A kind of olanzapine oral fast-dissolving film agent and preparation method thereof

Abstract

The invention belongs to the technical field of medicine, and in particular relates to olanzapine and an oral fast-dissolving film containing the composition. The oral instant film preparation is composed of olanzapine, film-forming material, solubilizer, plasticizer and other auxiliary materials, wherein the solubilizer is dibasic acid. In the present invention, under the action of a solubilizing agent, the dissolving ability of olanzapine in the hydrophilic film-forming material can be significantly improved, so that the content of the main drug is uniform, the dissolution is rapid, and there is no gritty feeling when taken orally, and the product has good mechanical properties. No organic solvent is used in the process, so the production safety is high. The preparation can be rapidly dissolved in the oral cavity without the need for water delivery, which can effectively avoid the ubiquitous phenomenon of vomiting and Tibetan medicine in patients with schizophrenia, and help to improve the medication compliance of such patients.

Description

Technical fields: [0001] The present invention belongs to the field of medical technology, specifically relates to a olanzapine oral instant film agent and a method of preparation thereof. Background: [0002] Olanzapine is a new type of atypical antipsychotic drug developed by Lilai in 1997 for the treatment of acute bipolar mania, which has the advantages of significant clinical efficacy (rapid onset of action, rapid sedation, rapid increase, direct therapeutic dose), excellent time to continue taking before discontinuation (TTD) and very low adverse reactions. It can significantly improve the negative (poor thinking, emotional indifference, lack of will, etc.) and positive symptoms (hallucinations, delusions, associations, excitement, exaggeration, suspicion of victimization, hostility, etc.) in patients with schizophrenia. Since the listing of olanzapine to 2017, the cumulative amount of oral tablets has reached 55 billion US dollars and ranks first in China's anti-schizophre...

AI Technical Summary

Problems solved by technology

However, the film-forming materials used in oral instant film preparations are generally hydrophilic polymers, but olanzapine is almost insoluble in water, and it is difficult to evenly disperse in the hydrophilic solution, so that it is impossible to obtain a product with uniform main drug content and good dissolution performance. Oral fast dissolving film

Patent CN 104546807 A uses gelatin as the main film-forming material, which can significantly increase the drug loading of olanzapine and can melt quickly in the oral cavity, but gelatin, as a natural polymer material with protein structure, is brittle and has poor mechanical properties after forming a film. Even adding a solubilizer is difficult to meet the requirements of oral fast-dissolving film

In patent CN 102920683 A, 20% ethanol is used as latent solvent to increase the solubility of olanzapine in film-forming materials, but ethanol, as a flammable and explosive organic solvent, will bring some unsafe factors to large-scale industrial production

And the prior art also discloses that olanzapine and polymer auxiliary materials are first prepared into solid dispersions, or prepared into new dosage forms such as clathrates and micelles, and then film-forming materials and other auxiliary materials are added to prepare olanzapine orally. Instant film agent, however, these pretreatment methods that it adopts all have the characteristics of high price of auxiliary materials, difficult process, high equipment requirements, etc., and then increase the production cost

Images