CN103027900B - Repaglinide tablet and preparation method thereof - Google Patents
Repaglinide tablet and preparation method thereof Download PDFInfo
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- CN103027900B CN103027900B CN201210369291.2A CN201210369291A CN103027900B CN 103027900 B CN103027900 B CN 103027900B CN 201210369291 A CN201210369291 A CN 201210369291A CN 103027900 B CN103027900 B CN 103027900B
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Abstract
The invention relates to a repaglinide tablet and a preparation method thereof. The repaglinide tablet comprises repaglinide, starch, microcrystalline cellulose, magnesium stearate, sodium bicarbonate and an adhesive according to the weight percentage of 1:(30-50):(15-20):(0.1-0.5):(1-2):(0.1-1). The repaglinide tablet disclosed by the invention has excellent slow-release effect and dissolution rate and also has good preparation stability.
Description
Technical field
The present invention relates to a kind of pharmaceutical composition for the treatment of diabetes, relate in particular to a kind of repaglinide tablet and preparation method thereof.
Background technology
Diabetes are a kind of hyperglycemia, glucosuria, and with the chronic disease of multiple complications, are a kind of syndromes being caused by nature-nurture factor interaction, it is characterized by that insulin secretion lacks or opposing, or the hyperglycemia that causes of both common defects.According to nearest Epidemiological study, show, the onset diabetes rate of China by 0.67% before 15 years rise in recent years 3.21%, wherein type ii diabetes patient accounts for the more than 95% of sum, and men and women is without significant difference.
It is reported, Type 2 Diabetes In China number of patients is that the whole world is maximum.Within 2007, be 6,250 ten thousand people, be equivalent to the sum (4,850 ten thousand people) of the U.S., Europe and Japanese patients.Thereby, research treatment diabetes medicament important in inhibiting and huge demand space.
Repaglinide is the benzoic derivant of methyl methylamine, blood glucose new drug in control agent while being first meal, it can obviously improve plasma insulin level, and the sugar that reduces type ii diabetes patient closes hemoglobin (HbA1c) and post-prandial glycemia (PBG), is described as " blood sugar regulator used during user having meals ".Early to secrete mutually for patient the medicine that disappearance is carried out effective control postprandial hyperglycemia of etiological treatment.Gai Pinyou Denmark Novo Nordisk Co.,Ltd and German Boehringer Ingelheim company develop jointly.
Although but the existing preparation of repaglinide can be controlled blood glucose quickly, general duration of efficacy is short, can not realize the effect to blood sugar in diabetic patients concentration Sustainable Control.And the dissolubility of repaglinide is low, bioavailability is poor, so also will consider how to improve its dissolution during Formulation.
Summary of the invention
The object of the invention is to solve the problems of the technologies described above, a kind of taking convenience, the more long-acting and better repaglinide tablet of preparation stability are provided.
The object of the present invention is to provide a kind of repaglinide tablet, comprise repaglinide, starch, microcrystalline Cellulose, magnesium stearate, sodium bicarbonate and binding agent, in described tablet, each weight percentages of components is repaglinide: starch: microcrystalline Cellulose: magnesium stearate: sodium bicarbonate: binding agent=1:30-50:15-20:0.1-0.5:1-2:0.1-1.
Preferably, stating each weight percentages of components in tablet is repaglinide: starch: microcrystalline Cellulose: magnesium stearate: sodium bicarbonate: binding agent=1:30:15:0.2:1:0.5.
Preferably, described binding agent is selected from hydroxypropyl methylcellulose, PVP K30, K25.
The present invention also aims to provide a kind of method of preparing repaglinide tablet, comprise that (1) mixes repaglinide, starch, microcrystalline Cellulose, sodium bicarbonate by equivalent incremental method; (2) add binding agent and prepare soft material, sieve; (3) after dry, add magnesium stearate, mix rear tabletting.
Inventor's discovery, tablet of the present invention detects and study on the stability through release, has good sustained release ability and dissolution performance, and better stability of preparation.
Accompanying drawing explanation
Fig. 1 is embodiment 1 sample release profiles.
Fig. 2 is embodiment 2 sample release profiles.
Fig. 3 is embodiment 5 sample release profiles.
The specific embodiment
Below in conjunction with embodiment, the present invention is described in detail, but content of the present invention is not limited to this.
Embodiment 1(1000 sheet)
By recipe quantity, add above-mentioned each component, repaglinide, starch, microcrystalline Cellulose, sodium bicarbonate are mixed according to equivalent incremental method, add recipe quantity hydroxypropyl methylcellulose to prepare soft material, cross 24 mesh sieves and granulate.60 ℃ of dry 3h granulate, add magnesium stearate, mix rear tabletting.
Embodiment 2(1000 sheet)
By recipe quantity, add above-mentioned each component, repaglinide, starch, microcrystalline Cellulose, sodium bicarbonate are mixed according to equivalent incremental method, add recipe quantity PVP K30 to prepare soft material, cross 24 mesh sieves and granulate.60 ℃ of dry 3h granulate, add magnesium stearate, mix rear tabletting.
Embodiment 3(1000 sheet)
By recipe quantity, add above-mentioned each component, repaglinide, starch, microcrystalline Cellulose, sodium bicarbonate are mixed according to equivalent incremental method, add recipe quantity hydroxypropyl methylcellulose to prepare soft material, cross 24 mesh sieves and granulate.60 ℃ of dry 3h granulate, add magnesium stearate, mix rear tabletting.
By following formula preparation embodiment 4-7 tablet (each 1000), preparation method reference example 1.
| Prescription | Embodiment 4 | Embodiment 5 | Embodiment 6 | Embodiment 7 |
| Repaglinide | 5g | 5g | 5g | 5g |
| Starch | 150g | 150g | 200g | 250g |
| Microcrystalline Cellulose | 75g | 75g | 100g | 100g |
| Magnesium stearate | 1g | 1g | 1g | 1g |
| Sodium bicarbonate | 7.5g | 0 | 5g | 10g |
| Hydroxypropyl methylcellulose | 2.5g | 2.5g | 5g | 2.5g |
Experimental example 1 drug release determination
According to 2005 editions two appendix XD the 3rd methods of < < Chinese Pharmacopoeia > >, adopt the device of dissolution method (appendix XC the 3rd method), get the sample that embodiment 1, embodiment 2, embodiment 5 make, the hydrochloric acid solution of 100ml0.1mol/L of take is release medium, rotating speed is per minute 50 to turn, respectively at 2,4,8, within 12,24 hours, get solution 5ml, add the fresh medium of uniform temp, same volume simultaneously, institute's sample thief filters immediately, gets subsequent filtrate and measures.Get reference substance appropriate, by external standard method, calculate release.Release result as Figure 1-3.
From dissolution testing result, can find out, each formulation samples all can play good slow release effect, there is good Stable Release effect, wherein the slow release effect of embodiment 1 and embodiment 2 and dissolution all show excellence, in 24 hours, cumulative release all reaches 100%, the cumulative release degree of embodiment 5 is not good enough, within 24 hours, only discharges 80%.
Experimental example 2 stability experiments
Get embodiment 1, embodiment 2 and the prepared tablet samples of embodiment 5, under packing (aluminum-plastic packaged, to put in carton) condition, in 40 ℃, RH75% places 6 months, and in 0.5,1, sampling in the time of 3,6 months, investigates working sample stability, and result is as shown in table 1:
Table 1:40 ℃, RH75% accelerated stability experimental result
As can be seen from the table, embodiment 1 and embodiment 2 sample stabilities are good, and embodiment 5 relative stabilitys are poor.
Claims (3)
1. a repaglinide tablet, comprise repaglinide, starch, microcrystalline Cellulose, magnesium stearate, sodium bicarbonate and binding agent, in described tablet, each weight percentages of components is repaglinide: starch: microcrystalline Cellulose: magnesium stearate: sodium bicarbonate: binding agent=1:30:15:0.2:1:0.5.
2. repaglinide tablet as claimed in claim 1, is characterized in that, described binding agent is selected from hydroxypropyl methylcellulose, PVP K30, K25.
3. a method of preparing repaglinide tablet as described in claim 1-2 any one, comprises that (1) mixes repaglinide, starch, microcrystalline Cellulose, sodium bicarbonate by equivalent incremental method; (2) add binding agent and prepare soft material, sieve; (3) after dry, add magnesium stearate, mix rear tabletting.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201210369291.2A CN103027900B (en) | 2012-09-27 | 2012-09-27 | Repaglinide tablet and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210369291.2A CN103027900B (en) | 2012-09-27 | 2012-09-27 | Repaglinide tablet and preparation method thereof |
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| CN103027900A CN103027900A (en) | 2013-04-10 |
| CN103027900B true CN103027900B (en) | 2014-12-03 |
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| CN103432092B (en) * | 2013-08-07 | 2015-09-16 | 北京康立生医药技术开发有限公司 | A kind of slow releasing preparation of repaglinide |
| CN115154432B (en) * | 2022-07-22 | 2023-03-24 | 北京惠之衡生物科技有限公司 | Repaglinide tablet and preparation method thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101695491A (en) * | 2009-10-20 | 2010-04-21 | 中国药科大学 | Slow-release preparation of repaglinide |
| CN101843617A (en) * | 2010-03-05 | 2010-09-29 | 中国药科大学 | Slow release preparation of compound Repaglinide-metformin hydrochloride |
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101695491A (en) * | 2009-10-20 | 2010-04-21 | 中国药科大学 | Slow-release preparation of repaglinide |
| CN101843617A (en) * | 2010-03-05 | 2010-09-29 | 中国药科大学 | Slow release preparation of compound Repaglinide-metformin hydrochloride |
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Address after: 222047 Lianyungang economic and Technological Development Zone, Jiangsu Patentee after: JIANGSU HANSOH PHARMACEUTICAL GROUP Co.,Ltd. Address before: 222047 Lianyungang economic and Technological Development Zone, Jiangsu Patentee before: Jiangsu best Pharmaceutical Co.,Ltd. Address after: 222047 Lianyungang economic and Technological Development Zone, Jiangsu Patentee after: Jiangsu best Pharmaceutical Co.,Ltd. Address before: 222047 Lianyungang economic and Technological Development Zone, Jiangsu Patentee before: JIANGSU HANSOH PHARMACEUTICAL Co.,Ltd. |