A pharmaceutical composition comprising butylphthalide and borneol and applications thereof

Abstract

A pharmaceutical composition comprising butylphthalide and borneol is disclosed. The pharmaceutical composition has synergistic effects on treating cerebrovascular diseases especially ischemic cerebrovascular diseases, and is capable of obviously enhancing treating effects of the butylphthalide, reducing the effective dose of the butylphthalide, and reducing the using amount. Untoward effects of the pharmaceutical composition during long-term application can be reduced.

Description

technical field

[0001] The invention relates to a pharmaceutical composition containing butylphthalide and borneol and its application in the preparation of medicaments for treating cerebrovascular diseases. Background technique

[0002] Cerebrovascular disease (CVD) is a brain lesion caused by cerebrovascular abnormalities. Stroke generally refers to acute cerebrovascular disease. According to the survey data of 17 countries and regions by the World Health Organization, the incidence of cerebrovascular disease fluctuates between 15 and 287 / 100,000, and the regional distribution is different. The average incidence of cerebrovascular disease in my country is about 1.30 / 1.1 million, higher than that in Europe and the United States, and close to Japan. Data studies from all over the world show that the incidence of cerebrovascular disease increases with age. At present, China is facing the challenge of rapid aging. Cerebrovascular disease is the second major cause of serious ...

Examples

Embodiment 1

[0027] Embodiment 1: the preparation of injection medicine solution

[0028] (1) Preparation of 30% HP-β-CD

[0029] Take 600 g of HP-β-CD (hydroxypropyl-β-cyclodextrin), add 1200 mL of water for injection, stir to dissolve, and finally dilute to 2000 mL with water for injection, which is 30% HP-β-CD;

[0030] (2) Preparation of butylphthalide solution for injection

[0031] Weigh 4g each of s-butylphthalide and levo-butylphthalide respectively, then add 600mL 30% HP-β-CD respectively, stir until the solution is clear, and obtain it;

[0032] (3) Preparation of borneol solution for injection

[0033] Take 1 g of natural borneol, add 20mL of 95% ethanol, mix well, add 280mL of 30% HP-β-CD, stir until the solution is clear, and obtain;

[0034] (4) Preparation of butylphthalide + borneol solution for injection

[0035] Take the butylphthalide solution and borneol solution in a given ratio, mix them well, and get that, the mixing ratio is as follows:

[0036]

[0037] The ...

Embodiment 2

[0038] Embodiment 2: Preparation of oral medicinal liquid oil

[0039] (1) Preparation of Butylphthalide Liquid Oil

[0040] Respectively weigh 25g of butylphthalide and 25g of butylphthalide respectively, then add them into 225g of soybean oil respectively, and stir well to obtain the product;

[0041] (2) Preparation of borneol liquid oil

[0042] Take 10g of natural borneol, add it into 90g of soybean oil, stir and dissolve until the solution is clear, and you get it;

[0043] (3) Preparation of butylphthalide + borneol liquid oil

[0044] Take the butylphthalide medicinal liquid oil and borneol medicinal liquid oil in a given ratio, and mix them evenly to get the product. The mixing ratio is as follows:

[0045]

[0046] Above-mentioned medicinal liquid oil also can adopt conventional method as CN1623542A discloses the preparation method of soft capsule, is compressed into soft capsule.

Embodiment 3

[0047] Embodiment 3: Mouse global ischemia test (borneol dosage investigation)

[0048] 1 Animal experiment materials

[0049] 1.1 Drugs Test drugs: racemic butylphthalide (NBP) solution for injection prepared in Example 1, natural borneol solution for injection, racemic butylphthalide + natural borneol solution for injection, model control is 30% HP-β-CD .

[0050] 1.2 Animals SPF grade KM mice, male, 18-22 grams, provided by the Experimental Animal Center of Hebei Medical University; the experimental animal production license number is SCXK (Ji) 2008-1-003. Experimental animal use license number: SYXK (Ji) 2011-0059.

[0051] 1.3 Data processing The data were analyzed by variance analysis and intergroup test by SPSS11.5 statistical software.

[0052] 2 Mice global cerebral ischemia test

[0053] 2.1 Animal grouping and administration: 100 Kunming mice were randomly divided into 10 groups, namely the model control group (30% HP-β-CD), the NBP group (10 mg?kg -1 ), natu...

technical field

[0001] The invention relates to a pharmaceutical composition containing butylphthalide and borneol and its application in the preparation of medicaments for treating cerebrovascular diseases. Background technique

[0002] Cerebrovascular disease (CVD) is a brain lesion caused by cerebrovascular abnormalities. Stroke generally refers to acute cerebrovascular disease. According to the survey data of 17 countries and regions by the World Health Organization, the incidence of cerebrovascular disease fluctuates between 15 and 287 / 100,000, and the regional distribution is different. The average incidence of cerebrovascular disease in my country is about 1.30 / 1.1 million, higher than that in Europe and the United States, and close to Japan. Data studies from all over the world show that the incidence of cerebrovascular disease increases with age. At present, China is facing the challenge of rapid aging. Cerebrovascular disease is the second major cause of serious ...

Examples

Embodiment 1

[0027] Embodiment 1: the preparation of injection medicine solution

[0028] (1) Preparation of 30% HP-β-CD

[0029] Take 600 g of HP-β-CD (hydroxypropyl-β-cyclodextrin), add 1200 mL of water for injection, stir to dissolve, and finally dilute to 2000 mL with water for injection, which is 30% HP-β-CD;

[0030] (2) Preparation of butylphthalide solution for injection

[0031] Weigh 4g each of s-butylphthalide and levo-butylphthalide respectively, then add 600mL 30% HP-β-CD respectively, stir until the solution is clear, and obtain it;

[0032] (3) Preparation of borneol solution for injection

[0033] Take 1 g of natural borneol, add 20mL of 95% ethanol, mix well, add 280mL of 30% HP-β-CD, stir until the solution is clear, and obtain;

[0034] (4) Preparation of butylphthalide + borneol solution for injection

[0035] Take the butylphthalide solution and borneol solution in a given ratio, mix them well, and get that, the mixing ratio is as follows:

[0036]

[0037] The ...

Embodiment 2

[0038] Embodiment 2: Preparation of oral medicinal liquid oil

[0039] (1) Preparation of Butylphthalide Liquid Oil

[0040] Respectively weigh 25g of butylphthalide and 25g of butylphthalide respectively, then add them into 225g of soybean oil respectively, and stir well to obtain the product;

[0041] (2) Preparation of borneol liquid oil

[0042] Take 10g of natural borneol, add it into 90g of soybean oil, stir and dissolve until the solution is clear, and you get it;

[0043] (3) Preparation of butylphthalide + borneol liquid oil

[0044] Take the butylphthalide medicinal liquid oil and borneol medicinal liquid oil in a given ratio, and mix them evenly to get the product. The mixing ratio is as follows:

[0045]

[0046] Above-mentioned medicinal liquid oil also can adopt conventional method as CN1623542A discloses the preparation method of soft capsule, is compressed into soft capsule.

Embodiment 3

[0047] Embodiment 3: Mouse global ischemia test (borneol dosage investigation)

[0048] 1 Animal experiment materials

[0049] 1.1 Drugs Test drugs: racemic butylphthalide (NBP) solution for injection prepared in Example 1, natural borneol solution for injection, racemic butylphthalide + natural borneol solution for injection, model control is 30% HP-β-CD .

[0050] 1.2 Animals SPF grade KM mice, male, 18-22 grams, provided by the Experimental Animal Center of Hebei Medical University; the experimental animal production license number is SCXK (Ji) 2008-1-003. Experimental animal use license number: SYXK (Ji) 2011-0059.

[0051] 1.3 Data processing The data were analyzed by variance analysis and intergroup test by SPSS11.5 statistical software.

[0052] 2 Mice global cerebral ischemia test

[0053] 2.1 Animal grouping and administration: 100 Kunming mice were randomly divided into 10 groups, namely the model control group (30% HP-β-CD), the NBP group (10 mg?kg -1 ), natu...

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