Olanzapine oral instant film and preparation method thereof

Abstract

The invention belongs to the technical field of medicines, and particularly relates to olanzapine and an oral instant film containing the olanzapine. The oral instant film is composed of olanzapine, a film-forming material, a solubilizer, a plasticizer and other auxiliary materials, wherein the solubilizer is dibasic acid. According to the invention, the dissolving capacity of the olanzapine in the hydrophilic film-forming material can be obviously improved under the action of the solubilizer, so that the content of the main drug is uniform, the dissolution is rapid, the oral administration has no gritty feeling, the mechanical property of the product is good, meanwhile, no organic solvent is used in the whole production process, and the production safety is high. The preparation can be rapidly dissolved in the oral cavity, does not need to be taken with water, can effectively avoid the common phenomena of vomiting and drug storage of schizophrenic patients, and helps to improve the medication compliance of patients with schizophrenia.

Description

[0001] Technical field: [0002] The invention belongs to the technical field of medicine, and in particular relates to an oral fast-dissolving film of olanzapine and a preparation method thereof. [0003] Background technique: [0004] Olanzapine is a new type of atypical antipsychotic drug developed by Lilai Company in 1997 for the treatment of acute bipolar mania. Therapeutic dose directly), excellent duration of taking the drug before discontinuation (TTD) and extremely low adverse reactions. It can significantly improve the negative (poor thinking, apathy, lack of will, etc.) and positive symptoms (hallucinations, delusions, loose associations, excitement, exaggeration, suspicion, hostility, etc.) of patients with schizophrenia. Since the launch of olanzapine to 2017, the cumulative value of its oral tablets has reached 55 billion U.S. dollars and ranks first in my country's anti-schizophrenia drug market. Its structural formula is as follows: [0005] [0006] Curre...

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

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