A kind of indobufen solid preparation and preparation method thereof

Abstract

The invention discloses a solid preparation of indobufen and a preparation method thereof. The solid preparation comprises an indobufen compound and pharmaceutical auxiliary materials. The compound is composed of indobufen and cellulose ether at a mass ratio of 1:0.1- 1 It is formed under the action of an alkali catalyst; the preparation method is: under the action of an alkali catalyst, indobufen and cellulose ether are combined through chemical bonds to form a complex, and then the corresponding solid preparation is prepared by adding pharmaceutical excipients. The clinical value of the product is greatly improved through a simple, feasible and low-cost process. It solves a series of problems such as high difficulty in the implementation of the product preparation process, low product qualification rate, unstable clinical bioavailability, and inaccurate curative effect with individual differences in patients, and reduces the occurrence of clinical bleeding events and gastrointestinal problems.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an indobufen solid preparation and a preparation method. Background technique [0002] Indobufen, English name: Indobufen, chemical name: (±) 2-[4-(1-oxo-2-isoindolinyl)phenylbutanoic acid, CAS: 63610-08-2, molecular formula :C 18 h 17 NO 3 , molecular weight: 295.34, its chemical structural formula is: [0003] [0004] The drug is an anticoagulant drug developed by Farmitalia Carlo Erba Pharmacia (Pharmacia, now Pfizer). It was first launched in Italy in 1984, and then successively launched in other countries (Philippines, Portugal, Venezuela, Thailand, etc.) ; It is an antiplatelet drug that reversibly inhibits platelet aggregation in vitro, reversibly inhibits platelet cyclooxygenase in vivo, reduces the generation of thromboxane A2 (TXA2), and then inhibits platelet aggregation. Years of clinical trial literature have proved that in preventing the risk of e...

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Problems solved by technology

[0006] At present, based on the incidence of thrombosis and intermittent claudication, indobufen is a drug worthy of promotion, but the clinical bioavailability of this product is unstable, and there are problems of unsatisfactory curative effect due to individual differences in patients. It is an oral solid preparation of indobufen. Due to the slow clearance rate in the body, it is easy to cause the accumulation of the drug in the body, which in turn causes bleeding complications and increases the risk of frequent gastrointestinal disturbances

[0007] In order to solve the above problems, patent CN 103800336 A and patent CN 103239444 A disclose adding antagonists such as ticagrelor and clopidogrel to indobufen preparations, which can improve the efficacy of the drug to a certain extent compared with taking indobufen alone. Curative effect, reduce bleeding events and side effects of gastrointestinal tract, but this invention only uses the therapeutic effect of another drug to alleviate the problem, this method treats the symptoms but not the root cause, and even increases the cost of medication and produces side effects of newly added drugs; Patent CN 103221070 A and patent CN 102625658 B disclose the use of pharmaceutical composition or preparation of nanoparticles, cyclodextrin encapsulation and other technologies to solve the existing bioavailability problem and reduce the toxic and side effects of the drug, but the above two The technology uses special excipients, the current commercial application is small, and the preparation process is complicated, the quality control is difficult, and the production equipment and personnel technical level of the producer are high.

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