A kind of tetradosin enteric-coated sustained-release pellets, preparation method and application thereof

Abstract

The invention provides a tetrodotoxin enteric-coated and sustained-release pellet and a preparation method thereof, and relates to the field of a medicine preparation technology and application. The tetrodotoxin enteric-coated and sustained-release pellet sequentially comprises a blank pellet core, an upper medicine layer, a sustained-release layer, an isolation layer and an enteric layer from inside to outside, wherein the upper medicine layer is tetrodotoxin containing a cosolvent and a bonding agent; according to a weight ratio, the weight of the sustained-release layer accounts for 20 percent to 40 percent of the weight of the medicine containing pellet; the weight of the isolation layer accounts for 2 percent to 8 percent of the weight of the sustained-release pellet; the weight of the enteric layer accounts for 10 percent to 30 percent of the weight of the isolation pellet. The blank pellet core is used as a medicine carrier; a fluidized bed medication method is used for preparing the tetrodotoxin medicine-carried pellet; the sustained-release layer, the isolation layer and the enteric layer are sequentially sprayed to obtain the tetrodotoxin enteric-coated and sustained-release pellet. The advantages of medicine release controllability, a long-period pain relieving effect, good clinic use complaisance, high safety and the like are realized. In addition, the blank pellet core fluidized bed medication and coating method is applicable to the preparation of the ultra-low-specification tetrodotoxin medicine oral sustained-release preparation; the medication rate is high; the content uniformity is good.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparation technology and application, in particular to a tetrodosin enteric-coated sustained-release pellet and a preparation method thereof. Background technique [0002] Tetradosin (tetradotoxin) is a marine biotoxin mainly extracted from the viscera of puffer fish. It is a highly selective sodium ion channel blocker and has detoxification and analgesic effects. Tetradosin has high activity and high toxicity, and the clinical dosage is microgram level. Therefore, it has the advantages of good content uniformity and easy and accurate dosage control when prepared into injection or freeze-dried preparation. [0003] Most of the dosage forms of tetrodosin in clinical research at home and abroad are injections for intramuscular or intravenous administration. [0004] According to literature reports, after intramuscular injection of tetrodosin, the half-life of the drug in the body is short, and the e...

AI Technical Summary

Problems solved by technology

In order to maintain the drug effect, frequent intramuscular injections are required, which is difficult to meet the treatment needs of most patients, and the clinical compliance is poor

Simultaneously, the intramuscular injection dose of tetradosin used in clinical practice is usually not higher than 30 micrograms, such a low content, it is difficult to solve the problem of poor content uniformity of tetradosin pharmaceutical preparations by using existing technologies such as mixed granulation method to prepare oral tablets or capsules. Difficulties, thus restricting the application research of oral preparations

[0005] The technical problem to be solved in the present invention is the short half-life of the medicine that exists in the development of tetrodosin medicine, and the problems such as the poor compliance of the injection for clinical application (cannot be administered orally).

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