Study Of Preparation Of Baicalin Solid Self-microemulsifying Drug Delivery Systems Based On Liquisolid Technique

Baicalin is one of the main active ingredients of traditional Chinese medicine radix scutellariae, is extracted from radix scutellariae dry roots to a kind of flavonoids, has extensive pharmacological activity, antibacterial and anti-inflammatory effect is the most significant. But due to poor solubility in water, limiting its oral absorption, leading to a lower bioavailability.Many studies show that self-microemulsifying drug delivery systems can significantly increase the solubility of difficult soluble drugs, improve its bioavailability. Solid self-microemulsifying drug delivery systems is made up of the SMEDDS and appropriate solidified carrier.Compared with the traditional SMEDDS, its stability increased and prolonged storage, gastrointestinal tract irritation decreased, convenient to take. Therefore, this paper with baicalin as a model drug, using the liquisolid technique, the preparation of baicalin S-SMEDDS, so as to improve its dissolution, and improve its bioavailability.Firstly, this paper had quality control study of baicalin investigated by TLC identification and content determination. Determination of content respectively established UV and HPLC methods to determin baicalin from crude drug.And it established the method of determining release degrees of drug in vitro, which laid the foundation for the future prescription screening and the evaluation of the quality of preparation.By the baicalin of solubility test, selecting properties that the micro emulsion accessories is better, and to determine the scope of the prescription composition and proportion, drawing the ternary phase diagram preliminarily. Since the self-emulsifying time, drug-polymer interactions, and particle size as indexes, with overall effects of OD value is variable, central composite design-response surface methodology is used to optimize and verify the prescription,Baicalin self emulsifying preparationfor optimal prescription Tween 80-PEG-400- oleic acid ethyl ester, its mass ratio (1.13:0.52:0.2). Has carried on the preliminary evaluation of quality of SMEDDS, as a result, uniform and stable, after the emulsion particle size is small, and emulsifying time is short.On the basis of SMEDDS, using the liquisolid technique as a new technology of cured SMEDDS, according to the mathematical model of liquid-solid compression for liquid excipients, the kinds of carrier and coating materials and ratios of the drug in solution, R values was investigated. Ultimately selected the best baicalin S-SMEDDS prescription, according to the best prescription of three groups of samples was prepared, and the prescription verification, suggests that the prescription has good reproducibility.Properties of baicalin S-SMEDDS was studied. It studied the properties respectively from three aspects of the micro emulsion emulsion, the micro emulsion powder and the micro emulsion slice, by particle size, self-emulsifying time, powder liquidity, differential scanning calorimetry analysis, wettability powder, and the content uniformity and dissolution. It laid the foundation for the future to explore its rights to dissolve mechanism.The paper had quality control study of baicalin S-SMEDDS. It mainly investigated the shape, TLC identification, the critical relative humidity, determination of content and inspection.