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Long-acting benserazide sustained release microsphere composition and preparation method thereof

A technology of slow-release microspheres and benserazide, which is applied in drug combinations, medical preparations of non-active ingredients, pharmaceutical formulations, etc., can solve problems with movement and memory, and there is no relevant literature report on the preparation of benserazide microspheres method, inconvenience and other problems, to achieve the effect of good redispersibility

Inactive Publication Date: 2012-06-20
XIN HUA HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, drugs that require long-term administration but have a short half-life in the body should be prepared as sustained-release or controlled-release dosage forms; for the treatment of some tumors, some drugs need to be targeted to the disease, such as embolization microsphere preparations that target tumor blood vessels etc.; for Parkinson's disease, symptomatic Parkinson's syndrome needs to be taken three times a day due to the existing oral preparations, but for this type of patients, it is very inconvenient because they have problems with their actions and memory. It is a very good thing for them to take one medicine for a week or even a month; we have developed a sustained-release levodopa formulation with long-term efficacy based on the problems of this medicine, but due to Benserazide is very easily metabolized by enzymes in the body, and requires the help of enzyme inhibitors to achieve the desired therapeutic effect
[0003] After searching the prior art literature, it is found that there is no relevant literature reporting the method for preparing microspheres of benserazide

Method used

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  • Long-acting benserazide sustained release microsphere composition and preparation method thereof
  • Long-acting benserazide sustained release microsphere composition and preparation method thereof
  • Long-acting benserazide sustained release microsphere composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] ①Preparation of benserazide solution

[0028] a) 100mg of benserazide was prepared into an aqueous solution with a concentration of 2.5% by weight;

[0029] ②Preparation of benserazide sustained-release microsphere composition

[0030] (a) The polylactic acid (PLA, molecular weight is 90,000-140,000) that takes by weighing 37.5mg is mixed with the organic solution that is 15% dichloromethane and weighs 0.5mL above-mentioned ① benserazide solution and mixes and Stir, vortex or sonicate for 1-5 minutes to form a uniform suspension, that is, a water-in-oil (W / O) emulsion; the theoretical percentage of benserazide prepared into sustained-release microspheres is 15%.

[0031] (b) adding the emulsion obtained in step (a) to 10 mL of an aqueous solution of 5% sodium chloride and 1% polyethylene glycol (the molecular weight of PVA is 146,000-186,000, alcoholysis degree 98-99%) with a weight percent concentration and Stir, vortex or sonicate for 0.1-5 minutes to form double em...

Embodiment 2

[0039] ①Preparation of benserazide solution

[0040] a) 100mg of benserazide was prepared into an aqueous solution with a concentration of 2.5% by weight;

[0041] ②Preparation of benserazide sustained-release microsphere composition

[0042] (a) 295mg of polylactic acid (PLA, molecular weight: 90,000-140,000) was weighed to prepare an organic solution of 15% dichloromethane by weight, and 0.2mL of the above-mentioned benserazide solution was mixed and stirred. Vortex or sonicate for 1-5 minutes to form a uniform suspension, that is, a water-in-oil (W / O) emulsion; the theoretical percentage of benserazide prepared into sustained-release microspheres is 1%.

[0043] (b) adding the emulsion obtained in step (a) to 10 mL of an aqueous solution of 5% sodium chloride and 1% polyethylene glycol (the molecular weight of PVA is 146,000-186,000, alcoholysis degree 98-99%) with a weight percent concentration and Stir, vortex or sonicate for 0.1-5 minutes to form double emulsion;

[0...

Embodiment 3

[0051] ①Preparation of benserazide solution

[0052] a) 100mg of benserazide was prepared into an aqueous solution with a concentration of 2.5% by weight;

[0053] ②Preparation of benserazide sustained-release microsphere composition

[0054] (a) 37.5 mg of polylactic-glycolic acid (PLGA, molecular weight 6000-500,000) was weighed to prepare an organic solution of 15% dichloromethane by weight and 0.5 mL of the above-mentioned ① benserazide solution Mix and stir, vortex or sonicate for 1-5 minutes to form a uniform suspension, that is, a water-in-oil (W / O) emulsion; the theoretical percentage of benserazide prepared into sustained-release microspheres is 35%.

[0055] (b) adding the emulsion obtained in step (a) to 10 mL of an aqueous solution of 5% sodium chloride and 1% polyethylene glycol (the molecular weight of PVA is 146,000-186,000, alcoholysis degree 98-99%) with a weight percent concentration and Stir, vortex or sonicate for 0.1-5 minutes to form double emulsion;

[...

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Abstract

The invention relates to a long-acting benserazide sustained release microsphere composition. The composition comprises the following components in percentage by weight: 40 to 99 percent of degradable hydrophobic polymer and 1 to 60 percent of benserazide. The invention also provides a preparation method for the long-acting benserazide sustained release microsphere composition. The composition overcomes the defects of the conventional single oral administration scheme, administration loss of people with the disease due to the requirements of frequent oral administration, and ineffective treatment. The invention provides the preparation method using one W / O / W. The particle diameter of the composition can be controlled according to different needs and the composition does not pollute environment; and influences on the treatment effect of the benserazide can be avoided. The particle diameter can be adjusted and controlled to be between 1 mu n and 500 mu n according to needs. The freeze-drying powder of the composition is white, delicate and loose, does not collapse and conglutinate and has good dispersibility. Compared with an oral preparation of the same dosage, the composition is obviously better than the oral preparation in effect.

Description

【Technical field】 [0001] The invention relates to a sustained-release microsphere composition, in particular to a long-acting benserazide sustained-release microsphere composition and a preparation method thereof. 【Background technique】 [0002] In the pharmaceutical industry, from drug discovery to clinical application, the last link is drug preparation. A considerable part of the drugs need long-term frequent administration to be cured; some of them need local administration due to the high toxicity of systemic administration. To achieve these goals, raw materials must be prepared into corresponding dosage forms. For example, drugs that require long-term administration but have a short half-life in the body should be prepared as sustained-release or controlled-release dosage forms; for the treatment of some tumors, some drugs need to be targeted to the disease, such as embolization microsphere preparations that target tumor blood vessels etc.; for Parkinson's disease, sy...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/16A61K47/34A61P25/16
Inventor 刘振国袁伟恩郑瑞媛杨新新陈伟
Owner XIN HUA HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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