The Study On Tegafur Proliposome Soft Capsules

Objective: The purpose of research is to make the soft capsules of tegafur proliposome, improving the stability of proliposome and convenienting the application for clinic. The projects include the screening of optimizing prescriptions and producing process of the tegafur proliposome soft capsules, building the quality criterion and to study the initial stage stability of the soft capsules.Methods: (1) According to the product of malonaldehyde (MDA), the quantity of Vit-E as oxidation inhibitor was selected. (2) The method with Tartrazine as indicator was used to determine the dissolution rates of the soft gelatin capsule shell. To optimize the shell compositions by the mono factor trail and the method of design by uniform distribution. (3) The HPLC method was applied to determinate the concentration of phosphatidylcholine (PC) and phosphatidylethanolamine (PE) in soybean phospholipid. (4) According to the requirement of building the criterion, the quality criterion of the tegafur proliposome sofe capsule was established. (5) Accelerating test and long-term test was studied according to Chinese Pharmacopeia (Edition 2000).Results: (1) the quantity of Vit-E as oxidation inhibitor (contents≥ 70%) is 6%. (2) The optimizing prescription is that glycerin/gelatin =0.847, PEG400/gelatin=0.0586, the quantity of TiO2 from 0.3%~4% is not interfere with the dissolution rate of capsule shell. (3) The PC and PE can be detected at the same HPLC condition. The method is sensitive,accurate and reproducible. The recovery and precision of the method satisfied the requirements. (4) The quality criterion of the tegafur proliposome soft capsules can practicably control the quality. (5) The indexes were not obviously change in initial stage research.Conclusions: (1) Verified experiment made it known that the better proscription is reasonable and stable. (2) The quality control method is stable and has a good repeatability and can be used to control the quality of the proliposome soft capsules. (3) The tegafur proliposome soft capsule was stable under the different test condition in initial stage research.