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Medicinal composition for treating cardiovascular and cerebrovascular diseases and preparation method thereof

A technology for cardiovascular and cerebrovascular diseases and a composition, which is applied in the field of pharmaceutical preparations, can solve the problems of decreased absorption, poor water solubility of scutellarin, and poor bioavailability of scutellarin, and achieves high bioavailability, simple preparation method, good absorption effect

Inactive Publication Date: 2012-12-05
MACAU UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The poor bioavailability of scutellarin in the body is not only due to the poor water solubility of scutellarin, but more importantly, transport proteins in the small intestine such as human multidrug resistance-associated protein 2 (Multidrug resistance-associated protein 2, MRP2) and other efflux drugs lead to a decrease in its absorption, which greatly limits the clinical use and popularization of scutellarin preparations

Method used

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  • Medicinal composition for treating cardiovascular and cerebrovascular diseases and preparation method thereof
  • Medicinal composition for treating cardiovascular and cerebrovascular diseases and preparation method thereof
  • Medicinal composition for treating cardiovascular and cerebrovascular diseases and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] A pharmaceutical composition for treating cardiovascular and cerebrovascular diseases is prepared from the following components in percentage by weight: co-emulsifier 24%, emulsifier 47.7%, oil phase 28% and drug 0.3%.

[0042] The drug is scutellarin.

[0043] Described co-emulsifier is diethylene glycol monoethyl ether.

[0044] The emulsifier is a mixture of polyoxyethylene castor oil and caprylic capric macrogol glyceride (1:1 by weight).

[0045] The oil phase is a mixture (weight ratio: 1:1) of monolinoleic glyceride and coconut oil caprylic capric glyceride (Capmul MCM, purchased from Abitec, USA, the same below).

[0046] Preparation:

[0047] First, mix the co-emulsifier and emulsifier of diethylene glycol monoethyl ether, polyoxyethylene castor oil and caprylic capric acid macrogol glyceride evenly, then disperse scutellarin in it, and then slowly add Mix the oil phase of monolinoleic acid glyceride and coconut oil caprylic capric acid glyceride (Capmul MCM...

Embodiment 2

[0049] A pharmaceutical composition for treating cardiovascular and cerebrovascular diseases is prepared from the following components in weight percent: co-emulsifier 23.6%, emulsifier 46.3%, oil phase 30% and drug 0.1%.

[0050] The drug is scutellarin.

[0051] Described co-emulsifier is diethylene glycol monoethyl ether.

[0052] The emulsifier is a mixture of polyoxyethylene hydrogenated castor oil and caprylic capric macrogol glyceride (4:1 by weight).

[0053] The oil phase is a mixture of monolinoleic acid glyceride and coconut oil caprylic capric acid glyceride (Capmul MCM) (weight ratio is 2:1).

[0054] Preparation:

[0055] First disperse scutellarin in the oil phase of glyceryl monolinoleate and coconut oil caprylic capric acid glycerin (Capmul MCM) mixed uniformly, and then slowly add diethylene glycol monoethyl ether, polyoxyethylene The co-emulsifier and emulsifier of hydrogenated castor oil and caprylic capric acid macrogol glyceride are stirred at a consta...

Embodiment 3

[0057] A pharmaceutical composition for treating cardiovascular and cerebrovascular diseases is prepared from the following components in weight percentage: co-emulsifier 20%, emulsifier 49.9%, oil phase 30% and drug 0.1%.

[0058] The drug is scutellarin.

[0059] Described co-emulsifier is diethylene glycol monoethyl ether.

[0060] The emulsifier is a mixture of polyoxyethylene castor oil, polyoxyethylene hydrogenated castor oil and caprylic capric macrogol glyceride (weight ratio is 1:1:1).

[0061] The oil phase is glycerol monolinoleate.

[0062] Preparation:

[0063] First disperse scutellarin in glycerol monolinoleate, then slowly add diethylene glycol monoethyl ether, polyoxyethylene castor oil, polyoxyethylene hydrogenated castor oil and caprylic capric acid macrogol glycerin Co-emulsifier and emulsifier of ester, constant temperature magnetic stirring at 37°C to mix the components evenly, completely dissolve the drug, and obtain the scutellarin pharmaceutical com...

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Abstract

The invention relates to a medicinal composition for treating cardiovascular and cerebrovascular diseases and a preparation method thereof. The medicinal composition is prepared from the following components in percentage by weight: 0.1-0.3 percent of scutellarin, 20-25 percent of co-emulsifier, 40-50 percent of emulsifier and 25-30 percent of oil phase. The preparation method of the medicinal composition comprises the following steps of: (1) dispersing the scutellarin in the emulsifier and the co-emulsifier to obtain a mixture; (2) dispersing the mixture into the oil phase, magnetically stirring at a constant temperature of 25-37 DEG C to uniformly mix the components, and fully dissolving the medicament to obtain the medicinal composition of the scutellarin. According to the medicinal composition, the absorption and the bioavailability of the scutellarin are effectively improved by selecting and using a medicinal auxiliary material for inhibiting multi-drug resistance-associated protein 2 in a prescription; the preparation method is simple and convenient; and meanwhile, the medicinal composition can be applied to various oral dosage forms.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a pharmaceutical composition for treating cardiovascular and cerebrovascular diseases and a preparation method thereof. The pharmaceutical composition and preparation method of scutellarin. Background technique [0002] Erigeron breviscapus (Vant.) Hand Mazz is a total flavonoid component extracted from the dried whole herb of Compositae plant Erigeron breviscapus (Vant.) Hand Mazz. Scutellarin accounts for more than 90% of scutellarin, and its chemical name is 4,5,6-trihydroxyflavone-7-glucuronide. In recent years, scutellarin has been used to treat cardiovascular and cerebrovascular diseases. Studies have shown that it can protect neurons and prevent cytotoxicity, regulate vascular endothelial function, relieve cerebral vasospasm, improve microcirculation, reduce blood lipids, regulate immunity and reduce inflammation. Anti-free radical damage, inhibition of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61K47/34A61K47/44A61P9/00
CPCA61K31/7048A61P9/00
Inventor 易涛李良林伟基
Owner MACAU UNIV OF SCI & TECH
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