Pharmaceutical preparation containing racecadotril and preparation method thereof

Abstract

The invention discloses a pharmaceutical preparation containing racecadotril and a preparation method thereof, and belongs to the field of pharmaceutical preparations. The preparation comprises racecadotril, a taste masking material, a filling agent, a flavoring agent and a lubricant, the taste masking material is composed of NE30D and ethyl cellulose fine powder according to a certain proportion, and further aggregation of an acrylate copolymer is prevented through formation of an incompatible phase between ethyl cellulose and acrylate copolymer particles; the water vapor permeability and tension of the membrane are improved, so that the drug release rate is stabilized, the bitter taste of the drug is effectively covered, and the membrane is suitable for acute diarrhea treatment of infant and child patients; the product stability is good; the preparation method has the advantages of good drug entrapment performance, good taste masking effect, and simple preparation process by adopting a conventional wet granulation process, and is more suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a pharmaceutical preparation containing racecadotril and a preparation method thereof. Background technique [0002] The information disclosed in this background section is only intended to increase the understanding of the general background of the present invention, and is not necessarily taken as an acknowledgment or any form of suggestion that the information constitutes the prior art already known to those skilled in the art. [0003] Racecadotril (Racecadotril) is a kind of enkephalinase inhibitor, is the antidiarrheal drug of a kind of new mechanism of action developed by French Bioproject company, and it can inhibit enkephalinase selectively and reversibly, thereby Protect endogenous enkephalins from degradation, prolong the physiological activity of endogenous enkephalins in the digestive tract, directly inhibit the excessive secretion of ...

AI Technical Summary

Problems solved by technology

According to our experiments, it is difficult to obtain the ideal effect with this prescription and process. The curing time in the preparation process is long, and the requirements for the operation and control of the production process are strict, and the production efficiency is low. At the same time, the performance of the product still needs to be improved.

This is reflected in: Although the insoluble film-like structure formed by using NE30D material can obviously cover the bitter taste of racecadotril, but the Such materials are water-insoluble materials, and the mechanism for controlling their release is mainly through the pores formed by swelling or crystallization of surfactants to regulate drug release. The early stage of drug release is too slow, and the relatively fast drug release characteristics in the early stage of administration cannot be achieved to meet other requirements. In vivo absorption and rapid drug release requirements; at the same time, the copolymer in NE30D aqueous dispersion is usually in the form of small spherical particles , during the preparation process, small polymer particles aggregate, soften, and fuse with each other to form a film or skeleton. Therefore, this type of material usually needs to be cured to fully fuse the polymer film. Since this curing time is usually long, it makes The prepared preparations usually have the problems of reduced dissolution rate and poor stability during storage

[0009] patent CN102166197B uses sodium alginate, glycerin, etc. to spray-dry the drug to achieve microencapsulation treatment, thereby masking the bitter taste of the drug, but this process has a complicated preparation process , uneven microcapsule particle size, slow or incomplete dissolution, etc.; Patent CN107811973B crushes the drug into nano-fine powder, mixes ethanol and coconut oil, adds drug nano-fine powder and a small amount of filler to prepare a drug-containing solution, and then Spray it and the binder solution into the remaining filler. This process has problems such as high crushing requirements, complicated preparation process, difficulty in effectively masking taste without taste-masking materials, and residual organic solvents; patent CN110840848A dissolves the drug in polymer In ethylene glycol, the drug is formed into a solid dispersion to increase the solubility of the drug and taste masking. Due to the low solubility of racecadotril, there are problems such as high solid carrier usage or difficulty in fully dissolving the drug; patent CN106822907A prepares respectively Immediate-release granules and sustained-release granules achieve the purpose of biphasic drug release to cover up the bad taste of the drug, but there are problems such as uneven mixing and ineffective taste masking due to differences in the density of different granules; at the same time, the preparation steps and Complexity

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