Delhi Institute of Pharmaceutical science and Research DIPSAR

Ābu Road, India

Delhi Institute of Pharmaceutical science and Research DIPSAR

Ābu Road, India
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Nanda S.,M D University | Pathak D.P.,Delhi Institute of Pharmaceutical science and Research DIPSAR
Medicinal Chemistry Research | Year: 2013

In present research work, we report the synthesis, in vitro hydrolysis study and pharmacological evaluation of new mutual prodrugs of mefenamic acid (MA) and 1,2 dihydro-1,5-dimethyl-4-(1-methylethyl)-2-phenylpyrazol-3-one with the aim of improving the therapeutic potency and retard the adverse effects of gastrointestinal origin. The structure of the synthesized mutual ester prodrugs (MP1 and MP2) were confirmed by IR, 1H NMR, 13C NMR, mass spectroscopy and their formation was confirmed by TLC. The purity of the synthesized compounds was established by elemental analysis. The title compounds were tested for analgesic activity by acetic acid-induced writhing method; anti-inflammatory activity was tested by carrageenan-induced rat paw edema method and ulcerogenicity. The study of the analgesic activity revealed that both prodrugs (MP1 and MP2) have shown significant reduction (81.67, 63.90 %) in writhing response produced by acetic acid as compared to parent drug MA (61.10 %). Both mutual prodrugs showed better maximum anti-inflammatory effects (71.43, 85.71 %) and for longer time as compared to parent drug MA (53.14 %). The synthesized prodrugs were also found to be very less irritating to gastric mucosal membrane than parent drugs. The kinetics of ester hydrolysis was studied in simulated gastric fluid (SGF) at pH 1.2 and simulated intestinal fluid (SIF) at pH 7.4. The release of free MA from prodrugs showed negligible hydrolysis in SGF as compared to SIF. This indicated that prodrugs were sufficiently stable at pH 1.2 and do not break in the stomach, but release MA in SIF. © 2013 Springer Science+Business Media New York.

Agrawal S.S.,Delhi Institute of Pharmaceutical science and Research DIPSAR
Indian Journal of Natural Products and Resources | Year: 2014

Zuroor-e-Qula, a powdered polyherbal Unani formulation, known to possess antimicrobial and anti-inflammatory properties is recommended in cases of stomatitis and gastric ulceration. The freshly prepared formulation was evaluated for its mineral contents, microbial count, aflatoxins and pesticide residues. The results revealed that this formulation is free from such contaminants and its use is safe. © 2014 National Institute of Science Communication and Information Resources (NISCAIR). All rights reserved.

Agrawal S.S.,Delhi Institute of Pharmaceutical science and Research DIPSAR | Jose M.A.,Delhi Institute of Pharmaceutical science and Research DIPSAR
European Journal of Contraception and Reproductive Health Care | Year: 2011

Objective To evaluate the anti-ovulatory activity of H2 receptor blockers (ranitidine, famotidine and roxatidine) in albino rabbits considering the role of histamine in ovulation. Method The drugs were orally administered once daily for three days to adult female rabbits weighing between 1.3-2.0 kg (four groups of three animals). The control group received the 1% weight/volume gum acacia suspension. Thirty minutes after the administration of the last dose, a freshly prepared 0.4 % solution of cupric acetate was administered to each animal intravenously via the marginal ear vein (4 mg/kg body weight) to induce ovulation. To assess ovulation, laparotomy was carried out 48 h after cupric acetate injection. The ovaries were exposed, bleeding points on each ovary were counted, and the ovaries and uteri were subjected to histopathological evaluation. Results Based on the number of bleeding points (ovulation sites) observed on the ovary, H2 blockers showed varying degrees of anti-ovulatory activity. Roxatidine exerted the most pronounced activity. Histopathological observations of uterus and ovary confirmed the aforementioned observations. Conclusion H2 receptor blockers appeared to inhibit the cupric acetate-induced ovulation in albino rabbits. Our results seem to confirm the role of histamine in ovulation reported by other authors. © 2011 The European Society of Contraception and Reproductive Health.

Agnihotri S.,Delhi Institute of Pharmaceutical science and Research DIPSAR | Wakode S.,Delhi Institute of Pharmaceutical science and Research DIPSAR | Ali M.,Jamia Hamdard University
Natural Product Research | Year: 2012

Hydrodistilled oil obtained from the stem bark of Myrica esculenta Buch. Ham. ex D. Don (yield 0.3%) was analysed by capillary GC and GC-MS. The volatile oil consisted mainly of n-hexadecanol (25.2%), eudesmol acetate (21.9%), palmitic acid (11.6%), cis-β-caryophyllene (8.7%), n-pentadecanol (7.7%) and n-octadecanol (7.6%). The oil was found to be a potential antimicrobial agent against Bacillus pumilus, Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Pseudomonas aeruginosa, Candida albicans, Aspergillus niger and Saccharomyces cerevisiae. The essential oil exhibited significant topical anti-inflammatory activity compared to standard drug in Swiss albino mice ear. © 2012 Taylor & Francis Group, LLC.

Manchanda S.,Delhi Institute of Pharmaceutical science and Research DIPSAR | Sahoo P.K.,Delhi Institute of Pharmaceutical science and Research DIPSAR | Majumdar D.K.,Apeejay Stya University
Nanotechnology Reviews | Year: 2016

Chitosan-dextran sulfate nanoparticles of acetazolamide were formulated by using the ionic gelation technique, and evaluated for different attributes like particle size, ζ potential, drug entrapment, particle morphology, in vitro drug release, and in vivo efficacy. Particle size was observed to be changed with the increment of the drug/polymer ratio. Sustained in vitro drug release was exhibited by the particulate formulation that followed the Korsmeyer-Peppas kinetic model. Drug release from nanoparticles was found to occur, as shown by the results, through a combination of dissolution and diffusion. The optimized formulation had a particle size of 172.3 nm and ζ potential of 36.46 mV. The particles had a spherical shape and polydispersity index of 0.257. Decrease in crystallinity of the drug was indicated by powder X-ray diffraction and differential scanning calorimetry studies, in the optimized nanoparticle formulation. Approximately 2.5 times higher transcorneal permeation of drug was observed across the excised goat cornea, in comparison to the aqueous solution of drug, without any corneal damage, during ex vivo transcorneal studies. In vitro mucoadhesion studies showed 91.59% mucoadhesion. The in vivo studies involving ocular hypotensive activity in rabbits revealed significantly higher hypotensive activity with a p-value of <0.05, in contrast to a plain drug solution, with no signs of ocular irritation. The stability studies showed that the formulation was rather stable. © 2016 Walter de Gruyter GmbH, Berlin/Boston 2016.

Kirana H.,Delhi Institute of Pharmaceutical science and Research DIPSAR | Srinivasan B.P.,Delhi Institute of Pharmaceutical science and Research DIPSAR
Indian Journal of Experimental Biology | Year: 2010

In view of multi-dimensional activity of plant drugs beneficial to complex disorders like diabetes, the present study has been undertaken to evaluate the effect of aqueous extract of C. peltata roots on serum glucose, lipid profile, insulin, inflammatory marker namely tumour necrosis factor (TNF)-α and muscle glycogen in type 2 diabetic rats. Aqueous extract of C. peltata at 40 and 60 mg/kg dose significantly decreased both the fasting and postprandial blood glucose of type 2 diabetic rats; 60 mg/kg dose having more pronounced effect on hyperglycemia. An enhanced insulin levels by the aqueous extract is primary for its glucose and lipid lowering activity. The extract significantly decreased the elevated TNF-α in type 2 diabetic rats. The extract at 40 and 60 mg/kg dose increased the glycogen levels in skeletal muscle by 58 and 60% respectively. Improved glycogen in peripheral tissue such as skeletal muscle indicates the ability of plant drug to combat insulin resistance of type 2 diabetes.

Singh A.,R V Northland Institute | Sharma P.K.,Meerut Institute of Engineering and Technology MIET | Majumdar D.K.,Delhi Institute of Pharmaceutical science and Research DIPSAR
Journal of Liquid Chromatography and Related Technologies | Year: 2014

In the present work, a new reverse phase-high performance liquid chromatography (RP-HPLC) method was developed, validated, and compared for estimation of the bis-triazole antifungal fluconazole (FLZ), in different simulated biological fluids, that is, gastric fluid simulant (GFS, pH = 1.5), vaginal fluid simulant (VFS, pH = 4.2), topical simulated media-phosphate buffer (PB, pH = 6.8), blood plasma simulant-phosphate buffer saline (PBS, pH = 7.4) and in methanol. For RP-HPLC the chromatography was carried out on a octadecyl silane (ODS-3) Hypersil C18 column (250 mm × 4.6 mm × 5 μm) using water (pH 5.2, adjusted with orthophosphoric acid) and acetonitrile (80:20, v/v) as the mobile phase at a flow rate of 2.5 mL/min with detection at 260 nm. The calibration curve of standard FLZ was linear in the range 0.2-40 μg/mL, 0.1-40 μg/L, 0.2-40 μg/mL, 0.1-40 μg/mL, and 0.2-50 μg/mL, in GFS, VFS, PB, PBS, and in methanol, respectively. All the methods were validated with respect to linearity, precision, accuracy, and specificity for intra- and inter-day and satisfied the International Conference on Harmonisation (ICH) and United States Food and Drug Administration (USFDA'S) guidelines. Copyright © 2014 Taylor & Francis Group, LLC.

Agrawal S.S.,Delhi Institute of Pharmaceutical science and Research DIPSAR | Aggarwal A.,Delhi Institute of Pharmaceutical science and Research DIPSAR
Contemporary Clinical Trials | Year: 2010

The present study deals with transdermal drug delivery system (TDDS) of Carvedilol (CRV) and Hydrochlorothiazide (HCTZ). It compares the bioavailability of these two study drugs from a TDDS with conventional immediate release oral tablets in healthy volunteers. The TDDS was also evaluated for any adverse drug reaction. This was an open-label, randomised, single centre, two-treatment, two period, single dose, crossover pilot study of two formulations of cardiovascular agents. Subjects (n = 10) were randomised to have a TDDS applied to their abdominal skin for 72 h or receive one oral tablet each of CRV and HCTZ respectively in period I, followed by 1-week washout period. They received the alternative treatment in period II. A significant improvement in bioavailability was observed with the transdermal patches over oral tablets as observed by the mean AUC(0 - t) values 4004.37 ± 180.98 and 1824.30 ± 17.43 ng h/mL respectively for CRV and HCTZ as compared to 753.46 ± 53.34 and 392.89 ± 34.23 ng h/mL respectively, with the oral tablets. The TDDS possesses significant potential for skin irritation. The TDDS developed in our laboratory produced therapeutically effective plasma concentrations of the cardiovascular agents up to a range of 60 to 72 h (in different volunteers with a mean = 66 h). It could be concluded from these observations that the TDDS meets the intended goal of at least 2 day management of stage II hypertension with application of a single transdermal patch, hence improving patient compliance over the inconvenience seen with frequent oral administration. © 2010 Elsevier Inc. All rights reserved.

Agrawal S.S.,Delhi Institute of Pharmaceutical science and Research DIPSAR | Pruthi J.K.,Delhi Institute of Pharmaceutical science and Research DIPSAR
Contraception | Year: 2011

Background: Medroxyprogesterone acetate (MPA), which increases high-density lipoprotein level, has not been used as a progestin in combination with estrogen in a transdermal patch to date. The aim of the research was to develop and evaluate a matrix-type transdermal drug delivery (TDD) system of a combination of ethinylestradiol (EE) and MPA for interception. Study Design: The transdermal patch of EE and MPA was prepared using various film-forming polymers with and without n-dibutyl phthalate as plasticizer and with glycerol and sodium lauryl sulphate as penetration enhancer. All formulations were assayed using UV spectrophotometer by Vierordt's equation for EE and MPA. Results: The percentage cumulative release of F6 (optimized formulation) named as 'AGARPRU' was found to be 99.94%±1.25% and 69.99%±1.02% (mean±SD) through rat skin and 92.69%±2.22% and 53.51%±2.11% (mean±SD) through cadaver skin for EE and MPA, respectively. Pharmacodynamic studies of 'AGARPRU' in female Wistar rats showed 100% anti-implantation activity. The in vivo results showed prolonged T max of 36 h for both EE and MPA after transdermal administration compared to oral route (2 h). Moreover, the area under the curve of EE and MPA revealed an increase in bioavailability after transdermal administration as compared to oral route. Conclusion: These findings suggested that TDD formulation aimed for postcoital antifertility activity has been successfully developed in female Wistar rats. © 2011 Elsevier Inc. All rights reserved.

Agnihotri S.,Delhi Institute of Pharmaceutical science and Research DIPSAR | Wakode S.,Delhi Institute of Pharmaceutical science and Research DIPSAR | Agnihotri A.,R V Northland Institute
Indian Journal of Natural Products and Resources | Year: 2010

Plant drugs have been the major source for treatment of diseases for a long time. They have been used in traditional medicine on the basis of experiences and practice. With the advent of modern systems of medicine need has been felt to investigate the active constituents present in these plants. Various molecules have been isolated, characterized and tested for their related pharmacological activities. The active molecules have provided significant leads in the development of more effective synthetic molecules. Inflammation is the major condition associated with various diseases. Rheumatoid arthritis is one of the challenging disorders associated with inflammatory conditions. Various molecules have been isolated from plant drugs which have been proven very effective in such conditions. For example: a potent anti-inflammatory analgesic molecule Aspirin was developed from Salicin, a compound isolated from bark of Salix alba Linn. This paper provides an overview on the recent findings on some plants having anti-inflammatory activity and chemical constituents isolated from them.

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