Timed Release Of Yiguanjian Release Pellets

Yiguanjian was set up by the famous doctor Wei Zhixiu in Qing Dynasty, quoted from the book named Xu Ming Yi Lei An·Xin Wei Tong Men. This prescription is made of six medicines including Coastal Glehnia Root,Dwarf Lilyturf Root Tuber, Aahesive Rehmannia Root Tuber, Chinese Angelica, Barbury Wolfberry Fruit and Szechwan Chinaberry Fruit, which owns protective effect to liver and can be used to cure liver ailment. Clinically, it is mainly used to treat chronic hepatitis B, hepatocirrhosis, chronic hepatitis and so on. Yiguanjian is currently administrated in the form of traditional decoctions clinically. It is necessary to study the preparation using the modern technology in order to improve the bioavailability and decrease the times of drug administration. Therefore, this paper is focused on studying Yinguanjian sustained-release pellets of time-controlled release; it means to coat the drug-loading pill core with double decks, that is the inner swelling layer and the outer controlled layer. The water gradually permeated the outer layer in order to swell the inner layer. When the inner layer swelled to some extent, the outer layer would break which could trigger the drug completely, simultaneously releasing. By controlling the thickness of the controlling-release layer, we could regulate the rate of water permeating. Thus we could prepare two kinds of coated pellet that the time lag is 3 and 6 hours, respectively. By mixing the pellet core and the kinds of coated pellet at some ratio, the preparation could achieve the aim of sustained releasing and simultaneous releasing.This paper introduced the method of TLC, which was used to identify the fivemedicine materials: Aahesive Rehmannia Root Tuber, Radix Angelicae Sinensis, Barbury Wolfberry Fruit, Coastal Glehnia Root and Szechwan Chinaberry Fruit in the preparation. The Catalpol of Aahesive Rehmannia Root Tuber and the Ferulic of Radix Angelicae Sinensis were selected as the standard substance whose measuring method was set. A HPLC method was applied to measure the releasing degree. This method is credible with good fidelity, which was the good basis for the preparation study and the quality control.According to the theory of semi-bionic extracting, using the amount of indicative substance-Catalpol and Ferulic and dry-extravts as the standard, we selected out the best semi-bionic extracting technics' conditions of Yiguanjian. Applying orthogonal design test, we optimize the technics of alcohol precipitation method which could effectively remove the ordinary impurity of the medicine. The condition of the extracting and optima technics is credible with good recurrence. The experiment proved that the semi-bionic extracting method is better than the water extracting method and the alcohol precipitation of semi-bionic extracting method is better than the alcohol precipitation of water extracting method.The experiment of pharmic identified that the extracting of Yiguanjian applying optimized and refined technics had the obvious effect of reducing GPT, GOT and protective effect to liver with broad safe scope.Prepare Yiguanjian drug-loading pellets using extrusion-spheronization. By filtering the prescription and optimizing the technics, the yield of the target pellet is 78.2% and the appearance of the pellet is round and full. A fluid-bed spray processor was adopted for the coating of the buffer pellets. Using low-substituted hydroxypropyl cellulose (L-HPC) as the main coating material of the inner swelling layer increasing the weight of inner coating layer by 20% and 15%. It can achieve the effect of time-controlled release by controlling the thickness of the outer coating membrane wth surelease as the coating solution of the outer swelling layer. Yiguanjian sustained-release capsules were developed by encapsulating the three kinds of coated pellets whose coating load were 0%, 20% and 24% at equivalent ratio. Investigating the drug release the f₂ of Catalpol and Ferulic acid in Yiguanjian sustained-release pellets is 78.2. The release had no significant release, while the characteristics of sustained release could be obviously seen.