CN1424041A

CN1424041A - Kakonein preparations and their production

Info

Publication number: CN1424041A
Application number: CN 02155198
Authority: CN
Inventors: 苏娟; 张卫东; 吴伟
Original assignee: Second Military Medical University SMMU
Current assignee: Second Military Medical University SMMU
Priority date: 2002-12-19
Filing date: 2002-12-19
Publication date: 2003-06-18

Abstract

本发明是一种葛根素滴丸制剂及其制备方法。该滴丸制剂以葛根素为主要成份，与聚乙二醇、泊洛沙姆按一定工艺组配制成。本发明的滴丸制剂与其余剂相比，药物起效快、生物利用度高，制备工艺适合于工业化生产。The invention relates to a puerarin dripping pill preparation and a preparation method thereof. The dropping pill preparation takes puerarin as the main component, and is prepared according to a certain process group with polyethylene glycol and poloxamer. Compared with other preparations, the dropping pill preparation of the present invention has quick drug onset and high bioavailability, and the preparation process is suitable for industrialized production.

Description

Puerarin dropping pill formulation and preparation method thereof

Technical field

The invention belongs to medical technical field, being specifically related to a kind of is oral solid formulation of main component and preparation method thereof with puerarin (Puerarin), is a kind of puerarin dropping pill formulation and preparation method thereof specifically.

Background technology

Puerarin has pharmacological action comparatively widely; experimental results show that puerarin has dilating effect to coronary artery; can protect global ischemia cardiac muscle and myocardial ischemia reperfusion injury; reduce the acute myocardial infarction area; reduce myocardial oxygen consumption; prevent platelet adhesion, gathering and thrombosis, puerarin has significant protective effect to acute cerebral ischemia, and B-adrenergic receptor is had blocking effect.Clinically, puerarin is mainly used in the treatment of diseases such as coronary heart disease, angina pectoris, myocardial infarction, ischemic cerebrovascular, sudden deafness, retina artery and vein obstruction.

At present the preparation of puerarin is in the majority with injection clinically, for example puerarin glucose injection, puerarin sodium chloride injection etc., and injection exists the shortcoming of patient's medication inconvenience when curative effect can be affirmed.At present the solid preparation of puerarin has only tablet, because the dissolubility of puerarin is bad, and the performance that tablet exists as problems affect curative effects such as absorbing slowly, bioavailability is little, and coronary heart disease, angina pectoris belong to clinical acute disease, rapid onset needs first aid.

Summary of the invention

The object of the present invention is to provide a kind of drug effect is fast, bioavailability is high oral puerarin dropping pill formulation and preparation method.

The puerarin dropping pill formulation that the present invention proposes, be a kind of oral solid formulation, it is Main Ingredients and Appearance with the puerarin, with Polyethylene Glycol (requiring its molecular weight greater than 1500) and poloxamer is that the compatibility component is formulated, the weight proportion of each component is: 1 part of puerarin, Polyethylene Glycol 2.5-6.5 part, poloxamer 0.5-2.0 part.

The puerarin dropping pill formulation that the present invention proposes, its preferred component weight proportion is: 1 part of puerarin, Polyethylene Glycol 3-5 part, poloxamer 0.5-1 part.

The primary structure formula of Main Ingredients and Appearance puerarin of the present invention is a following formula I:

Formula I

The preparation method of the puerarin dropping pill formulation that the present invention proposes is as follows: by the weight proportion of each component Polyethylene Glycol, poloxamer are placed in the water-bath and heat, make it fusion; Add puerarin, stir, add anhydrous alcohol for medical use, stir hydrotropy; Continue to stir volatilization ethanol, 85～100 ℃ of heat preservation for standby use; Preheating DW-1 type drop pill machine, making fluid storage compartment constant temperature is fluid temperature, the coolant soybean oil is chilled to 10～12 ℃ in advance, drips system with 28～32 droplets/minute the speed of dripping; Collect drop pill at valve port, the filtering coolant, and absorb surperficial oil stain, and dry, promptly get the molding drop pill.

The puerarin dropping pill formulation that the present invention makes has the advantage that drug effect is fast, bioavailability is high, and its process conditions advanced person, is fit to the characteristics of industrial-scale production.The tablet of puerarin is just stripping 18% in 45 minutes in 0.3% sodium dodecyl sulfate solution, and the stripping in 15 minutes under identical leaching condition of puerarin drop pill is complete, can guarantee that thus the onset of puerarin drop pill is faster than tablet.

The specific embodiment

Further specifically describe the present invention below by embodiment.

Embodiment 1:

The weight proportion of puerarin drop pill each component is:

Puerarin 6.25g

Polyethylene Glycol (6000) 25.66g

Poloxamer (188) 5.50g

The method for preparing the puerarin drop pill is as follows:

Polyethylene glycol 6000 25.66g, poloxamer 1885.50g are placed in the water-bath and heat, make it fusion; Add the 6.25g puerarin, stir, add anhydrous alcohol for medical use 3.67ml, stir hydrotropy, continue to stir, volatilization ethanol, 95 ℃ of heat preservation for standby use; With the preheating of drop pill machine, fluid storage compartment constant temperature is 95 ℃ ± 2 ℃, and the coolant soybean oil is chilled to 10～12 ℃ in advance, regulates drip nozzle and the distance of cooling off liquid level, pours medicinal liquid into fluid storage compartment, starts valve, and medicinal liquid is dropwise splashed in the coolant, drips speed and is about 30 droplets/minute; Open and collect a mouthful valve, collect drop pill, gauze filtering coolant, and absorb surperficial remaining oil stain, and spread out, dry, promptly get the drop pill of molding.

Embodiment 2:

The weight proportion of puerarin drop pill each component is:

Puerarin 8.05g

Polyethylene Glycol (4000) 20.13g

Poloxamer (188) 16.10g

The method for preparing the puerarin drop pill is as follows:

Polyethylene Glycol (4000) 20.13g, poloxamer (188) 16.10g are placed in the water-bath and heat, make fusion; Add the 8.05g puerarin, stir, add anhydrous alcohol for medical use 4.57ml, stir hydrotropy, continue to stir, volatilization ethanol, 88 ℃ of heat preservation for standby use; With the preheating of drop pill machine, fluid storage compartment constant temperature is 90 ℃ ± 2 ℃, and the coolant soybean oil is chilled to 10～12 ℃ in advance, regulates drip nozzle and the distance of cooling off liquid level, pours medicinal liquid into fluid storage compartment, starts valve, and medicinal liquid is dropwise splashed in the coolant, drips speed and is about 28 droplets/minute; Open and collect a mouthful valve, collect drop pill, gauze filtering coolant, and absorb surperficial remaining oil stain, and spread out, dry, promptly get the drop pill of molding.

Embodiment 3:

The weight proportion of puerarin drop pill each component is:

Puerarin 4.35g

Polyethylene Glycol (1500) 26.10g

Poloxamer (188) 6.53g

The method for preparing the puerarin drop pill is as follows:

Polyethylene Glycol (1500) 26.10g, poloxamer (188) 6.53g are placed in the water-bath and heat, make fusion; Add the 4.35g puerarin, stir, add anhydrous alcohol for medical use 5.32ml, stir hydrotropy, continue to stir, volatilization ethanol, 98 ℃ of heat preservation for standby use; With the preheating of drop pill machine, fluid storage compartment constant temperature is 98 ℃ ± 2 ℃, and the coolant soybean oil is chilled to 10～12 ℃ in advance, regulates drip nozzle and the distance of cooling off liquid level, pours medicinal liquid into fluid storage compartment, starts valve, and medicinal liquid is dropwise splashed in the coolant, drips speed and is about 32 droplets/minute; Open and collect a mouthful valve, collect drop pill, gauze filtering coolant, and absorb surperficial remaining oil stain, and spread out, dry, promptly get the drop pill of molding.

Embodiment 4:

The weight proportion of puerarin drop pill each component is:

Puerarin 6.40g

Polyethylene Glycol (6000) 25.60g

Poloxamer (188) 12.8g

The method for preparing the puerarin drop pill is as follows:

Polyethylene Glycol (6000) 6.40g, poloxamer (188) 12.8g are placed in the water-bath and heat, make fusion; Add the 6.40g puerarin, stir, add anhydrous alcohol for medical use 7.08ml, stir hydrotropy, continue to stir, volatilization ethanol, 95 ℃ of heat preservation for standby use; With the preheating of drop pill machine, fluid storage compartment constant temperature is 95 ℃ ± 2 ℃, and the coolant soybean oil is chilled to 10～12 ℃ in advance, regulates drip nozzle and the distance of cooling off liquid level, pours medicinal liquid into fluid storage compartment, starts valve, and medicinal liquid is dropwise splashed in the coolant, drips speed and is about 30 droplets/minute; Open and collect a mouthful valve, collect drop pill, gauze filtering coolant, and absorb surperficial remaining oil stain, and spread out, dry, promptly get the drop pill of molding.

Claims

1. A puerarin dripping pill preparation is characterized in that taking puerarin as the main component, and polyethylene glycol and poloxamer with a molecular weight greater than 1500 are formulated as compatible components, and the weight ratio of each component is: : 1 part of puerarin, 2.5-6.5 parts of polyethylene glycol, 0.5-2.0 parts of poloxamer.

2. The puerarin dripping pill preparation described in Note 1 of the claim is characterized in that the weight ratio of each component is: 1 part of puerarin, 3 to 5 parts of polyethylene glycol, and 0.5 to 1 part of poloxamer. share.

3. A preparation method of puerarin dripping pills as claimed in claim 1, characterized in that the specific steps are as follows:

(1) According to the weight proportion of each component, heat polyethylene glycol and poloxamer on a water bath to melt them, add puerarin, stir evenly, add medicinal absolute ethanol, stir to aid dissolution, Stir continuously, volatilize ethanol, keep warm at 90-100°C for later use;

(2) Preheat the DW-1 type dripping pill machine, keep the temperature of the liquid storage room at the temperature of the liquid medicine, pre-cool soybean oil as the coolant to 10-12°C, and drip at a dropping speed of 28-32 drops/min;

(3) Collect the dripping pills at the valve port, filter out the coolant, absorb the oil stains on the surface, and dry them to obtain the shaped dripping pills.