Posted by admin on Oct 31, 2021 in |
MER kinase is an important tyrosine-kinase receptor that is associated with a variety of cancers, including mantle cell lymphomas, pituitary adenomas and T-cell acute lymphoblastic leukemia. Identification of new MERTK inhibitors assumes crucial importance. Only one ligand-based pharmacophore model is reported to date for MERTK inhibitors. There are many more molecules with improved enzyme inhibitory activity reported since the publishing of this model. Because of this fact, we decided to develop a pharmacophore model for the MERTK inhibitors to assist in virtual screening using Phase for this purpose. Hydrogen bond donors, hydrogen bond acceptors, rings, positively ionizable groups, and hydrophobic groups were considered as key elements contributing to ligand activity for the pharmacophore model. Pharmacophore modelling was followed by extensive validation of the developed pharmacophore models. The developed pharmacophore model highlighted the importance of the positively ionizable groups and a ring structure. We have used these models for database screening to arrive at few hits. So findings in this study were proved to be useful in the optimization and...
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Posted by admin on Oct 31, 2021 in |
Aim: The present work for the development and in-vitro evaluation of sustained floating hollow microspheres (SFHM). Materials and methods: Sustained floating hollow microspheres were prepared by means of HPMC K4M, ethylcellulose and sodium alginate in various concentrations by using the solvent evaporation method using dichloromethane as solvent. The floating hollow microspheres of Labetalol HCl were formulated by the solvent evaporation method. SFHM was characterized using surface morphology by scanning electron microscopy (SEM), buoyancy studies, in-vitro floating behavior, incorporation efficiency, drug loading, production yield in-vitro drug release, and drug release kinetics studies. Results: The mean particle size ranges from 74.36± 1.02 to 102.0 ± 2.87µm. The entrapment efficiency of the drug ranges between 74.23 ± 2.12 to 80.82 ± 2.23%. The drug loading varies between 105.8 ± 1.46 to 125.2 ± 1.36µg/mg. The prepared hollow microspheres are exhibit good flowability. The in-vitro studies show release up to 12 h. The release kinetics data showed the best fit to the non-fickian release (diffusion and swelling). Conclusion: The outcomes conclude that Labetalol...
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Posted by admin on Oct 31, 2021 in |
Rosuvastatin is an antihyperlipidemic agent belonging to BCS class II Drugs with low aqueous solubility and high permeability. Objective: To formulate Rosuvastatin nanosuspension by Emulsification solvent diffusion technique by QbD approach and its evaluation. A 2² factorial design was employed to study the effect of independent variables [SLS (X1) and amount of PVP K -30(X2)] and dependent variables [total drug content (Y1) and PDI (Y2)]. Methods: Four nanosuspensions were prepared and evaluated for their saturation solubility, particle size, zeta potential, SEM, TEM, and in-vitro drug release study. Results: The particle size and PDI of all formulations were in a range of 215-38nm & 0.1-0.9, respectively. The drug content was ranged from 69 %-79%. From the design space F1 (SLS 4mg, PVPK-30, 25mg) and based on the mean particle size of 215nm, PDI of 0.2, drug content of 79%, and cumulative drug release 91%, F1 was selected as an optimum formulation with a zeta potential of -35.2mV. Conclusion: It can be concluded that Rosuvastatin formulated as nanosuspension formulation can enhance...
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Posted by admin on Oct 31, 2021 in |
The main objective of this study was to formulate a Sustained release tablet by wet granulation method. A sustained release tablet of trazadone hydrochloride was prepared by using synthetic polymer. The prepared tablets were evaluated for their diameter, thickness, drug content, Hardness, friability, weight variation. The thickness and diameter of the tablet range from 5.43±0.288 to 5.76±0.05 and 09.68±0.577 to 10.04±0.04, respectively. Drug content was studied, and its ranges from 92.03 to 98.60%. Hardness was studied; its ranges 5.5 to 6.5 kg/cm2, Friability ranges 0.71 to 0.95%, Weight variation ranges between 434±1.49 to 460±1.23. FTIR and DSC analysis does not show any interaction of drug with Excipient. The formulation was optimized on the basis of acceptable pre and post-compression parameters. The results of dissolution studies indicated that Batch F4 containing eudragit RL 100 exhibited drug release of 88.06% at the end of 12 h to provide sufficient concentration for achieving satisfactory therapeutic value for an extended period of time. Optimized batch best fitted to Higuchi model. The n value...
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Posted by admin on Oct 31, 2021 in |
The present study aims to formulate and evaluate clopidogrel bisulfate capsule-loaded nanoparticles. Clopidogrel bisulfate nanoparticles were produced by the nano-precipitation method and emulsification solvent evaporation method using ethylcellulose polymer at different ratios and characterized for particle size drug entrapment efficiency dissolution testing scanning electron microscopy imaging (SEM) and compatibility studies (Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). Optimized nanoparticles were filled into capsules with different concentrations of HPMC 4 KM and further evaluated. The prepared nanoparticles characterized and found to be the particle size was ranged from 100-2500 nm, and entrapment efficiency was ranged from 23.88 ± 0.20 % to 90.53 ± 0.31%. Amongst all formulations, F6 and F10 were considered for further optimization showed dissolution 53.20 ± 0.27 and 39.87 ± 0.12 % at the end of the first hour with entrapment efficiency 70% and 79%, respectively. SEM of clopidogrel bisulfate nanoparticles confirmed small particles without aggregation. The particle size of F6 and F10 obtained was 287.6 and 349.8 nm, respectively. Compatibility studies revealed that...
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