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Osmotic pump type controlled-release preparation containing donepezil and its salt and preparation method thereof

An osmotic pump controlled release and donepezil technology, which is applied to non-active ingredients in medical preparations, pharmaceutical formulations, active ingredients of heterocyclic compounds, etc., can solve the problems of low solubility in water, difficult and slow drug release, etc. The effect of low toxicity, low risk of adverse reactions, and simple preparation process

Active Publication Date: 2016-05-25
CHENGDU KANGHONG PHARMA GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The present invention overcomes the difficulties in preparation technology in the prior art, for example, how to use simple and easy preparation technology to develop appropriate osmotic pressure active substances and film-forming materials to prepare osmotic drugs that can be slowly released at a constant rate or close to a constant rate. Pump preparations, overcome the relatively low solubility in water of donepezil hydrochloride itself (55g / L -1 left and right), the problem that its drug is not easy to release completely, and it is necessary to ensure that its prescription process has good stability between batches of products in industrialized large-scale production

Method used

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  • Osmotic pump type controlled-release preparation containing donepezil and its salt and preparation method thereof
  • Osmotic pump type controlled-release preparation containing donepezil and its salt and preparation method thereof
  • Osmotic pump type controlled-release preparation containing donepezil and its salt and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0101] Tablet core prescription (by weight percentage of tablet core, 100mg / tablet, 1000 tablets):

[0102]

[0103] Insoluble semipermeable membrane prescription (in terms of insoluble semipermeable membrane weight percent):

[0104]

[0105] Preparation:

[0106] According to the above-mentioned tablet core prescription and dosage, the main drug and auxiliary materials are sieved, mixed evenly, and directly compressed into a tablet core; cellulose acetate, diethyl phthalate, polyethylene glycol 1500 are dissolved in acetone-water (95: 5, V / V) to make a semi-permeable membrane coating solution, the tablet core is coated, the coating weight gain is 4%, after coating, it is activated at 60 ° C for 4 hours, and a laser or mechanical drill is used on the coated tablet Punch at least one small hole on the surface, the hole diameter is controlled at 0.4mm, that is.

[0107] Detect the release rate (table 11) of this preparation in 0.1M hydrochloric acid:

[0108] Table 11 em...

Embodiment 2

[0111] Tablet core prescription (by weight percentage of tablet core, 100mg / tablet, 1000 tablets):

[0112]

[0113] Insoluble semipermeable membrane prescription (in terms of insoluble semipermeable membrane weight percent):

[0114]

[0115] Preparation:

[0116] Take donepezil hydrochloride, microcrystalline cellulose, lactose, mannitol, polyethylene glycol 6000, and polyvinylpyrrolidone K30 according to the above tablet core prescription and dosage, mix evenly, add an appropriate amount of 70% ethanol solution to granulate, dry, granulate, and add micropowder The silica gel is mixed evenly, and the tablet core is obtained by tableting; cellulose acetate, triethyl citrate, and polyethylene glycol 1500 are dissolved in acetone-water (95:5) to make a semi-permeable membrane coating solution, and the tablet core Carry out coating, the weight gain of coating is 5%, activate at 40 ℃ for 24 hours after coating, punch at least one small hole on the surface of the coated tab...

Embodiment 3

[0121] Tablet core prescription (by weight percentage of tablet core, 100mg / tablet, 1000 tablets):

[0122]

[0123] Insoluble semipermeable membrane prescription (in terms of insoluble semipermeable membrane weight percent):

[0124] Name Feed Amount Weight Percentage

[0125] Coating material Cellulose acetate 33.383.3%

[0126] Porogen polyethylene glycol 4006.716.7%

[0127] Preparation:

[0128] Sieve the main drug and auxiliary materials according to the above-mentioned tablet core prescription and dosage, mix them evenly, and directly compress into tablet cores; dissolve cellulose acetate and polyethylene glycol 400 in acetone-water (95:5, V / V) to prepare Form a semi-permeable membrane coating solution, coat the tablet core, increase the weight of the coating by 8%, activate it at 60°C for 8 hours after coating, and punch at least one small hole on the surface of the coated tablet with a laser or a mechanical drill. Control it at 0.6mm, that is to say.

[0129] ...

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Abstract

The invention discloses an osmotic pump type controlled release preparation containing donepezil and its salt and a preparation method thereof. The controlled release preparation comprises a tablet core containing the pharmaceutical active substance donepezil and its salt, an insoluble semipermeable membrane and at least one drug release hole. The controlled release preparation has better burst release control on drugs, the drug release rate is close to zero, and the difficulties of great inter-batch differences and poor process stability in amplified production of osmotic pump controlled release tablets are overcome. Thus, large-scale production of the osmotic pump type controlled release preparation containing donepezil and its salt can be realized.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an osmotic pump type controlled-release tablet containing donepezil and a salt thereof and a preparation method thereof. Background technique [0002] According to the statistics of Alzheimer's Association International (ADI), before 2050, there will be 27 million dementia patients in China alone, and it is estimated that about 10% of people in their 70s will suffer from dementia, and those in their 80s are expected to suffer from dementia. 30% of people will suffer from the disease. Asia's aging population is rapidly increasing, and within 40 years more than half of the world's dementia patients will come from Asia, and China's proportion will be particularly large. With the advent of an aging society, the incidence of such diseases will become higher and higher, and their impact on society will also increase. [0003] Donepezil is a novel, highly effective cholinest...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/44A61K9/22A61K9/36A61K9/32A61K31/445A61K47/42A61K47/38A61K47/36A61K47/34A61P25/28A61K47/10A61K47/32
Inventor 柯潇郑强
Owner CHENGDU KANGHONG PHARMA GRP
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