Gardenia Bo Pi Soft Capsule

Zhizi-Baipi soft capsule was a new type Chinese traditional medicine preparation, which was prepared by extracting and refining the three herbs: Fuctus Gdeniae, Cortex Phellodendri and Radix Glycyrrhizae. The recipe was originated from Zhizi-baipi soup recorded in "Shanghan Lun", which was mainly used to treat icteric hepatitis, itch of skin and eczema etc. Based on the original recipe, Zhizi-Baipi soft capsule was designed and prepared to improve the formulation processe, so as to elevate its bioavailability and be more convenient to use.According to literature and experiments, the HPLC method was employed in this paper to determine the content of geniposide, berberine and glycyrrhizin as well as their dissolution. The TLC method was used to identify the three herbs.To facilitate the preparation process ,to remove the inactive components as far as possible, and to decrease the dose, in this paper, the main active components of the three herbs was chosen to investigate the influence of mixed decoction and separated decoction on the content of index component. The results indicated that the content of berberine in mixed decoction was far lower than that in separated decoction. So, the three herbs were extracted separately, and their refining techniques were investigated. (1) Study of herb extracting process: the water-extracting processes of the three herbs were studied by orthogonal experiment with the content of effective components and solid-extract percent as index. Solvent amount, extracting time, and extracting times were chosen as factors, and three levels were selected for every factor to optimize the processes. The ultimate extracting processes were determined as follows: a) The Fuctus Gdeniae powder was extracted with 8-fold water for 1h by refluxing, and repeated for 3 times, b) The Cortex Phellodendri powder was extracted with 10-fold water for 1h by refluxing, and repeated for 3 times, c) The Radix Glycyrrhizae powder was extracted with 8-fold water for 1.5h by decoction, and repeated for 3 times.(2) Study of refining processes of herb extract: Clarifiers (chitosan and ZTC) as well as alcohol-precipitating method was employed to refine the wate-extract of Fuctus Gdeniae, Cortex Phellodendri and Radix Glycyrrhizae, respectively. The contents of the three index components in the corresponding refined extract were tested. Meanwhile, the solid-extract percent and the method's simplicity were considered to determine the final refining methods. The methods were finally chosen as follows:a) The Fuctus Gdenia extract was refined using ZTCⅡ1+1 claricant; b) The Cortex Phellodendri extract was refined by alchol-precipitating method at room temperature; c) The Radix Glycyrrhizae extract was refined using ZTCⅡ1+1 claricant.The formulation of the content and the capsule shell of Zhizi-Baipi soft capsule were screened in this paper. The ratio between extract and diluent, the size of extract powder, the kinds of suspending agent and wetting agent were studied to test the influences on the physical stability of the content with the sedimentation ratio of the content suspension as the test index. The final formulation of content was determined as follows: the ratio between extract and castor oil was 1:1.5. Glyceryl monostearate was used as the suspending agent, accounting for 1% of castor oil. Span-80 was used as the wetting agent, accounting for 0.5% of castor oil. With the dissolution rate of lemon yellow added in the capsule shell as the index, ratio between gelatin and glycerin, storage temperature, drying time, supplements added and the content were investigated to test their influence on the solubility of capsule shell. The final formulation of capsule shell was fixed as follows: gelatin: glycerin: water: fumaric acid: titanium dioxide (1: 0.5: 1.3: 0.15: 0.008, w/w). The dissolution of geniposide and berberine were measured in PBS 7.4, water and chlorhydric acid solution (0.1M), respectively. The pH7.4 PBS was selected as the dissolution medium in vitro. The dissolution of geniposide and berberine reached 90% and 80% respectively within 60 min.Induced by carbon tetrachloride, hepatic injury micewas selected as pharmacodynamics model. The drug action of Zhizi-Baipi soft capsule was evaluated using the activity of ALT and AST in serum and the extent of hepatic injury as indices. The results indicated that this preparation obviously provided the action of decreasing aminopherase and protected the hepatic cell.