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Pharmaceutical compositions of donepezil having specific in vitro dissolution profile or pharmacokinetics parameters

A kind of technology of donepezil and composition, applied in the field of timed release pharmaceutical composition of donepezil

Inactive Publication Date: 2015-12-16
LUPIN LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0018] However, or GI side effects (nausea, vomiting, and diarrhea) were disclosed on the label of the label, and when they occurred, side effects occurred more frequently at the 10 mg / day dose than at the 5 mg / day dose, and more frequently at the 23 mg dose (extended release formulation) than at the 5 mg / day dose. Occurs more frequently with the 10 mg dose

Method used

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  • Pharmaceutical compositions of donepezil having specific in vitro dissolution profile or pharmacokinetics parameters
  • Pharmaceutical compositions of donepezil having specific in vitro dissolution profile or pharmacokinetics parameters

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0151] Brief manufacturing process:

[0152] 1 Weigh donepezil HCl, sodium starch glycolate, hydroxypropyl methylcellulose, lactose and hydroxypropyl cellulose, sieving and mixing together.

[0153] 2 Use pure water to granulate the mixture of step 1 with appropriate granulation parameters, and then dry the granules.

[0154] 3 The dried granules are sieved through a suitable sieve.

[0155] The remaining amount of 4-hydroxypropyl methylcellulose, lactose and microcrystalline cellulose is sieved through a suitable sieve and mixed with the granules of step 3.

[0156] 5 Colloidal silicon dioxide and magnesium stearate are sieved through a suitable sieve and mixed with the blend of step 4.

[0157] 6 Compress the lubricating blend of step 5 with a circular punch using appropriate physical parameters.

[0158] 7 Ethyl cellulose, hydroxypropyl methyl cellulose and triethyl citrate were dissolved in a mixture of isopropanol and dichloromethane under continuous stirring.

[0159] 8 Coat the com...

Embodiment 2

[0165] Brief manufacturing process:

[0166] 1 Weigh donepezil HCl, sodium starch glycolate, hydroxypropyl methylcellulose, lactose and hydroxypropyl cellulose, sieving and mixing together.

[0167] 2 Use pure water to granulate the mixture of step 1 with appropriate granulation parameters, and then dry the granules.

[0168] 3 The dried granules are sieved through a suitable sieve.

[0169] The remaining amount of 4-hydroxypropyl methylcellulose, lactose and microcrystalline cellulose is sieved through a suitable sieve and mixed with the granules of step 3.

[0170] 5 Colloidal silicon dioxide and magnesium stearate are sieved through a suitable sieve and mixed with the blend of step 4.

[0171] 6 Compress the lubricating blend of step 5 with a circular punch using appropriate physical parameters.

[0172] 7 Ethyl cellulose, hydroxypropyl methyl cellulose and triethyl citrate were dissolved in a mixture of isopropanol and dichloromethane under continuous stirring.

[0173] 8 Coat the com...

Embodiment 3

[0176] Brief manufacturing process:

[0177] 1 Hardened sugar balls

[0178] 1.1 The sugar balls are sieved using a vibrating screen.

[0179] 1.2 Triethyl citrate and hydroxypropyl methylcellulose are dissolved in a mixture of isopropanol and dichloromethane under continuous stirring.

[0180] 1.3 The sugar spheres are loaded in the fluidized bed processor and fluidized.

[0181] 1.4 All the solutions of step 1.2 are sprayed on the sugar balls at a suitable temperature.

[0182] 1.5 The hardened sugar balls of step 1.4 are dried in a fluidized bed processor at a suitable temperature.

[0183] 1.6 The dried hardened sugar balls of step 1.5 are passed through a suitable sieve and the fines are discharged.

[0184] 2 Drug loading

[0185] 2.1 Add hydroxypropyl cellulose to pure water to obtain a clear solution.

[0186] 2.2 Add donepezil hydrochloride to the solution in step 2.1 to obtain a clear solution.

[0187] 2.3 Add talc to the solution of step 2.2 under continuous stirring and filter...

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Abstract

A timed release pharmaceutical composition comprising donepezil is provided wherein the single dose AUC (14-22) of the said composition administered in the morning is about % to about 30% less than the single dose AUC (2-10) of an immediate release composition of donepezil administered in the night, wherein both the compositions have equivalent dose of donepezil.

Description

Technical field [0001] The present invention relates to a time-release pharmaceutical composition of donepezil, wherein the composition provides a plasma donepezil concentration curve corresponding to the circadian rhythm of acetylcholine (Ach) levels in the brain. The composition reduces the incidence of sleep disorders including difficulty falling asleep, multiple awakenings during sleep, nightmares, disturbed sleep-wake rhythms, and early morning awakening, and also reduces the incidence of sleep disorders in subjects suffering from Alzheimer's disease. The observed incidence of sunset effects is reduced. Oral administration of the composition reduces the incidence of gastrointestinal (GI) side effects. Background technique [0002] Chemically as (±)-2,3-dihydro-5,6-dimethoxy 2-[[1-(phenylmethyl)-4-piperidinyl]methyl]-1H-indene-1- The ketone known donepezil is a reversible inhibitor of acetylcholinesterase. Currently in trade name or The following are sold in tablet dosag...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/28A61K9/24A61P25/28A61K31/445A61K9/22A61K9/00A61K9/50
CPCA61K9/0004A61K9/2018A61K9/2054A61K9/2086A61K9/2846A61K9/2866A61K9/5026A61K9/5078A61K31/445A61P25/20A61P25/28A61P43/00A61K9/167
Inventor D·S·巴贺利C·A·沙阿S·A·加德夫N·沙玛S·詹德兰A·A·德希穆克
Owner LUPIN LTD
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