Self-emulsifier containing breviscapine phosphatidylcholine complex, and preparation method and use thereof

Abstract

The invention discloses a self-emulsifier containing a breviscapine phosphatidylcholine complex, and a preparation method and a use thereof. The self-emulsifier comprises the following components, by mass, 0.1-16% of breviscapine, 0.1-32% of phosphatidylcholine, 20-70% of an oily phase, 10-50% of a surfactant, and 0-40% of a cosurfactant. An insoluble dug breviscapine is processed to prepare a breviscapine phosphatidylcholine complex, and the breviscapine phosphatidylcholine complex is treated as an intermediate carrier to prepare the self-emulsifier containing the breviscapine phosphatidylcholine complex. The breviscapine phosphatidylcholine complex can effectively solve a bad fat solubility problem of breviscapine and substantially improve the drug loading capability of the self-emulsifier; and the self-emulsifier can increase the dissolution rate of breviscapine, promote breviscapine to penetrate epithelial cells, promote the lymphatic transport of drugs to a certain degree, reduce the hepatic first pass metabolism of the drugs and improve the oral bioavailability of breviscapine. Oral administration tests of rats show that the self-emulsifier containing the breviscapine phosphatidylcholine complex can substantially improve the absorption of breviscapine and improve the oral bioavailability of breviscapine.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and relates to a self-emulsifying agent with scutellarin phospholipid complex as an intermediate carrier and its preparation method and application. The self-emulsifying agent can significantly improve the oral absorption of scutellarin and increase the oral bioavailability. Background technique [0002] Breviscapine is a flavonoid extracted from the plant Erigeron breviscapus of Compositae. The English name is Breviscapine or Erigeron Breviscapus. The main active ingredient is scutellarin (see the chemical structure figure 1 ), its content accounts for more than 95% of the total flavonoids. Breviscapine has significant curative effect on cardiovascular and cerebrovascular diseases such as cerebral infarction, obliterative arteriosclerosis and myocardial infarction. However, the oral absorption of breviscapine is very poor, and the absolute bioavailability of beagle dogs is only 0.4%. Accor...

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Problems solved by technology

However, the oral absorption of breviscapine is very poor, and the absolute bioavailability of beagle dogs is only 0.4%. According to the analysis of comprehensive literature reports, the possible reasons include poor water solubility, weak lipophilicity, easy to be absorbed by gastric acid, intestinal anaerobic bacteria, liver Drug degradation by enzymes, complex transformation in vivo, and drug efflux by membrane transporters, etc.

In addition, breviscapine needs to be administered in large doses for multiple times in clinical practice, and there are "peak and valley" fluctuations in blood drug concentration, and the curative effect is not stable enough

[0003] Chinese patent literature (CN1593449A) discloses "a kind of breviscapine self-emulsifying soft capsule and its preparation method", but, because scutellarin has poor fat solubility, the drug loading capacity of the self-emulsifying preparation is limited, therefore, the self-emulsifying preparation Unable to meet high dose administration, at the same time, its stability needs to be improved

However, the supersaturation-promoting substances play a role after the drug is dispersed, and the solubilization ability is limited, so it is difficult to fundamentally solve the problem of poor fat solubility of scutellarin

In addition, self-emulsifiers prepared by promoting supersaturation technology are likely to face the problem of drug re-precipitation after redispersion

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