P.Palanisamy

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.

Nonionic surfactant vesicles (niosomes) were formulated with an aim of enhancing the oral bioavailability of Decitabine, an anti-cancer drug. Niosomes were formulated by conventional thin film hydration technique with different molar ratios of surfactant, cholesterol and dicetyl phosphate. The formulated niosomes were found spherical in shape, ranging from 2.95 𝜇m to 10.91 𝜇m in size. Vesicles with 1 : 1 : 0.1 ratios of surfactant : cholesterol : dicetyl phosphate with each grade of span were found to have higher entrapment efficiencies, which were further selected for in vitro studies. Vesicles formulated with sorbitan monostearate were found to have maximum drug release (99.091%) at the end of 24 hours and followed zero order release kinetics. In conclusion, noisome could be a promising delivery for Decitabine with improved oral bioavailability and prolonged release profiles.

The present study involved preparation of solid dispersions of Olmesartan medoxomil to improve the aqueous solubility and dissolution rate in order to enhance bioavailability. Olmesartan is a BCS Class II anti-hypertensive drug, having low aqueous solubility and low bioavailability of 26%.  In the present study, solid dispersions of Olmesartan with different carriers like Poloxamer 407, PEG 4000  and crospovidone in different ratios (1 : 1, 1 : 2, 1 : 3, 1 : 4) were prepared by solvent evaporation method.  The formulations were further characterized for percentage yield, drug content, in vitro release study,  and stability study. In vitro release studies revealed that the solid dispersions prepared by solvent evaporation method crospovidone (1 : 4) was considered as the best formulation because of its faster drug release among all formulations.  Infrared spectroscopy (IR) studies revealed that no interactions exist between drug and polymer. Powder X-ray diffraction studies showed a significant decrease in crystalline nature of drug in solid dispersions. In conclusion, solid dispersions of Olmesartan in crospovidone (1:4) have shown to be a promising approach to enhance the bioavailability of Olmesartan.

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.