Rāichūr, India
Rāichūr, India

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Prakash P.R.,Net Pharmacy College | Soujanya C.,Net Pharmacy College
Asian Journal of Pharmaceutical and Clinical Research | Year: 2010

The present research has been undertaken with the aim to develop a topical gel formulation of etoricoxib, which would attenuate the gastrointestinal relater toxicities associated with oral administration. Etoricoxib is a highly selective cyclooxygenase-2 (cox-2) inhibitor. In the present study gels with carbopol, HPMC K4M, MC, HPC were prepared with different permeation enhancers like, DMSO, lemongrass oil, menthe oil, oleic acid. They were evaluated for physicochemical properties, drug release. After in vitro evaluation of gel formulations, ex vivo permeation of etoricoxib was evaluated across rat epidermis and human cadaver skin. The best formulation was then evaluated for the anti-inflammatory and skin irritation study. And were kept for stability studies for period of three months and found that they were stable and finally it was concluded that the formulation F25 was the best and comparable with that of marketed product.

Ramaprasad G.C.,Mangalore University | Ramaprasad G.C.,Biocon | Kalluraya B.,Mangalore University | Sunil Kumar B.,Net Pharmacy College | Mallya S.,Mangalore University
Medicinal Chemistry Research | Year: 2013

In search of pharmalogically active molecules in the class of oxadiazoles, the present article deals with the synthesis of 5-(5′-fluoro-2′- methoxybiphenyl-3-yl)-1,3,4-oxadiazol-2(3H)-one 2 from its hydrazide analog 1. The compound 2 was regioselectively N-alkylated with alkyl halides and produced the compounds 3a-f. Compound 3f was further functionalized with substituted benzenesulfonyl chlorides to give compounds 3g-j. The synthesized compounds were characterized by elemental and spectral analysis. Newly synthesized compounds were tested for their in vivo anti-inflammatory, analgesic, and in vitro antimicrobial activities. The compounds 3a-c were found to have promising anti-inflammatory and analgesic activities. Compounds 3b, 3f, and 3g showed significant antibacterial and antifungal activities. © 2013 Springer Science+Business Media New York.

Kumar S.,Net Pharmacy College | Alagawadi K.,KLE University | Rao M.,Net Pharmacy College
Indian Journal of Pharmacology | Year: 2011

Objectives: To evaluate the antiobesity effects of the ethanolic extract of Argyreia speciosa roots in rats fed with a cafeteria diet (CD). Materials and Methods: Obesity was induced in albino rats by feeding them a CD daily for 42 days, in addition to a normal diet. Body weight and food intake was measured initially and then every week thereafter. On day 42, the serum biochemical parameters were estimated and the animals were sacrificed with an overdose of ether. The, liver and parametrial adipose tissues were removed and weighed immediately. The liver triglyceride content was estimated. The influence of the extract on the pancreatic lipase activity was also determined by measuring the rate of release of oleic acid from triolein. Results: The body weight at two-to-six weeks and the final parametrial adipose tissue weights were significantly lowered (P < 0.01 and P < 0.05, respectively) in rats fed with the CD with Argyreia speciosa extract 500 mg/kg/day as compared to the CD alone. The extract also significantly reduced (P < 0.01) the serum contents of leptin, total cholesterol, low density lipoprotein (LDL), and triglycerides, which were elevated in rats fed with CD alone. In addition, the extract inhibited the induction of fatty liver with the accumulation of hepatic triglycerides. The extract also showed inhibition of pancreatic lipase activity by using triolein as a substrate. Conclusions: The ethanolic extract of Argyreia speciosa roots produces inhibitory effects on cafeteria diet-induced obesity in rats.

Ramaprasad G.C.,Mangalore University | Ramaprasad G.C.,Biocon | Kalluraya B.,Mangalore University | Kumar B.S.,Net Pharmacy College | Hunnur R.K.,Net Pharmacy College
European Journal of Medicinal Chemistry | Year: 2010

A series of biphenyl-1,3,4-oxadiazoles namely 5-[substituted-(1,1′- biphenyl)-3-yl]-1,3,4-oxadiazole-2(3H)-thiones and its S-alkyl derivatives have been synthesized by multi step organic synthesis involving Suzuki-Miyaura coupling using palladium catalyst. The synthesized compounds were characterized by 1H NMR, 13C NMR, 19F NMR, IR and LCMS spectroscopic properties. They were tested for their antimicrobial and analgesic activities. Some of them showed significant activity. © 2010 Elsevier Masson SAS. All rights reserved.

Palusa S.K.G.,Jawaharlal Nehru Technological University | Palusa S.K.G.,NET Pharmacy College | Udupi R.H.,NET Pharmacy College | Himabindu V.,Jawaharlal Nehru Technological University | Sridhara A.M.,Kuvempu University
Organic Communications | Year: 2011

Novel pyrimidine substituted 1,3,4-oxadiazole derivatives (11a-k) were synthesized from the condensation of different substituted aromatic carboxylic acids with substituted pyrimidine carboxy hydrazide using POCl 3 as condensing agent. Their structures were characterized by physical and spectral studies. The synthesized compounds were evaluated for their in vitro antimicrobial and anti-inflammatory activity. Some of the newly synthesized compounds showed good antimicrobial and anti-inflammatory activities. © 2011 Reproduction is free for scientific studies.

Ramaprasada G.C.,Mangalore University | Ramaprasada G.C.,Biocon | Kallurayaa B.,Mangalore University | Sunil Kumarb B.,Net Pharmacy College | Sahana Mallyaa,Mangalore University
Der Pharma Chemica | Year: 2012

A series of 3-(5'-fluoro-2'-methoxybiphenyl-3-yl)-6-(substituted)[1,2,4]-triazolo[3,4-b][1,3,4]-thiadiazole (3a-j) were synthesized by conventional and microwave irradiation methods. Microwave method proved to be a rapid and better yield compare to that of conventional method. The structures of these compounds were established on the basis of spectral and analytical data. These novel compounds were screened for their antibacterial and anticancer activity. The promising compounds 3b and 3g have been identified.

Puthiyapurayil P.,Mangalore University | Puthiyapurayil P.,Biocon | Poojary B.,Mangalore University | Chikkanna C.,SDM College Ujire | Buridipad S.K.,NET Pharmacy College
European Journal of Medicinal Chemistry | Year: 2012

On account of the reported anticancer activity of triazolothiadiazines, we have synthesized a novel series of 6-arylsubstituted-3-[2-(4-substitutedphenyl) propan-2-yl]-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines and tested for in-vitro cytotoxicity by trypan blue exclusion and MTT assay. These compounds were also evaluated for their in-vivo anthelmintic activity, as well as in-vitro antimicrobial studies. Amongst the tested compounds, the compound 7j was the most promising cytotoxic agent with IC50 value of 10.54 μM in MCF-7 cells. The compounds 7l and 7q exhibited excellent anthelmintic activity. The compounds 7d, 7f, 7j, 7l, 7o, 7p and 7r showed good antibacterial activity, whereas compounds 7e and 7k exhibited excellent antifungal activity. The structures of newly synthesized compounds were characterized by IR, 1H NMR, 13C NMR and LCMS analysis. © 2012 Elsevier Masson SAS. All rights reserved.

Goudanavar P.,Net Pharmacy College | Reddy S.,Net Pharmacy College | Hiremath D.,Net Pharmacy College | Udupi R.,Net Pharmacy College
Journal of Applied Pharmaceutical Science | Year: 2013

The present study was to prepare and evaluate the floating microspheres of Esomeprazole magnesium trihydrate as a model drug for prolongation of the gastric retention time for oral delivery. EMT is a proton pump inhibitor which acts by irreversibly blocking the(H+K+)-ATPase enzyme system of the gastric parietal cell. Its half life is 1-1.5 hrs. EMT poor absorption may be because of degradation in gastric acid which can be prevented by incorporation of sodium bi carbonate which is a systemic antacid and act as buffer. The EMT floating microspheres were prepared by double emulsion solvent diffusion method by using Ethyl cellulose and different grades of HPMC like K4M, K15M, using Dichloromethane and alcohol solvent systems. EMT Floating microspheres were evaluated for micromeritic properties, particle size, % yield, In-Vitro buoyancy, incorporation efficiency and drug release. The prepared microspheres were found to be spherical and free flowing and remain buoyant for more than 10 hrs and the particle sizes of microspheres were found to be in the range of 67.24±4.57 μm to 106.35±5.67μm. Incorporation efficiency was found in the range of54.75±3.51to 83.97±2.54. In-vitro release profile of optimized formulations follows firstorder non-Fickian (Anomalous) release indicates diffusion and dissolution controlled release. FT-IR and DSC studies revealed the absence of any chemical interaction between drug and polymers used. During the stability period selected microspheres were found to be stable with respect to Entrapment efficiency and drug release characteristics.

Ramaprasad G.C.,Mangalore University | Ramaprasad G.C.,Biocon | Kalluraya B.,Mangalore University | Sunil Kumar B.,Net Pharmacy College
Medicinal Chemistry Research | Year: 2014

A series of S-alkyl derivatives of 3-(substituted-(1,1′-biphenyl)-3- yl)[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole-6-thiol (4a-j) were synthesized by conventional and microwave irradiation methods. Microwave method proved to be a rapid and better yield compare to that of conventional method. The synthesized compounds were characterized by 1H NMR, 13C NMR, 19F NMR, IR, LCMS, and elemental spectroscopic analysis. These compounds were screened for their in vitro anticancer activity by MTT assay. Among the tested compounds, the compound 4c was the most promising anticancer agent with IC50 value 12 μM in HT29 cell line. © Springer Science+Business Media 2014.

Patil P.B.,Net Pharmacy College | Gupta V.R.M.,Pulla Reddy Institute of Pharmacy | Udupi R.H.,Net Pharmacy College | Srikanth K.,Pulla Reddy Institute of Pharmacy | Prasad B.S.G.,Pulla Reddy Institute of Pharmacy
Research Journal of Pharmaceutical, Biological and Chemical Sciences | Year: 2010

Mefenamic acid, a non steroidal anti-inflammatory drug is poorly water soluble. Addition of surfactant to the dissolution medium improves the dissolution of pure drug by facilitating the drug release process at the solid/liquid interface and micelle solubilization in the bulk. In the present study a dissolution medium was developed. The composition of the dissolution medium was selected on the basis of solubility data of Mefenamic acid at 37° C. The solubility data revealed that water consisting of 2% w/v sodium lauryl sulphate shall be suitable dissolution medium. The discriminating power of the selected dissolution medium (2% w/v sodium lauryl sulphate in water.) relative to the other dissolution medium was evaluated. The results further justified that the usage of 2% w/v sodium lauryl sulphate in water serves as most suitable dissolution medium for Mefenamic acid.

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