CN103690498A - Preparation method capable of improving stability of repaglinide tablets - Google Patents
Preparation method capable of improving stability of repaglinide tablets Download PDFInfo
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- CN103690498A CN103690498A CN201310697473.7A CN201310697473A CN103690498A CN 103690498 A CN103690498 A CN 103690498A CN 201310697473 A CN201310697473 A CN 201310697473A CN 103690498 A CN103690498 A CN 103690498A
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- repaglinide
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- magnesium stearate
- microcrystalline cellulose
- hydrogen phosphate
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Abstract
The invention discloses a repaglinide tablet composition. The composition comprises repaglinide, a diluting agent, a disintegrating agent, a solubilizer and a lubricant. The invention also discloses a preparation method of the repaglinide tablet composition, wherein powder is directly compressed into tablets, so that the influence of humidity on the product quality in the drying process can be avoided, the production operation is convenient, the content of related substances is low, and the stability is excellent.
Description
Technical field:
The invention belongs to field of pharmaceutical preparations, be specifically related to a kind of preparation method that improves repaglinide tablet stability.
Background technology:
Repaglinide is novel fugitive oral insulin secretion accelerating antidiabetic drug.Repaglinide stimulating pancreas uelralante reduces blood sugar level rapidly.This effect depends on the β of function cell in islets of langerhans.From the difference of other oral insulin secretion accelerating antidiabetic drug be repaglinide by the receptors bind with different to close ATP mono-dependent potassium channel in β cell membrane.It makes β cell depolarization, opens calcium channel, the inflow of calcium is increased.The secretion of insulin in this process induction β cell.Repaglinide (repaglinide, RG, trade name NovoNorm) be by German Novo Nordisk Co.,Ltd in 1998
the U.S.the take the lead in line oral antidiabetic drug for the treatment of type Ⅱdiabetes mellitus of listing can be simulated physiological insulin secretion in patient body, effectively controls post-prandial glycemia, have absorb fast, rapid-action, action time is short, do not increase patient
body weight, safe feature.Repaglinide has wide market prospect, and its medication frequency occupies the second in antidiabetic drug according to the literature, and medicine frequency speedup ranks first in conventional oral antidiabetic drug.
The repaglinide of listing is NovoNorm (import) and inspires confidence in and carry out enlightening (domestic) at home, there is family more than 20 in Yan producer, but it is the major technique obstacle in formulation and technology development process that the related substance of repaglinide preparation exceeds standard, the invention provides a kind of good stability, the tablet that its related substances is low, and can reach good blood sugar decreasing effect.
Summary of the invention
For the defect existing in prior art, an object of the present invention is to provide a kind of repaglinide, this repaglinide has very high stability, and drug effect is remarkable.
Another object of the present invention is that the preparation method of repaglinide is simplified.
For reaching above object, the technical solution used in the present invention is: a kind of repaglinide, and the component that this sheet contains following weight portion:
The supplementary material composition of repaglinide of the present invention is preferably as follows:
Repaglinide piece preparation method of the present invention is as follows:
1. repaglinide, calcium hydrogen phosphate, microcrystalline Cellulose, mannitol, carboxymethyl starch sodium, magnesium stearate, cosolvent are sieved, standby;
2. get repaglinide, calcium hydrogen phosphate, microcrystalline Cellulose, mannitol, carboxymethyl starch sodium, the cosolvent mix homogeneously of recipe quantity:
3. after adding magnesium stearate, again mix;
4. measure content of powder, determine sheet weight, tabletting.
The preparation method of repaglinide of the present invention is preferably as follows:
1. repaglinide, calcium hydrogen phosphate, microcrystalline Cellulose, mannitol, carboxymethyl starch sodium, magnesium stearate, cosolvent are crossed to 80-120 mesh sieve, standby;
2. the repaglinide, calcium hydrogen phosphate, microcrystalline Cellulose, mannitol, carboxymethyl starch sodium, cosolvent of getting recipe quantity is by the equivalent mode mix homogeneously that progressively increases: after adding magnesium stearate, again mix;
3. measure content of powder, determine sheet weight, tabletting.
Because the preparation technology of repaglinide provided by the invention is powder direct pressure closing, therefore, compare with wet granulation technology, have simple to operate, better stability of preparation, related substance low (in Table 1), thereby clinical more secure when used.
Table 1
By following test and embodiment, technical method of the present invention is further described, but not as limitation of the present invention.
Embodiment 1
Embodiment 1 preparation method:
1. repaglinide is crossed to 100 mesh sieves, calcium hydrogen phosphate, microcrystalline Cellulose, vertical compression lactose monohydrate, carboxymethyl starch sodium, magnesium stearate are crossed 80 mesh sieves, standby;
2. take repaglinide, calcium hydrogen phosphate, microcrystalline Cellulose, vertical compression lactose monohydrate, the carboxymethyl starch sodium of recipe quantity, by the equivalent method of progressively increasing, cross 60 mesh sieve mix homogeneously; The magnesium stearate mix homogeneously that adds again recipe quantity;
3. measure content of powder, determine sheet weight, tabletting.
Embodiment 2
Embodiment 2 preparation methoies:
1. repaglinide is crossed to 100 mesh sieves, calcium hydrogen phosphate, microcrystalline Cellulose, vertical compression mannitol, carboxymethyl starch sodium, magnesium stearate are crossed 80 mesh sieves, standby;
2. take repaglinide, calcium hydrogen phosphate, microcrystalline Cellulose, vertical compression mannitol, the carboxymethyl starch sodium of recipe quantity, by the equivalent method of progressively increasing, cross 60 mesh sieve mix homogeneously; The magnesium stearate mix homogeneously that adds again recipe quantity;
3. measure content of powder, determine sheet weight, tabletting.
Embodiment 3
Embodiment 3 preparation methoies:
1. repaglinide is crossed to 100 mesh sieves, calcium hydrogen phosphate, meglumine, microcrystalline Cellulose, vertical compression mannitol, carboxymethyl starch sodium, magnesium stearate are crossed 80 mesh sieves, standby;
2. take repaglinide, calcium hydrogen phosphate, meglumine, microcrystalline Cellulose, vertical compression mannitol, the carboxymethyl starch sodium of recipe quantity, by the equivalent method of progressively increasing, cross 60 mesh sieve mix homogeneously; The magnesium stearate mix homogeneously that adds again recipe quantity;
3. measure content of powder, determine sheet weight, tabletting.
Embodiment 4
Embodiment 4 preparation methoies:
1. Rui Gelie is crossed to 100 mesh sieves, calcium hydrogen phosphate, poloxamer, microcrystalline Cellulose, vertical compression mannitol, carboxymethyl starch sodium, magnesium stearate are crossed 80 mesh sieves, standby;
2. take repaglinide raw material, calcium hydrogen phosphate, poloxamer, microcrystalline Cellulose, vertical compression mannitol, the carboxymethyl starch sodium of recipe quantity, by the equivalent method of progressively increasing, cross 60 mesh sieve mix homogeneously; The magnesium stearate mix homogeneously that adds again recipe quantity;
3. measure content of powder, determine sheet weight, tabletting.
Embodiment 5
Embodiment 5 preparation methoies:
1. repaglinide is crossed to 100 mesh sieves, calcium hydrogen phosphate, meglumine, poloxamer, microcrystalline Cellulose, vertical compression mannitol, carboxymethyl starch sodium, magnesium stearate are crossed 80 mesh sieves, standby;
2. take repaglinide raw material, calcium hydrogen phosphate, meglumine, poloxamer, microcrystalline Cellulose, vertical compression mannitol, the carboxymethyl starch sodium of recipe quantity, by the equivalent method of progressively increasing, cross 60 mesh sieve mix homogeneously; The magnesium stearate mix homogeneously that adds again recipe quantity;
3. measure content of powder, determine sheet weight, tabletting.
Embodiment 6
Embodiment 6 preparation methoies:
1. repaglinide is crossed to 100 mesh sieves, calcium hydrogen phosphate, meglumine, poloxamer, microcrystalline Cellulose, vertical compression mannitol, carboxymethyl starch sodium, magnesium stearate are crossed 80 mesh sieves, standby;
2. take repaglinide, calcium hydrogen phosphate, meglumine, poloxamer, microcrystalline Cellulose, vertical compression mannitol, the carboxymethyl starch sodium of recipe quantity, by the equivalent method of progressively increasing, cross 60 mesh sieve mix homogeneously; The magnesium stearate mix homogeneously that adds again recipe quantity;
3. measure content of powder, determine sheet weight, tabletting.
Embodiment 7
Embodiment 7 preparation methoies:
1. repaglinide is crossed to 100 mesh sieves, calcium hydrogen phosphate, meglumine, poloxamer, microcrystalline Cellulose, vertical compression mannitol, carboxymethyl starch sodium, magnesium stearate are crossed 80 mesh sieves, standby;
2. take repaglinide, calcium hydrogen phosphate, meglumine, poloxamer, microcrystalline Cellulose, vertical compression mannitol, the carboxymethyl starch sodium of recipe quantity, by the equivalent method of progressively increasing, cross 60 mesh sieve mix homogeneously;
3. in the supplementary material mixing, add water, soft material processed, granulates, and 50 ℃ dry; Granulate, adds magnesium stearate mix homogeneously;
4. measure dry granule drug content, determine sheet weight, tabletting.
Each embodiment prescription, technique and related substance contrast:
From related substance and stability angle, contrast known powder vertical compression technique good.
Above-described embodiment just illustrates of the present invention, and the present invention also can implement with other ad hoc fashion or other particular form, and does not depart from main idea of the present invention or substitutive characteristics.Therefore, the embodiment of description all should be considered as illustrative but not determinate from the viewpoint of any.Scope of the present invention should illustrate by the claim of adding, and any and the intention of claim and the variation of scope equivalence also should be within the scope of the present invention.
Claims (6)
1. a repaglinide, is characterized in that: its adjuvant forms and comprises diluent, disintegrating agent, solubilizing agent, lubricant; Direct powder compression after raw material is mixed with adjuvant.
2. a kind of repaglinide claimed in claim 1, is characterized in that, repaglinide, calcium hydrogen phosphate, microcrystalline Cellulose, mannitol, carboxymethyl starch sodium, magnesium stearate, cosolvent are crossed to 80-120 mesh sieve, mix homogeneously, direct compression.
3. a kind of repaglinide claimed in claim 1, is characterized in that its supplementary material consists of:
4. a kind of repaglinide claimed in claim 1, is characterized in that, its supplementary material composition is preferably:
。
5. the repaglinide described in claim 1-2, is characterized in that, described cosolvent is glycerol, sodium lauryl sulphate, tween, span, PEG, meglumine, poloxamer.
6. repaglinide claimed in claim 5, is characterized in that, described cosolvent is preferably meglumine, poloxamer.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310697473.7A CN103690498A (en) | 2013-12-18 | 2013-12-18 | Preparation method capable of improving stability of repaglinide tablets |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201310697473.7A CN103690498A (en) | 2013-12-18 | 2013-12-18 | Preparation method capable of improving stability of repaglinide tablets |
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| CN201310697473.7A Pending CN103690498A (en) | 2013-12-18 | 2013-12-18 | Preparation method capable of improving stability of repaglinide tablets |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101548972A (en) * | 2008-04-03 | 2009-10-07 | 北京德众万全药物技术开发有限公司 | Solid pharmaceutical composition containing repaglinide |
| CN102267959A (en) * | 2011-07-06 | 2011-12-07 | 海南锦瑞制药股份有限公司 | Repaglinide crystal, preparation method thereof, and solid oral preparation containing same |
| CN102784127A (en) * | 2011-05-20 | 2012-11-21 | 江苏豪森医药集团连云港宏创医药有限公司 | Solid pharmaceutical composition, preparation method and application |
-
2013
- 2013-12-18 CN CN201310697473.7A patent/CN103690498A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101548972A (en) * | 2008-04-03 | 2009-10-07 | 北京德众万全药物技术开发有限公司 | Solid pharmaceutical composition containing repaglinide |
| CN102784127A (en) * | 2011-05-20 | 2012-11-21 | 江苏豪森医药集团连云港宏创医药有限公司 | Solid pharmaceutical composition, preparation method and application |
| CN102267959A (en) * | 2011-07-06 | 2011-12-07 | 海南锦瑞制药股份有限公司 | Repaglinide crystal, preparation method thereof, and solid oral preparation containing same |
Non-Patent Citations (1)
| Title |
|---|
| 丁钢等: "瑞格列奈片的制备和质量标准研究", 《广东药学院学报》 * |
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Application publication date: 20140402 |
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