Proniosomal Telmisartan Tablets: Formulation, in vitro Evaluation and in vivo Comparative Pharmacokinetic Study in Rabbits

摘要

Objective: The?purpose?of?this?study?was?to prepare proniosomal vesicles of Telmisartan (TEL) to be compressed into tablets which will be further evaluated in vitro and in vivo. Materials and Methods: An experimental design was adopted using surfactants of different HLB values (span 40-brij 35), different cholesterol ratios (20– 50%) and different phospholipid types (egg yolk-soyabean). Different responses were measured followed by tablet manufacturing. The highest EE was shown in F3 (85%) while the lowest value was obtained in F7 (8.4%). Finally, zeta potential results were in the range of ? 0.67 to ? 27.6 mv. Compressibility percent revealed that F5 showed an excellent flowability characteristic with a value of 9.74± 1.61 while F3 and F6 showed good flowability characteristics. By the end of the release, F6 showed approximately 90% drug release. Results: F6 was selected for the in vivo study; Csubmax/sub was increased by 1.5-fold while AUCsub0-∞/sub also increased significantly by 3-fold when compared with commercial tablet and finally, tsubmax/sub was increased by 3-fold indicating sustained release pattern. The relative bioavailability was also increased by 3.2-fold. Conclusion: The results of this study suggested that the formulation of compressed tablets containing more stable proniosomal powder extended the release of TEL and increased its bioavailability as well.