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

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...

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

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