Pramipexole dihydrochloride sustained-release preparation and preparing method thereof

Abstract

The invention discloses a pramipexole dihydrochloride sustained-release preparation and a preparing method thereof, and belongs to the field of pharmaceutical preparations. The invention provides thepramipexole dihydrochloride sustained-release preparation which is prepared from the following raw and auxiliary materials by weight: 1-5 parts of pramipexole dihydrochloride, 35-140 parts of a sustained-release material, 130-400 parts of a skeleton material, 300-750 parts of a diluent, 10-20 parts of a flow aid, and 5-15 parts of a lubricant. The invention also provides the preparing method of the sustained-release preparation, wherein the preparing method includes the following steps: (1) taking pramipexole dihydrochloride, and crushing; (2) mixing the sustained-release material and pramipexole dihydrochloride evenly; (3) adding the skeleton material and the diluent, and mixing evenly; (4) making the mixture obtained in the step (3) into dry particles; (5) mixing the dry particles with the lubricant and the flow aid, to obtain an intermediate; and (6) tabletting. Under the specific ratio and granulating process, the sustained-release preparation has the advantages of uniform content,stable release and reliable quality, can be released evenly in various dissolving media with different pH, and is suitable for oral administration once a day.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a pramipexole hydrochloride sustained-release preparation and a preparation method thereof. Background technique [0002] Parkinson's disease (PD) is a common neurodegenerative disease. The main pathological change of Parkinson's disease is the degeneration and death of dopamine (DA) neurons in the substantia nigra of the midbrain, which leads to a significant decrease in the content of DA in the striatum and causes the disease. The exact cause of this pathological change is still unclear. Genetic factors, environmental factors, aging, oxidative stress, etc. may all be involved in the degeneration and death process of PD dopaminergic neurons. [0003] Pramipexole is a synthetic derivative of aminobenzothiazole. Pramipexole hydrochloride in the present invention refers to pramipexole dihydrochloride monohydrate, chemical name: monohydrate dihydrochloride (S)-2-amino-6-...

AI Technical Summary

Problems solved by technology

[0006] Most of the pramipexole hydrochloride sustained-release tablets currently on the market are three times a day, which brings great inconvenience to Parkinson's patients with limited mobility

Chinese patent CN104606162A discloses a sustained-release preparation of pramipexole hydrochloride. The release of the sustained-release tablet is still too fast, especially in the early stage, as high as 80% has been released in 12 hours, and the release is less than 20% from 12 hours to 24 hours. The release is not stable enough

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