A kind of tandospirone enteric-coated pellets and its preparation method and application

Abstract

The invention provides a tandospirone enteric-coated pellet and a preparation method thereof. The enteric-coated pellet is prepared by adding tandospirone or a pharmaceutically acceptable salt thereof as an active ingredient and adding pharmaceutically acceptable auxiliary materials . The present invention also provides the use of the tandospirone enteric-coated pellets in the preparation of an anti-anxiety drug for enteral administration. The tandospirone enteric-coated pellets prepared by the invention have stable quality, no disintegration in the stomach, large distribution area in the intestinal tract, good disintegration and dissolution properties, high bioavailability, less irritation to the digestive tract mucosa, and less side effects , The patient's medication compliance is high. It can be used to treat patients with the following diseases: anxiety state caused by various neurosis, anxiety state accompanied by physical diseases such as essential hypertension and peptic ulcer, mild and moderate depression; especially suitable for digestive system diseases Patients who cause anxiety, patients with gastric mucosal injury or easy bleeding, and elderly patients who need long-term medication.

Description

technical field [0001] The invention relates to tandospirone enteric-coated pellets, a preparation method and application thereof, and belongs to the field of medicines. Background technique [0002] Tandospirone is a new type of anti-anxiety drug successfully developed by Sumitomo Pharmaceutical Co., Ltd. of Japan. It was first approved to be marketed in Japan in 1996. It entered the Chinese market in 2004 and has been widely used in the field of anti-anxiety treatment in China. [0003] Tandospirone can selectively act on 5-HT1A receptors in the brain, and the action sites are concentrated in the hippocampus, amygdala and other brain limbic systems in the emotional center and project to the raphe nucleus of the 5-HT energy nerve. By activating the presynaptic 5 -HT1A receptors, inhibit neuron discharge, reduce the synthesis of 5-HT, and at the same time have a partial excitatory effect on the post-synaptic 5-HT1A receptors, so as to comprehensively regulate the 5-HT functi...

AI Technical Summary

Problems solved by technology

The above-mentioned gastric-soluble preparations have overlooked a very important problem: tandospirone is a kind of irritating compound, and after melting in the stomach, the local drug dose is very large, which will stimulate the gastric mucosa; To achieve a long-term release effect (usually only need to take the medicine once or twice a day), their drug content is 1.5 to 3 times higher than that of ordinary oral preparations, and if a sudden release occurs in the stomach, the local drug dose will also be too large , thereby irritating the gastric mucosa

[0006] Judging from the evidence of adverse reactions reported during the clinical use of existing tandospirone preparations, the adverse reactions of the digestive system with a relatively high incidence (incidence rate ≥ 1%) include: nausea, vomiting, loss of appetite, oral Thirst, abdominal discomfort, stomach pain, bloating, abdominal distension, diarrhea, etc. This is especially unfavorable for patients with anxiety caused by digestive system diseases, patients with gastric mucosal injury or bleeding, and elderly patients who need long-term medication

These patients not only have low tolerance to irritating substances, which can easily induce adverse reactions in the digestive system, resulting in low drug compliance, but also due to digestive tract dysfunction, poor drug absorption and low drug bioavailability, which will seriously affect the therapeutic effect

[0007] The technologies disclosed above all have the characteristics of releasing a large amount of drugs in the stomach, accompanied or possibly accompanied by excessive local drug doses, and fail to solve the problem of irritation to the digestive tract after taking the drugs

So far, the enteric-coated tandospirone that can improve the medication compliance and therapeutic effect of patients with anxiety caused by digestive system diseases, patients with gastric mucosal injury or bleeding easily, and elderly patients who need long-term medication, and can be absorbed and utilized efficiently Preparations have not yet been reported

Images