Benserazide sustained-release microspherical composition and preparation method thereof

A technology for sustained-release microspheres and compositions, which is applied in the directions of pharmaceutical combinations, pharmaceutical formulations, and medical preparations of inactive ingredients, etc., can solve the problems in the method, action and memory of microspheres prepared by benserazide, which are not reported in relevant literature. , inconvenience and other problems, to achieve the effect of good re-dispersibility, avoid the effect of the effect, and improve the therapeutic effect

Inactive Publication Date: 2012-01-18
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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  • Benserazide sustained-release microspherical composition and preparation method thereof
  • Benserazide sustained-release microspherical composition and preparation method thereof
  • Benserazide sustained-release microspherical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] ①Put 100mg of benserazide into 0.4-10μm with a microscope first, if not, pulverize it into 0.4-5μm with a pulverizer;

[0030] ② Preparation of benserazide sustained-release microsphere composition

[0031] (a) 37.5 mg of polylactic acid (PLA, with a molecular weight of 90,000-140,000) weighed into a dichloromethane organic solution with a concentration of 15% by weight and 12.5 mg of benserazide microparticles weighed in ① were mixed and stirred , vortex or ultrasonic for 1-5 minutes to form a uniform suspension, that is, a solid-in-oil (S / O) emulsion; the theoretical percentage content of benserazide to be prepared is 25% slow-release microspheres.

[0032] (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%) aqueous solution Stir, vortex or sonicate for 0.1-5 minutes to form a double emulsion;

[0033] (c) adding the d...

Embodiment 2

[0040] ①Preparation of benserazide microparticles

[0041] 100mg benserazide, first observe with a microscope whether it is 0.4-10μm, if not, it can be pulverized into 0.4-5μm with a pulverizer;

[0042] ② Preparation of benserazide sustained-release microsphere composition

[0043] (a) Weigh 495 mg of polyglycolic acid-polylactic acid (PLGA, d, l-lactide: 46-52% Mole and glycolide 48-54% Mole; molecular weight 5000-6000) to prepare a weight percent concentration of 30% The organic solution of dichloromethane and 5 mg of benserazide particles obtained by weighing ① are mixed and stirred, vortexed or ultrasonicated for 1-5 minutes to form a uniform suspension, that is, a solid-in-oil (S / O) emulsion; will be prepared as The theoretical percentage of benserazide is 1% slow-release microspheres.

[0044] (b) adding the emulsion obtained in step (a) to 10 mL of an aqueous solution of polyethylene glycol (the molecular weight of PVA is 146,000-186,000, the degree of alcoholysis 98...

Embodiment 3

[0052] ①Preparation of benserazide microparticles

[0053] 100mg benserazide, first observe with a microscope whether it is 0.4-10μm, if not, it can be pulverized into 0.4-5μm with a pulverizer;

[0054] ② Preparation of benserazide sustained-release microsphere composition

[0055] (a) 37.5 mg of polyglycolic acid-polylactic acid (PLGA, d, l-lactide: 46-52% Mole and glycolide 48-54% Mole; molecular weight 5000-6000) were weighed to prepare a weight percent concentration of 15 % organic solution of dichloromethane and 12.5 mg of benserazide microparticles obtained by weighing ① are mixed and stirred, vortexed or ultrasonicated for 1-5 minutes to form a uniform suspension, that is, a solid-in-oil (S / O) emulsion; The theoretical percentage content of prepared benserazide is 25% slow-release microspheres.

[0056] (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-...

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Abstract

The invention relates to a benserazide sustained-release microspherical composition, which comprises the following components by weight percent: 40%-99% of a degradable hydrophobic polymer and 1%-60% of benserazide. The invention also provides a preparation method of the benserazide sustained-release microspherical composition. The invention can overcome the instability of benserazide during the storage process and improve the pharmaceutical therapeutic effect on patients. The method for preparing the microspherical composition can avoid the defects of low entrapment rate of the conventional W / O and W / O / W, and environmental pollution of S / O / O caused by serious burst release. In the invention, the grain diameter of the microspherical composition prepared by the method can be controlled according to different demands without environmental pollution, and the influence on the therapeutic effect of benserazide can be prevented. The surfaces of the obtained granules are smooth and rounded, the granules are regular without adhesion, the grain diameter can be regulated and controlled from 1mum to 5mum as required, and freeze-drying powder of the granules is white, exquisite and loose, is not collapsed and adhered, and has good redispersibility.

Description

【Technical field】 [0001] The invention relates to a composition in the technical field of pharmaceutical preparations and a preparation method thereof, in particular to a benserazide sustained-release microsphere composition and a preparation method thereof. 【Background technique】 [0002] From drug discovery to clinical application in the pharmaceutical industry, the last link is drug preparation. A considerable number of these drugs require long-term and frequent administration to cure; some require topical administration due to the high toxicity of systemic administration. To achieve these goals, APIs 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 into 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 targeting tumor blood ves...

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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