CN102784127A - Solid pharmaceutical composition, preparation method and application - Google Patents
Solid pharmaceutical composition, preparation method and application Download PDFInfo
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- CN102784127A CN102784127A CN201210112773XA CN201210112773A CN102784127A CN 102784127 A CN102784127 A CN 102784127A CN 201210112773X A CN201210112773X A CN 201210112773XA CN 201210112773 A CN201210112773 A CN 201210112773A CN 102784127 A CN102784127 A CN 102784127A
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Abstract
The invention relates to a solid pharmaceutical composition, a preparation method and an application. The invention relates to a solid pharmaceutical composition including repaglinide and its preparation method, and an application of the solid pharmaceutical composition for treating diabetes.
Description
Technical field
The present invention relates to a kind of solid composite medicament, especially comprise pharmaceutical composition of repaglinide and preparation method thereof, and the purposes in the treatment anti-diabetic.
Background technology
Diabetes are a kind of hyperglycemia, glucosuria, and with the chronic disease of multiple complications, are a kind of syndromes that is caused by the nature-nurture factor interaction, it is characterized by that insulin secretion lacks or opposing, or the hyperglycemia that both common defects caused.Show according to nearest Epidemiological study, the onset diabetes rate of China by 0.67% before 15 years rise in recent years 3.21%, wherein the type ii diabetes patient accounts for more than 95% of sum, and the men and women does not have significant difference.
It is reported that Chinese type 2 diabetes mellitus number of patients is that the whole world is maximum.2007 is 6,250 ten thousand people, is equivalent to the sum (4,850 ten thousand people) of the U.S., Europe and Japanese patients.Thereby research treatment diabetes medicament has significance and huge demand space.
Repaglinide is the benzoic derivant of methyl methylamine; Blood glucose new drug in the control agent when being first meal; It can obviously improve plasma insulin level, and the sugar that reduces the type ii diabetes patient closes hemoglobin (HbA1c) and post-prandial glycemia (PBG), is described as " blood sugar regulator used during user having meals ".Be early to secrete the medicine that disappearance is carried out effective control postprandial hyperglycemia of etiological treatment mutually to the patient.These article are developed jointly by Denmark Novo Nordisk Co.,Ltd and German Boehringer Ingelheim company.
Though but the existing preparation of repaglinide blood sugar control quickly, general duration of efficacy is short, can not realize the effect to diabetics blood sugar concentration Sustainable Control.
Summary of the invention
The object of the present invention is to provide a kind of taking convenience, more long lasting repaglinide compositions.
The object of the present invention is to provide a kind of pharmaceutical composition of repaglinide, comprise repaglinide, filler, binding agent, lubricant and other adjuvants.
Preferably, said preparation is a slow release.
The weight ratio scope of each component is in the said pharmaceutical composition: repaglinide 1%-10%; Filler 20%-50%; Binding agent 10%-25%; Lubricant 10%-30%; Other adjuvants 5%-40%.
Preferably, the weight ratio of each component is repaglinide 2%-5%, filler 30%-50%, binding agent 10%-20%, lubricant 10%-20%, other adjuvants 10%-30%.
In the said pharmaceutical composition, filler is selected from one or more in lactose, starch, hypromellose or the mannitol, preferred lactose or ethyl cellulose; Binding agent is selected from one or more in starch, dextrin, polyvinyl alcohol, polyvinylpyrrolidone or the carboxymethyl cellulose, preferably polyethylene ketopyrrolidine or hydroxy methocel; Lubricant is selected from one or more in glyceryl monostearate, magnesium stearate or the Pulvis Talci, preferred magnesium stearate; Other adjuvants can be correctives or disintegrating agent, the preferred hydroxypropyl emthylcellulose of disintegrating agent, Sodium Hydroxymethyl Stalcs.
Another object of the present invention also is to provide the purposes of said pharmaceutical composition in the treatment diabetes.
Description of drawings
Fig. 1 is that the drug accumulation of embodiment one preparation discharges the line of writing music.
Fig. 2 is that the drug accumulation of embodiment two preparations discharges the line of writing music.
Fig. 3 is that the drug accumulation of embodiment three preparations discharges the line of writing music.
Fig. 4 is that the drug accumulation of embodiment four preparations discharges the line of writing music.
Fig. 5 is that the drug accumulation of embodiment five preparations discharges the line of writing music.
The specific embodiment
To combine embodiment to come the present invention is done detailed description below, but content of the present invention is not limited thereto.
Embodiment 1 (1000)
Press recipe quantity and add above-mentioned each component; Repaglinide 6g wherein; Repaglinide, polyvinylpyrrolidone are prepared into solid dispersion according to solvent method, ground the back and cross 100 mesh sieves, add direct compression behind lactose, magnesium stearate, the Sodium Hydroxymethyl Stalcs mixing then.
Embodiment 2 (1000)
Press recipe quantity and add above-mentioned each component; Repaglinide 6g wherein; Repaglinide, polyvinylpyrrolidone are prepared into solid dispersion according to solvent method, ground the back and cross 100 mesh sieves, press behind recipe quantity adding hypromellose, Pulvis Talci, the sorbitol direct compression behind the mixing respectively.
Embodiment 3
After pressing recipe quantity adding repaglinide (6g), ethyl cellulose, hydroxy methocel, beta-schardinger dextrin-, Sodium Hydroxymethyl Stalcs mixing, add the magnesium stearate mixing, then direct compression.
Embodiment 4 (1000)
After pressing recipe quantity adding repaglinide (6g), ethyl cellulose, hydroxy methocel, beta-schardinger dextrin-, Sodium Hydroxymethyl Stalcs mixing, add the magnesium stearate mixing, then direct compression.
Embodiment 5 (1000)
The test of experimental example 1 dissolution
After pressing recipe quantity adding repaglinide (6g), ethyl cellulose, hydroxy methocel, beta-schardinger dextrin-, Sodium Hydroxymethyl Stalcs mixing, add the magnesium stearate mixing, then direct compression.
By " 2005 editions two appendix XD three therapeutic methods of traditional Chinese medicine of Chinese pharmacopoeia adopt the device of dissolution method (the appendix XC three therapeutic methods of traditional Chinese medicine), get each embodiment gained sample respectively, are release medium with the hydrochloric acid solution of 100ml0.1mol/L; Rotating speed is that per minute 50 changes, respectively at 1,2, and 4; 8,12,14; Got solution 5ml in 24 hours, adopt HPLC to carry out drug release determination, its result such as Fig. 1 are to shown in Figure 5.
The test of experimental example 2 preparation stabilities
Get embodiment 1-5 sample, place 40 ℃ of temperature respectively, make an experiment under relative humidity RH75% ± 10% condition, at duration of test, respectively at sampling in 0,3,6,9,12,18,24 month, the content of repaglinide in the test sample.
Content assaying method and result
Instrument: HPLC chromatograph of liquid
Chromatographic condition: chromatographic column: Kromasil C18 (200mm*4.6mm, 5um); Mobile phase: 0.05mol/L ammonium acetate buffer (the 3.85g ammonium acetate is dissolved in the 1000mL water, and using glacial acetic acid to regulate pH is 4.0)-methanol (20: 80); Flow velocity 1.0mL/min; Detect wavelength 243nm; Sample size 20 μ L.
The preparation of solution: get the tablet powder 10mg among the embodiment respectively, the accurate title, decide, and places the 100mL volumetric flask; With mobile phase dissolving and be diluted to scale, get this liquid 1.0mL, place the 20mL volumetric flask; Add mobile phase and be diluted to scale, shake up, as need testing solution.With Hengrui Medicine Co., Ltd., Jiangsu Prov.'s product batch number is that the refining repaglinide (content is 99.80) that forms of 990412 crude drug is as reference substance.
Prepare test sample, reference substance solution according to the method described above respectively, precision is measured 20uL injection chromatograph of liquid respectively, and the record peak area is pressed external standard method with calculated by peak area content.The result is as shown in the table:
Experimental result, from testing result, the dissolution of each embodiment sample and preparation stability all show preferable.
Claims (10)
1. a solid composite medicament comprises repaglinide, filler, binding agent, lubricant and other pharmaceutical carriers, and preferably, said preparation is a slow release.
2. solid composite medicament as claimed in claim 1 is characterized in that, the weight ratio scope of each component is: repaglinide 1%-10%, filler 20%-50%, binding agent 10%-25%, lubricant 10%-30%, other carriers 5%-40%.
3. solid composite medicament as claimed in claim 2 is characterized in that, the weight ratio of each component is repaglinide 2%-5%, filler 30%-50%, binding agent 10%-20%, lubricant 10%-20%, other carriers 10%-30%.
4. solid composite medicament as claimed in claim 3 is characterized in that said filler is selected from one or more in lactose, starch, hypromellose, ethyl cellulose or the mannitol, preferred lactose or ethyl cellulose.
5. solid composite medicament as claimed in claim 3 is characterized in that said binding agent is selected from one or more in starch, dextrin, polyvinyl alcohol, polyvinylpyrrolidone or the carboxymethyl cellulose, preferably polyethylene ketopyrrolidine or hydroxy methocel.
6. solid composite medicament as claimed in claim 3 is characterized in that said lubricant is selected from one or more in glyceryl monostearate, magnesium stearate or the Pulvis Talci, preferred magnesium stearate.
7. solid composite medicament as claimed in claim 3 is characterized in that, said other carriers can be correctives or disintegrating agent, preferred beta-schardinger dextrin-of correctives or sorbitol, the preferred hydroxypropyl emthylcellulose of disintegrating agent, Sodium Hydroxymethyl Stalcs.
8. a method for preparing like any described solid composite medicament of claim 1-7 comprises processing solid dispersion after repaglinide and the filler mixing, then tabletting after other components of mixing.
9. the method for preparing solid composite medicament as claimed in claim 8 is characterized in that, said solid dispersion adopts solvent method, fusion method, coprecipitation or fusion-solvent method.
10. like the purposes of any described solid composite medicament of claim 1-7 in the treatment diabetes.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210112773.XA CN102784127B (en) | 2011-05-20 | 2012-04-17 | Solid pharmaceutical composition, preparation method and application |
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| CN201110135802.X | 2011-05-20 | ||
| CN201110135802 | 2011-05-20 | ||
| CN201210112773.XA CN102784127B (en) | 2011-05-20 | 2012-04-17 | Solid pharmaceutical composition, preparation method and application |
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| Publication Number | Publication Date |
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| CN102784127A true CN102784127A (en) | 2012-11-21 |
| CN102784127B CN102784127B (en) | 2014-07-16 |
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| CN201210112773.XA Active CN102784127B (en) | 2011-05-20 | 2012-04-17 | Solid pharmaceutical composition, preparation method and application |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103690498A (en) * | 2013-12-18 | 2014-04-02 | 北京华禧联合科技发展有限公司 | Preparation method capable of improving stability of repaglinide tablets |
Citations (6)
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| US20040176457A1 (en) * | 2003-02-27 | 2004-09-09 | Hemmingsen Lisbeth Tofte | Novel NIDDM regimen |
| KR20080026754A (en) * | 2006-09-21 | 2008-03-26 | 주식회사 삼양사 | Release controlled particle comprising a biologically active substance, and preparing method thereof |
| CN101204394A (en) * | 2007-11-23 | 2008-06-25 | 杭州华东医药集团生物工程研究所有限公司 | Composite containing pioglitazone HCL and repaglinide |
| CN101695491A (en) * | 2009-10-20 | 2010-04-21 | 中国药科大学 | Slow-release preparation of repaglinide |
| CN101822672A (en) * | 2009-03-05 | 2010-09-08 | 深圳南方盈信制药有限公司 | Compound with metformin and repaglinide, preparation method thereof and application thereof |
| CN101843617A (en) * | 2010-03-05 | 2010-09-29 | 中国药科大学 | Slow release preparation of compound Repaglinide-metformin hydrochloride |
-
2012
- 2012-04-17 CN CN201210112773.XA patent/CN102784127B/en active Active
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20040176457A1 (en) * | 2003-02-27 | 2004-09-09 | Hemmingsen Lisbeth Tofte | Novel NIDDM regimen |
| KR20080026754A (en) * | 2006-09-21 | 2008-03-26 | 주식회사 삼양사 | Release controlled particle comprising a biologically active substance, and preparing method thereof |
| CN101204394A (en) * | 2007-11-23 | 2008-06-25 | 杭州华东医药集团生物工程研究所有限公司 | Composite containing pioglitazone HCL and repaglinide |
| CN101822672A (en) * | 2009-03-05 | 2010-09-08 | 深圳南方盈信制药有限公司 | Compound with metformin and repaglinide, preparation method thereof and application thereof |
| 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 |
Non-Patent Citations (1)
| Title |
|---|
| PATEL MANVI, ET AL.: "Preparation, Characterization and in Vitro Evaluation of Repaglinide Binary Solid Dispersions with Hydrophilic Polymers", 《INTERNATIONAL JOURNAL OF DRUG DEVELOPMENT & RESEARCH》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103690498A (en) * | 2013-12-18 | 2014-04-02 | 北京华禧联合科技发展有限公司 | Preparation method capable of improving stability of repaglinide tablets |
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| CN102784127B (en) | 2014-07-16 |
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Address after: 222000 Jiangsu province Lianyungang Kaitai Dapu Road Industrial Area Patentee after: JIANGSU HANSOH PHARMACEUTICAL GROUP LIANYUNGANG HONGCHUANG PHARMACEUTICAL CO., LTD. Address before: 222000 Jiangsu province Lianyungang Kaitai Dapu Road Industrial Area Patentee before: Jiangsu Hansoh Pharmaceutical Group Lianyungang Hongchuang Medical Co., Ltd. |
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Effective date of registration: 20160323 Address after: 222047 Lianyungang economic and Technological Development Zone, Jiangsu Patentee after: JIANGSU HANSOH PHARMACEUTICAL GROUP LIANYUNGANG HONGCHUANG PHARMACEUTICAL CO., LTD. Address before: 222000 Jiangsu province Lianyungang Kaitai Dapu Road Industrial Area Patentee before: JIANGSU HANSOH PHARMACEUTICAL GROUP LIANYUNGANG HONGCHUANG PHARMACEUTICAL CO., LTD. |