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Ligustrazine phosphate compound and medicine composition containing the ligustrazine compound and gingko leaf effective ingredient

A technology of ligustrazine phosphate and compounds, applied in the field of medicine, can solve problems such as stability, solubility difference, small binding strength, difference in clinical drug effect, etc., to ease the blood drug concentration curve, improve bioavailability, bioavailability high effect

Active Publication Date: 2014-06-04
弘和制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Compounds with different crystal structures are in different energy states due to the difference in molecular arrangement order. Generally, amorphous drugs have greater potential energy, and the bonding strength between particles is smaller than that of crystal forms. The total unit surface free The energy is large, and the surface between the particles is easy to hydrate, resulting in a difference in solubility from that of crystalline drugs
The molecules in the unit cell of different crystal forms are different in spatial configuration, conformation, and arrangement, resulting in significant differences in stability, solubility, etc., resulting in different stability of the preparation, resulting in different dissolution rates of the preparation in the body, directly Affect the absorption, distribution, excretion and metabolism of preparations in the body, and ultimately lead to differences in clinical efficacy due to differences in bioavailability

Method used

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  • Ligustrazine phosphate compound and medicine composition containing the ligustrazine compound and gingko leaf effective ingredient
  • Ligustrazine phosphate compound and medicine composition containing the ligustrazine compound and gingko leaf effective ingredient
  • Ligustrazine phosphate compound and medicine composition containing the ligustrazine compound and gingko leaf effective ingredient

Examples

Experimental program
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Effect test

Embodiment 1

[0039] Embodiment 1, the preparation of ligustrazine phosphate compound

[0040] 1) Take 100g of ligustrazine phosphate monohydrate raw material at room temperature, add 300ml of a mixed solvent of ethanol and tetrahydrofuran (the volume ratio of ethanol to tetrahydrofuran is 3:1), stir and dissolve, and obtain the ethanol / tetrahydrofuran solution of ligustrazine phosphate;

[0041] 2) Add 0.01% w / v activated carbon to the ethanol / tetrahydrofuran solution of ligustrazine phosphate obtained in step 1), stir and adsorb for 15 minutes, filter, collect the filtrate, and set aside;

[0042] 3) Add chloroform to the filtrate dropwise under an ultrasonic field with a frequency of 18KHz until crystallization occurs;

[0043] 4) Turn off the ultrasonic field, lower the temperature to 0° C., and stand at this temperature for 6 hours; filter, wash the filter cake with chloroform, and dry it in vacuum for 2 hours to obtain the ligustrazine phosphate compound.

[0044] The X-ray powder di...

Embodiment 2

[0045] Embodiment 2, the preparation of ligustrazine phosphate compound

[0046] 1) Take 100g of ligustrazine phosphate monohydrate raw material at room temperature, add 1000ml of a mixed solvent of ethanol and tetrahydrofuran (the volume ratio of ethanol to tetrahydrofuran is 8:1), stir and dissolve, and obtain the ethanol / tetrahydrofuran solution of ligustrazine phosphate;

[0047] 2) Add 0.01% w / v activated carbon to the ethanol / tetrahydrofuran solution of ligustrazine phosphate obtained in step 1), stir and adsorb for 15 minutes, filter, collect the filtrate, and set aside;

[0048] 3) Add chloroform to the filtrate dropwise under an ultrasonic field with a frequency of 20KHz until crystallization occurs;

[0049] 4) Turn off the ultrasonic field, lower the temperature to 5° C., and stand at this temperature for 2 hours; filter, wash the filter cake with chloroform, and dry it in vacuum for 2 hours to obtain the ligustrazine phosphate compound.

[0050] The X-ray powder d...

Embodiment 3

[0051] Embodiment 3, the preparation of ligustrazine phosphate compound

[0052] 1) Take 100g of ligustrazine phosphate monohydrate raw material at room temperature, add 700ml of a mixed solvent of ethanol and tetrahydrofuran (the volume ratio of ethanol to tetrahydrofuran is 5:1), stir and dissolve, and obtain an ethanol / tetrahydrofuran solution of ligustrazine phosphate;

[0053] 2) Add 0.01% w / v activated carbon to the ethanol / tetrahydrofuran solution of ligustrazine phosphate obtained in step 1), stir and adsorb for 15 minutes, filter, collect the filtrate, and set aside;

[0054] 3) Add chloroform to the filtrate dropwise under an ultrasonic field with a frequency of 23KHz until crystallization occurs;

[0055] 4) Turn off the ultrasonic field, lower the temperature to 3° C., and stand at this temperature for 4 hours; filter, wash the filter cake with chloroform, and dry it in vacuum for 4 hours to obtain the ligustrazine phosphate compound.

[0056] The X-ray powder dif...

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Abstract

The invention belongs to the technical field of medicine, and specifically relates to a ligustrazine phosphate compound and a medicine composition containing the ligustrazine compound and gingko leaf effective ingredient. The chemical structure formula of the ligustrazine phosphate compound is shown in the formula (I), the X-ray powder diffraction spectrogram (shown in the figure 1) of the compound is measured by using the Cu-Kalpha ray. The medicine composition contains the ligustrazine phosphate compound and the gingko leaf effective ingredient, the gingko leaf effective ingredient is gingko biloba extract extracted from the gingko leaf, wherein the weight of the contained ligustrazine phosphate compound is 1-100 times the weight of the gingko biloba extract, preferably 5-50 times, and more preferably 5-20 times, and most preferably 10 times, the weight of the gingko biloba extract is counted according to total flavone of the gingko. The ligustrazine phosphate compound provided by the invention is a new crystal form compound different from the crystal form in the prior art, and the new crystal form compound has obviously improved stability.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a ligustrazine phosphate compound and a pharmaceutical composition containing the ligustrazine compound and ginkgo biloba active ingredients. Background technique [0002] Ginkgo biloba extract contains active ingredients such as total flavonoids and total lactones, and total flavonoids are the main active ingredients of Ginkgo biloba extract. The content of total flavonoids in Ginkgo biloba leaves is 0.5% to 1% (W / W), mainly in the form of glycosides, and the main aglycones are quercetin, kaempferol and isorhamnetin. Ginkgo biloba total flavonoids contained in Ginkgo biloba extract can expand coronary vessels, cerebral blood vessels, promote blood circulation and remove blood stasis, and improve symptoms and memory functions caused by cerebral ischemia. Ginkgo biloba extract can improve cerebral circulation, glucose metabolism and respiration in patients with cereb...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D241/12A61K31/4965A61P7/02A61P9/10
CPCA61K31/4965A61K36/16C07D241/12A61K2300/00
Inventor 郑建勇苏大明田慧
Owner 弘和制药有限公司