Medicine composition comprising butylphthalide and cosolvent

Abstract

The invention relates to the field of medicine, particularly to a medicine composition comprising butylphthalide and cosolvent, and aims to adopt a novel cosolvent to improve the water solubility of butylphthalide, develop clinically required solid, semisolid or liquid preparations of butylphthalide, and better exert the therapeutical effect of butylphthalide. The composition can be used for preparing a plurality of dosage forms such as tablets, capsules, ointment, cream, gel, transfusion, aqueous acupuncture, powder for injection, oral liquid and the like. Compared with the prior art, the medicine composition realizes better safety and improvement on the water solubility of butylphthalide.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a pharmaceutical composition containing butylphthalide and a cosolvent. Background technique [0002] Butylphthalide (3-n-butylphthalide, NBP for short), full name 3-butyl-1 (H)-isobenzofuranone, also known as apigenin A, is an active substance extracted from celery and its seeds. Components can also be artificially synthesized. Butylphthalide is a light yellow clear oily liquid with celery aroma and strong volatility. It is easily soluble in methanol, soluble in ethanol, ether and chloroform, but insoluble in water. Its molecule contains a chiral carbon atom, so it has two optical isomers, namely L-butylphthalide and D-butylphthalide, and its structural formula is as follows: [0003] [0004] Pharmacodynamic studies have shown that butylphthalide can increase cerebral blood flow in the ischemic area and improve microcirculation in the ischemic area, significantly reduce the infarct...

AI Technical Summary

Problems solved by technology

The soft capsules prepared are olive-shaped capsules No. 6-8, which are large in shape, and two capsules need to be taken orally at a time, and three times a day. The patient has difficulty swallowing, and the bioavailability is low. The gelatin in it is easy to age, resulting in slower disintegration, making it difficult to control the product quality during storage, and affecting the absorption and efficacy in the body

Chinese patent 200710062273.9 discloses a butylphthalide tablet and its preparation method, which uses cyclodextrin powder after inclusion of butylphthalide and common tablet excipients to prepare butylphthalide tablets, although this method is to a certain extent It solves the problem that the oily butylphthalide bulk drug is difficult to make oral solid preparations and the existing butylphthalide soft capsules have poor stability, but its drug loading is low, the preparation process is complicated, and the feasibility of practical application is poor

Chinese patent 201510905949.0 discloses a butylphthalide drug complex and its preparation method and sustained-release preparation. It adopts silica to absorb butylphthalide and coats it with a sustained-release coating to make a sustained-release preparation. Although this method reduces Butylphthalide is taken daily, but it does not solve the problem of poor water solubility and difficulty in absorption and utilization in the body

Chinese patent CN200510102355.2 discloses the prescription and preparation method of butylphthalide intravenous emulsion, which can solve the insoluble problem of butylphthalide in water, but the emulsifier soybean lecithin is used in the prescription, and soybean lecithin is easily oxidized into lysophospholipid. There are serious potential safety hazards; and the preparation process of the emulsion is relatively complicated, and it is difficult to control the product quality in industry

Chinese patent CN200410012533.8 discloses a freeze-dried powder injection of butylphthalide, which can also solve the insoluble problem of butylphthalide in water, but a large amount of emulsifiers and co-emulsifiers need to be used in the prescription, and the composition of the prescription and the preparation process are uniform. It is more complicated, and there is also the problem that the quality of industrial products is difficult to control

Chinese patent CN200410075068.2 discloses a butylphthalide self-emulsifying drug delivery system, which can also solve the problem of butylphthalide being insoluble in water, but the self-emulsifying drug delivery system needs to be in the gastrointestinal tract or at a body temperature of 37°C and under gentle stirring The oil-in-water emulsion can be formed spontaneously, and the individual variation of patients after medication is large, so it is difficult to ensure the consistency or constant of the curative effect in the body

Chinese patent CN200610081440.X discloses a concentrated solution of butylphthalide for injection. In the prescription, a non-aqueous solvent, a solubilizer and a cosolvent must be used at the same time to solve the problem of water insolubility of butylphthalide. Big security risk

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