CN1110140A - Drug composition for curing dysmnesia and dementia and its preparing method - Google Patents
Drug composition for curing dysmnesia and dementia and its preparing method Download PDFInfo
- Publication number
- CN1110140A CN1110140A CN 94103416 CN94103416A CN1110140A CN 1110140 A CN1110140 A CN 1110140A CN 94103416 CN94103416 CN 94103416 CN 94103416 A CN94103416 A CN 94103416A CN 1110140 A CN1110140 A CN 1110140A
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- huperzine
- dementia
- dysmnesia
- dextrin
- curing
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The present invention provides a medicine composition for curing benign dysmnesia, encephalic organic disturbance and dementia and its preparation method. Said composition contains huperzin A, starch, dextrin and magnesium stearate. Its preparation process is as follows: firstly the huperzin A is made into a solution, and then the solution is added in a mixed excipient.
Description
The present invention relates to a kind of pharmaceutical composition for the treatment of benign memory deficits, brain organic dysmnesia and dementia and preparation method thereof.
Benign memory deficits, brain organic dysmnesia are senile common frequently-occurring diseases with dementia.Along with the increase of aging population, the incidence rate of the senile memory dysfunction in countries in the world is in rising trend.In recent years, about central cholinergic system mediator system and anticholinergic agent the influence of study, memory is caused people's attention day by day.Report was abroad once arranged, can promote normal person and presenile dementia patient's memory ability specifically with the physostigmine intravenous injection, but untoward reaction is serious, action time is of short duration.
Huperzine A (huperzine A) chemistry (5R by name, 9R, 11E)-5-amino-11-ethylidene-5,6,9,10-tetrahydrochysene-7-methyl-5,9-methylene ring suffering is (b)-2(1H) ketone also, be the reversibility cholinesterase inhibitor of China's initiative, it increases, and memory keeps and the memory represents effect is better than physostigmine.
The huperzine A consumption is very little, and every day, total amount was 200-400 μ g, side effect can occur when dosage is big.Existing people reports pharmacodynamic action (Wang Yue-e etc., the Acta Pharmacologica Sinica 1986 of its injection; 7:110-3), senile memory function goes down and dull-witted palpus long-term prescription because for the treatment of, and adopts very inconvenience of intramuscular injection.Also see the clinical effect observation report (Zhang Cilu etc., new drug and clinical nineteen ninety November) of treatment huperzine A tablet, but only be experimental drug, do not make commercially available medicine as yet memory.The prescription and the technology that contain the pharmaceutical composition of huperzine A there is no report.
Because the huperzine A using dosage belongs to trace, but in solid preparation as principal agent, shared weight only be 1/1300 of adjuvant, ordinary preparation technology solution uniformity problem difficulty.
The huperzine A chemical property is extremely unstable, to light, heat, wet all responsive.Increased certain degree of difficulty for the development of its preparation.
The objective of the invention is to prepare a kind of stable performance, huperzine A new oral solid preparation that bioavailability is good, easy to use.
The present invention with huperzine A as principal agent, with the proportioning of adjuvant be 1: 1300, therefore employed adjuvant is had relatively high expectations, necessary stable performance, principal agent is not produced adsorption, do not influence the stability of principal agent, its finished product has dissolution rate and bioavailability preferably, on a large amount of experiment basis, selected optimum formula.
The technology that the present invention adopts is, earlier the huperzine A crude drug is dissolved, be dispersed in the adjuvant, adjuvant can be that diluent (as starch etc.), disintegrating agent, excipient (as sucrose etc.), binding agent (as dextrin etc.), lubricant (as magnesium stearate) are made.
Adopt prescription provided by the invention and technology, easy to prepare, cost is low, better stability of preparation, and bioavailability is good.
Invention is achieved in that
Prescription
Huperzine A 0.02-0.4%
Starch 20-80%
Sucrose 5-50%
Dextrin 5-40%
Magnesium stearate 0.5-2.0%
Technology
Take by weighing supplementary product starch, sucrose and dextrin respectively, with the equivalent method mix homogeneously of rising progressively, it is standby to make admixed excipients.It is standby that huperzine A is made the alcohol-water mixed solution.The huperzine A drips of solution is added in the above-mentioned admixed excipients, and with an amount of washing with alcohol, make soft material, granulate through 16 order nylon mesh, in 65 ℃ ± 5 ℃ oven dryings, through 20 order nylon mesh granulate once, add magnesium stearate, mix homogeneously, tabletting, the heavy 65mg of sheet, finished product packing is in the dark glass bottle of sealing.
Embodiment-huperzine A sheet
1, take by weighing starch 30.5g, sucrose 20.1g, dextrin 14.0g, it is standby to make admixed excipients with the equivalent method of rising progressively.
2, take by weighing huperzine A 0.025g, it is standby to make 20% ethanol liquid.
3, the huperzine A drips of solution is added in the admixed excipients, and, makes soft material, granulate through 16 order nylon mesh, in 65 ℃ of oven dryings with 20% washing with alcohol.
4, dried granule with 20 order nylon mesh granulate once adds magnesium stearate 0.38g, mix homogeneously, tabletting, the heavy 65mg of sheet.
5, sheet is loaded in the tinplate lid Brown Glass Brown glass bottles and jars only sealing.
Prove that through stability test the preparation stable performance was placed 2 years through room temperature, its content is 98.8%.The preparation bioavailability is good, and the uniformity meets Chinese Pharmacopoeia (90 editions) requirement.
Prove that through clinical use the huperzine A sheet is 83.6% to the total effective rate of benign memory deficits, brain organic dysmnesia and dementia treatment, be better than the total effective rate (62.5%) of positive control drug piracetam, learning by statistics to handle has significant difference.
Claims (5)
1, a kind of benign memory deficits, brain organic obstacle and dull-witted pharmaceutical composition for the treatment of is characterized by and contain huperzine A, starch, dextrin and magnesium stearate.
2, pharmaceutical composition according to claim 1, its prescription is:
Huperzine A 0.02-0.4%
Starch 20-80%
Sucrose 5-50%
Dextrin 5-40%
Magnesium stearate 0.5-2.0%
3, pharmaceutical composition according to claim 1, its packing are the dark glass bottles.
4, the described preparation of drug combination technology of a kind of claim 1 is characterized by huperzine A dissolving earlier, adds in the admixed excipients then.
5, preparation technology according to claim 5, it is characterized by the used solvent of dissolving huperzine A is ethanol.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 94103416 CN1110140A (en) | 1994-04-07 | 1994-04-07 | Drug composition for curing dysmnesia and dementia and its preparing method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 94103416 CN1110140A (en) | 1994-04-07 | 1994-04-07 | Drug composition for curing dysmnesia and dementia and its preparing method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1110140A true CN1110140A (en) | 1995-10-18 |
Family
ID=5031069
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 94103416 Pending CN1110140A (en) | 1994-04-07 | 1994-04-07 | Drug composition for curing dysmnesia and dementia and its preparing method |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1110140A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102151268A (en) * | 2011-03-28 | 2011-08-17 | 王义明 | Compound preparation for treating Alzheimer's disease and preparation method thereof |
| CN102258518A (en) * | 2010-05-28 | 2011-11-30 | 中国科学院上海药物研究所 | Application of huperzine A to preparation of medicament for treating glaucoma and/or ischemia-induced optic nerve damage |
-
1994
- 1994-04-07 CN CN 94103416 patent/CN1110140A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102258518A (en) * | 2010-05-28 | 2011-11-30 | 中国科学院上海药物研究所 | Application of huperzine A to preparation of medicament for treating glaucoma and/or ischemia-induced optic nerve damage |
| CN102151268A (en) * | 2011-03-28 | 2011-08-17 | 王义明 | Compound preparation for treating Alzheimer's disease and preparation method thereof |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C01 | Deemed withdrawal of patent application (patent law 1993) | ||
| WD01 | Invention patent application deemed withdrawn after publication |