Anti-cancer Effect And Preparation Of Stomach Remaining Floating Tablets On The Extraction Of Trapa Bispinosa Roxb. Shells

Trapa bispinosa Roxb. (TbR), an anti-cancer Traditional Chinese Medicine, has not yet been available in medicinal market, nor was introduced sufficiently in Chinese Pharmacopeia. The only clinical application was WTTC developed in Japan, which had a poor patient compliance due to its large volume of broth. In this study, an optimized extracting method, a new preparation in the form of stomach floating tablet together with tests on toxicity, pharmacodynamics and therapeutic anti-cancer effects were carried out for TbR.Purpose: is to formulate an effective preparation for stomach cancer based on TbR. Method: An optimized extracting method for active components of TbR was obtained through the orthogonal experiments, the anti-cancer effect of TbR was evaluated by MTT-drug sensitivity experiments and through an inoculation of mouse frontal carcinoma cells to Kunming mouse, absorption and acute toxicity of TbR were studied in ex vivo stomach and in intact animals respectively, and finally a preparation technology for stomach floating tablet was formulated for TbR by using wet granulation and rolling-baskets method. Result: The best extracting method was found to extract by backstreaming twice with 65% ethanol of 20 times in volume followed by extracting by backstreaming twice with water of 30 times in volume, for 1.5h each time. The extracting rate for the final target extraction product was 21.3% by weight, with 20.4% of polycose and 11.3% ofβ-sitosterol in the extraction. The extracting rate for polycose was 4.4% and forβ-sitosterol was 2.4%. The extraction of TbR had significant anti-cancer effect but little toxicity: the in vitro tumor growth inhibiting rate was 77.6% as evaluated by MTT test, and the in vivo tumor inhibiting rate was 50.29% as evaluated by tumor size of inoculated gastric epithelial cancer cells. The ingredients for stomach floating tablet was formulated as 15% HPMC K15M,15% HPMC K4M, 6.25% NaHCO3, 5% SDS, 5% PVP, 3.75% lactose, and 50% extraction powder of TbR shells. After all the compositional ingredients were mixed and sieved through 100 mesh screen, then granulated with 99% ethanol through 20 mesh screen and dried at 45℃for 5h, finally pressed into tablets. The drug releasing rate of the tablet at 10h was more than 90%. Conclusion: the extraction of TbR showed anti-cancer activity, and the stomach floating tablets formulated could increase the stomach retention time thus increase the bioavailability of TbR.