30 results about "Cetilistat" patented technology

The invention relates to a new process for one-pot preparation of cetilistat; the one-pot reaction is adopted, separation steps are sample, the product yield is high, the product quality is good, and the new process is especially suitable for industrialized production.

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.

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 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 actos, 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 actos 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.

The invention belongs to the field of medicine compositions for treating obesity and II-type diabetes, and definitely, relates to a medicine composition of cetilistat and a preparation method thereof. A cetilistat tablet prepared from the medicine composition through the preparation method has excellent dissolving-out effect. The preparation method is simple and is suitable for industrial production.

The invention discloses a preparation method of cetilistat; the method has the advantages of concise process, easily obtained raw materials, and mild reaction conditions, and is suitable for industrialized production. According to a reaction route, 2-amino-5-methyl benzoic acid and hexadecyl chloroformate serve as starting raw materials, firstly, amino acylation is carried out, an intermediate is purified, then cyclization is carried out, and the target compound is obtained through a two-step reaction.

The invention provides a composition with a lipase inhibitor and a hydroxymethyl-glutaryl coenzyme A reductase inhibitor, and a pharmaceutical preparation with the composition. Preferentially, the lipase inhibitor is one of orlistat and cetilistat, and the hydroxymethyl-glutaryl coenzyme A reductase inhibitor is one of atorvastatin, rosuvastatin, simvastatin, fluvastatin, pravastatin, lovastatin and pitavastatin or pharmaceutically-acceptable salt thereof. The composition can have the synergistic antibacterial effect and the synergistic histamine releasing inhibition effect, and therefore thetreatment effect and economic characteristics of bacterial infection-caused allergic disease patients can be improved.

The present invention relates to a cetilistat crystal, which has good solubility and good stability, and is not easily subjected to crystal transition. The invention further provides a preparation method of the cetilistat crystal, wherein the method has characteristics of good reproducibility, easy condition control, high crystal yield, high crystal purity, and industrialized large-scale production.

The present invention relates to a cetilistat crystal, which has good solubility and good stability, and is not easily subjected to crystal transition. The invention further provides a preparation method of the cetilistat crystal, wherein the method has characteristics of good reproducibility, easy condition control, high crystal yield, high crystal purity, and industrialized large-scale production.

The invention provides a eutectic compound formed by a lipase inhibitor and a hydroxy methylglutaryl coenzyme A reductase inhibitor and composition containing the eutectic compound. The eutectic compound is characterized in that the lipase inhibitor is selected from one of orlistat and cetilistat; the hydroxy methylglutaryl coenzyme A reductase inhibitor is selected from one of atorvastatin, rosuvastatin, simvastatin, fluvastatin, pravastatin, lovastatin and pitavastatin or pharmacologically acceptable salts thereof. The eutectic compound can simultaneously have synergistic antibacterial action and synergistic histamine release inhibition function, so that the treatment effect on patients with allergic diseases caused by bacterial infection and the economic characteristics can be improved.

The invention discloses a medical composition for losing weight or treating hyperlipidemia, belonging to the field of medicines, and in particular relates to a medical composition containing orlistat or cetilistat and rosuvastatin calcium, 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 rosuvastatin calcium is accidentally found to have obvious synergistic effect on the aspects of reducing the serum total cholesterol, the serum triglyceride and the low density lipoprotein cholesterin.

The invention relates to a method for detecting cetilistat in a weight-losing health-care product. The method comprises the following steps: providing a reference substance solution, wherein a reference substance in the reference substance solution contains cetilistat; taking a weight-losing health-care product sample, extracting with methanol, collecting an extracting solution, and preparing a test solution; and detecting the reference solution and the test solution by adopting a high performance liquid chromatography-tandem mass spectrometry method, and determining whether the weight-losing health-care product sample contains the cetilistat or/and the content of the cetilistat according to a detection result. According to the method disclosed by the invention, the separation and detection of the cetilistat in the weight-losing health-care product are realized by adopting a proper extraction solvent and matching with proper detection conditions, the technical blank of the detection of the cetilistat in the weight-losing health-care product is filled, and a theoretical basis is laid for applying a high performance liquid chromatography-tandem mass spectrometry technology to the detection of the cetilistat in the weight-losing health-care product.

The invention discloses a method of preparing Cetilistat through a one-pot method. The method comprises the following steps that 2-amino-5-toluic acid is sequentially reacted with cetyl chloroformate and methane sulfonyl chloride in a mixed solution, and the Cetilistat is obtained through the one-pot method. According to the method, with selection of a mixed solution system as a reaction medium and the methane sulfonyl chloride as a lactonization reagent and adoption of the one-pot method to prepare the Cetilistat, an obtained product is high in yield and purity; the process is simple and not tedious, separation and purification of an intermediate are not needed, postprocessing is liable to operate, requirement on equipment is not high, the industrial production is facilitated.

The invention belongs to the field of medicinal preparations and relates to cetilistat tablets, in particular to cetilistat tablets capable of effectively increasing the active ingredient dissolution rate and a preparation method thereof. The preparation method includes the steps that an active ingredient and a polymer support are prepared into solid dispersion, and the cetilistat tablets are obtained through wet or dry granulation, wherein the solid dispersion can be blended with accessory materials including a filling agent, a binding agent, a disintegrating agent and a lubricating agent. The cetilistat tablets are high in active ingredient dissolution rate, good in technological reproducibility and suitable for industrial production and provide a research basis for other cetilistat preparations.