CN1436531A - Donepezil hydrochloride dripping pills - Google Patents
Donepezil hydrochloride dripping pills Download PDFInfo
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- CN1436531A CN1436531A CN 02110065 CN02110065A CN1436531A CN 1436531 A CN1436531 A CN 1436531A CN 02110065 CN02110065 CN 02110065 CN 02110065 A CN02110065 A CN 02110065A CN 1436531 A CN1436531 A CN 1436531A
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- donepezil hydrochloride
- dripping pills
- polyoxyethylene
- stearate
- medicine
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Abstract
Donepezil hydrochloride guttate pills contains Donepezil hydrochloride 6-16 wt%, water soluble supplementary material polyglycol-4000 0-94 wt% and polyethenoxy searate 0-94 wt%. The present invention is easy in separating dosage and has high biological utilization, stable quality and easy-to-control production condition.
Description
The present invention relates to a kind of donepezil hydrochloride dripping pills agent, belong to the Western medicine preparation technical field.
Donepezil hydrochloride be a kind of Alzheimer type for the treatment of slightly to the medicine of moderate dementia, also got permission treatment simultaneously to child attention obstacle deficiency disease.The medicine that can slow down Alzheimer development in clinical has antioxidant, oxidase inhibitor, anti-inflammatory agent and cholinesterase inhibitor and still at the biological engineering medicine such as the cranial nerve renovation agent of experimental stage.Oneself gains public acceptance wherein can to correct or slow down choline function goes down among the central nervous system curative effect of medication.Obtain drugs approved by FDA treatment Alzheimer type in recent years and slightly had only romotal and donepezil hydrochloride to the medicine of moderate dementia.Donepezil hydrochloride is the piperidines cholinesterase inhibitor, its therapeutical effect is the acetylcholine hydrolyzation that causes of reversibility acetylcholine esterase inhibition and increase the acetylcholine amount of acceptor site, also has the direct effect of disposal, neurotransmitter receptor or ion channel to peptide.This medicine has the selectivity of height to acetylcholinesterase, its effect surpasses butyrylcholine esterase more than 1000 times, and tacrine is then basic identical, so, donepezil hydrochloride causes that than romotal the side effect of maincenter periphery cholinergic is little, and romotal has the neural liver toxicity of blood.Therefore donepezil hydrochloride has more market prospect.
Donepezil hydrochloride preparation commonly used clinically at present is the conventional tablet of 5mg.This medicine (1) price height, drug treatment is long; (2) according to patient's state of an illness difference, need the 2.5-10mg various dose respectively, and patient compliance is poor; (3) be insoluble drug, bioavailability is low.
The objective of the invention is at the problems referred to above, a kind of water solublity low dose is provided, dosage is cut apart conveniently, reduces to increase the gradient of dosage, improves the drop pill of bioavailability, and dosage is 2.5mg.
Technical characterstic of the present invention is: having selected for use water-soluble solid to disperse rerum natura pharmaceutic adjuvant Polyethylene Glycol and polyoxyethylene (40) stearate is carrier, and medicine is suspended in the melting carrier, adopts dropping preparation method to make micropill.
Donepezil hydrochloride dripping pills of the present invention is achieved in that its composition comprises donepezil hydrochloride, water soluble adjuvant Macrogol 4000 and polyoxyethylene (40) stearate, and the percentage by weight of each composition is donepezil hydrochloride 6-16, Macrogol 4000 0-94 and polyoxyethylene (40) stearate 0-94.。
The preparation of donepezil hydrochloride dripping pills of the present invention is that the donepezil hydrochloride crude drug is added in fused adjuvant Polyethylene Glycol and polyoxyethylene (40) stearate, 80 ℃ of stirrings, mixings, splash in the liquid paraffin solidify, filter, dry, packing promptly.
This product, was deposited six months under the condition of relative humidity 75% 40 ℃ of temperature, and its content and dissolution result are as follows:
The donepezil hydrochloride dripping pills shelf-stability
Time (moon) content (%) dissolution (%)
0 99.7 93.36
1 100.4 94.28
3 101.2 94.57
6 99.6 92.78
This drop pill advantage is that swallow conveniently (1), especially is fit to dull-witted patient's administration; (2) dosage is cut apart conveniently, can need because of treatment, uses the consumption of suiting the medicine to the illness that is suitable for the patient; (3) reduce the gradient of increase dosage, thereby reduced the side effect that patient occurs because of the dose dumping increase, and can select best price treatment ratio; (4) can sublingual administration, improve bioavailability.In addition, the workshop of drop pill does not have dust, helps labor protection.This product steady quality and working condition are easy to control, and the ball method of double differences is different little, and content is more accurate.
The embodiment of the invention:
Example 1:
Per 1000 consumptions of writing out a prescription
Donepezil hydrochloride 2.5g
Macrogol 4000 7.85g
Polyoxyethylene (40) stearate 7.85g
The liquid paraffin condensing agent
Operating procedure: Polyethylene Glycol and polyoxyethylene (40) stearate are put in the beaker, be heated to 80 ℃ of fusions, donepezil hydrochloride is added wherein stirring, mixing, 80 ℃ ± insulation below 2 ℃, syringe needle with φ 1mm, mixed liquor is splashed in refrigerative liquid paraffin, and sedimentation was placed after 30 minutes, filtered, dry, promptly.Every heavily about 17mg of ball, hydrochloric donepezil 2.5mg.
Example 2:
Per 1000 consumptions of writing out a prescription
Donepezil hydrochloride 5g
Macrogol 4000 15.7g
Polyoxyethylene (40) stearate 15.7g
The liquid paraffin condensing agent
Operating procedure: Polyethylene Glycol and polyoxyethylene (40) stearate are put in the beaker, be heated to 80 ℃ of fusions, donepezil hydrochloride is added wherein stirring, mixing, 80 ℃ ± insulation below 2 ℃, syringe needle with φ 2mm, mixed liquor is splashed in refrigerative liquid paraffin, and sedimentation was placed after 30 minutes, filtered, dry, promptly.Every heavily about 34mg of ball, hydrochloric donepezil 5mg.
Claims (1)
1, a kind of donepezil hydrochloride dripping pills agent, it is characterized in that comprising donepezil hydrochloride, water soluble adjuvant Macrogol 4000 and polyoxyethylene (40) stearate composition, the percentage by weight of each composition is donepezil hydrochloride 6-16, Macrogol 4000 0-94, polyoxyethylene (40) stearate 0-94.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB021100659A CN1175813C (en) | 2002-02-07 | 2002-02-07 | Donepezil hydrochloride dripping pills |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB021100659A CN1175813C (en) | 2002-02-07 | 2002-02-07 | Donepezil hydrochloride dripping pills |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1436531A true CN1436531A (en) | 2003-08-20 |
| CN1175813C CN1175813C (en) | 2004-11-17 |
Family
ID=27628157
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB021100659A Expired - Lifetime CN1175813C (en) | 2002-02-07 | 2002-02-07 | Donepezil hydrochloride dripping pills |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1175813C (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101090737B (en) * | 2004-12-27 | 2010-09-08 | 卫材R&D管理有限公司 | Method for stabilizing dementia-resisting medicine |
-
2002
- 2002-02-07 CN CNB021100659A patent/CN1175813C/en not_active Expired - Lifetime
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101090737B (en) * | 2004-12-27 | 2010-09-08 | 卫材R&D管理有限公司 | Method for stabilizing dementia-resisting medicine |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1175813C (en) | 2004-11-17 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| C41 | Transfer of patent application or patent right or utility model | ||
| TR01 | Transfer of patent right |
Effective date of registration: 20160519 Address after: 273400 Shandong Feixian County North Ring Road No. 1 Patentee after: Shandong Xinshidai Pharmaceutical Industry Co., Ltd. Address before: 250100 Ji'nan Industrial Road, Shandong, No. 106 Patentee before: Wang Zhigang |
|
| CX01 | Expiry of patent term | ||
| CX01 | Expiry of patent term |
Granted publication date: 20041117 |