Indobufen-containing pharmaceutical composition and preparation method thereof

Abstract

The invention relates to the technical field of pharmaceutical preparations, in particular to a pharmaceutical composition containing indobufen and a preparation method thereof.The pharmaceutical composition is prepared from, by weight, 50-200 parts of indobufen, 100 parts of polyethylene glycol, 20 parts of xylitol and 30-50 parts of pregelatinized starch. The tablet has the advantages of small dosage of auxiliary materials, low production cost, high taking compliance, good dissolution rate effect and suitability for large-scale production.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a pharmaceutical composition containing indobufen and a preparation method thereof. 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] Indobufen is an anti-coagulant drug developed by Farmitalia Carlo Erba Pharmacia (Pharmacia, now Pfizer), which is an anti-platelet aggregation drug that reversibly inhibits platelet aggregation in vitro and reversible in vivo Inhibit platelet cyclooxygenase, reduce the generation of thromboxane A2 (TXA2), and then inhibit platelet aggregation. Years of clinical trial literature have proved that in preventing the risk of embolism, indobufen can significantly reduce platelet aggregation, reduce the incidence o...

AI Technical Summary

Problems solved by technology

[0005] The reference preparation of indobufen tablets listed on the CDE is trade name: Ibustrin, specification: 0.2g, manufacturer Pfizer Italia S.r.l, in order to achieve clinical effectiveness, a large number of excipients are added to the reference preparations on the market, and the used There are many kinds of excipients. Through the analysis of the listed preparations by the inventor, it is found that the excipients of the reference preparation are: lactose, microcrystalline cellulose, sodium carboxymethyl starch, magnesium lauryl sulfate and magnesium stearate, although the specifications are only 0.2g, but the weight of the tablet reaches about 520mg, which is relatively large, which poses a relatively big challenge for patients to take, especially for the elderly, the tablet is too heavy and difficult to take, and if the size is small, you need to take several tablets to achieve the clinical effect At present, there are many domestic generic drugs, but no improvement has been made to address this situation.

[0006] Chinese patent application CN105853364A discloses a solid preparation of indobufen and its preparation method. The solid preparation includes an indobufen compound and pharmaceutical excipients. The compound is composed of indobufen and cellulose ether at a mass ratio of 1 : 0.1-1 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 by chemical bonds to form a complex, and then the corresponding solid preparation is prepared by adding pharmaceutical excipients , this technology greatly improves the clinical value of the product through a simple, feasible and low-cost process, and solves the problem of high difficulty in the implementation of the product preparation process, low product qualification rate, unstable clinical bioavailability, and individual patient A series of problems with uncertain efficacy, reducing the occurrence of clinical bleeding events and gastrointestinal problems

Although the patent application has improved the bioavailability, no comparative study with the original preparation was found, nor did it improve the problem of large amount of preparation excipients and difficulty in taking it by patients

[0007] Chinese patent application CN107281149A discloses a pharmaceutical composition of indobufen and its quality control method, which significantly accelerates the dissolution rate of the drug in the body, especially under gastric acid conditions, but it has not been compared with the reference preparations already on the market research, and did not improve the above problems

Images