study was aimed to prepare SNEDDS to augment solubility, release rate, and oral bioavailability of BCS class II drug, efavirenz (EFV). A series of oil, surfactant, and co-surfactant was screened out by a ternary phase diagram to locate a better homogenous mixture. The prepared SNEDDS was evaluated regarding its appearance, mean droplet size, phase separation, in vitro drug release, and oral bioavailability. Among the screened oil, surfactant, and co-surfactant, Labrafil M 2125 CS, Tween 80, and Transcutol®P mixture exhibited superior solubilizing capacity, respectively. Optimized SNEDDS exhibits 98.39% drug release. SNEDDS dissolution behavior was attributed to oil/surfactant ratios and properties of the surfactant phase. It also de...
The present work reports preparation of irbesartan (IBS) loaded nanofibre mats using electrospinn... more The present work reports preparation of irbesartan (IBS) loaded nanofibre mats using electrospinning technique. The prepared nanofibres were characterized by scanning electron microscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction analysis, in vitro diffusion and ex vivo skin permeation studies. FTIR studies revealed chemical compatibility of IBS and polyvinyl pyrrolidine (PVP K-30). SEM images confirmed formation of nanofibres wherein IBS existed in amorphous form as revealed by DSC and
The purpose of this study was to achieve incorporation of a higher amount of wax during the prepa... more The purpose of this study was to achieve incorporation of a higher amount of wax during the preparation of ibuprofen beads by a melt solidification technique for better integrity and prolonged drug release by using a combination of waxes. A mixture of cetyl alcohol (CA) and ...
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Papers by Ravindra Kamble