Drug sustained and controlled release microparticle preparation for treating intestinal diseases, and preparation method thereof

Abstract

The present invention discloses a drug sustained and controlled release microparticle preparation for treating intestinal diseases. The preparation comprises: a pill core containing the drug, wherein the pill core contains 5-aminosalicylic acid and an assistant material; an isolation layer for providing a smooth and flat surface for the microparticle and preventing the drug from penetrating into a sustained release coating layer, wherein the penetration of the drug into the sustained release coating layer can affect the release effect, the used material of the isolation layer comprises one or a plurality of materials selected from a water-soluble polymer and an anti-adhesion agent; the sustained release coating layer for slowly releasing the drug, wherein different drug release levels can be achieved through adjusting the thickness of the sustained release coating layer, the used material of the sustained release coating layer mainly adopts a sustained-release material; an enteric-coating layer, the enteric-coating layer is provided for avoiding the early release of the drug in gastric juice, reducing stimulation of the main drug to stomach, increasing the local concentration of the drug in the lesion location, the used material of the enteric-coating layer mainly adopts a polymer enteric material. The invention further discloses a preparation method for the microparticle preparation. According to the present invention, the drug and the sustained release coating material are uniformly dispersed on the surface of the pellet, such that the problem of mixing uniformity of the assistant material and the main drug can be effectively solved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a sustained and controlled release pellet or particle preparation of a drug (5-aminosalicylic acid) for treating intestinal diseases; Methods for controlled release of pellet or microparticle formulations. Background technique [0002] Mesalazine (ie, 5-aminosalicylic acid) is mainly used clinically for the treatment of Crohn's disease and ulcerative colitis. But its dosage is higher (up to 4g is often used in the prescription), and the stomach is stimulated to a certain extent, and the diseased part of the treatment is in the colon. Most oral products on the market are prepared by slow-release and controlled-release methods. Products to reduce the number of times of taking and the stimulation to the human body, and improve the curative effect. However, the technology involved in most products and inventions cannot achieve the expected purpose, mainly beca...

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Problems solved by technology

In the general preparation production process, it is difficult to ensure that the sustained-release polymer material is evenly mixed with the main drug and other excipients, thus easily affecting the release effect of the drug and affecting the quality of the drug

[0006] The Chinese patent whose patent number is CN00808889.6 also has the above-mentioned defects, and cannot achieve the purpose of intestinal localized release; and improving the drug loading capacity; and the content disclosed in the patent of CN200480010790.6 can not solve the problem of early release in gastric juice; the patent of CN200810232858.5 discloses a colon-targeted tablet preparation technology, and The dosage of Qin is relatively high, and the specifications of the produced tablets are generally larger (if the tablets are small, the number of tablets that the patient needs to take will be greatly increased). The impact is relatively large (especially when passing through the pylorus), so it is easy to cause large individual differences and affect the curative effect

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