Anand Pharmacy College
Anand Pharmacy College
Lalwani J.T.,Intas Pharmaceuticals Ltd |
Thakkar V.T.,Anand Pharmacy college
International Journal of Pharmacy and Pharmaceutical Sciences | Year: 2013
Objectives: To develop a stable formulation for self emulsifying drug delivery systems (SEDDS) in order to enhance the solubility, rate and extent of drug release and oral bioavailability of the poorly soluble drug, ezetimibe. Experimental work done: A solubility of drug was determined in various oils, surfactants and co-surfactants by using spectrophotometric method. Pseudo-ternary phase diagrams were constructed to study the phase behavior and the most efficient self emulsifying regions when the system was diluted with water. Prepared solid SEDDS were filled in hard gelatin capsule and in vitro release was performed using a USP Type-II apparatus. Results and discussion: Ezetimibe shows highest solubility in Capmul PG8 (oil), Tween 80 and Cremophore EL (surfactant), and propylene glycol (co-surfactant) so these vehicles were selected for further study. A microemulsion region was found to be increase in pseudo-ternary phase diagrams when surfactant concentration increased as compared to co-surfactant when diluted with water, and the final formulation with good self-emulsifying ability as well as a high solubilization capacity was established. The optimized formulation F5 showed highest release rate (97.3 %) among all the solid SEDDS formulations and marketed tablet (Ezetimibe USP 10 mg). The mean particle size of the resultant emulsion was about 16.46 nm and the ζ-potential of the solid SEDDS in distilled water was -19.9 mV, determined by Zetasizer Nano S 90 (Malvern Instruments, U.K). Conclusions: In this study, a new ezetimibe solid SEDDS containing oil phase (Capmul PG 8) of 11.11%, Tween 80:Cremophor EL (1:1) of 59.26%, and propylene glycol of 29.63 % was developed from data of evaluation of drug solubility in various solvents performed and detailed study of pseudo-ternary phase behavior. The resultant emulsion was negative charged, with a small mean size and a narrow particle size distribution. The release rate of ezetimibe from solid SEDDS was faster than from conventional tablets.
Patel N.V.,Anand Pharmacy College |
Patel J.K.,Nootan Pharmacy College |
Shah S.H.,Lj Institute Of Pharmacy
Pharmazie | Year: 2011
Budesonide is a potent glucocorticoid with high affinity for the glucocorticoid receptor, which is used for the treatment of inflammatory bowel diseases. Current oral formulations of budesonide present low efficacy against ulcerative colitis because of the premature drug release in the upper part of the gastrointestinal tract. The objective of this study was to develop a colon specific delivery system for budesonide to increase the efficacy in the treatment of ulcerative colitis using a statistical procedure. Pellets were prepared by powder layering of budesonide on nonpareils (0.5-0.6 mm) in a coating pan. Drug-layered pellets were coated with an inner layer of a combination of Eudragit® RL PO and RS PO and an outer layer of Eudragit FS in a fluidized-bed apparatus. Central composite design was used to study the effect of three independent variables. The independent variables selected were amount of Eudragit FS outer coating (X 1), proportion of Eudragit RL PO in the inner coating (X 2), amount of Eudragit RL PO-RS PO inner coating (X 3). Fifteen batches were prepared and evaluated for amount of drug released in 6 h (Y 1), amount of drug released in 12 h (Y 2). The proportion of the more hydrophilic polymer Eudragit RL PO had the most significant effect on drug release - higher proportion gave faster release; the amount of inner and outer coat did not have a significant effect on the rate of drug release at either 6 or 12 h in the range studied. The computer optimization process and contour plots predicted the levels of independent variables X 1, X 2, and X 3 (0.79, 0.69 and 0.35 respectively), for colon targeting.
Suthar V.,Gujarat University |
Butani S.,Nirma University |
Gohel M.,Anand Pharmacy College
Journal of Drug Delivery Science and Technology | Year: 2016
The aim of current research was to develop and characterize solid self-emulsified nanostructures (S-SEN) loaded with a BCS class II drug, Lercanidipine hydrochloride (LCH). The liquid self-emulsified nanostructures (L-SEN) were prepared using rice bran oil and glyceryl monooleate (GMO) as oil phase and Tween 80 and propionic acid as surfactant and co-surfactant respectively. Phase diagrams were constructed to identify the suitable composition which spontaneously form nanoemulsion that is not affected by dilution and temperature. The L-SEN was characterized for self-nanoemulsification time, % transmittance, cloud point, globule size, zeta potential and in-vitro drug release. The optimized formulation was adsorbed onto Neusilin US2 to prepare S-SEN. Flow property was found to be excellent and XRD, DSC and SEM revealed that the LCH was converted into amorphous form and hence dissolution was improved. A mathematical model was adopted and three dimensionless parameters, dissolution number, Dn, dose number, Do, and absorption number, An were calculated. The fraction of dose absorbed was estimated for pure untreated LCH (<0.1) and S-SEN (>0.9). This calculation and the convolution derived plasma concentration-time profile suggested that more than 90% drug would get absorbed from S-SEN. Hence S-SEN can be proposed as useful dissolution enhancement strategy for LCH. © 2015 Elsevier B.V. All rights reserved.
Patel P.K.,Maliba Pharmacy College |
Patel M.A.,Ck Pithawala Institute Of Pharmaceutical Science And Research |
Vyas B.A.,Maliba Pharmacy College |
Shah D.R.,Maliba Pharmacy College |
Gandhi T.R.,Anand Pharmacy College
Journal of Ethnopharmacology | Year: 2012
Ethnopharmacological relevance: A well-known traditional herb Solanum xanthocarpum is widely used in India for the management of different ailments including urolithiasis. This study was designed to rationalize the use of Solanum xanthocarpum in kidney stone and to investigate its mechanism of action. Materials and methods: The saponin rich fraction prepared from fruits of Solanum xanthocarpum (SXS) was evaluated for antiurolithiatic activity by in vitro and in vivo studies. In ethylene glycol (EG, 0.75 in drinking water for 28 days) induced urolithiasis model, two different experimental doses (20 mg/kg and 40 mg/kg, p.o.; for 28 days) of saponin rich fraction were selected by dose fixation study. After 28 days, various biochemical parameters were measured in urine, serum and kidney homogenate. Kidneys were also subjected to histopathological analysis. Results: In vitro calcium oxalate crystal (CaOx) nucleation as well as aggregation was inhibited in artificial urine solution by SXS. The lithogenic treatment caused polyuria, damage renal function and oxidative stress, manifested as increased malondialdehyde, depleted reduced glutathione and decreased antioxidant enzyme catalase activities of the kidneys, which were prevented by simultaneous administration with SXS. Lithogenic treatment also caused crystalluria, hyperoxaluria, hypercalciuria, hypocitrauria, and hypomagnesaemia. Deposition of CaOx in renal tissue and cellular injury were seen in histopathology. Co-administration of SXS had potential to prevent these pathological changes due to lithogenic treatment. Moreover, SXS raised level of glycosaminoglycan, a stone inhibitor macromolecule found in urine which decreased. Conclusion: The antiurolithiatic activity in Solanum xanthocarpum is mediated possibly through the inhibition of CaOx crystal formation and its effect on the urinary concentration of stone-forming constituents and nephrolithiasis inducing factors and this study rationalizes its medicinal use in urolithiasis. © 2012 Elsevier Ireland Ltd.
Patel N.,Saurashtra University |
Thakkar V.,Anand Pharmacy College |
Moradiya P.,Anand Pharmacy College |
Gandhi T.,Anand Pharmacy College |
Gohel M.,Anand Pharmacy College
Journal of Drug Delivery Science and Technology | Year: 2015
Sexually transmitted infections and unplanned pregnancies present a great risk to the reproductive health of women. Therefore, female-controlled vaginal products directed toward disease prevention and contraception is needed urgently. The purpose of this investigation was to develop poloxamer based thermo sensitive contraceptive vaginal in situ hydrogel of curcumin, a plant-derived diferuloylmethane compound. Different formulations using different ratio of poloxamer 407/188 and mucoadhesive polymer - HPMC K4M were prepared and optimized by box behnken experimental design (BBD). Formulations were optimized on the basis of gelation temperature (°C), gel strength (gm/cm2), Mucoadhesive strength (dyne/cm2), viscosity (Pa) and % drug release. Optimized formulation was subjected to In Vitro sperm immobilization study on 5 fertile human volunteers' ejaculate sample. The quantitative effect of independent variables on dependent variables at different levels could be predicted by polynomial equations. From BBD, that batch containing 19.96% Poloxamer 407, 3.83% Poloxamer 188, 0.91% HPMC K4M was optimized. Total 100% Sperm immobilization was achieved within 15 min by optimized formulation for 3.5 ml of dose. Stability study of optimized batch shows no change in physical and chemical characteristics. Curcumin would be successfully formulated as thermo sensitive In Situ gelling mucoadhesive system for contraception. © 2015 Elsevier B.V.
Solanki T.,Anand Pharmacy College |
Shah P.,Anand Pharmacy College |
Patel K.,Anand Pharmacy College
Indian Journal of Pharmaceutical Sciences | Year: 2014
High performance thin layer chromatographic method for simultaneous estimation of olmesartan medoxomil, amlodipine besylate and hydrochlorothiazide was developed and validated as per ICH guidelines. Moreover, robustness testing was performed applying a central composite design with k factor having 2 k factorial runs, 2k axial experiments and two center points. High performance thin layer chromatographic separation was performed on aluminium plates precoated with silica gel 60F 254 and toluene:chloroform: methanol:acetonitrile:formic acid (2:7:1.8:0.8:0.2% v/v) as optimized mobile phase. The detection wavelength for simultaneous estimation of three drugs was 232nm. The R f values for olmesartan medoxomil, amlodipine besylate and hydrochlorthiazide were 0.78, 0.20 and 0.45, respectively. Percent recoveries in terms of accuracy for the marketed formulation was found to be 101.3-104.4, 100.7-104 and 101.5-103.9 for, olmesartan medoxomil, amlodipine besylate and hydrochlorthiazide, respectively. The pooled %relative standard deviation values for repeatability studies and intermediate precision studies was found to be less than 2% for olmesartan medoxomil, amlodipine besylate and hydrochlorthiazide, respectively. All the three factors evaluated in the robustness testing by central composite design were found to have an insignificant effect on the retention factor. However, methanol content in total mobile phase as a factor appeared to have significant effect on robustness, compared to band size and developing distance and hence it is important to be carefully controlled. In summary, a novel, simple, accurate and reproducible high performance thin layer chromatographic method was developed, which would be of use in quality control of these tablets.
Panchal H.,Anand Pharmacy College |
Shah M.B.,JKK Nataraja Dental College and Hospital
Journal of AOAC International | Year: 2017
In this study, a simple and rapid LC with tandem MS method was developed and validated for the simultaneous determination of kaempferol and quercetin in Thespesia populnea extract. The compounds were eluted using a Gemini C18 column (50 × 2.0 mm, 3 μm), with the mobile phase consisting of acetonitrile-0.3% formic acid in water at the flow rate of 0.400 mL/min. The assay exhibited a linear dynamic range of 25-2500 ng/mL for both kaempferol and quercetin. The values for intra- and interday precision and accuracy were well within the generally accepted criteria for analytical methods (<15%). Selectivity, linearity, LOD, LOQ, accuracy, and precision were evaluated for both analytes. The proposed method is accurate and sensitive and can be used for the routine quantification of kaempferol and quercetin in the herbal extract and in polyherbal formulations.
Patel A.,Anand Pharmacy College
Indian Drugs | Year: 2015
Withaferin A, a steroidal lactone which is present in dry root extract of Withania somnifera (WSe), is reported to possess numerous pharmacological activities and shows poor aqueous solubility. the purpose of this study is to enhance the dissolution rate and oral bioavailability of WSe by incorporating it in self nano emulsifying drug delivery system (SNeDDS). capmul McM-based SNeDDS formulation with tween 20 as surfactant and ethanol as co surfactant was developed for oral delivery of withaferin A. Optimised SNEDDS was evaluated for its self-emulsifcation time and viscosity, droplet size. The optimised SNeDDS formulation containing withaferin A, capmul McM(12.4%), tween 20 (58.2%) and ethanol (29%), and showed higher in vitro drug release as compared to pure WSe. these results demonstrate the potential use of SNeDDS for improving the oral bioavailability of poor water soluble compounds such as withaferin A.
Patel N.,Anand Pharmacy College |
Patel J.,Nootan Pharmacy College |
Shah S.,L J Institute Of Pharmacy
Acta Pharmaceutica | Year: 2010
The aim of this study was to investigate the combined influence of 3 independent variables in the compression coated tablet of mesalamine for ulcerative colitis. A 3-factor, 3-level Box-Behnken design was used to derive a second order polynomial equation and construct contour plots to predict responses. The independent variables selected were: percentage of polymers (pectin and compritol ATO 888) in compression coating (X1), coating mass (X2) and coating force (X3). Fifteen batches were prepared and evaluated for percent of drug released in 5 h (Y5), time required for 50 % mesalamine to dissolve (t50) with rat cecal (RC) content and without rat cecal content (t50), percent of drug released in 24 h in the presence of rat cecal content (Y24 with RC). Transformed values of independent and dependent variables were subjected to multiple regressions to establish a full-model second-order polynomial equation. F was calculated to confirm the omission of insignificant terms from the full-model equation. The computer optimization process and contour plots predicted the levels of independent variables X1, X2, and X3 (0, 0.2 and -0.15, respectively) for colon targeting and total percent of drug released up to 24 h.
Parikh M.,Anand Pharmacy College |
Patel K.,M. S. University of Baroda |
Soni S.,Anand Pharmacy College |
Gandhi T.,Anand Pharmacy College
Journal of Atherosclerosis and Thrombosis | Year: 2014
The nuclear receptor liver X receptor [LXR] is activated by endogenous oxidized derivatives of cholesterol. It constitutes a critical receptor in the regulation of various physiological functions related to the development of metabolic and cardiovascular diseases, such as atherosclerosis and diabetes, as well as various other disorders. Both isoforms of LXR, LXRα [NR1H3] and LXRβ [NR1H2], form heterodimers with the isoforms of the retinoid X receptor [RXR], which then regulate the gene expression by binding to DNA sequences associated with target genes. LXR acts as a cholesterol sensor in response to an increased concentration of cholesterol in cells and induces the transcription of genes that protect cells from cholesterol overload. LXRs play numerous roles in controlling cholesterol homeostasis via their actions on bile acid synthesis and metabolism/excretion, reverse cholesterol transport and cholesterol absorption/excretion in the intestines. Therefore, these receptors show great potential as pharmacological targets for anti-atherosclerotic activities. Recent discoveries have also emphasized the important involvement of LXRs in the pathogenesis of diabetes, Alzheimer's disease, inflammation, adrenal steroid synthesis, skin aging and male fertility. However, LXR activation has also been shown to stimulate lipogenesis via sterol regulatory element binding protein-1c, leading to liver steatosis and hypertriglyceridemia. This review summarizes recent scientific discoveries and the biological actions of LXR with a special focus on the involvement of this type of receptor in important diseases and conditions.