Vincristine Sulfate Liposome (Fudan Zhangjiang)

Controlled release (CR) matrix tablet of Prochlorperazine maleate was developed to improve its patient compliance.

Tablet formulations F1, F2 and F3 based on different concentrations of Methocel(®) K100 LV-CR Premium, were compacted by direct compression method while tablet formulations F4, F5 and F6, based on distinct blends of Methocel(®) K100 LV-CR Premium and Ethocel(®) Standard 7FP Premium, were compressed by flow-bound dry granulation-slugging method. The prepared powder mixtures, granules and tablets were evaluated for their physicochemical performance. Bioequivalence study of the optimized test tablet versus reference-conventional Stemitil(®) tablet was conducted on rabbits, using HPLC-UV system at λ(max) 254 nm.

The test tablet, containing 28% Methocel(®) and 58% Ethocel(®) (F6) exhibited desired zero order kinetics for 24 h and was found stable at accelerated storage conditions for 6 months. In vitro drug release rate decreased as the Ethocel(®) content in the blend was increased, perhaps due to slower penetrability of water. Hydrodynamic conditions and hardness of tablets could not affect drug release kinetics. The tablet displayed significantly (p < 0.05) optimized peak drug concentration-C(max) (45 ± 3.42 vs. 64.5 ± 4.03), extended half life-t(1/2) (16.071 ± 3.97 vs. 5.257 ± 1.314 h) and bioequivalence to the reference tablet taken three times a day (1409 ± 15 ng·h/mL vs. 1346 ± 23 ng h/mL). The tablet showed strong Level A correlation (R(2) = 0.8458) between drug absorbed in vivo and drug released in vitro.

The developed tablet may be adopted by pharmaceutical industry to improve patient compliance of the Prochlorperazine maleate.