The Study Of Berberine Hydrochloride Tablets For Colon-targeted Preparation

[Objective] Colon-targeted coating tablets of berberine hydrochloride were established to achieve the colon-targeted drug delivery and raise the antibacterial curative effect, which depended on the common advantage of pH-sensitive drug delivery system. [Method] Based on pre-experiment, proper excipients were screened. Quick release and high expanding property tablet cores were got by orthogonal experiment design. Acrylic acid resin II and III were used as coating material to make pH-sensitive system. Adjusting coating thickness to make the drug pass the stomach and small intestine, then release in the colon. Based on the preliminary experiment above, berberine hydrochloride controlled-release tablets for colon-targeted delivery were prepared. 0.1mol/1 hydrochloric solution and phosphatic buffer solution of pH6.8 and pH7.4 were used to simulate the condition of stomach, small intestine and colon. A spectrophotometric method for the determination of this preparation was also established. The quality of the preparation was evaluated by means of assay, dissolution test as well as stability test. [Result]The optional tablet cores and coating formulations were determined. Berberine hydrochloride controlled-release tablets for colon-targeted delivery based on the preliminary experiment above were not more than 15% dissolved in three hours in pH6.8 PBS and not less than 75% dissolved in one hour in pH7.4 PBS. This preparation conformed to the quality requirements under Tablets of Appendix I A of Pharmacopoeia of P.R. China (part II, Edi 2005).The tablets were considered to be stable in the condition of light, heat, wetness, accelerated test and long-termed storage test. [Conclusion] The preparation process of berberine hydrochloride controlled-release tablets for colon-targeted delivery was practicable and the drug could be released in colon as expected. At the same time, the method of quality control was proved to be accurate and credible. The period of validity was considered to be two years.