31 results about "Cetilistat" patented technology

The invention discloses a method for preparing cetiristat, which belongs to the technical field of pharmaceutical preparation methods and is used to solve the problem of high "three wastes", low yield and high cost in the existing preparation method. The method comprises: (1) esterifying compound A (2-amino-5-methylbenzoic acid) or a salt thereof; (2) acylating the esterified product obtained in step 1 with n-hexadecyl chloroformate; (3) Deesterifying the compound obtained in step 2 to obtain 2-(hexadecyloxycarbonyl)amino-5-methylbenzoic acid; (4) cyclizing the compound obtained in step 3 to obtain the target product. By improving the production steps, a synthetic method is provided which is simple and efficient, convenient for industrial production and capable of obtaining high-quality cetiristat.

The invention relates to cetilistat solid dispersion, and a medicinal preparation prepared from the solid dispersion. The cetilistat and one or both of the carriers hydroxypropyl cellulose and copovidone are prepared into a solid dispersion to significantly improve the solubility of the cetilistat, and overcome low solubility of cetilistat, so that the prepared medicinal preparation achieves good dissolution, and has increased bioavailability.

The invention discloses a cetilistat pellet and a preparation method thereof. The pellet comprises a pill core, then the pill core is loaded with drugs to prepare a cetilistat drug-loaded pill, and finally the pill is coated with a gastric-soluble coating layer. The cetilistat pellet prepared by the preparation method not only effectively maintains the original properties of the citilistat, but also guarantees the quick and even dissolution of drugs, and the pellet is capable of being prepared into various common dosage forms in pharmacy.

The invention provides a method for preparing cetilistat. According to the method, 2-amidogen-5-methyl benzoic acid is adopted as an initial raw material, under existence of pyridine, the 2-amidogen-5-methyl benzoic acid reacts with chlorine acid cetyl alcohol ester in the first place, a midbody 2-(((hexadecane oxygroup) carbonyl) amidogen)-5-methyl benzoic acid is obtained, then dehydrogenation cyclization reagent is utilized to obtain the cetilistat, and the feeding sequence in step 1 is the 2-amidogen-5-methyl benzoic acid, alkali and the chlorine acid cetyl alcohol ester in sequence. The method has the remarkable advantages that the route is simple, operation is less, atom economy is better than that of other routes, and the cetilistat is suitable for large-scale production; the purity of the cetilistat at the reaction endpoint is larger than 98%, and through simple postprocessing, a final product which meets medical standards can be obtained, wherein the purity is larger than 99.5%, and the single impurity is smaller than 0.1%; the utilized solvent including dichloromethane and pyridine can be recycled for mechanical application, and the method is environmentally friendly.

The invention discloses a medical composition for treating metabolic syndromes, belonging to the field of medicines, and in particular relates to a medical composition containing orlistat or cetilistat and heparin, wherein the composition is solid preparations such as compressed tablets, dispersible tablets, sustained release tablets, capsules, granules, and the like. In experiments, the medical composition containing the orlistat or the cetilistat and the heparin is accidentally found to have obvious synergistic effect on the aspects of reducing the blood pressure, the serum total cholesterol, the serum triglyceride and the low density lipoprotein cholesterin and enhancing the carbohydrate tolerance.