Alprostadil injection preparation

Abstract

The invention belongs to the technical field of medicines and discloses an injection preparation prepared from alprostadil serving as a raw material. The injection preparation is characterized by comprising the following components in part by weight: 0.01 part of alprostadil, 200 parts of soybean oil, 36 parts of phospholipid, 50 parts of glycerin and 4.8 parts of oleic acid. Through a preferabletest of a preparation process, the preparation process of adjusting the pH value of foremilk to be between 5.4 and 6.0 and treating the foremilk by using a nanomachine for 5 times under the pressure of 50MPa so as to prepare lipid microspheres with the average uniform particle size of between 100 and 280nm and performing flowing steam sterilization at the temperature of 121 DEG C for 15 minutes is determined. The preparation process has the advantages of high stability, small impurity quantity and the like.

Description

technical field

[0001] The invention belongs to the technical field of medicine, and in particular relates to an injection preparation whose raw material is alprostadil. Background technique

[0002] Alprostadil (PGE1) is a biologically active substance widely present in the body. Alprostadil has various physiological effects such as dilating blood vessels, inhibiting platelet aggregation, inhibiting the formation of thromboxane A2, and protecting vascular endothelial cells. It can specifically act on In the ischemic area, the blood vessels narrowed after the lesion can be obviously expanded, and the hypoxia condition of the brain tissue can be improved. Literature reports have confirmed that the combination of PGE1 injection for intravenous injection with lipid microspheres as the drug carrier and nimodipine can effectively prevent the occurrence of subarachnoid hemorrhage cerebral vasospasm, and no cerebral vasospasm occurred in the PGE1 group, suggesting that PGE1 can be...

Examples

Embodiment 1

[0054] An alprostadil injection preparation is characterized in that in the injection, 0.01 g of alprostadil, 200 g of soybean oil, 36 g of phospholipids, 50 g of glycerin, and 4.8 g of oleic acid.

[0055] (1) Take glycerin, add water for injection, make it dissolve, make glycerin aqueous solution, keep the temperature: 40-50 ℃, use it as the water phase, and set aside;

[0056] (2) Weigh oleic acid, add activated carbon for needles according to 1% of the mass, stir at 60°C for 30min, filter, and set aside;

[0057] (3) Mix phospholipids with soybean oil, stir to dissolve, mix evenly, and keep the temperature: 40-50°C as the oil phase;

[0058] (4) Oleic acid and alprostadil are added to the oil phase, stirred, mixed evenly, and set aside;

[0059] (5) (1) and (4) are mixed, and the homogenizer is sheared at high speed to form uniform colostrum;

[0060] (6) Adjusting the pH value of the obtained colostrum to 5.4-6.0, after mixing evenly, passing through a nanomachine at 50MP...

Embodiment 2

[0063] An alprostadil injection preparation is characterized in that in the injection, 0.01 g of alprostadil, 200 g of soybean oil, 36 g of phospholipids, 50 g of glycerin, and 4.8 g of oleic acid.

[0064] (1) Take glycerin, add water for injection, dissolve, and make 7.5% glycerin aqueous solution, as the water phase, for subsequent use;

[0065] (2) (1) and phospholipid are quickly sheared to uniform dispersion with a homogenizer;

[0066] (3) Weigh oleic acid, add activated carbon for needles according to 1% of the mass, stir at 60°C for 30min, filter, and set aside;

[0067] (4) get alprostadil, oleic acid and soybean oil and mix, stir and dissolve, mix homogeneously, as oil phase;

[0068] (5) (1) and (4) are mixed, and the homogenizer is sheared at high speed to form uniform colostrum;

[0069] (6) The obtained colostrum is adjusted to a pH value of 5.5, and after mixing evenly, it passes through a nanomachine at 50 MPa for 5 times to obtain lipid microspheres with a ...

Embodiment 3

[0072] An alprostadil injection preparation is characterized in that in the injection, 0.01 g of alprostadil, 200 g of soybean oil, 36 g of phospholipids, 50 g of glycerin, and 4.8 g of oleic acid.

[0073] (1) Take glycerin, add water for injection, dissolve, and make 7.5% glycerin aqueous solution, as the water phase, for subsequent use;

[0074] (2) (1) and phospholipid are quickly sheared to uniform dispersion with a homogenizer;

[0075] (3) Weigh oleic acid, add activated carbon for needles according to 1% of the mass, stir at 60°C for 30min, filter, and set aside;

[0076] (4) get alprostadil, oleic acid and soybean oil and mix, stir and dissolve, mix homogeneously, as oil phase;

[0077] (5) (1) and (4) are mixed, and the homogenizer is sheared at high speed to form uniform colostrum;

[0078] (6) Adjust the pH value of the obtained colostrum to 5.50, after mixing evenly, pass through a nanomachine at 50MPa for 5 times to obtain lipid microspheres with a uniform part...

technical field

[0001] The invention belongs to the technical field of medicine, and in particular relates to an injection preparation whose raw material is alprostadil. Background technique

[0002] Alprostadil (PGE1) is a biologically active substance widely present in the body. Alprostadil has various physiological effects such as dilating blood vessels, inhibiting platelet aggregation, inhibiting the formation of thromboxane A2, and protecting vascular endothelial cells. It can specifically act on In the ischemic area, the blood vessels narrowed after the lesion can be obviously expanded, and the hypoxia condition of the brain tissue can be improved. Literature reports have confirmed that the combination of PGE1 injection for intravenous injection with lipid microspheres as the drug carrier and nimodipine can effectively prevent the occurrence of subarachnoid hemorrhage cerebral vasospasm, and no cerebral vasospasm occurred in the PGE1 group, suggesting that PGE1 can be...

Examples

Embodiment 1

[0054] An alprostadil injection preparation is characterized in that in the injection, 0.01 g of alprostadil, 200 g of soybean oil, 36 g of phospholipids, 50 g of glycerin, and 4.8 g of oleic acid.

[0055] (1) Take glycerin, add water for injection, make it dissolve, make glycerin aqueous solution, keep the temperature: 40-50 ℃, use it as the water phase, and set aside;

[0056] (2) Weigh oleic acid, add activated carbon for needles according to 1% of the mass, stir at 60°C for 30min, filter, and set aside;

[0057] (3) Mix phospholipids with soybean oil, stir to dissolve, mix evenly, and keep the temperature: 40-50°C as the oil phase;

[0058] (4) Oleic acid and alprostadil are added to the oil phase, stirred, mixed evenly, and set aside;

[0059] (5) (1) and (4) are mixed, and the homogenizer is sheared at high speed to form uniform colostrum;

[0060] (6) Adjusting the pH value of the obtained colostrum to 5.4-6.0, after mixing evenly, passing through a nanomachine at 50MP...

Embodiment 2

[0063] An alprostadil injection preparation is characterized in that in the injection, 0.01 g of alprostadil, 200 g of soybean oil, 36 g of phospholipids, 50 g of glycerin, and 4.8 g of oleic acid.

[0064] (1) Take glycerin, add water for injection, dissolve, and make 7.5% glycerin aqueous solution, as the water phase, for subsequent use;

[0065] (2) (1) and phospholipid are quickly sheared to uniform dispersion with a homogenizer;

[0066] (3) Weigh oleic acid, add activated carbon for needles according to 1% of the mass, stir at 60°C for 30min, filter, and set aside;

[0067] (4) get alprostadil, oleic acid and soybean oil and mix, stir and dissolve, mix homogeneously, as oil phase;

[0068] (5) (1) and (4) are mixed, and the homogenizer is sheared at high speed to form uniform colostrum;

[0069] (6) The obtained colostrum is adjusted to a pH value of 5.5, and after mixing evenly, it passes through a nanomachine at 50 MPa for 5 times to obtain lipid microspheres with a ...

Embodiment 3

[0072] An alprostadil injection preparation is characterized in that in the injection, 0.01 g of alprostadil, 200 g of soybean oil, 36 g of phospholipids, 50 g of glycerin, and 4.8 g of oleic acid.

[0073] (1) Take glycerin, add water for injection, dissolve, and make 7.5% glycerin aqueous solution, as the water phase, for subsequent use;

[0074] (2) (1) and phospholipid are quickly sheared to uniform dispersion with a homogenizer;

[0075] (3) Weigh oleic acid, add activated carbon for needles according to 1% of the mass, stir at 60°C for 30min, filter, and set aside;

[0076] (4) get alprostadil, oleic acid and soybean oil and mix, stir and dissolve, mix homogeneously, as oil phase;

[0077] (5) (1) and (4) are mixed, and the homogenizer is sheared at high speed to form uniform colostrum;

[0078] (6) Adjust the pH value of the obtained colostrum to 5.50, after mixing evenly, pass through a nanomachine at 50MPa for 5 times to obtain lipid microspheres with a uniform part...

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