CN104546778A - Medical composition of Gliclazide sustained release preparation and preparation method of medical composition - Google Patents
Medical composition of Gliclazide sustained release preparation and preparation method of medical composition Download PDFInfo
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- CN104546778A CN104546778A CN201410827178.3A CN201410827178A CN104546778A CN 104546778 A CN104546778 A CN 104546778A CN 201410827178 A CN201410827178 A CN 201410827178A CN 104546778 A CN104546778 A CN 104546778A
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- gliclazide
- hpmc
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- medical composition
- glyceryl behenate
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Abstract
The invention relates to a composition of a Gliclazide sustained release tablet. The composition comprises the following components: 15-25% of Gliclazide, 45-55% of dicalcium phosphate and 5-10% of docosanoic acid glyceride, which are added internally, and 5-10% of HPMC4M, 15-25% of HPMCK100lv, 0.2-0.5% of silicon dioxide, and 0.5-1% of magnesium stearate, which are added externally. The composition is characterized in that the docosanoic acid glyceride is adopted, so that the release degree of the Gliclazide sustained release tablet can be effectively controlled, and the stability is better.
Description
Technical field
The invention belongs to medical art, in particular to the application of Glyceryl Behenate in Gliclazide sustained-release tablet.
Background technology
Diabetes are one of modal chronic noninfective diseases, and current whole world diabetics exceedes 100,000,000, and type 2 diabetes mellitus accounts for the total crowd's of diabetes 90%.Diabetes are risk factors of cardiovascular disease, and relevant to its high case fatality rate.Britain perspective diabetes study (UKPDS) proves, hyperglycemia is one of principal element that diabetic vascular complications occurs.At present to make every effort to glycemic control, as far as possible close to normal level, so just can prevent or reduce the complication of diabetes in metabolism and blood vessel to the treatment of type 2 diabetes mellitus.Diet control and motion are the first-line treatment means of type 2 diabetes mellitus, but to many patients these methods alone, blood glucose is difficult Satisfactory Control still, therefore need the treatment of application hypoglycemic drug.Sulfonylurea drugs is oral antidiabetic drug the most frequently used at present, and its Main Function is the insulin secretion stimulating B cell, and hypoglycemic activity is that doctor and patient generally acknowledge.
Should admit that reducing blood sugar medicine is that good glycemic control has established solid foundation, but the difficulty that doctor faces is many patients can not adhere to the therapeutic scheme of repeatedly taking medicine that doctor specifies for a long time, and the poor compliance that patient takes medicine has become the major reason of crowd's poor blood glucose control.If only take the blood glucose that 1 medicine just can control whole day every day, then the present situation that glycemic control is good not may remarkable improvement.Gliclazide sustained-release tablet is the improvement novel form of gliclazide, employs hydrophilic matrix in making, and when oral 1 time of every day, active component can discharge in optimal manner, the secretion pattern of human insulin and blood sugar level is fluctuated and matches.Its absorption is not subject to the impact of pH in digestive tract and food.
Summary of the invention
Content of the present invention mainly Glyceryl Behenate is preparing the application on Gliclazide sustained-release tablet, and Glyceryl Behenate effectively can control the release of gliclazide, thus more effectively reaches slow release object.Moisture Control is below 2%, and stability is higher.Specifically, realize by the following method.
Described Gliclazide sustained-release tablet, comprises following drug component by weight:
table 1gliclazide medicine forms
1. adopt wet granulation and inside and outside add mode, reach the object effectively controlling gliclazide release, concrete preparation technology is as follows:
By gliclazide, Glyceryl Behenate, calcium hydrogen phosphate mix homogeneously, water soft material, dry, moisture Control, below 2%, adds other adjuvant, mix homogeneously, tabletting.
2. the advantage of this technique is that technique is simple, effectively can control the stripping in early stage of Gliclazide sustained-release tablet, and preparation stabilization.
3., in order to better interpretation the present invention, describe technical scheme of the present invention in detail with specific embodiment below, but the present invention is not limited to this.
Accompanying drawing explanation
fig. 1embodiment 1-3 with listing preparation diamicron at pH7.4 medium stripping curve In Vitro Dissolution curve
fig. 2embodiment 1-3 with listing preparation diamicron at aqueous medium stripping curve In Vitro Dissolution curve
fig. 3embodiment 1-3 with listing preparation diamicron at pH4.5 medium stripping curve In Vitro Dissolution curve
fig. 4embodiment 1-3 with listing preparation diamicron at pH1.0 medium stripping curve In Vitro Dissolution curve
Detailed description of the invention
Embodiment 1
1. prescription composition
2. preparation technology
Gliclazide, Glyceryl Behenate, calcium hydrogen phosphate mix homogeneously, water soft material, granulates, dry, controls moisture less than 2%, additional HPMC 4M, HPMC 100lv, silicon dioxide, magnesium stearate, mix homogeneously, tabletting.
Embodiment 2
1. prescription composition
Gliclazide, Glyceryl Behenate, calcium hydrogen phosphate mix homogeneously, water soft material, granulates, dry, controls moisture less than 2%, additional HPMC 4M, HPMC 100lv, silicon dioxide, magnesium stearate, mix homogeneously, tabletting.
Embodiment 3
1. prescription composition
2. preparation technology: gliclazide, HPMC K4M, calcium hydrogen phosphate mix homogeneously, water soft material, granulates, dry, controls moisture less than 2%, additional HPMC 4M, HPMC 100lv, silicon dioxide, magnesium stearate, mix homogeneously, tabletting.
With release profiles and related substance for evaluation index is entered it
row is investigated
Release compares
Embodiment 1-3 with
francethe diamicron that Shi Weiya company produces carries out vitro release and compares.Device according to drug release determination method (Chinese Pharmacopoeia version in 2010 two annex X D first methods) compares, pH7.4, water, pH4.5 and pH1.0 dissolution medium is adopted to carry out stripping curve coupling, stripping volume 900ml, rotating speed 100rpm, operates in accordance with the law, samples respectively at 1h, 2h, 4h, 6h, 8h, 12h, get 10ml, abandon 5ml, subsequent filtrate, as need testing solution, carries out ultraviolet detection.Separately get gliclazide reference substance appropriate, accurately weighed, after adding the dissolving of a small amount of acetonitrile, being diluted to concentration by release medium is the solution that every 1ml about contains 16 μ g, shakes up, in contrast product solution.Get need testing solution and reference substance solution, according to ultraviolet visible spectrophotometry (Chinese Pharmacopoeia version in 2010 two annex IV A), at 226nm, 290nm wavelength, place measures absorbance respectively, obtain the difference of 226nm and 290nm absorbance, calculate the burst size of every sheet at different time respectively.
table 1embodiment 1-3 and listing preparation diamicron are at pH7.4 medium stripping curve In Vitro Dissolution result (%)
| Diamicron | Embodiment 1 | Embodiment 2 | Embodiment 3 | |
| 0h | 0 | 0 | 0 | 0 |
| 1h | 12.57 | 19.35 | 9.77 | 20.32 |
| 2h | 24.81 | 29.24 | 20.77 | 34.73 |
| 4h | 51.65 | 56.92 | 42.86 | 44.82 |
| 6h | 73.37 | 73.41 | 66.50 | 66.86 |
| 8h | 87.64 | 85.02 | 80.05 | 85.76 |
| 12h | 99.37 | 95.38 | 88.78 | 97.04 |
| Similar factors f2 | — | 67 | 57 | 59 |
table 2embodiment 1-3 and listing preparation diamicron are at aqueous medium stripping curve In Vitro Dissolution result (%)
| Diamicron | Embodiment 1 | Embodiment 2 | Embodiment 3 | |
| 0h | 0 | 0 | 0 | 0 |
| 1h | 5.66 | 9.53 | 10.37 | 13.53 |
| 2h | 16.81 | 20.13 | 22.60 | 30.13 |
| 4h | 40.85 | 47.92 | 35.23 | 57.92 |
| 6h | 60.91 | 66.58 | 55.38 | 76.58 |
| 8h | 77.16 | 80.82 | 70.06 | 87.82 |
| 12h | 94.90 | 92.17 | 86.01 | 92.17 |
| Similar factors f2 | — | 66 | 59 | 46 |
table 3embodiment 1-3 and listing preparation diamicron are at pH4.5 medium stripping curve In Vitro Dissolution result (%)
| Diamicron | Embodiment 1 | Embodiment 2 | Embodiment 3 | |
| 0h | 0 | 0 | 0 | 0 |
| 1h | 3.90 | 6.48 | 8.05 | 15.34 |
| 2h | 9.69 | 16.96 | 15.40 | 25.44 |
| 4h | 25.80 | 27.99 | 21.07 | 39.76 |
| 6h | 42.25 | 47.80 | 33.27 | 59.86 |
| 8h | 59.99 | 65.22 | 50.01 | 73.12 |
| 12h | 80.22 | 77.34 | 70.34 | 83.06 |
| Similar factors f2 | — | 66 | 56 | 44 |
table 4embodiment 1-3 and listing preparation diamicron are at pH1.0 medium stripping curve In Vitro Dissolution result (%)
| Diamicron | Embodiment 1 | Embodiment 2 | Embodiment 3 | |
| 0 | 0 | 0 | 0 | 0 |
| 1 | 13.7 | 15.35 | 9.3 | 19.44 |
| 2 | 19.23 | 23.53 | 14.32 | 26.42 |
| 4 | 33.89 | 36.11 | 23.09 | 38.64 |
| 6 | 45.11 | 50.03 | 42.91 | 60.85 |
| 8 | 73.88 | 75.43 | 63.82 | 83.94 |
| 12 | 92.54 | 95.34 | 74.14 | 99.24 |
| Similar factors f2 | — | 74 | 50 | 51 |
F2 factorization method is the method for the similarity evaluating stripping curve, and the stripping curve f2 of self-control sample and reference preparation is greater than 50, then think that both are similar.By
table 1-4,
fig. 1-4 can find out, embodiment 1 stripping result is better than embodiment 2,3, more close with reference preparation.
Related substance compares
table 5embodiment 1-3 contrasts at high temperature 60 DEG C of related substances with listing preparation diamicron
By the contrast of embodiment 1,2,3 stripping data, embodiment 1 adopts the pharmaceutical composition of Glyceryl Behenate, and the stripping curve of four dissolution mediums is higher with reference preparation matching degree; By the contrast of embodiment 1,2,3 related substance, it is high that embodiment 2 impurity p-methylphenyl sulphonylamine increases relative embodiment 1,3, and it is fast that embodiment 3 impurity B increased comparatively embodiment 1 at 0 day, 10 days.
By the investigation of release and related substance, embodiment 1 adopts the pharmaceutical composition of Glyceryl Behenate, effectively can not only control the stripping of Gliclazide delayed-release preparation, and have good stability.
Claims (3)
1. a compositions for Gliclazide sustained-release tablet, is characterized in that: add part in blocker is present in, and is prepared into granule with active component and excipient, then with Extra Section mixed with excipients after tabletting; Inside add part and Extra Section composed as follows:
Inside add part
Gliclazide 15 ~ 25%
Calcium hydrogen phosphate 45 ~ 55%
Glyceryl Behenate 5 ~ 10%
Extra Section
HPMC K4M 5～10％
HPMC K100lv 15～25％
Silicon dioxide 0.2 ~ 0.5%
Magnesium stearate 0.5 ~ 1%.
2. Gliclazide sustained-release tablet according to claim 1, the blocker inside adding part can adopt in HPMC K4M, PVP K30, Glyceryl Behenate one or more.
3. the technique adopted according to claim 1 is wet granulation, its preparation technology is as follows: gliclazide, calcium hydrogen phosphate and Glyceryl Behenate mix homogeneously, water soft material, 30 orders are granulated, and dry, moisture Control is below 2%, 30 order granulate, add HPMC K4M, HPMC K100lv, silicon dioxide, magnesium stearate, mix homogeneously, tabletting.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201410827178.3A CN104546778A (en) | 2014-12-25 | 2014-12-25 | Medical composition of Gliclazide sustained release preparation and preparation method of medical composition |
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| CN201410827178.3A CN104546778A (en) | 2014-12-25 | 2014-12-25 | Medical composition of Gliclazide sustained release preparation and preparation method of medical composition |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110585155A (en) * | 2019-10-18 | 2019-12-20 | 山东鲁抗医药股份有限公司 | Gliclazide tablet (II) and preparation method thereof |
| CN111329841A (en) * | 2020-03-04 | 2020-06-26 | 山东鲁抗医药集团赛特有限责任公司 | Gliclazide sustained release tablet and preparation method thereof |
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| WO2006061697A1 (en) * | 2004-12-06 | 2006-06-15 | Themis Laboratories Private Limited | Sulfonylurea compositions and a process for its preparation |
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| EP2468268A1 (en) * | 2010-12-21 | 2012-06-27 | Sanovel Ilac Sanayi ve Ticaret A.S. | Combination composition of vildagliptin and gliclazide |
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2014
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Patent Citations (5)
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| WO2006061697A1 (en) * | 2004-12-06 | 2006-06-15 | Themis Laboratories Private Limited | Sulfonylurea compositions and a process for its preparation |
| CN1985819A (en) * | 2006-11-21 | 2007-06-27 | 北京润德康医药技术有限公司 | Slow released preparation containing metformin hydrochloride and gliclazide and its preparing process |
| EP2468268A1 (en) * | 2010-12-21 | 2012-06-27 | Sanovel Ilac Sanayi ve Ticaret A.S. | Combination composition of vildagliptin and gliclazide |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110585155A (en) * | 2019-10-18 | 2019-12-20 | 山东鲁抗医药股份有限公司 | Gliclazide tablet (II) and preparation method thereof |
| CN111329841A (en) * | 2020-03-04 | 2020-06-26 | 山东鲁抗医药集团赛特有限责任公司 | Gliclazide sustained release tablet and preparation method thereof |
| CN111329841B (en) * | 2020-03-04 | 2021-11-19 | 山东鲁抗医药集团赛特有限责任公司 | Gliclazide sustained release tablet and preparation method thereof |
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