Maharashtra Institute of Pharmacy
Maharashtra Institute of Pharmacy
Pund S.,Maharashtra Institute of Pharmacy |
Rasve G.,Maharashtra Institute of Pharmacy |
Borade G.,Maharashtra Institute of Pharmacy
European Journal of Pharmaceutical Sciences | Year: 2013
Venlafaxine, a dual acting antidepressant is a new therapeutic option for chronic depression. Depression is a common mental disorder associated with the abnormalities in neuronal transport in the brain. Since the nose-to-brain pathway has been indicated for delivering drugs to the brain, we analyzed the transport of venlafaxine through sheep nasal mucosa. Transmucosal permeation kinetics of venlafaxine were examined using sheep nasal mucosa mounted onto static vertical Franz diffusion cells. Nasal mucosa was treated with venlafaxine in situ gel (100 μl; 1% w/v) for 7 h. Amount of venlafaxine diffused through mucosa was measured using validated RP-HPLC method. After the completion of the study histopathological investigation of mucosa was carried out. Ex vivo studies through sheep nasal mucosa showed sustained diffusion of venlafaxine with 66.5% permeation in 7 h. Transnasal transport of venlafaxine followed a non-Fickian diffusion process. Permeability coefficient and steady state flux were found to be 21.11 × 10-3 cm h-1 and 21.118 μg cm-2 h-1 respectively. Cumulative amount permeated through mucosa at 7 h was found to be 664.8 μg through an area of 3.14 cm2. Total recovery of venlafaxine at the end of the permeation study was 87.3% of initial dose distributed (i) at the mucosal surface (208.4 μg; 20.8%) and (ii) through mucosa (664.8 μg; 66.5%). Histopathological examinations showed no significant adverse effects confirming that the barrier function of nasal mucosa remains unaffected even after treatment with venlafaxine in situ gel. Permeation through sheep nasal mucosa using in situ gel demonstrated a harmless nasal delivery of venlafaxine, providing new dimension to the treatment of chronic depression. © 2012 Elsevier B.V. All rights reserved.
Boldhane S.,Piramal Health Care Ltd |
Kuchekar B.,Maharashtra Institute of Pharmacy
Acta Pharmaceutica | Year: 2010
Metoprolol succinate (MS) gastroretentive (GR) controlled release system was formulated to increase gastric residence time leading to improved drug bioavailability. Box-Behnken model was followed using novel combinations of sodium alginate (SA), sodium carboxymethylcellulose (NaCMC), magnesium alumino metasilicate (MAS) as independent variables. Floating lag time (Flag), t25, t50, t75 sub>, diffusion exponent as dependent variables revealed that the amount of SA, NaCMC and MAS have a significant effect (p < 0.05) on t25, t50, t75 sub> and Flag. MSGR tablets were prepared and evaluated for mass, thickness, hardness, friability, drug content and floating property. Tablets were studied for dissolution for 24 h and exhibited controlled release of MS with floating for 16 h. The release profile of the optimized batch MS01 fitted first-order kinetics (R2 = 0.9868, n = 0.543), indicating non-Fickian diffusion or anomalous transport by diffusion and swelling.
Kulkarni A.D.,Maharashtra Institute of Pharmacy |
Bari D.B.,Maharashtra Institute of Pharmacy |
Surana S.J.,R C Patel Institute Of Pharmaceutical Education And Research |
Pardeshi C.V.,Maharashtra Institute of Pharmacy
Journal of Drug Delivery Science and Technology | Year: 2016
Present investigation deals with design, development and evaluation of chitosan-based spray-dried nasal mucoadhesive microspheres loaded with diltiazem hydrochloride (DTZ HCl). The principal objectives were to improve therapeutic efficacy through increased residence of microspheres on the nasal mucosa, and avoidance of hepatic first-pass metabolism. Formulation samples were characterized for preliminary physico-chemical parameters, mucoadhesiveness, drug release and release kinetics, mucosal toxicity, stability, and in vivo studies. Central composite experimental design was utilized herein to evaluate the influence of process and formulation variables product performance. Numerical and graphical optimization techniques were used for selecting optimum sample of prepared microspheres, further confirmed by three dimensional response surface plots and multilinear regression model. Results of ANOVA validated the significance of suggested models. Our findings suggest that DTZ-loaded spray-dried chitosan microspheres formulation could be used as a promising approach for intranasal administration which, in sum, improves therapeutic efficacy of the formulation. © 2015 Elsevier B.V. All rights reserved.
Thombre N.A.,Maharashtra Institute of Pharmacy |
Gide P.S.,Maharashtra Institute of Pharmacy
Drug Delivery | Year: 2016
Context: An oral dosage form containing floating bioadhesive gastroretentive microspheres forms a stomach-specific drug delivery system for the treatment of Helicobacter pylori.Objectives: To prepare and evaluate controlled release floating bioadhesive gastroretentive chitosan-coated amoxicillin trihydrate-loaded Caesalpinia pulcherrima galactomannan (CPG)-alginate beads (CCA-CPG-A), for H. pylori eradication.Materials and methods: CCA-CPG-A beads were prepared by ionotropic gelation, using 23 factorial design with quantity of drug, combination of CPG with sodium alginate and concentration of calcium chloride as variables. Beads facilitated mucoadhesion to gastric mucosa with floating nature caused by chitosan coating for wide distribution throughout GIT. Developed beads were evaluated for characteristics like beads size-morphology, entrapment efficiency, DSC, XRD, FTIR, swelling ratio, in vitro mucoadhesion, in vitro drug release, in vitro floating and in vitro H. pylori growth inhibition studies. CCA-CPG-A beads were studied in Wistar rats for in vivo gastric mucoadhesion, in vivo H. pylori growth inhibition studies using PCR amplification of isolated DNA, rapid urease test.Result: Developed beads possess drug release of 79-92%, entrapment efficiency of 65-89%, mucoadhesion of 61-89%. In vivo mucoadhesion study showed more than 85% mucoadhesion of beads even after 7th hour. In vitro-in vivo growth inhibition study showed complete eradication of H. pylori.Discussion: CPG-alginate and chitosan in beads interacts with gastric mucosubstrate surface for prolonged gastric residence with floating bioadhesion mechanism for H. pylori eradication in rats.Conclusion: Floating bioadhesive CCA-CPG-A beads offer a promising drug delivery system for H. pylori eradication at lower dose, reduced adverse effect and enhance bioavailability. © 2014 Informa Healthcare USA, Inc.
Shinde P.B.,Maharashtra Institute of Pharmacy
International Journal of Pharmacy and Pharmaceutical Sciences | Year: 2012
Recent studies have increased our understanding on the mechanistic basis of the proposed probiotic health effects. Although they are effective in curing the disease for which they are prescribed, the effect on the indigenous gut flora may persist even after cessation of the treatment. The concern about undesired side effects of use of antibiotics as therapeutic agents produced a climate in which both consumer and manufacturer are looking for alternatives. Probiotics are being considered as effective alternative. Well designed human studies have demonstrated that specific probiotic strains have health benefits in the human population. These have led to a wide acceptation of the probiotic concept. However, current probiotics have not been selected for specific purposes. Novel methods to select and characterize target-specific probiotic strains are thus needed. In addition to the traditional selection procedures, in recent years, knowledge on intestinal microbiota, nutrition, immunity and mechanisms of action has increased dramatically and can now be combined with genomic data to allow the isolation and characterization of new target- or site-specific probiotics. We should expect to see new, third generation probiotics emerging in the near future and also new selection criteria further defining the targets of future probiotics.
Auti P.B.,Maharashtra Institute of Pharmacy
Mini-Reviews in Medicinal Chemistry | Year: 2014
The 1, 4-dihydropyridines (DHPs), a class of drugs possess a wide variety of biological and pharmacological actions. It represents one of the most important groups of calcium-channel modulating agents and has experienced widespread use in the treatment of cardiovascular disease which includes antihypertensive, antianginal, vasodilator and cardiac depressants activities. It also shows antibacterial, anticancer, antileishmanial, anticoagulant, anticonvulsant, antitubercular, antioxidant, antiulcer, CFTR, antimalarials, neuroprotection properties, HIV-1 protease inhibitors, antifertility activities and many more. There are many drugs available in market which contains 1, 4-dihydropyridines ring as basic scaffold. Basic motive of this review is to disclose various therapeutic applications of 1, 4-dihydropyridine derivatives reported by other researchers during their research work in 2001 to 2011. ©2014 Bentham Science Publishers.
Sangshetti J.N.,Dr. Babasaheb Ambedkar Marathwada University |
Chabukswar A.R.,Maharashtra Institute of Pharmacy |
Shinde D.B.,Dr. Babasaheb Ambedkar Marathwada University
Bioorganic and Medicinal Chemistry Letters | Year: 2011
Sodium bisulfite has been reported first time for the synthesis of 2,5-disubstituted 1,3,4-oxadiazole using microwave and conventional method in ethanol-water. The yields obtained are in the range of 90-95% using microwave and 87-91% using conventional method. All the synthesized compounds (8a-8s) are novel and were evaluated for their in vitro antifungal activity. SAR for the series has been developed by comparing their MIC values with miconazole and fluconazole. Some of the compounds from the series like 8k was equipotent with miconazole against Candida albicans and Fusarium oxysporum. Also compound 8n was equipotent with miconazole against F. oxysporum. © 2010 Elsevier Ltd. All rights reserved.
Thombre N.A.,Maharashtra Institute of Pharmacy |
Gide P.S.,Maharashtra Institute of Pharmacy
Carbohydrate Polymers | Year: 2013
The galactomannan from the seeds of Caesalpinia pulcherrima L. was isolated and purified by precipitation method using alcohol to get C. pulcherrima (CP) gum. CP gum was studied for its physicochemical and rheological properties. The composition of CP gum was found to contain mannose:galactose:glucose:xylose in a proportion of 2.8:1:0.1:0.08, with M/G ratio 2.80. The molecular weight (M w) for CP gum was obtained to be approximately 2.72 × 10 6 Da by static light scattering measurements and 2.79 × 10 6 Da using Mark-Houwink relationship. The intrinsic viscosity by Huggins and Kraemer plots using capillary viscometry was obtained as 12-12.5 dl/g. The rheological behavior of aqueous galactomannan solutions was studied at 25 °C, using steady-shear and dynamic oscillatory measurements. The various concentrations of CP gum exhibits shear thinning non Newtonian behavior at high shear rate and Newtonian flow at low shear rate. Experimental data in steady shear has been correlated and found a better fitting with the Cross and Carreau models. A graph of the specific viscosity at zero shear rate (ηsp0) against coil overlap parameter (C[η]) was plotted and the slope of the lines in dilute and semi-dilute regions were found to be 1.23 and 4.1 respectively. The critical concentration (C*) was found to be about 3.8/[η]. The linear viscoelastic region for CP gum solutions presented nature as that of macromolecular solutions. At all shear rates and frequencies, ηap and η* had almost similar magnitudes, which shows its reasonable agreement with the Cox-Merz rule. The present investigation shows the suitability of CP gum as a pharmaceutical aid application like viscosity modifier, release retardants, binders. © 2013 Elsevier Ltd. All rights reserved.
Shiledar R.R.,Maharashtra Institute of Pharmacy |
Tagalpallewar A.A.,Maharashtra Institute of Pharmacy |
Kokare C.R.,Maharashtra Institute of Pharmacy
Carbohydrate Polymers | Year: 2014
A novel bilayered mucoadhesive buccal patch of zolmitriptan was prepared using xanthan gum (XG) as mucoadhesive polymer. Hydroxypropyl methylcellulose E-15 was used as film-former and polyvinyl alcohol (PVA) was incorporated, to increase the tensile strength of the patches. To study the effect of independent variables viz. concentrations of XG and PVA, on various dependent variables like in vitro drug release, ex vivo mucoadhesive strength and swelling index, 32 factorial design was employed. In vitro drug release studies of optimized formulation showed initially, rapid drug release; 43.15% within 15 min, followed by sustained release profile over 5 h. Incorporation of 4% dimethyl sulfoxide enhanced drug permeability by 3.29 folds, transported 29.10% of drug after 5 h and showed no buccal mucosal damage after histopathological studies. In conclusion, XG can be used as a potential drug release modifier and mucoadhesive polymer for successful formulation of zolmitriptan buccal patches. © 2013 Elsevier B.V. All rights reserved.
Jagdale S.,Maharashtra Institute of Pharmacy
Current drug delivery | Year: 2013
Simvastatin is a hypolipidemic drug used in atherosclerosis. It has short elimination half life (2-3 hours) and narrow absorption window. It is mainly absorbed from stomach. The objective of this research was to develop gastroretentive floating tablets of Simvastatin using combination of release retardant polymers like Polyox WSR 205, Polyox WSR N12K and HPMC K4M. Material and methods: 3(2) full Factorial design was applied to design the experiments and tablets were prepared by direct compression. Prepared floating tablets were evaluated for hardness, floating time, friability, % drug content, swelling index, in-vitro drug release study and mean gastric retention period by invivo X-ray study. Statistical analysis was done using design expert software and model fitting was carried out using PCP DISSO. Design expert software was validated by comparing predicted results with observed results. Statistical analysis data revealed that tablets from formulation batch D3 (containing HPMC K4M 10% and POLYOX WSR 205 35%) and formulation batch E2 (HPMC K4M 10% and Polyox WSR N12K 25%) were promising system exhibiting excellent floating properties and drug release pattern. Stability studies revealed that all formulations were physically and chemically stable. In-vivo X-ray imaging of formula D3 and formula E2 shows mean gastric retention time of 6 ± 0.5 hours.