Posted by admin on Sep 30, 2018 in |
Crystal structures of target are an indispensible tool in modern methods of rational drug design and discovery. Hence, judicious selection of crystal structures for virtual screening and ligand docking is essential. In recent times, a number of new chemical entities (NCEs) have been introduced into the drug discovery pipeline with these methods in treatment of type 2 diabetes. Dipeptidyl peptidase 4 (DPP 4) enzyme splits an incretin based glucoregulatory hormone glucagon like peptide -1(GLP-1) from N-terminal of peptide, where penultimate amino acid is either alanine or proline. Several DPP 4 inhibitors, “gliptins”, are approved for management of type 2 diabetes or are under clinical trials. Crystal structures of DPP 4 have been released by various research groups that may assist rapid discovery of new DPP 4 inhibitors. 18 crystal structures of DPP 4 bound to various inhibitors are analyzed in the present work to gain insight into interactions between the protein and ligands. Chemically all DPP 4 inhibitors are diverse in nature but occupy same binding site. Key amino...
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Posted by admin on Sep 30, 2018 in |
The optimized microparticles of Verapamil hydrochloride entrapped in Poly(lactide-co-glycolide) (Verapamil HCl-PLGA) was prepared through solvent displacement method and lyophilization. The optimization parameters for the formulation include particle size, polydispersity index, zeta potential, and entrapment efficiency. The final product was further characterized based on percent particle recovery, redispersibility, percent drug loading, drug release kinetics, and morphology. Increasing the PLGA 75:25 concentrations resulted to an increase in the particles size, polydispersity index and entrapment efficiency, and a decrease in zeta potential. The increase in poloxamer 188 concentration led to a decrease in zeta potential and an increase in the entrapment of the drug. Lastly, the increase in the pH of the non-solvent phase resulted to an increase in particle size. The addition of sucrose led to an unfavorable increase in the particle size and polydispersity index and a decrease in zeta potential and entrapment efficiency after lyophilization. The final product of the process was a heterogeneous sized (<10µm) irregularly shaped particles with an acceptable particle recovery, redispersibility, and percentage drug loading,...
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Posted by admin on Sep 30, 2018 in |
Cyamopsis tetragonoloba is widely used by people and is found to have multiple medicinal utilities. Four (chloroform, ethyl acetate, methanolic and aqueous) extracts of Cyamopsis tetragonoloba fruit were therefore, analysed by Gas Liquid Chromatography and Mass Spectrometry analysis to assess their phytochemical constituents. The chloroform extract of Cyamopsis tetragonoloba fruits showed the presence of thirty one phytochemical constituents of which the major phytochemical compounds were Tetracontane and Stigmasterol. The ethyl acetate extract of Cyamopsis tetragonoloba fruit showed the presence of fifty phytochemical constituents. The important phytochemical compounds were stigmasterol and 4-tert-butylcalix [4] arene. Thirty eight phytochemicals were reported in the methanolic extract. The most important ones in term of peak area and retention time were mome inositol and 7-tetradecenal (Z). Mome inositol and 10, 12- Hexadecadien-1-ol was the primary components in a total of 30 phytochemicals obtained from the aqueous...
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Posted by admin on Sep 30, 2018 in |
The aim of the study was to develop an easy, sensible and rapid method for the estimation of amikacin in both pure and marketed formulation by pre derivatisation technique using reverse phase C18 column in HPLC. In this RP-HPLC method Shimadzu LC 20 AD of PDA detector was used with LC solutions software. In this method gradient elution with a mobile phase of acetonitrile and acetate buffer in the ratio of 25:75 v/v at the flow rate of 2 mL/min and run time of 10 min were used. Validation parameters of HPLC were found at detection wavelength of 272 nm. Linearity was observed with a concentration range of 10 – 50 µg/mL with R2 = 0.99. The method was robust with wavelength 271 and 273 nm with a flow rate of 1.8 and 2.2 mL/min showed good results. The retention time of drug was found at 8.9 min and assay showed 98.1%. RP-HPLC method was validated as per ICH guidelines and can be used for routine quantitative analysis of...
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Posted by admin on Sep 30, 2018 in |
A simple and rapid stability indicating HPLC method for acotiamide hydrochloride was developed and validated. The stationary phase used was thermo gold cyno (250 × 4.6 mm) 5 μ with a mobile phase consisting of mixture of acetonitrile and 10 mM KH2PO4 in water in the ratio of 80:20 v/v at a flow rate of 0.8ml/min. Detection was carried at 284 nm. The retention time observed was 8.1 ± 0.2 min. The column was maintained at ambient temperature and 20 μl of solutions were injected. The eluted compound was detected by using PDA detector. The linear regression analysis data for calibration plot show good relationship with coefficient of regression value, r2=0.99 in the concentration range 10-50 μg/ml. The stress degradation studies were performed as per ICH guidelines. Acotiamide hydrochloride degraded with acid/base hydrolysis, thermal, oxidation and photolytic stress. The method was validated as per ICH Q2A (R1) guideline with respect to linearity, accuracy, precision, specificity and robustness. This method can be used for monitoring the stability of acotiamide...
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