CN103565761B - Galanthamine hydrobromide orally disintegrating tablet - Google Patents
Galanthamine hydrobromide orally disintegrating tablet Download PDFInfo
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- CN103565761B CN103565761B CN201210249186.5A CN201210249186A CN103565761B CN 103565761 B CN103565761 B CN 103565761B CN 201210249186 A CN201210249186 A CN 201210249186A CN 103565761 B CN103565761 B CN 103565761B
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- galanthamine hydrobromide
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- cavity disintegration
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Abstract
The invention provides a galanthamine hydrobromide orally disintegrating tablet, which has the characteristics of simple prescription, simple process, low cost and wide application, etc.
Description
Technical field
The present invention relates to pharmaceutical field, be specifically related to a kind of galanthamine hydrobromide oral cavity disintegration tablet.
Background technology
Galanthamine hydrobromide is anticholinesterase drug, former in poliomyelitis sequela and myasthenia gravis.It is a kind of Reversible cholinesterase inhibitor.Acetylcholine esterase in body can be suppressed, make release in body or slow down from the destruction of the acetylcholine of external injection, thus strengthen acetylcholine to the effect of each organ, easily through blood brain barrier, and there is obvious impact to central nervous system.This product has become the choice drug for the treatment of alzheimer disease at present, because the curative effect of this product is at least equal with tacrine, but this product is without liver toxicity, liver function test that it goes without doing; Toleration comparatively tacrine is good, is high special to neuron acetylcholinesterase.In neuron and erythrocyte, the ability of its acetylcholine esterase inhibition is stronger than the ability of acetylcholine esterase inhibition in blood plasma 50 times.This product is the competitive inhibitor of acetylcholinesterase, and tacrine is noncompetitive, and this product is maximum in the activity of the region that height choline lacks as postsynaptic region, and this point is highly beneficial, because response to treatment is mainly at postsynaptic regions mediate.This product not with protein bound, therefore the less impact may taken food or take medicine simultaneously.Inventor considers the concrete clinical manifestation of patients with Alzheimer disease, namely a part of patient loses function of deglutition, difficulty is brought to conventional tablet and taking of capsule, have developed the Orally disintegrated galantamine hydrobromide tablet that applicable old dementia patients uses for this reason, be characterized in that this product puts into energy disintegrate stripping rapidly behind patient oral cavity, just can solve specific demand clinically.
The tabletting method that existing galanthamine hydrobromide oral cavity disintegration tablet is conventional is freeze-drying, solid solution method, spray drying method and direct compression process, before 3 kinds of method requirements to technique higher, and direct compression technique is simple, with low cost, is widely used.
Prior art [Lu Jihong etc., the development of galanthamine hydrobromide oral cavity disintegration tablet, " Chinese Journal of Modern Applied Pharmacy " 08 phase in 2009] disclose a kind of prescription of galanthamine hydrobromide oral cavity disintegration tablet direct compression, micropowder silica gel sweet by principal agent galanthamine hydrobromide and adjuvant mannitol, citric acid, sodium bicarbonate, MCC, PVPP, A Siba, magnesium stearate, strawberry essence etc. form.
Patent application CN200610096693.4 discloses a kind of galanthamine hydrobromide oral cavity disintegration tablet and preparation method thereof, namely adopts direct powder compression to obtain by after the mixing such as galanthamine hydrobromide, filler, disintegrating agent, lubricant.
Although above-mentioned prior art all directly compressible obtains galanthamine hydrobromide oral cavity disintegration tablet, prescription composition is complicated, and production cost is high.
Prepare a kind of formulation and technology simple, with low cost, yield is high, good stability, and disintegrate is rapid, and is applicable to the galanthamine hydrobromide oral cavity disintegration tablet of conventional tablet machines production, is the technical problem that the present invention puts forth effort to solve.
Summary of the invention
The invention provides a kind of galanthamine hydrobromide oral cavity disintegration tablet obtained by direct compression technique, it is composed as follows:
Galanthamine hydrobromide 4-6g,
Microcrystalline Cellulose 64-66g,
Disintegrating agent 9-11g,
Acidic flavoring agent 5-7g,
Sweeting agent 2.7-2.9g,
Sodium bicarbonate 1.3-1.5g,
Lubricant 0.7-0.9g,
Make 1000.
Particularly, the present invention relates to following four kinds of galanthamine hydrobromide oral cavity disintegration tablets, its composition is as follows respectively:
(1)
Galanthamine hydrobromide 4g,
Microcrystalline Cellulose 64g,
Low-substituted hydroxypropyl cellulose 9g,
Citric acid 5g,
Stevioside 2.7g,
Sodium bicarbonate 1.3g,
Magnesium stearate 0.7g,
Make 1000.
(2)
Galanthamine hydrobromide 5g,
Microcrystalline Cellulose 65g,
Low-substituted hydroxypropyl cellulose 10g,
Citric acid 6g,
Stevioside 2.8g,
Sodium bicarbonate 1.4g,
Magnesium stearate 0.8g,
Make 1000.
(3)
Galanthamine hydrobromide 5.5g,
Microcrystalline Cellulose 65.5g,
Low-substituted hydroxypropyl cellulose 10.5g,
Citric acid 6.5g,
Stevioside 2.85g,
Sodium bicarbonate 1.45g,
Magnesium stearate 0.85g,
Make 1000.
(4)
Galanthamine hydrobromide 6g,
Microcrystalline Cellulose 66g,
Low-substituted hydroxypropyl cellulose 11g,
Citric acid 7g,
Stevioside 2.9g,
Sodium bicarbonate 1.5g,
Magnesium stearate 0.9g,
Make 1000.
Wherein, microcrystalline Cellulose has the effect of filler, and low-substituted hydroxypropyl cellulose has the effect of disintegrating agent, and citric acid and stevioside have the effect of correctives, and sodium bicarbonate has the effect of assisting disintegrate, and magnesium stearate has the effect of lubricant.
In addition, present invention also offers a kind of preparation method of galanthamine hydrobromide oral cavity disintegration tablet, comprise the various component mixing of above-mentioned galanthamine hydrobromide oral cavity disintegration tablet, adopt conventional tablet machines to carry out tabletting, to obtain final product.
By the prescription screening to the component of galanthamine hydrobromide oral cavity disintegration tablet and a large amount of of content thereof, the discovery that inventor is surprised, prescription of the present invention, without the need to extra fluidizer---micropowder silica gel, still can adopt direct compression process to produce.And it is good that galanthamine hydrobromide oral cavity disintegration tablet prepared by the present invention has character, good stability, the features such as disintegrate is rapid.
In addition, due to direct compression process technique self, during oral cavity disintegration tablet disintegrate, larger granule may be produced, thus cause bringing grittiness in oral cavity.The present invention is by the scientific matching of each component, the galanthamine hydrobromide oral cavity disintegration tablet not only disintegrate rapid (disintegration is about 12 seconds) of preparation, and the granule produced is much smaller than 710 μm (in testing processes of disintegration, the granule of generation can all by 50 mesh sieves).Therefore, there is not grittiness problem in the galanthamine hydrobromide oral cavity disintegration tablet that prepared by the present invention.
Therefore, the present invention, by scientifically selecting component and the content thereof of galanthamine hydrobromide oral cavity disintegration tablet, achieves following technique effect: 1) technique is simple, without the need to complicated technologies such as freeze-drying, solid solution method, spray drying methods; 2) product yield is high; 3) product characteristics are good; 4) product stability is good; 5) product disintegrate is rapid; 5) product is without grittiness.
Detailed description of the invention
Detailed description of the invention is only and further explains and describes the present invention, should not be interpreted as any limitation of the invention.
The raw material that the present invention is used and adjuvant are commercially available.
Embodiment 1 ~ 4 galanthamine hydrobromide oral cavity disintegration tablet
The prescription (making 1000) of galanthamine hydrobromide oral cavity disintegration tablet sees the following form:
Preparation technology: by the various component mixing of the galanthamine hydrobromide oral cavity disintegration tablet of recipe quantity, adopt conventional tablet machines to carry out tabletting, to obtain final product.
The yield of experimental example 1 galanthamine hydrobromide oral cavity disintegration tablet, disintegration and stability study (40 DEG C, RH75%)
As follows, galanthamine hydrobromide oral cavity disintegration tablet obtained with reference examples (embodiment 1 of patent application CN200610096693.4) for embodiment 1 ~ 4 is carried out Detection of Stability: simulating under the terms of packing that goes on the market, place 6 months under 40 DEG C and relative humidity 75% condition, in 0,3,6 month sample analysis, result compared with zero month sample.
Related substance
Instrument: Shimadzu LC-10A high performance liquid chromatograph system (being equipped with: LC-10ATVP pump and SPD-10AVP UV-detector)
Chromatographic condition: chromatographic column is take octadecylsilane chemically bonded silica as the stainless steel column of filler 4.6 × 150mm, granularity 5um (shimpack-CLCODS post).Mobile phase: methanol-0.05mol/L Spirit of Mindererus. (pH to 3.5 adjusted by 0.05mol/L Spirit of Mindererus. acetic acid) (15: 85) determined wavelength: 289nm.Sample size: 20ul.Flow velocity: 1.0ml/min.
Disintegration
Instrument: 10ml syringe one (internal diameter 1.5cm, outlet is positioned at the centre of syringe lower end); 50 mesh sieves.
Solvent: water
Algoscopy: get above-mentioned syringe 1, the rubber tube that exit, lower end cover has one section of 2cm long, and clamp with a tongs, to put on digestion instrument or disintegration tester and fixing, add in its upper end the water that 2ml temperature is 37 DEG C, the Lower Half of syringe to be immersed in 37 DEG C of thermostatic circulation baths in digestion instrument or disintegration tester constant temperature 5 minutes, add this product 1, start to record disintegration, and observe disintegrate situation, should complete disintegrate in 1 minute.Take out syringe, decontrol tongs, make solution by 50 eye mesh screens.Should all pass through.Measure 6 times all can in 1 minute disintegrate completely and all by 50 eye mesh screens.
Result of the test is as follows:
Result of the test shows, galanthamine hydrobromide oral cavity disintegration tablet prepared by the present invention is compared with reference examples: 1) yield is higher; 2) character zero difference; 3) stability is better; 4) disintegration is less.
Claims (2)
1. a galanthamine hydrobromide oral cavity disintegration tablet, it is composed as follows:
Galanthamine hydrobromide 4-6g,
Microcrystalline Cellulose 64-66g,
Low-substituted hydroxypropyl cellulose 9-11g,
Citric acid 5-7g,
Stevioside 2.7-2.9g,
Sodium bicarbonate 1.3-1.5g,
Magnesium stearate 0.7-0.9g,
Make 1000,
Further, the preparation method of above-mentioned galanthamine hydrobromide oral cavity disintegration tablet is: mixed by various component, adopts conventional tablet machines to carry out tabletting, to obtain final product.
2. a kind of galanthamine hydrobromide oral cavity disintegration tablet according to claim 1, it is composed as follows:
Galanthamine hydrobromide 4g,
Microcrystalline Cellulose 64g,
Low-substituted hydroxypropyl cellulose 9g,
Citric acid 5g,
Stevioside 2.7g,
Sodium bicarbonate 1.3g,
Magnesium stearate 0.7g,
Make 1000.
3. a kind of galanthamine hydrobromide oral cavity disintegration tablet according to claim 1, it is composed as follows:
Galanthamine hydrobromide 5g,
Microcrystalline Cellulose 65g,
Low-substituted hydroxypropyl cellulose 10g,
Citric acid 6g,
Stevioside 2.8g,
Sodium bicarbonate 1.4g,
Magnesium stearate 0.8g,
Make 1000.
4. a kind of galanthamine hydrobromide oral cavity disintegration tablet according to claim 1, it is composed as follows:
Galanthamine hydrobromide 5.5g,
Microcrystalline Cellulose 65.5g,
Low-substituted hydroxypropyl cellulose 10.5g,
Citric acid 6.5g,
Stevioside 2.85g,
Sodium bicarbonate 1.45g,
Magnesium stearate 0.85g,
Make 1000.
5. a kind of galanthamine hydrobromide oral cavity disintegration tablet according to claim 1, it is composed as follows:
Galanthamine hydrobromide 6g,
Microcrystalline Cellulose 66g,
Low-substituted hydroxypropyl cellulose 11g,
Citric acid 7g,
Stevioside 2.9g,
Sodium bicarbonate 1.5g,
Magnesium stearate 0.9g,
Make 1000.
6. a preparation method for galanthamine hydrobromide oral cavity disintegration tablet, comprises the various component mixing of arbitrary for claim 1-5 described galanthamine hydrobromide oral cavity disintegration tablet, adopts conventional tablet machines to carry out tabletting, to obtain final product.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210249186.5A CN103565761B (en) | 2012-07-19 | 2012-07-19 | Galanthamine hydrobromide orally disintegrating tablet |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210249186.5A CN103565761B (en) | 2012-07-19 | 2012-07-19 | Galanthamine hydrobromide orally disintegrating tablet |
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| Publication Number | Publication Date |
|---|---|
| CN103565761A CN103565761A (en) | 2014-02-12 |
| CN103565761B true CN103565761B (en) | 2015-03-25 |
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| CN201210249186.5A Active CN103565761B (en) | 2012-07-19 | 2012-07-19 | Galanthamine hydrobromide orally disintegrating tablet |
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Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN111012762B (en) * | 2019-11-05 | 2023-03-14 | 浙江工业大学 | Galanthamine hydrobromide oral instant film agent and preparation method thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1931140A (en) * | 2006-10-18 | 2007-03-21 | 耿燕 | Orally disintegrated galantamine hydrobromide tablet and its prepn process |
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1931140A (en) * | 2006-10-18 | 2007-03-21 | 耿燕 | Orally disintegrated galantamine hydrobromide tablet and its prepn process |
Non-Patent Citations (1)
| Title |
|---|
| 新型口服固体速释制剂-口腔速崩片;贺建昌等;《药学实践杂志》;20001231;第18卷(第3期);151-153 * |
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Effective date of registration: 20161020 Address after: 200131 China (Shanghai) free trade test area, Copernicus Lou, 1, Room 501 Patentee after: Shanghai Zhitong Medical Technology Co.,Ltd. Address before: 050035 No. 219, Taishan street, hi tech Industrial Development Zone, Hebei, Shijiazhuang Patentee before: Hebei Zhitong Pharmaceutical Group Co., Ltd. |