Breviscapine-phosphotide compound and its preparing process

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...

Examples

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.

[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...

Examples

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.