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Mogili R.,Jawaharlal Nehru Technological University Anantapur | Mogili R.,Siddhartha Institute of Pharmaceutical science | Kanala K.,Jawaharlal Nehru Technological University Anantapur | Chandu B.R.,P.A. College | Bannoth C.K.,Jawaharlal Nehru Technological University Anantapur
Chromatographia | Year: 2011

A simple, sensitive, selective, rapid, rugged, reproducible and specific liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was used for quantitative estimation of rizatriptan (RZ) in human plasma using rizatriptan-d 6 (RZD6) as internal standard (IS). Chromatographic separation was performed on Ascentis Express RP Amide C18, 50 × 4.6 mm, 2.7 μm column with isocratic mobile phase composed of 10 mM ammonium formate:acetonitrile (20:80 v/v) at flow rate of 0.5 mL min-1. RZ and RZD6 were detected with proton adducts at m/z (amu) 270.2 → 201.2 and 276.1 → 207.1, respectively, in multiple reaction monitoring (MRM) positive mode. Liquid-liquid extraction was used and validated over a linear concentration range of 0.1-100.0 ng mL-1 with correlation coefficient r 2 ≥ 0.9981. The limit of quantification (LOQ) and limit of detection (LOD) were found to be 0.1 ng mL-1 and 12.5 fg, respectively. Intra- and inter-day precision were within 1.7-3.1% and 2.8-3.7%, and accuracy within 96.0-101.7% and 99.7-101.4% for RZ. Drug was found to be stable throughout three freeze-thaw cycles. The method was successfully employed for analysis of plasma samples following oral administration of RZ (10 mg) in 25 healthy Indian male human volunteers under fasting conditions. © 2011 Springer-Verlag. Source


Srinivasan R.,Siddhartha Institute of Pharmaceutical science | Jayakar B.,Salem College
International Journal of Pharma and Bio Sciences | Year: 2011

The present study deals with the application of α N-Phthilimido and acetylated tyrosine and determination of tyrosinase inhibitory activity which serves as an useful target in the treatment of hyper pigmentation skin disorder. The tyrosinase inhibitory activity of α N-Phthilimido tyrosine found to be highly significant (p< 0.0001) when compared with that of acetyltyrosine. Source


Srinivasan R.,Siddhartha Institute of Pharmaceutical science | Reddy C.U.M.,Sri Ramachandra ollege of Pharmacy | Jayakar B.,Salem College
International Journal of Pharma and Bio Sciences | Year: 2011

After glucose, amino acids like glutamine, methonine, glycine, alanine, phenyl alanine are a major metabolite necessary synthesizing for the cancer cell. In the synthesis of DNA and RNA, major portions of nitrogen atoms are supplied by amino acids. Structural variants of amino acids may antagonize enzymes involved in DNA and RNA synthesis. A QSAR (quantitative structure-activity relationships) study was performed on some previously synthesized amino acid analogues in order to get insight in the substitution requirements for their anticancer activity as well as to overcome the symmetry restriction of De Novo model and time consuming determination of partition coefficients of Hansch analysis. A good QSAR model was obtained considering anticancer activity, i.e., log % of tumor weight inhibition which expresses the biological activity, of three phthilimido derivatives which is a analogues of amino acid as dependent variable and substitution contribution at specific position as independent variable as evidenced by the statistical data (r = 0.8122, s = 0.1196, F = 1.3755). Source


Jayakar B.,Salem College | Srinivasan R.,Siddhartha Institute of Pharmaceutical science
International Journal of Pharma and Bio Sciences | Year: 2010

The phthaloyl and acetyl group are common protecting groups from are common protecting group for amines in organic synthesis 1 and are also important pharmacophores 2. Common method are imide synthesis include dehydrative condensation of an anhydride and amino acid at high temperature, the acid-catalyzed cyclization of N-substituted amic acid. Abdol Reza Hajipour 3, rapidly synthesised Phthalimide derivatives by microwave irradiation. A simple extremely fast, and high yielding method for the reaction of phthalic anhydride with a number of amino acids using microwave irradiation under solventless dry condition has been developed. The aim of the study was to design, synthesize and investigate the antimicrobial and antifungal activities, anticancer activities of some α N-Phthilimido and acetylated derivatives of amino acids. The chemical structures of the titled compound were confirmed by IR, 13CNMR and elemental analysis. All the compounds were screened for antimicrobial activity against gram positive, gram negative bacteria (Escherichia coli, Klebsiella, Staphylococcus epidermitis, Bacillus cereus, Micrococcus leteus, Staphylococcus aureus) and fungal strains (Candida albicans, Aspergillus niger). Source


Ravi Kumar K.,Siddhartha Institute of Pharmaceutical science | Babu Rao Ch.,Siddhartha Institute of Pharmaceutical science | Chandra Sekhar K.B.,Jawaharlal Nehru Technological University Anantapur
International Journal of ChemTech Research | Year: 2010

A simple, rapid and selective RP-HPLC method has been developed for quantification Capecitabine from bulk drug and pharmaceutical formulations using a mobile phase consisting mixture of Buffer and acetonitrile in the ratio (80:40) (v/v) at the flow rate of 1.2 ml/min. An Hypersil BDS C8, 250, 5mm, was used as stationary phase. The retention time for Capecitabine was 15min. Linearity was observed in the concentration range of 40 to 60 μg/ml, with good linearity response greater than 0.997. The mean % recovery obtained is 100.1%. The proposed method is precise, accurate, selective and rapid for the determination of Capecitabine in capsules. Source

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