B.S.Venkateshwarlu

In the present research work an attempt was made to formulate and evaluate  CR tablets of Ranolazine by using different polymers, polymers namely HPMC Phthalate and Eudragit S 100. Drug polymer interaction studies were carried out by using FTIR analysis which confirmed that there were no interactions between the drug and excipients. All the physical parameters of Drug & Drug – excipients (wet granules) carried out. The results indicate that all formulations were within the pharmacopoeial  specifications. The various formulations of CR tablets of Ranolazine were formulated by using various concentration different polymers HPMC Phthalate and Eudragit S 100. The tablets were evaluated for pre compression and post compression parameters and In-vitro dissolution. The results indicated that the, physical parameters of formulated tablets were within the Pharmacopeial specifications. The controlled release tablets of Ranolazine formulations was optimized on the basis of different physical parameters and mainly with the comparison of formulations on the basis of in-vitro dissolution study and the optimized formulation F4 were found to be 97.0 % drug release within 24 hours. The kinetic studies To know the kinetic drug release, the data was treated according to different model. The drug release data of F1-F5 fitted to Higuchi plots were best fit into Higuchi equation and diffusion mechanism. The zero order plots for all formulation were found linear. The result shows that, drug release rate for the F4 formulation follow the zero order mechanism. The accelerated stability studies of selected formulation (F4) showed that there were no significant changes.

The present study focuses on developing sustained release matrix tablets of Ibrutinib aiming to increase the therapeutic efficacy, reduce the frequency of administration and to improve the patient compliance. Sustained release matrix tablets of Ibrutinib, were developed by using different drug polymer ratios HPMC phthalate, Eudragit L 100, Eudragit S 100 as matrix former. All lubricated formulations were compressed by direct compression and by wet granulation method. Compressed tablets were evaluated for uniformity of weight, content of active ingredient, friability, hardness, thickness, in-vitro dissolution, and swelling index. All the formulation showed compliance with pharmacopoeial standards. Among the different formulation, B8 showed sustained release of drug for 12 hours with 86.55% release. The selected formulation (B8) was subjected to stability studies for three months at 25°C/60% RH, 30°C/65% RH and 40°C/75% RH and showed stability with respect to release pattern and all physical parameters. The regression coefficient value of Higuchi plot was found to be 0.9925 that showed that drug was released by diffusion mechanism. The slope value of korsmeyer-peppas equation was found to be 0.5062 which indicating that drug was released by non-fickian release mechanism. The R2 value for Hixson Crowell plot was found to be 0.9919 which indicates that drug release was limited by drug particle dissolution rate and erosion of the polymer matrix. Thus, drug in combination with Eudragit S 100 were found to be effective in retarding the release of Ibrutinib.