Research Of Nanoemulsion Hydrolyzate And Its Solid Preparation To Promote Intestinal Absorption Of Water-soluble Drug

Objective: Based on the previous work, FD4 and ceftriaxone as the model drugs, which are researched the promoting effect of purified nanoemulsion hydrolyzate for water-soluble drug intestinal absorption, further comparative research on nanoemulsion Hydrolyzate solid preparation to explore appropriate prescription and preparation process.Methods:(1) Centrifuged lipolysis solusion, which are extracted with dichloromethane, rotary evaporation.(2) To establish the in vivo analysis methods of FD4 and ceftriaxone, study on the effect of purified nanoemulsion hydrolyzate for FD4 and ceftriaxone intestinal absorption with duodenal intubation for animal model of rat, compare with the bioavailability between nanoemulsion and nanoemulsion hydrolyzate.(3) By freeze-drying, spray-drying, the solid adsorbent three methods choose the best process for the preparation of solid lipid intermediates. To prepare the Lipid formulations pellets by extrusion spheronization, single factor study choose the pellet preparation. Further, make a preliminary evaluation on in vitro release and stability of pellets.Results: 1 When the ratio of 1:2,The supernatant is extracted best with methylene chloride; the precipitate is reconstituted by micellar solutions of bile salts, adjust pH=5, the solution become clear, with a 1:2 ratio of methylene chloride can obtain the best rate.2 Nanoemulsion and its purified lipolysis product can promote FD4 and ceftriaxone intestinal absorption, improve their absolute bioavailability and purified lipolysis product in promoting absorption of more significant.3 The process of the solid adsorbent is the most simple and convenient, silica powder with best adsorption properties of the adsorbent.The optimal formulation and process conditions of pellets preparation: lipid delivery systems:MCC:PVPP:Lactose:silica powder = 30:35:15:15:5, extrusion speed 30 rpm, spheronization speed 600 rpm, spheronization time 5 min.Conclusion: The purified lipolysis product can significantly promote intestinal absorption of different molecular weights water-soluble drugs, has good prospects for further application development. Using pellet form to solidify lipid preparations, all parameters in a good condition, is expected to as a solid dosage form of this prescription.