Tandospirone enteric-coated tablets and preparation method thereof

Abstract

The invention provides application of tandospirone in anti-anxiety drugs for intestinal administration and further provides tandospirone enteric-coated tablets and a preparation method thereof. The tandospirone enteric-coated tablets are prepared by using tandospirone or pharmaceutically-acceptable salt thereof as an active ingredient and adding pharmaceutically-acceptable excipients. The preparation method includes: mixing tandospirone or the pharmaceutically-acceptable salt and the excipients, granulating, and tabletting to obtain tablet cores; sequentially performing isolation layer coating, enteric layer coating and modification layer coating on the tablet cores, finally polishing and waxing to obtain the tandospirone enteric-coated tablets. The tandospirone enteric-coated tablets prepared by the method are stable in quality, high in disintegration and dissolution performance, little in damage to digestive tract mucous membranes, little in side effect and high in administration compliance, can be used for treating anxiety state caused by various neuroses, anxiety state accompanied by body diseases like primary hypertension and digestive ulcer and light-and-moderate depression, and is especially suitable for patients with anxiety, gastric mucosal lesion or proneness to bleeding caused by digestive system diseases and old patients needing long-time administration.

Description

technical field [0001] The invention relates to a new application of tandospirone, a tandospirone enteric-coated preparation and a preparation method thereof, belonging 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 acts selectively on 5-HT in the brain 1A Receptors, the action sites are concentrated in the hippocampus, amygdala and other limbic systems of the emotional center and project to the raphe nucleus of the 5-HT nerve, through the activation of presynaptic 5-HT 1A Receptors, inhibit neuron firing, reduce the synthesis of 5-HT, and at the same time inhibit the post-synaptic 5-HT 1A The receptor has a partial agonistic effect, so as to comprehensively reg...

AI Technical Summary

Problems solved by technology

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

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

[0006] So far, the marketed preparations of tandospirone only have film-coated tablets, and orally disintegrating tablets (CN200610021715.0), sustained-release tablets (CN200610021419.0), and osmotic pump-type controlled-release tablets (US5185158, US5330762, US5858407) reported in literature Oral dosage forms such as oral dosage forms, the above prior art all begin to release medicine in the stomach, fail to solve the irritation problem to digestive tract after taking medicine, fail to improve the patient who is anxious caused by digestive system disease, the patient of gastric mucosa injury or easy bleeding, Medication compliance and therapeutic efficacy in elderly patients taking long-term medication, while enteric-coated tablets have not been reported

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