Posted by admin on Apr 30, 2020 in |
Vildagliptin chemically (S)-1-[N-(3-hydroxy-1- adamantyl) glycyl] pyrrolidine-2-carbonitrile, is a potent dipeptidyl peptidase IV (dip-IV) inhibitor, a drug for the treatment of diabetes. DPP-IV inhibitors represent a new class of oral antihyperglycemic agents to treat patients with type 2 diabetes. The Present work describes the development and validation of a new simple, accurate, precise and stability-indicating HPTLC method for the determination of Vildagliptin in the tablet dosage form. The chromatographic separation was achieved by using Chloroform: n-Butanol: Methanol (5:2:3 v/v/v) as mobile phase and UV detection at 227nm. The developed method was validated with respect to linearity, accuracy, precision, the limit of detection, the limit of quantitation and robustness as per ICH guidelines. The described method was linear over a concentration range of 2000-20000 ng/ml for the assay of Vildagliptin. The assay was found to be 99.8%. The limit of detection (LOD) and the limit of quantification (LOQ) for Vildagliptin was found to be 357.31 ng/band and 1082.76 ng/band respectively. The drug was subjected to stress conditions of acid hydrolysis, alkali...
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Posted by admin on Apr 30, 2020 in |
Cefpodoxime Proxetil is third generation, broad-spectrum Cephalosporin Antibiotic & it has an oral bioavailability of only 50% and biological half life 2 h so to improve it’s bioavailability sustain release matrix formulation was designed. Sustained release matrix tablets of Cefpodoxime Proxetil prepared by direct compression method based on combination of natural Acacia gum & Karaya gum polymers. 32 full factorial designs optimization study was carried out by using Design Expert Software to find the effect of independent variables, i.e., Acacia gum (X1) and Karaya gum (X2) concentration on dependent variables i.e., Hardness & % CDR. The drug excipient mixtures were subjected to preformulation studies. The tablets were subjected to physicochemical studies, in-vitro drug release, kinetic studies and stability studies. FTIR and DSC studies shown there was no interaction between drug and polymers. Matrix tablet of Cefpodoxime Proxetil were formulated well in term of hardness 5.07 ± 0. 5.93 ± 0.03 kg/cm2, thickness 2.25 ± 0.1 mm to 3.33 ± 0.3 mm, weight variation were within limits. In-vitro release studies...
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Posted by admin on Apr 30, 2020 in |
Taxol is an important drug used for the treatment of various types of cancer. It is primarily obtained from Taxus brevifolia bark and has a long history of the developmental program of 50 years. It functions as a microtubule-stabilizing compound and inhibits mitosis of cancer cells, thereby providing a protective role in the treatment of cancers. In addition to it, taxol also interferes with a number of biochemical pathways and protein to bring about apoptosis and cell death. Since its inception, taxol has undergone various levels of modifications and formulations with a motive of making its action more effective. This has led to the development of Paclitaxel by Bristol-Myers Squibb for large scale commercialization. Consequently other semi-synthetic variants such as Docetaxel and Cabazitaxel were also developed for better actions. All these compounds are collectively called as Taxanes and contain a common ringed baccatin III structure in its molecule. This review is an attempt to illustrate the gradual development of anticancer taxanes from its precursor Taxol and its various pharmacological...
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Posted by admin on Apr 30, 2020 in |
Sitagliptin was invented in 2006 as a DPP-4 inhibitor. It is soluble in water to the extent of 0.03 mg/mL as thus suffers bioavailability problems. It was converted into phosphate monohydrate salt with solubility 50 mg/mL, which solved bioavailability problems. In this research, an attempt is made to convert it from its crystalline form into spherical crystals. Spherical crystals have better bulk properties and can adapt to direct compression tableting. This kind of innovation saves the time needed for granulation and can be compressed directly just by adding lubricant and disintegrant. In this research sitagliptin, phosphate monohydrate was made as spherical crystals using water as a solvent, ethanol as anti-solvent, and chloroform as bridging liquid. 32 factorial designs for optimization was applied to get an optimized batch with a concentration of bridging liquid and anti-solvent as independent and Carr’s index and yield as dependent variables. Batch F7 was considered optimized with a yield of 97.5%. Spherical crystals thus obtained were characterized using X-Ray diffraction, SEM, % compressibility, and flowability....
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Posted by admin on Apr 30, 2020 in |
The kinetic of conjugated reactions of S-oxidation and perhydrolysis of Mezlocillin (Mezl) with potassium caroate in alkaline medium is studied by the increase of forming product light absorbance at 290 nm. Baypen® – powder Mezl sodium monohydrate in flacons for preparation of solution for injections (Mezl 1.0 g). Peroxomonosulfate acid as triple potassium salt 2КНSO5∙КНSO4∙K2SO4 (Oxone®) of “extra pure” qualification was used as oxidant. A scheme of peroxoacid oxidation and perhydrolysis conjugated reactions of Mezl by means of potassium caroate is proposed. A new spectrophotometric method for quantitative determination of sodium Mezl in Baypen ® preparation using potassium caroate (KHSO5) as analytical reagent was proposed. At pH 3-4 for 1 mole of penicillin, 1 mole of KHSO5 is consumed, the quantitative interaction is achieved within a time of more than 1 min (observation time). The results were obtained by the recommended procedure for seven replicate titrations of mixtures containing the three species at various concentrations. RSD = 1.32%, δ = +0.49%. It can be seen that Mezl can be...
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