Compound injection preparation for treating cardiovascular and cerebrovascular diseases and preparation method thereof

Abstract

The invention discloses a compound injection preparation for treating cardiovascular and cerebrovascular diseases and a preparation method thereof. The preparation method comprises the following steps of: taking alprostadil and edaravone as active pharmaceutical ingredients, and compounding the alprostadil and the edaravone according to a certain ratio to form a certain injection preparation. With the adoption of the compound injection preparation, heart vessels or brain vessels can be effectively dilated, the chronic arterial occlusive diseases, caused by thromboangiitis obliterans, diabetes and the like, can be effectively treated, and meanwhile, the pain generated in the conventional injection of an alprostadil preparation can be remarkably abated due to the adoption of the compound preparation of the alprostadil and the edaravone.

Description

technical field

[0001] The invention belongs to the technical field of medicine, and relates to a compound injection preparation with edaravone and alprostadil as main active pharmaceutical ingredients and a preparation method thereof. The compound preparation can effectively treat cardiovascular and cerebrovascular diseases. Background technique

[0002] Alprostadil has another name called prostaglandin E1 (prostaglandin E1, PGE1), and its chemical name is: 11a, 15 (S)-bishydroxyl-9-keto-13-antiprostenic acid, and its chemical structural formula is as follows:

[0003]

[0004] Alprostadil is an endogenous physiologically active substance with various physiological and pharmacological effects. It can expand blood vessels, inhibit platelet aggregation, thromboxane A2 generation, atherosclerotic lipid plaque formation and immune complexes, and can expand peripheral and coronary vessels, reduce gastric juice secretion, and stimulate small intestine and uterine peristalsis. ...

Examples

Embodiment 1

[0042] The preparation of embodiment 1 compound water injection

[0043] formula:

[0044]

[0045]

[0046] Preparation:

[0047] Take a certain amount of polyethylene glycol and dissolve it in water for injection, the final concentration is 400mg / ml (w / v). Add the prescribed amount of dextran and mix well. Get the alprostadil and edaravone of prescription quantity, be dissolved in above-mentioned solution, until completely dissolving; Add the sodium bisulfite of prescription quantity and stir to dissolve. The obtained solution was filtered with a 0.22 μm microporous membrane, and the filtrate was filled and sealed in ampoules.

Embodiment 2

[0048] The preparation of embodiment 2 compound fat emulsion (high content)

[0049] formula:

[0050]

[0051] Preparation:

[0052] Under the protection of nitrogen, take the prescribed amount of alprostadil and edaravone and put them into the prescribed amount of soybean oil, and stir at 70° C. to fully dissolve into a solution. Then add the prescribed amount of emulsifier and mix. After the dissolution is complete, add the prescribed amount of oleic acid and vitamin E. After mixing evenly, a mixed oil phase A is formed; 60ml of water for injection and the prescribed amount of glycerin are mixed at 70°C to form a water phase B. ;Under the protection of nitrogen, slowly add the water phase B to the oil phase A at 70°C for mixing, disperse at a high speed of 3000r / min, and stir mechanically for 60 minutes to make colostrum. Homogenize for 7 to 8 times under high temperature to obtain a uniform milky solution; filter the above milky solution, seal it with nitrogen gas, st...

Embodiment 3

[0053] The preparation of embodiment 3 compound fat emulsion (in content)

[0054] formula:

[0055]

[0056] Preparation method: with the preparation method of Example 2.

technical field

[0001] The invention belongs to the technical field of medicine, and relates to a compound injection preparation with edaravone and alprostadil as main active pharmaceutical ingredients and a preparation method thereof. The compound preparation can effectively treat cardiovascular and cerebrovascular diseases. Background technique

[0002] Alprostadil has another name called prostaglandin E1 (prostaglandin E1, PGE1), and its chemical name is: 11a, 15 (S)-bishydroxyl-9-keto-13-antiprostenic acid, and its chemical structural formula is as follows:

[0003]

[0004] Alprostadil is an endogenous physiologically active substance with various physiological and pharmacological effects. It can expand blood vessels, inhibit platelet aggregation, thromboxane A2 generation, atherosclerotic lipid plaque formation and immune complexes, and can expand peripheral and coronary vessels, reduce gastric juice secretion, and stimulate small intestine and uterine peristalsis. ...

Examples

Embodiment 1

[0042] The preparation of embodiment 1 compound water injection

[0043] formula:

[0044]

[0045]

[0046] Preparation:

[0047] Take a certain amount of polyethylene glycol and dissolve it in water for injection, the final concentration is 400mg / ml (w / v). Add the prescribed amount of dextran and mix well. Get the alprostadil and edaravone of prescription quantity, be dissolved in above-mentioned solution, until completely dissolving; Add the sodium bisulfite of prescription quantity and stir to dissolve. The obtained solution was filtered with a 0.22 μm microporous membrane, and the filtrate was filled and sealed in ampoules.

Embodiment 2

[0048] The preparation of embodiment 2 compound fat emulsion (high content)

[0049] formula:

[0050]

[0051] Preparation:

[0052] Under the protection of nitrogen, take the prescribed amount of alprostadil and edaravone and put them into the prescribed amount of soybean oil, and stir at 70° C. to fully dissolve into a solution. Then add the prescribed amount of emulsifier and mix. After the dissolution is complete, add the prescribed amount of oleic acid and vitamin E. After mixing evenly, a mixed oil phase A is formed; 60ml of water for injection and the prescribed amount of glycerin are mixed at 70°C to form a water phase B. ;Under the protection of nitrogen, slowly add the water phase B to the oil phase A at 70°C for mixing, disperse at a high speed of 3000r / min, and stir mechanically for 60 minutes to make colostrum. Homogenize for 7 to 8 times under high temperature to obtain a uniform milky solution; filter the above milky solution, seal it with nitrogen gas, st...

Embodiment 3

[0053] The preparation of embodiment 3 compound fat emulsion (in content)

[0054] formula:

[0055]

[0056] Preparation method: with the preparation method of Example 2.

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