Oral-applied slow-releasing or release-controllable solid clozapine

Abstract

An oral-applied slow-releasing or release-controlalble solid clozapine for treating psychosis is prepared from clozepine, skeleton assistant material and filler (starch, hydroxypropyl cellulose, ethylcellulose, etc.). Its advantages are high curative effect, and stable concentration of medicine in blood.

Description

technical field [0001] The invention relates to an oral western medicine preparation for treating schizophrenia, in particular to an oral slow and controlled release solid preparation of clozapine. Background technique [0002] Clozapine is an atypical antipsychotic drug, which has good curative effect on positive or negative symptoms of schizophrenia. It is different from traditional or classic antipsychotic drugs in that it has higher clinical efficacy and is more There is no extrapyramidal side effect at a low daily dose, and it can still increase the curative effect by about 30% in different degrees for those who have no significant curative effect on traditional antipsychotic drugs or those who are resistant to treatment, so it is especially suitable for refractory schizophrenia. Although clozapine hardly produces extrapyramidal side effects, it is still found to have more adverse reactions in other aspects in clinical application, including: one of the common ones is h...

AI Technical Summary

Problems solved by technology

Although clozapine hardly produces extrapyramidal side effects, it is still found to have more adverse reactions in other aspects in clinical application, including: one of the common ones is headache, dizziness, listlessness, hyperhidrosis, oral Excessive salivation, nausea or vomiting, constipation and weight gain; secondly, restlessness, confusion, blurred vision, elevated blood pressure, severe continuous headache; thirdly, tachycardia, hypotension or Cardiovascular problems such as orthostatic hypotension and syncope; the fourth is elevated body temperature; the fifth is prone to arrhythmia or delirium or respiratory depression when overdose

The above adverse reactions are mostly related to the large fluctuations in the dosage and plasma concentration of clozapine, which affects its wide clinical application to a certain extent.

At present, most of the clozapine preparations used in China are traditional common preparations, and the oral blood concentration fluctuates greatly, and there is a phenomenon of "peak and valley" of blood concentration. concentration, so that poisoning or serious adverse reactions may occur; low concentration may be far below the required therapeutic concentration, so that no curative effect can be produced

After retrieving the published Chinese patent documents, it is found that most of the patents (applications) involved use clozapine as an adjuvant, such as patent No. ZL9710478.5 "Anshen Zhenkuang Pill and its preparation method" and patent No. An antipsychotic pharmaceutical composition for calming the mind "disclosed drug formula, the proportion of clozapine and the absolute content of a single tablet are relatively low, so it is difficult to effectively exert the drug effect of clozapine