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Breviscapine-phosphotide compound and its preparing process

A technology of breviscapine phospholipids and breviscapine, applied in the field of medicine, can solve the problems of poor stability of breviscapine

Inactive Publication Date: 2002-07-24
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For injection, in order to obtain the effective concentration, the pH of the solution needs to be adjusted to 6.3-8.3. Our research shows that the greater the pH value, the worse the stability of scutellarin. In order to improve the stability, there is a patent (publication number: CN 1187356 The Stable Prescription and Process of Breviscapine Injection) Antioxidants such as sodium bisulfite were added to the prescription of the injection, or it was made into freeze-dried powder (publication number: CN1133180 Freeze-dried Breviscapine for Injection preparation and preparation process; publication number: CN1095934 breviscapine powder injection and preparation method), however, the preparation of complexes by using phospholipids, and controlling the pH value below 7.5 to ensure the stability of scutellarin has not been reported

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0004] Example 1: Weigh 2 g of scutellarin, place it in 300 ml of absolute ethanol, and heat to reflux. After the scutellarin is completely dissolved, add 4 g of hydrogenated soybean lecithin, and continue to heat and reflux. After the hydrogenated soybean lecithin is completely dissolved, Heating was stopped, and the resulting solution was left at room temperature for 24 hours, and the precipitate was collected by filtration and washed with ethanol. The precipitate was vacuum-dried at 40°C to obtain a light yellow-white complex. Take this compound, breviscapine, and the physical mixture of breviscapine and hydrogenated soybean lecithin for infrared (IR) analysis, and the result is "P=O" in the spectrum of "physical mixture of breviscapine and hydrogenated soybean lecithin" The peak of the group (at 1240cm -1 ), while the "complex" at 1240cm -1 The peak disappears, proving the formation of "breviscapine phospholipid complex".

Embodiment 2

[0005] Example 2: Weigh 2g of scutellarin, put it in 300ml of absolute ethanol, and heat to reflux. After the scutellarin is completely dissolved, add 3g of soybean lecithin and continue to heat and reflux. After the soybean lecithin is completely dissolved, stop heating , The resulting solution was left at room temperature for 24 hours, and the precipitate was collected by filtration and washed with ethanol. The precipitate was vacuum-dried at 40°C to obtain a pale yellow complex.

Embodiment 3

[0006] Example 3: Weigh 2 g of scutellarin, place it in 300 ml of tetrahydrofuran, and heat to reflux. After the scutellarin is completely dissolved, add 5 g of egg yolk lecithin, and continue to heat and reflux. After the egg yolk lecithin is completely dissolved, stop heating, and the obtained The solution was subjected to reduced pressure to recover tetrahydrofuran to obtain a light yellow semi-solid, which was washed with ethanol and vacuum-dried at 40°C to obtain a light yellow compound.

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PUM

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Abstract

A breviscapine-phosphotide composition in the form of oral preparation or injection is prepared from breviscapine and soybean (or egg yolk, or synthetic) lecithine in a wt ratio of 1:(0.5-50) through heating, reflux, washing and drying. Its advantages are high stability and durability, and quickly taking its curative effect.

Description

[0001] Technical field: the present invention relates to the technical field of medicine, specifically it is a breviscapine phospholipid complex and a preparation method thereof. Background technique: [0002] Breviscapine is an active ingredient of flavonoids separated and extracted from the plant Erigeron breviscapus, mainly scutellarin. Breviscapine can expand cerebral blood vessels, reduce cerebral vascular resistance, increase cerebral blood flow, improve microcirculation, and have the effect of resisting platelet aggregation. Clinically used for the treatment of cerebral thrombosis, cerebral infarction, cardiovascular disease, acute viral myocarditis in children, hyperviscosity, vertigo, thrombophlebitis, retinal vein occlusion, chronic asthmatic bronchitis, acute initial renal failure , adjuvant treatment of diabetes, etc. Because the molecular structure of breviscapine contains carboxyl groups, it is insoluble in weak acid (duodenum and small intestine) to strong acid...

Claims

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Application Information

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IPC IPC(8): A61K31/662A61P9/10
Inventor 邓意辉
Owner SHENYANG PHARMA UNIVERSITY
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