Butylphthalide hard capsule, and preparation method thereof

Abstract

The invention discloses a butylphthalide hard capsule. The butylphthalide hard capsule comprises an oily content, and a hard capsule shell used for coating the oily content; the oily content comprises, by weight, 15 to 40% of butylphenyl phthaleine and 60 to 85% of an oleaginous base. The hard capsule shell is composed of a capsule body and a capsule cover connected through sleeving, and an annular sealing membrane.

Description

technical field [0001] The invention relates to a preparation of butylphthalide for treating cerebral ischemia and a preparation method thereof, in particular to a butylphthalide hard capsule and a preparation method thereof. Background technique [0002] Butylphthalide is a drug for treating cerebral ischemic diseases. It is the main active ingredient in celery and its seeds, and has a strong and special smell. Butylphthalide can block multiple pathological links of brain damage caused by ischemic stroke, has a strong anti-ischemic effect, significantly improves the microcirculation and blood flow in the ischemic brain area, and increases the capillary blood flow in the ischemic area. Quantity; reduce cerebral edema, reduce the infarct size of regional cerebral ischemia in rats; improve brain energy metabolism and microcirculation and blood flow in ischemic brain areas, inhibit nerve cell apoptosis, and have anti-thrombotic and anti-platelet aggregation effects . This pro...

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Problems solved by technology

However, the above-mentioned pharmaceutical problems of soft capsules are difficult to solve, which restricts the clinical application of butylphthalide, making more drug developers focus on the development of other oral solid dosage forms

In 2013, the invention patent 201310709855.7 applied by CSPC NBP Pharmaceutical Co., Ltd. uses gelatin capsules or hypromellose capsules to prepare butylphthalide liquid hard capsules. For gelatin hard capsules, the gelatin material has not changed. The problem that gelatin is easy to cause cross-linking has not been solved, and there is a certain amount of aldehyde impurities in the current process of butylphthalide before the ring closure, which can cross-link with gelatin. Butylphthalide itself is an oily liquid, and its The nature of high fluidity increases the degree of crosslinking again, therefore, compared with soft gelatin capsules made of gelatin hard capsules, there is no significant improvement in disintegration and related substance levels during placement; for hypromellose hard capsules As far as capsules are concerned, the gas permeability of this material is significantly better than that of gelatin capsules, which leads to the easy oxidation of the drug and the increase of related substances during the placement process. Therefore, butylphthalide and other easily oxidizable drugs are not suitable for making hypromellone Cellulose Hard Capsules

[0005] In addition, in the above-mentioned prior art, the technology of butylphthalide hard capsules does not consider sealing, but the hard capsules made of liquid drugs are prone to liquid leakage, and the stability is poor due to the high air flow and permeability of the hard capsules, and the increase of related substances Therefore, it is necessary to adopt sealing technology to make up for the shortage of ordinary hard capsules for containing liquid medicines

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