Rasagiline mesylate microsphere preparation and preparation method thereof

Abstract

The invention discloses a rasagiline sustained-release microsphere preparation. The rasagiline sustained-release microsphere preparation contains rasagiline mesylate, a lactide-glycolide copolymer anda release regulator. The invention also discloses rasagiline mesylate microspheres prepared by adopting a multiple emulsion solvent evaporation method. A proper amount of release regulator is added into an inner water phase, so that the burst release amount of the drug-loaded microspheres can be remarkably reduced; the stability of the colostrum is improved, and the inter-batch difference causedby poor stability of the colostrum can be avoided; and the micromorphology of the drug-loaded microspheres is improved. The drug-loaded microspheres prepared by the improved method have high encapsulation efficiency and low burst release amount, and can realize uniform and slow release of drugs.

Description

technical field [0001] The invention relates to pharmaceutical preparations, in particular to rasagiline mesylate microspheres and a preparation method thereof. Background technique [0002] Parkinson's disease is a primary chronic progressive movement disorder that mostly affects the elderly. The prevalence of Parkinson's disease among people over 65 years old in my country is about 1.7%, and most Parkinson's patients are sporadic cases. The pathogenesis of Parkinson's is the lesion or necrosis of dopaminergic neurons in the central nigrostriatal pathway, resulting in a reduction or absence of dopamine in the striatum. The first symptom of Parkinson's disease is usually a tremor or clumsiness in one limb that then spreads to the other limb. The main clinical manifestations are bradykinesia, resting tremor, posture and gait disorder, and muscle rigidity. In severe cases, it is accompanied by mental impairment such as memory impairment and dementia, which seriously affects ...

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Problems solved by technology

For example, the drug tends to be distributed on the surface of the microspheres, resulting in a higher initial drug release, which increases the risk of side effects; the poor stability of the prepared colostrum will significantly increase the batch-to-batch variation in the microsphere preparation process, although the researchers Attempts to improve the stability of colostrum through various methods (such as adding surfactants, reducing the density difference between oil and water, etc.), but still have little effect

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