Preclinical Study On The Granule Inhibiting Liver Injury Caused By Anti-Tuberculosis Drugs

In order to develop a new preparation of the granule inhibiting liver injury caused by anti-tuberculosis drugs, its extraction method, formalizing process, qualitative identification of main components and protective effect on acute liver injury had been investigated.1.Via orthogonal design, the volatile oil extraction condition was optimized to investigate the total content of volatile oil, and the water extraction condition was optimized to investigate the solids yield and the soluble content in ethanol solution.The transferring rate of the volatile oil and percentage recovery of inclusion were used as indicators to explore the optimum inclusion process of B-cyclodextrin. TLC method was applied to detect the main content change of the volatile oil before and after inclusion.The best volatile oil extraction condition was to add 6 folds water into the crud drugs, for soaking 1 hour and refluxing for 6 hours. The best water extraction condition was 9,7,7 folds water for 3 times and 0.5 hour each time. The optimum inclusion condition was B-cyclodextrin: volatile oil (6:1) refluxing and stirring for 1h at 50℃. TLC determination showed that the main contents of the volatile were the same as the ones after being included.2.By observing the difficulty of granulation, the distribution of granule size, the solubility of granule and the dosage, orthogonal design was applied to evaluate comprehensively the formability of the liver-protecting granule. It was the optimum formalizing process that extractive powder with no more than 2.6% moisture content and soluble starch in proportion as 1:1.5 was mixed and wetted with60%ofethanol.3. TLC method could identify the four main contents of the liver-protecting granule. Negative control solution of the samples did not interfere. The identification method was simple, rapid and sensitive and could be the method of quality control of the preparation.4. Acute liver injury model was induced by intraperitoneal injection of 0.12%CCl4. The test group was given the granule inhibiting liver injury caused by anti-tuberculosis drugs. The levels of ALT and AST in serum and MDA and SOD in the liver tissue were measured with liver index and pathological changes of the liver tissue were observed under optic microscope. The drug significantly lowered serum ALT and AST, MDA and SOD in the liver tissue and the liver index, and markedly ameliorated the liver damage.