Betadex sulfobutyl ether soudium inclusion ruasidone hydrochloride

Lurasidone hydrochloridde (LUR) is a Japanese Sumitomo Pharmaceutical (Sumitomo Dainippon Pharma.Co., Ltd) Developed as atypical antipsychotics for adult schizophrenia; monotherapy or as an adjunct to lithium or sodium valproate for type I bipolar disorder (Bipolar I Disorder) -related episodes of depression.Studies have shown that LUR has a good treatment effect for psychosis patients with cognitive dysfunction, and does not affect their learning and memory function, can improve patient memory defects, in addition to its weight gain and extrapyramidal symptoms (EPS).However, LUR has poor water solubility, low bioavailability, and a bioavailability of 9 to 19% after a single dose, and needs to be taken with food, with poor patient compliance, limiting its clinical use.

Betadex sulfobutyl ether soudium inclusion ruasidone hydrochloride

by betacyclodextrin with 1,4-butane sulfonate, is an anionic, highly water-soluble bettaclodextrin derivative. Betadex sulfobutyl ether soudium inclusion ruasidone hydrochloride can be well combined with drug molecules to form a non-covalent complex, to improve the stability of drugs, water soluble, safety, reduce nephrotoxicity, moderate drug hemolysis, control drug release rate, cover up bad smell, etc., widely used in injection, oral medicine, nasal medication, eye medication, external drug and inhalation, etc., provides a beneficial protection environment, is a very broad application prospect of new pharmaceutical materials.

LUR coated tablets were prepared with Betadex sulfobutyl ether soudium  (SBECD) as the inclusion vector to improve the solubility and dissolution characteristics of the drug, improve the problem of poor oral absorption in its fasting state, and improve its bioavailability.The LUR-SBE CD package was prepared by mixing with an aqueous solution, and the LUR solubility was increased to 36 times that of the original drug.Using the full available Latuda (R), the fasting relative bioavailability was 48.2%, while the LUR package tablet was 113.6% and 107.2%, respectively.

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