Posted by admin on Mar 31, 2016 in |
Helminthes infections are more common in poor countries where people suffer from poor health hygiene and sanitation, though there are lot of marketed drugs available for these disease but the interesting thing about antihelminthics is that they are either pypirazine or benzimidazole derivatives, so as medicinal chemist the attention will be drawn towards these different moieties which exert same biological action, in this present work five derivatives of piperazine were synthesized by conventional methods using two schemes, by scheme 1 three compounds were synthesized which were Bis benzyl derivatives of pierazine and by scheme 2 already prepared piperazine 2,5 di one was reacted with benzimidazole derivatives to yield finally two benzimidazole linked piperazine derivatavies and these two different classes of piperazine deiatives were screened for antihelminthic activity against Pheretima posthuma to compare their potency in context of calculating paralyzing and death time. Result showed that bis-benzyl derivatives possess to some extent better activity than that of benzimidazole linked piperazine...
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Posted by admin on Mar 31, 2016 in |
Travoprost and Timolol Maleate are used in treatment of glaucoma by decreasing intra ocular pressure. The present study was designed to develop and validate a simple, sensitive, precise, and specific reverse phase high-performance liquid chromatographic (HPLC) method for simultaneous determination of Travoprost and Timolol maleate in ophthalmic dosage form. Chromatographic separation of these two drugs was achieved on Hypersil BDS C18 column (250 x 4.6 mm, 5 μm) as stationary phase with a mobile phase Water (pH2 adjusted with OPA): Methanol (85:15% v/v) at a flow rate of 0.8 ml/min and PDA detection at 233 nm. The method was carried out at 40oC. The retention times of Timolol maleate and Travoprost were found to be 2.48±0.01 min, 5.10±0.1min respectively. The proposed method was validated for system suitability, linearity, accuracy, precision, LOD, LOQ and robustness. The calibration curves were linear in the concentration range of 25% to 150% of the working concentration (r2 = 0.999) for both the drugs in binary mixture. The LOD was found to be 0.002 μg/ml...
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Posted by admin on Mar 31, 2016 in |
This study was undertaken to evaluate the antioxidant, anti-inflammatory and anticoagulant activities of aqueous extract and organic fractions of Thymus zygis. Water, dichloromethane, ethyl acetate and methanol were used as extractant solvents. The fractions were analyzed by HPLC and screened for their antioxidant activity in vitro using different assay. In vivo, the fractions were evaluated by use of the oil croton-induced ear edema and carrageenan-induced paw edema model in mice and rat, respectively. Prothrombin Time and Partial Thromboplastin Time were used to determine the effect of aqueous extract, methanol, aqueous fractions and coumarone-rich extract on intrinsic, extrinsic and/or common pathway of the coagulation cascade. All fractions were found to possess considerable antioxidant activity and the rosmarinic acid is the major polyphenol compound in majority fractions. In comparison with the indometacin, the hydrophobic fractions presented stronger anti-inflammatory activity in the croton oil induced edema. Methanol and acetate ethyl fractions (50 mg/kg) significantly reduced the edema induced by carrageenan and their effect was comparable to the reference drug indometacin (10 mg/kg)....
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Posted by admin on Mar 31, 2016 in |
Increase in complexity and cost associated with pediatric safety and efficacy studies have reduced the interest of pharmaceutical companies to study bio-therapeutics in pediatric population. Dose recommendations are being made as per patient body weight or body surface area, with the assumption of linearity in body size dose adjustments. In the present study, newer approach i.e. flat fixed age-based dosing is explored. Stochastic simulations were performed on once-a-day (OD) and twice-a-day (BD) dosage regimens of a fixed dose combination (FDC) of ceftriaxone/sulbactam (2/1) to identify a promising dose range that can effectively evaluate exposure-response (E-R) relationships of the FDC against bacterial infection in pediatric population. Selected dose range of 60-120 mg/kg of FDC was evaluated against ESBL infection using in-vitro systems (dilution method and hollow fiber method). Effect of dose, dose frequency, severity of infection and age groups were analyzed in age-based subgroups i.e. neonates, infant, child and toddler. Recommended dose for infants, child and toddler were 75-120 mg/kg based on severity of infection. However, physiologically-induced reduction in drug’s...
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Posted by admin on Mar 31, 2016 in |
Plants served as potent sources of bioactive compounds since ages. The understanding of phytochemical constitution of each and every plant on earth is the preliminary and the most important step in drug discovery. As Operculina turpethum(L.) Silva Manso is traditionally used for various ailments, the understanding of phytochemical composition of the plant is very essential. The present study was an attempt to identify the phenolic compounds present in the leaf of the plant O. turpethum. Total phenol and flavonoid content was determined from the methanol extract of the leaf and the extract was subjected to HPLC analysis with seven standard compounds. A gradient mobile phase comprising acetonitrile and 0.1% phosphoric acid was used to get the phenolic profile. The quantity of each compound present in the extract was calculated from the peak area and expressed in mg/ ml of sample injected. The first mobile phase revealed the presence of compounds viz., coumarin, ferulic acid, catechin, salicylic acid, rutin, vanillin and gallic acid. Among the seven identified phenolics, coumarin was...
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