Butylphthalide preparation and preparation method thereof

Abstract

The invention provides a butylphthalide preparation and a preparation method thereof. Specifically, the invention provides the butylphthalide preparation, and oleic acid is used as a solubilizing auxiliary material, so that the oral bioavailability of the butylphthalide preparation is improved, the individual difference is reduced, and the adverse reaction is reduced. The preparation has the advantages of being good in medicine stability, convenient to package, transport and store and the like, the preparation process is simple, and industrial production is easy.

Description

technical field

[0001] The invention relates to a butylphthalide preparation and a preparation method thereof, in particular to a butylphthalide oral preparation. Background technique

[0002] Butylphthalide is one of the main components of celery seed volatile oil. It is a domestic new drug of category 1.1. It is an anti-ischemic drug and is suitable for the treatment of mild and moderate acute ischemic stroke. Butylphthalide can increase cerebral perfusion, the number of capillaries, and cerebral blood flow in ischemic areas, improve energy metabolism in global cerebral ischemia, enhance protein synthesis, and protect neurons from various causes; it can also reduce cerebral edema, Protect mitochondrial function, increase antioxidant effect, thereby exert anti-apoptotic effect, and protect damaged brain cells.

[0003] The chemical name of butylphthalide is (±)-3-butyl-1(3H)-isobenzofuranone, and its structural formula is as shown in formula (I), which is light yellow or c...

Examples

Embodiment 1

[0035] Soft capsules with butylphthalide content of 100mg / capsule

[0036]

[0037] Preparation:

[0038] a. Capsule shell preparation: weigh 2kg of gelatin, 0.8kg of glycerin, and 2kg of water;

[0039] b. Glue: Stir and mix water and glycerin first, heat at 65°C, add gelatin, and keep stirring until it is completely dissolved, then keep vacuum to defoam until the bubbles completely disappear, and finally, place it in an insulated bucket at 55°C to keep warm.

[0040] c. Heat butylphthalide and oleic acid at 50°C to dissolve and stir evenly, and heat to 50°C before use.

[0041] d. Put the uniformly stirred capsule contents into the automatic soft capsule press machine, and press out soft capsules. The specific conditions are: the temperature of the content insulation barrel is 50°C, the air pressure is 0.5MPa, the heating temperature of the glue is 65°C, and the direct injection method is adopted. , spray washing temperature 44 ℃, rubber thickness 0.8mm.

Embodiment 2

[0043] Butylphthalide content 100mg / tablet

[0044]

[0045] Preparation:

[0046] a. Dibasic calcium phosphate and β-cyclodextrin are mixed uniformly to be a solid mixture;

[0047] b. Mix butylphthalide and oleic acid evenly to be a liquid mixture;

[0048] c. Add the liquid mixture of step b to the solid mixture of step a, stir, absorb the oil, and granulate;

[0049] d. Add Magnesium Stearate and total blend.

[0050] e. Tabletting to prepare a tablet with a butylphthalide content of 100 mg / tablet.

Embodiment 3

[0052] Soft capsules with butylphthalide content of 100mg / capsule

[0053]

[0054] The preparation method refers to Example 1.

technical field

[0001] The invention relates to a butylphthalide preparation and a preparation method thereof, in particular to a butylphthalide oral preparation. Background technique

[0002] Butylphthalide is one of the main components of celery seed volatile oil. It is a domestic new drug of category 1.1. It is an anti-ischemic drug and is suitable for the treatment of mild and moderate acute ischemic stroke. Butylphthalide can increase cerebral perfusion, the number of capillaries, and cerebral blood flow in ischemic areas, improve energy metabolism in global cerebral ischemia, enhance protein synthesis, and protect neurons from various causes; it can also reduce cerebral edema, Protect mitochondrial function, increase antioxidant effect, thereby exert anti-apoptotic effect, and protect damaged brain cells.

[0003] The chemical name of butylphthalide is (±)-3-butyl-1(3H)-isobenzofuranone, and its structural formula is as shown in formula (I), which is light yellow or c...

Examples

Embodiment 1

[0035] Soft capsules with butylphthalide content of 100mg / capsule

[0036]

[0037] Preparation:

[0038] a. Capsule shell preparation: weigh 2kg of gelatin, 0.8kg of glycerin, and 2kg of water;

[0039] b. Glue: Stir and mix water and glycerin first, heat at 65°C, add gelatin, and keep stirring until it is completely dissolved, then keep vacuum to defoam until the bubbles completely disappear, and finally, place it in an insulated bucket at 55°C to keep warm.

[0040] c. Heat butylphthalide and oleic acid at 50°C to dissolve and stir evenly, and heat to 50°C before use.

[0041] d. Put the uniformly stirred capsule contents into the automatic soft capsule press machine, and press out soft capsules. The specific conditions are: the temperature of the content insulation barrel is 50°C, the air pressure is 0.5MPa, the heating temperature of the glue is 65°C, and the direct injection method is adopted. , spray washing temperature 44 ℃, rubber thickness 0.8mm.

Embodiment 2

[0043] Butylphthalide content 100mg / tablet

[0044]

[0045] Preparation:

[0046] a. Dibasic calcium phosphate and β-cyclodextrin are mixed uniformly to be a solid mixture;

[0047] b. Mix butylphthalide and oleic acid evenly to be a liquid mixture;

[0048] c. Add the liquid mixture of step b to the solid mixture of step a, stir, absorb the oil, and granulate;

[0049] d. Add Magnesium Stearate and total blend.

[0050] e. Tabletting to prepare a tablet with a butylphthalide content of 100 mg / tablet.

Embodiment 3

[0052] Soft capsules with butylphthalide content of 100mg / capsule

[0053]

[0054] The preparation method refers to Example 1.

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