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Pramipexole dihydrochloride slow-release tablet with high content uniformity and preparation method thereof

A technology for pramipexole hydrochloride and sustained-release tablets, which is applied in the field of pramipexole hydrochloride sustained-release tablets and its preparation, and can solve unqualified content uniformity and release standard deviation, increased research and development costs, and sample quality differences, etc. problems, to avoid incomplete drug release

Inactive Publication Date: 2012-12-26
SHANDONG QIDU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

On the one hand, the amount of sustained-release excipients required by the powder direct compression process to ensure 24-hour sustained release is higher than that of the wet granulation process, which increases research and development costs; on the other hand, the prescription ratio of pramipexole hydrochloride in sustained-release tablets is 0.1% ~1.5%, which is a low-dose and low-content drug, there is a risk of unqualified powder direct compression content uniformity and release standard deviation (RSD), which may vary due to batch-to-batch differences in the particle size, fluidity, and bulk density physical properties of raw materials and excipients. Resulting in variance in sample quality from batch to batch

Method used

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  • Pramipexole dihydrochloride slow-release tablet with high content uniformity and preparation method thereof
  • Pramipexole dihydrochloride slow-release tablet with high content uniformity and preparation method thereof
  • Pramipexole dihydrochloride slow-release tablet with high content uniformity and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0039]The pramipexole hydrochloride sustained-release tablets shown in Table 1 were prepared.

[0040] Table 1. The pramipexole hydrochloride sustained-release tablets of embodiment 1

[0041]

[0042] Remarks: Ethanol water solution is used in the granulation process, it is removed by drying and does not exist in the final product.

[0043] Preparation method: dissolve the pramipexole hydrochloride and hypromellose of prescription quantity in 40% ethanol aqueous solution, and use it as a drug-containing adhesive for subsequent use; place hypromellose and microcrystalline cellulose in a fluidized bed, After mixing for 3-5 minutes, spray the drug-containing binder into the bed for granulation. After spraying, dry; add magnesium stearate, mix evenly, and press into tablets. The hardness range is controlled at 5-10kg.

Embodiment 2

[0045] Prepare pramipexole hydrochloride sustained-release tablets shown in Table 2.

[0046] Table 2. The pramipexole hydrochloride sustained-release tablets of embodiment 2

[0047]

[0048] Remarks: Ethanol water solution is used in the granulation process, it is removed by drying and does not exist in the final product.

[0049] Preparation method: Dissolve the prescribed amount of pramipexole hydrochloride and hypromellose in 70% ethanol aqueous solution, and use it as a drug-containing adhesive for later use; place hypromellose and microcrystalline cellulose in a high-shear wet process In the granulator, mix evenly, spray the drug-containing binder into the high-shear wet granulator at a constant speed to granulate, and dry; add magnesium stearate, mix evenly, and press into tablets. The hardness range is controlled at 6-12kg .

Embodiment 3

[0051] Prepare pramipexole hydrochloride sustained-release tablets shown in Table 3.

[0052] Table 3. The pramipexole hydrochloride sustained-release tablets of embodiment 3

[0053]

[0054] Remarks: Ethanol water solution is used in the granulation process, it is removed by drying and does not exist in the final product.

[0055] Preparation method: dissolve pramipexole hydrochloride and hypromellose of prescribed quantity in 60% ethanol aqueous solution, and use it as a drug-containing adhesive for subsequent use; place hypromellose and microcrystalline cellulose in a fluidized bed, After mixing for 3-5 minutes, spray the drug-containing binder into the bed for granulation. After spraying, dry; add magnesium stearate, mix evenly, and press into tablets. The hardness range is controlled at 5-10kg.

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Abstract

The invention belongs to the field of pharmaceutic preparations, and particularly provides a pramipexole dihydrochloride slow-release tablet with high content uniformity and a preparation method thereof. The invention provides the pramipexole dihydrochloride slow-release tablet which is independent of pH (potential of hydrogen) during drug release, is slowly released in buffer solutions with pHs of 1.2, 4.5 and 6.8 for 24 hours, reaches final release amounts above 85 percent without exception and only needs to be taken once every day. The preparation method provided by the invention is simple and practicable, relative standard deviations (RSDs) of the content uniformity and the release rate of the low-dose medicine, namely the pramipexole dihydrochloride can be guaranteed to be far below the RSD in a limit requirement, the between difference is small and the repeatability is high.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a pramipexole hydrochloride sustained-release tablet with high content uniformity and a preparation process thereof. Background technique [0002] The chemical name of pramipexole hydrochloride is: (S)-2-amino-4,5,6,7-tetrahydro-6-propylamine-benzothiazole monohydrate dihydrochloride, and its structural formula is: [0003] The molecular formula of pramipexole hydrochloride is C 10 h 17 N 3 S 2HCl H 2 O, with a molecular weight of 302.26, is used to treat the signs and symptoms of idiopathic Parkinson's disease. For patients with Parkinson's disease, as a non-ergot dopamine receptor agonist, it can highly selectively stimulate dopamine receptors, thereby improving the symptoms of patients. It is a new generation of drugs superior to ergot derivatives. In 2002, pramipexole was approved by the European Union for the first-line treatment of Parkinson's dis...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/428A61K47/38A61P25/16
Inventor 袁洪雨李长军李洁张涛李后涛付成业高希波
Owner SHANDONG QIDU PHARMA
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