CN103271888A - Pregabalin orally disintegrating tablet and dispersible tablet and preparation method thereof - Google Patents
Pregabalin orally disintegrating tablet and dispersible tablet and preparation method thereof Download PDFInfo
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- CN103271888A CN103271888A CN2013102411032A CN201310241103A CN103271888A CN 103271888 A CN103271888 A CN 103271888A CN 2013102411032 A CN2013102411032 A CN 2013102411032A CN 201310241103 A CN201310241103 A CN 201310241103A CN 103271888 A CN103271888 A CN 103271888A
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Abstract
The invention belongs to technical field of medicine, and particularly relates to a pregabalin orally disintegrating tablet and a dispersible tablet and the preparation method thereof. A prescription of the pregabalin orally disintegrating tablet and dispersible tablet contains at least one disintegrating agent and insoluble auxiliary material at a certain ratio, so that the disintegration time of six pregabalin orally disintegrating tablets is less than three minutes in one hundred ml of water at the temperature of 2o DEG C, while the disintegration time of pregabalin dispersible table is less than 30 seconds in 2 ml of water at the temperature of 24 DEG C. The bulk pharmaceutical chemicals of pregabalin orally disintegrating tablet and dispersible tablet are controlled in smaller grain size (74 to 250 microns). Combined with the technology of wet granulation, the problem of poor compressibility of pregabalin powder is solved. The solubility of pregabalin orally disintegrating tablet and dispersible tablet can reach more than 85 percent within 15 minutes in different PH mediums.
Description
Technical field
The invention belongs to medical technical field, be specifically related to lyrica oral cavity disintegration tablet and dispersible tablet and preparation method thereof.
Background technology
Lyrica is white crystalline powder, and pKa is 4.2 and 10.6, belongs to medicine soluble in water.Lyrica capsule 2004 is mainly used in treating diabetic peripheral neuralgia, herpes post herpetic neuralgia and auxiliary treatment epilepsy partial seizure in U.S.'s listing.Lyrica solution (20 mg/ml) 2010 mainly is applicable to and swallows inconvenient patient in U.S.'s listing.But the lyrica solution inconvenient patient carry, and do not help long preservation.
The taking and improve stability of drug of patient for convenience, the dispersible tablet that the present invention has developed lyrica is used for substituting the lyrica solution.For the accuracy that further helps to swallow inconvenient patient and improve administration, the present invention has developed the oral cavity disintegration tablet of lyrica.The compressibility of lyrica powder is relatively poor, and lyrica dispersible tablet and the oral cavity disintegration tablet of the present invention exploitation have overcome the relatively poor problem of lyrica compressibility, and makes their disintegration time meet the requirement of pharmacopeia.
Summary of the invention
The object of the present invention is to provide a kind of medicine stability good, patient carries, the lyrica dispersible tablet of taking convenience and oral cavity disintegration tablet and preparation method thereof.
Lyrica dispersible tablet provided by the invention refer to can be in aqueous medium fast disintegrate become the tablet of suspensoid, be used for oral administration.Lyrica oral cavity disintegration tablet provided by the invention refers to and can quick disintegrate be convenient to the tablet that patient swallows in mouth.Lyrica dispersible tablet provided by the invention and oral cavity disintegration tablet, constituent content is by weight in its prescription:
The lyrica medicine, 10%-50%,
Disintegrating agent, 5%-30%,
The slightly solubility adjuvant, 80%-20%,
All the other are adjuvant,
Total amount is 100%.
Among the present invention, described disintegrating agent is a kind of in polyvinylpolypyrrolidone, carboxymethyl starch sodium, the cross-linking sodium carboxymethyl cellulose etc. or wherein several, finds that by screening polyvinylpolypyrrolidone can make the disintegration time of lyrica dispersible tablet of the present invention and oral cavity disintegration tablet the shortest.
Among the present invention, described slightly solubility adjuvant comprises microcrystalline Cellulose, low-substituted hydroxypropyl cellulose etc.Contain water solublity adjuvant (as mannitol, lactose) in the tablet of water soluble drug more for a long time, and disintegration time mainly is to determine that by the corrosion of tablet we find to add some slightly solubility adjuvants can make disintegration time shorten.Optimal proportion can be screened by experiment by required release request.
Among the present invention, described adjuvant comprises: the correctives that tablet medicine is commonly used, fluidizer, lubricant, bulking agent (solubility adjuvant) etc.Wherein, correctives has sucralose, strawberry essence, citric acid etc.; Fluidizer has silicon dioxide etc.; Lubricant has sodium stearyl fumarate etc.; Bulking agent (solubility adjuvant) has mannitol etc.Adjuvant can add by selectivity.
The present invention is about the preparation method of lyrica oral cavity disintegration tablet or dispersible tablet, and concrete steps are:
1. with lyrica, inner phase (comprising the part correctives, bulking agent (solubility adjuvant), bulking agent (slightly solubility adjuvant) and disintegrating agent) mixes in wet granulator;
2. adding an amount of water granulates;
3. sieve behind the particle drying of Huo Deing;
Granule after 4. sieving and other foreign ministers (comprise remaining correctives, bulking agent (solubility adjuvant), bulking agent (slightly solubility adjuvant), disintegrating agent, and fluidizer and lubricant) mix;
5. final mixture obtains the tablet of required hardness with the punch die tabletting of 12mm.
In the above-mentioned preparation process, the part bulking agent in the inner phase (slightly solubility adjuvant) and the amount of disintegrating agent are generally decided as required, and the 40--60% that is respectively these component total amounts usually is advisable.Correctives, bulking agent (solubility adjuvant) can distribute arbitrarily.
The compressibility of lyrica powder is relatively poor, but the crude drug of the technology by wet granulation and control dispersible tablet and oral cavity disintegration tablet is at smaller particle diameter (74-250 μ m), can success overcome this problem.Final lyrica dispersible tablet and oral cavity disintegration tablet are the circular piece of 10-15mm.The hardness of 150mg lyrica sheet oral cavity disintegration tablet is between 25-90N, and the hardness of 150mg lyrica dispersible tablet is between 60-130N.
Lyrica dispersible tablet of the present invention (6) disintegration time in the water of 20 ℃ of 100ml is less than 3 minutes, and lyrica oral cavity disintegration tablet disintegration time in the water of 24 ℃ of 2ml is less than 30 seconds.Preparation has good stable.Lyrica dispersible tablet of the present invention and the stripping of oral cavity disintegration tablet in different pH medium can reach greater than 85% in 15 minutes.
Description of drawings
Fig. 1 is the lyrica oral cavity disintegration tablet, lyrica capsule and the solution stripping curve (50rpm oar method) in the 900mlpH1.2 medium.
Fig. 2 is the lyrica oral cavity disintegration tablet, lyrica capsule and the solution stripping curve (50rpm oar method) in the 900mlpH4.5 acetate buffer solution.
Fig. 3 is the lyrica oral cavity disintegration tablet, lyrica capsule and the solution stripping curve (50rpm oar method) in the 900mlpH6.8 phosphate buffer.
Fig. 4 is the stripping curve (50rpm oar method) of lyrica oral cavity disintegration tablet stability sample in the 900mlpH1.2 medium.
The specific embodiment
Below by specific embodiment, further introduce the inventive method.Example 1 is the lyrica oral cavity disintegration tablet, and example 2 is the lyrica dispersible tablet.
Embodiment
1.The lyrica oral cavity disintegration tablet
The prescription of lyrica oral cavity disintegration tablet sees Table 1:
The prescription of table 1 lyrica oral cavity disintegration tablet:
Preparation method:
1. lyrica, sucralose, mannitol, citric acid, microcrystalline Cellulose and polyvinylpolypyrrolidone mix in wet granulator;
2. adding an amount of water granulates;
3. sieve behind the particle drying of Huo Deing;
4. the granule after sieving and other foreign ministers (strawberry essence, mannitol, microcrystalline Cellulose, polyvinylpolypyrrolidone, silicon dioxide and sodium stearyl fumarate) mix;
5. final mixture obtains the tablet of required hardness with the punch die tabletting of 12mm.
Disintegration time research
Disintegration time is an important indicator of oral cavity disintegration tablet.Lyrica oral cavity disintegration tablet of the present invention disintegration time 14 seconds in 30 ℃ of 900ml water, disintegration time is 15 seconds in 24 ℃ of 2ml water, meets American Pharmacopeia to the requirement of oral cavity disintegration tablet.In the tablet of water soluble drug (lyrica), contain the water solublity adjuvant (as mannitol, lactose) more for a long time, disintegration time mainly is to determine that by the corrosion of tablet we find to add some slightly solubility adjuvants (microcrystalline Cellulose) can make disintegration time shorten.The amount of microcrystalline Cellulose is from 0mg in prescription, and when 172.5mg was increased to 227.5mg, lyrica oral cavity disintegration tablet disintegration time had dropped to 15 seconds from 34,31 seconds (seeing Table 2).
The amount of table 2 microcrystalline Cellulose is to the influence of lyrica oral cavity disintegration tablet disintegration time
Stripping curve
The lyrica oral cavity disintegration tablet compares (seeing Fig. 1,2,3) at the stripping curve of different pH (1.2,4.5 and 6.8) and the stripping of lyrica solution and lyrica capsule.The lyrica oral cavity disintegration tablet can reach greater than 85% in 15 minutes in the medium of different pH, and is suitable with the release of lyrica solution.
Stability study
The lyrica oral cavity disintegration tablet is stored in and investigates stability under the condition of 40oC and 75% relative humidity.The disintegration time of 1 month stability sample sees Table 3.Stability sample was seen Fig. 4 at the stripping curve of pH1.2 in 1 month.The result shows that the lyrica oral cavity disintegration tablet is stable under one month accelerated test.
The disintegration time (second) of table 3 lyrica oral cavity disintegration tablet stability sample in 30 ℃ of 900ml water
Embodiment
2.The lyrica dispersible tablet
The constituent of lyrica dispersible tablet sees Table 4, and it and commercially available lyrica solution have certain similarity, can replace the lyrica solution.
The constituent of table 4 lyrica dispersible tablet
Preparation method:
1. lyrica, sucralose, mannitol, citric acid, microcrystalline Cellulose and polyvinylpolypyrrolidone mix in wet granulator;
2. adding an amount of water granulates;
3. sieve behind the particle drying of Huo Deing;
4. the granule after sieving and other foreign ministers (strawberry essence, mannitol, microcrystalline Cellulose, polyvinylpolypyrrolidone, silicon dioxide and sodium stearyl fumarate) mix;
5. final mixture obtains the tablet of required hardness with the punch die tabletting of 12mm.
Disintegration time research
Disintegration time also is an important indicator of dispersible tablet.Lyrica dispersible tablet of the present invention disintegration time in 22 ℃ of 900ml water is ~ 24 seconds, and disintegration time is ~ 75 seconds (6) in 20 ℃ of 100ml water, meets European Pharmacopoeia to the requirement of dispersible tablet.
Stability study
The lyrica dispersible tablet is stored in and investigates stability under the condition of 40oC and 75% relative humidity.The disintegration time of 1 month stability sample sees Table 5.The result shows that the lyrica dispersible tablet is stable under one month accelerated test.
The disintegration time (second) of table 5 lyrica dispersible tablet stability sample in 22 ℃ of 900ml water
Claims (4)
1. a lyrica dispersible tablet or oral cavity disintegration tablet is characterized in that constituent content is by weight in the prescription:
The lyrica medicine, 10%-50%,
Disintegrating agent, 5%-30%,
The slightly solubility adjuvant, 80%-20%,
All the other are adjuvant,
Total amount is 100%;
Described disintegrating agent is a kind of in polyvinylpolypyrrolidone, carboxymethyl starch sodium, the cross-linking sodium carboxymethyl cellulose or wherein several;
Described slightly solubility adjuvant is microcrystalline Cellulose, low-substituted hydroxypropyl cellulose;
Described adjuvant comprises: correctives, fluidizer, lubricant, solubility adjuvant.
2. lyrica dispersible tablet according to claim 1 or oral cavity disintegration tablet is characterized in that described correctives is selected from sucralose, strawberry essence, citric acid; Described fluidizer is selected silicon dioxide for use; Described lubricant is selected sodium stearyl fumarate for use; The solubility adjuvant is selected mannitol for use.
3. the preparation method of a lyrica dispersible tablet as claimed in claim 1 or oral cavity disintegration tablet is characterized in that concrete steps are:
(1) with lyrica, inner phase mixes in wet granulator; Described inner phase is part correctives, solubility adjuvant, slightly solubility adjuvant and disintegrating agent;
(2) adding an amount of water granulates;
(3) sieve behind the particle drying of Huo Deing;
(4) granule after sieving and foreign minister mix; Described foreign minister comprises remaining correctives, solubility adjuvant, slightly solubility adjuvant, disintegrating agent, and fluidizer and lubricant;
(5) final mixture obtains the tablet of required hardness with the punch die tabletting of 12mm.
4. the preparation method of lyrica dispersible tablet according to claim 3 or oral cavity disintegration tablet, the amount of part slightly solubility adjuvant in the inner phase and disintegrating agent that it is characterized in that is respectively the 40--60% of these component total amounts.
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| CN2013102411032A CN103271888A (en) | 2013-06-18 | 2013-06-18 | Pregabalin orally disintegrating tablet and dispersible tablet and preparation method thereof |
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Cited By (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3130355A4 (en) * | 2014-04-07 | 2017-12-20 | Yungjin Pharmaceutical Co., Ltd. | Pharmaceutical composition containing pregabalin with improved stability and method for preparing same |
| CN109125287A (en) * | 2018-10-25 | 2019-01-04 | 千辉药业（安徽）有限责任公司 | A kind of Pregabalin tablet and preparation method thereof |
| JP2019052147A (en) * | 2017-09-13 | 2019-04-04 | 大原薬品工業株式会社 | Pregabalin-containing orally disintegrating tablet with improved chemical stability |
| CN110613689A (en) * | 2018-06-19 | 2019-12-27 | 北京万全德众医药生物技术有限公司 | Orally disintegrating tablet containing amphiphilic polymer-pregabalin compound |
| CN110742868A (en) * | 2019-11-20 | 2020-02-04 | 合肥拓锐生物科技有限公司 | Mirogabalin Besilate orally disintegrating tablet |
| JP2020045367A (en) * | 2018-06-13 | 2020-03-26 | 大原薬品工業株式会社 | Intraoral disintegrable tablet that includes flavoring agent-containing granules and can be more easily taken |
| CN111939133A (en) * | 2019-05-16 | 2020-11-17 | 鲁南制药集团股份有限公司 | Zolpidem tartrate tablet and preparation method thereof |
| CN112107550A (en) * | 2019-06-19 | 2020-12-22 | 北京万全德众医药生物技术有限公司 | Pregabalin orally disintegrating tablet preparation and preparation method thereof |
| CN112121020A (en) * | 2019-06-24 | 2020-12-25 | 北京万全德众医药生物技术有限公司 | Preparation method of pregabalin orally disintegrating tablet |
| CN114469880A (en) * | 2022-02-21 | 2022-05-13 | 广州帝奇医药技术有限公司 | Pregabalin composition suitable for powder tabletting and application thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1806800A (en) * | 2006-02-23 | 2006-07-26 | 北京阜康仁生物制药科技有限公司 | Pharmaceutical composition making pregabalin as active ingredient, its preparation method and uses |
| CN1827095A (en) * | 2006-04-14 | 2006-09-06 | 北京润德康医药技术有限公司 | Pharmaceutical composition using pregabalin as active ingredient, its preparation method and use |
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2013
- 2013-06-18 CN CN2013102411032A patent/CN103271888A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1806800A (en) * | 2006-02-23 | 2006-07-26 | 北京阜康仁生物制药科技有限公司 | Pharmaceutical composition making pregabalin as active ingredient, its preparation method and uses |
| CN1827095A (en) * | 2006-04-14 | 2006-09-06 | 北京润德康医药技术有限公司 | Pharmaceutical composition using pregabalin as active ingredient, its preparation method and use |
Cited By (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3130355A4 (en) * | 2014-04-07 | 2017-12-20 | Yungjin Pharmaceutical Co., Ltd. | Pharmaceutical composition containing pregabalin with improved stability and method for preparing same |
| JP2019052147A (en) * | 2017-09-13 | 2019-04-04 | 大原薬品工業株式会社 | Pregabalin-containing orally disintegrating tablet with improved chemical stability |
| JP2020045367A (en) * | 2018-06-13 | 2020-03-26 | 大原薬品工業株式会社 | Intraoral disintegrable tablet that includes flavoring agent-containing granules and can be more easily taken |
| CN110613689A (en) * | 2018-06-19 | 2019-12-27 | 北京万全德众医药生物技术有限公司 | Orally disintegrating tablet containing amphiphilic polymer-pregabalin compound |
| CN109125287A (en) * | 2018-10-25 | 2019-01-04 | 千辉药业（安徽）有限责任公司 | A kind of Pregabalin tablet and preparation method thereof |
| CN111939133A (en) * | 2019-05-16 | 2020-11-17 | 鲁南制药集团股份有限公司 | Zolpidem tartrate tablet and preparation method thereof |
| CN112107550A (en) * | 2019-06-19 | 2020-12-22 | 北京万全德众医药生物技术有限公司 | Pregabalin orally disintegrating tablet preparation and preparation method thereof |
| CN112121020A (en) * | 2019-06-24 | 2020-12-25 | 北京万全德众医药生物技术有限公司 | Preparation method of pregabalin orally disintegrating tablet |
| CN110742868A (en) * | 2019-11-20 | 2020-02-04 | 合肥拓锐生物科技有限公司 | Mirogabalin Besilate orally disintegrating tablet |
| CN114469880A (en) * | 2022-02-21 | 2022-05-13 | 广州帝奇医药技术有限公司 | Pregabalin composition suitable for powder tabletting and application thereof |
| WO2023155682A1 (en) * | 2022-02-21 | 2023-08-24 | 广州帝奇医药技术有限公司 | Pregabalin composition suitable for powder tableting and use thereof |
| CN114469880B (en) * | 2022-02-21 | 2024-02-02 | 广州帝奇医药技术有限公司 | Pregabalin composition suitable for powder tabletting and application thereof |
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Application publication date: 20130904 |