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.
Snehlata H.S.,Maharashtra Institute of Pharmacy |
Payal D.R.,Maharashtra Institute of Pharmacy
International Journal of Current Pharmaceutical Review and Research | Year: 2011
Fenugreek (Trigonella foenum-graecum L.), plant is widely distributed throughout the world and which belongs to the family Fabacecae. The yields can be significant increase in quantity and quality through the suitable management of cultivation, irrigation and harvesting. The plant contains active constituents such as alkaloids, flavonoids, steroids, Saponins etc. It is an old medicinal plant. It has been commonly used as a traditional food and medicine. Fenugreek is known to have hypoglycemic, and hypocholesterolaemic, effects, Anti-inflammatory effects. Recent research has identified fenugreek as a valuable medicinal plant with potential for curing diseases and also as a source for preparing raw materials of pharmaceutical industry, like in steroidal hormones. Since fenugreek is a self-pollinated crop, a mutation breeding method can be used to generate mutants with a determinate growth habit. Irradiation and chemical mutagens can be used to produce point mutations in fenugreek. This review gives view mainly on the biological activities of some of the fenugreek compounds isolated, pharmacological actions of the fenugreek extracts, clinical studies and genetic, bredding and biotechnological studies.
Pund S.,Maharashtra Institute of Pharmacy |
Borade G.,Maharashtra Institute of Pharmacy |
Rasve G.,Maharashtra Institute of Pharmacy
Phytomedicine | Year: 2014
Berberine, an isoquinoline alkaloid, has wide biological and pharmacological actions. Despite the promising pharmacological effects and safety of berberine, poor oral absorption due to its extremely low aqueous solubility results in poor oral systemic bioavailability. This limits its clinical usage. This study describes the development and characterization of self-nanoemulsifying drug delivery system (SNEDDS) of berberine in liquid as well as solid form with improved solubility, dissolution and in vivo therapeutic efficacy. The SNEDDS of berberine were prepared using Acrysol K-150, Capmul MCM and polyethylene glycol 400. The formulations were characterized for various in vitro physicochemical characteristics. In vivo efficacy was evaluated in acetic acid induced inflammatory bowel model in rats. Anti-angiogenic activity of the developed SNEDDS of berberine was studied using chick chorioallantoic membrane assay. SNEDDS of berberine rapidly formed nanoemulsions with globule size of 17-45 nm. The in vitro rate and extent of release of berberine from SNEDDS was significantly higher than berberine alone. Chick chorioallantoic membrane assay revealed potent anti-angiogenic activity of SNEDDS of berberine. These studies demonstrate that the SNEDDS of berberine is a promising strategy for improving its therapeutic efficacy and have potential application in the treatment of chronic inflammatory conditions and cancer. © 2013 Elsevier GmbH.
Jagdale S.C.,Maharashtra Institute of Pharmacy |
Pawar C.R.,Maharashtra Institute of Pharmacy
Current Drug Delivery | Year: 2014
Floating pulsatile is combined approach designed according to circadian rhythm to deliver the drug at right time, in right quantity and at right site as per pathophysiological need of disease with prolong gastric residence and lag phase followed by burst release. As the migraine follows circadian rhythm in which headache is more painful at the awakening time, the dosage form should be given during night time to release drug when pain get worsen. Present work deals with formulation and optimization of floating pulsatile tablet of sumatriptan succinate. Core tablet containing crospovidone as superdisintegrant (10%) showed burst release. Lag time was maintained using swellable polymer as polyoxN12K and xanthum gum. 32 experimental design was carried out. Developed formulations were evaluated for physical characteristics, in vitro and in vivo study. Optimized batch F2 with concentration of polyox N12K (73.43%) and xanthum gum (26.56%) of total polymer weight showed floating lag time 15±2 sec, drug content 99.58±0.2 %, hardness 6±0.2 Kg/cm2 and drug release 99.54±2% with pulsatile manner followed lag period of 7±0.1h. In vivo x-ray study confirms prolong gastric residence of system. Programmable pulsatile release has been achieved by formulation F2 which meet demand of chronotherapeutic objective of migraine. © 2014 Bentham Science Publishers.
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.
Pangarkar P.A.,Maharashtra Institute of Pharmacy
International Journal of Pharmacy and Technology | Year: 2013
More than one third of drug in pharmaceutical industry show polymorphism. These polymorphic or crystalline drugs have their stringent and specific physicochemical properties. These stringencies regarding physicochemical properties make it difficult for the formulation of such drugs into suitable dosage form. Various methods are available for the improvement of physiochemical properties of these medicinal agents, but most of the time they fail to give the satisfied results. To resolve all these complications, the prior study of polymorphic properties can be very helpful. Crystalline drugs always have their thermodynamic as well as kinetic properties. As such these properties make them crystalline but at the same time these drugs get it difficult for ideal formulation. This review covers the information regarding drug polymorphism as detail as possible. The methods, newer techniques in the field of crystallization, sophisticated techniques for the characterization of crystal forms and the regulatory consideration have been discussed in detailed. The role of crystallization processes in pharmaceutical science and technology can be associated, both, with its influence on the solid-state properties of the drug substances and with an effect on drug product stability and performance. The concept of crystal and particle engineering applied to pharmaceutical substances requires, first of all, reproducibility and consistency of the solid-state properties.
Datar P.A.,Maharashtra Institute of Pharmacy |
Limaye S.A.,Maharashtra Institute of Pharmacy
Anti-Inflammatory and Anti-Allergy Agents in Medicinal Chemistry | Year: 2015
Mannich bases were selected for 2D QSAR study to derive meaningful relationship between the structural features and analgesic activity. Using the knowledge of important features a novel series was designed to obtain improved analgesic activity. A series of novel Mannich bases 1-(N-substituted amino)methyl]-2-substituted benzimidazole derivatives were synthesized and were screened for analgesic activity. Some of these compounds showed promising analgesic activity when compared with the standard drug diclofenac sodium. © 2015 Bentham Science Publishers.
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.