Study On The Compound Curcumin Microcapsule

Curcumin is the main active ingredient of Zingiberaceaec, Curcuma plants. It has obvious hypolipidemic, anti-oxidation and scavenging free radicals and other physiological functions. However there are a number of issues with curcumin, such as low solubility in water, the biotransformation in the course of intestinal absoption, poor stability, resulting in low oral bioavaibility, and limiting it's clinical use. Piperine, which is a glucruonic acid inhibitors in liver and intestines, is a alkaloid ingredient that extracted from the fruit of pepper plant. It can be used to inhibit the curcumin's biotransformation in the course of intestine and improve the bioavailability of curcumin. The pharmacology and pharmacodynamic researches indicated that combination of curcumin and piperine can potentiated the anti-atherosclerosis and hypolipidemic effect. Microencapsulation technology was used to increase curcumin's stability, and promoted absorption, increased bioavailability. In addition, according to the characteristics of hyperlipidemia disease, in order to minimize the times of administration and facilitate the clinical application, develop it as sustained-release solid oral formulation.Firstly, a summary of research progress of new dosage form of traditional Chinese medicine, especially of sustained-release microcapsule. Including microcapsule's coating materials, preparation methods, quality evaluation methods, and so on.Secondly, studied on the preparation of compound curcumin microcapsule. Choosed natural polymer chitosan and alginate as coating materials, and used complex coacervation for microcapsule's preparation. Adopted the single factor method to studied the impact of the concentration of sodium alginate, concentration of calcium chloride, the concentration of chitosan, and pH of chitosan solution on the preparation of the microcapsule. Choosed the encapsulation efficiency and the drug loading of microcapsules as the chief index, the shape and size of microcapsule as the assist index. Ultimately determined the optimal condition was: concentration of alginate solution was 2%, concentration of calcium chloride was 2%, the concentration of chitosan was 0.3%, and pH of chitosan solution was 3.5. The verification test results showed the optimal conditions for the preparation of compound curcumin microcapsule dispersed evenly-roundness of the ball, the encapsulation efficiency of curcumin was more than 85%, indicated that the preparation of microcapsule was stable, simple and workable.Eventually, studied on the quality evaluation methods of compound curcumin microcapsule. Investigated the shape of microcapsule and its size determination, established the TLC Identification method of curcumin, the determination method of curcumin and piperine in microcapsule by HPLC and studied on dissolution testing methods in of curcumin vitro. Studied on the three batches of compound curcumin microcapsule samples, the results show that microcapsule has spherical shape and the distribution of size is uniform, the method for assay of curcumin and piperine is simple, accurate, reproducibility. The mean drug loading of curcumin and piperine in compound curcumin microcapsules is 25.96% and 1.32%. The accumulate release Q and t1/2 are linear. The release mechanism of the curcumin from the compound curcumin microcapsules followed Higuchi equation.