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Gliclazide sustained-release tablets

A technology for gliclazide and sustained-release tablets, which is applied in the field of gliclazide sustained-release tablets and their preparation, can solve the problems of reaching a very high blood drug concentration, low medication compliance of patients, and many daily doses, and the like. The effect of stable drug release rate, good drug stability and high bioavailability

Active Publication Date: 2017-11-24
浙江康德药业集团股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

CN101744781A discloses a gliclazide dispersible tablet, which adopts a dry granulation process; the tablet can disintegrate rapidly after oral administration, and has the characteristics of convenient taking, fast absorption and high bioavailability, but due to its rapid disintegration, absorption The rapidity of the drug also causes the drug to reach a high blood concentration in the body in a short period of time, which can easily cause hypoglycemia. In addition, it also has the disadvantage of taking more times a day
The preparation is prepared by adding citric acid and polyvinyl acetate to gliclazide. Polyvinyl acetate is widely used in sustained-release preparations, causing the side effects of gliclazide to gradually appear, mainly affecting the human stomach. Intestinal irritating effect, especially when taken on an empty stomach, can easily cause reactions such as nausea, vomiting, and diarrhea, resulting in low compliance of patients with medication, and also restricting the use of many patients

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1 Meglumine dosage screening test

[0029] Weigh glyceryl behenate, divide it into 6 equal portions, 90g each, heat to 65-70°C to melt respectively, add meglumine 1, 2, 4, 8, 12, 16g, under the condition of keeping warm at 65-70°C, add 30g of gliclazide respectively, stir for 60min with an electric stirrer, and observe whether the gliclazide melts.

[0030] Table 1: Meglumine Dosage Screening

[0031] Meglumine Dosage

Embodiment 2

[0032] Preparation of Embodiment 2 Gliclazide Sustained-release Tablets

[0033]

[0034] Preparation Process:

[0035] ①Take glyceryl behenate, heat to 65-70°C to melt, keep warm and add the prescribed amount of meglumine while stirring;

[0036] ②Continue to keep warm at 65-70°C, add gliclazide at the same time, use an electric stirrer to stir for more than 30 minutes until it melts, quickly put it into ice-water mixture to solidify, and put it in a desiccator to dry after it is completely solidified, and the drying temperature is lower than 60 ℃, drying time is 2h, grind, and pass through 80 mesh sieve to obtain drug-loaded granules;

[0037] ③Mix the drug-loaded granules with the prescribed amount of mannitol (passed through a 100-mesh sieve) and magnesium stearate evenly, and press into tablets, Φ9mm punched tablets, and control the hardness within the range of 40-60N.

Embodiment 3

[0038] Preparation of Example 3 Gliclazide Sustained-release Tablets

[0039]

[0040]

[0041] Preparation Process:

[0042]①Take glyceryl behenate, heat to 65-70°C to melt, keep warm and add the prescribed amount of meglumine while stirring;

[0043] ②Continue to keep warm at 65-70°C, add gliclazide at the same time, use an electric stirrer to stir for more than 30 minutes until it melts, quickly put it into ice-water mixture to solidify, and put it in a desiccator to dry after it is completely solidified, and the drying temperature is lower than 60 ℃, drying time is 2h, grind, and pass through 80 mesh sieve to obtain drug-loaded granules;

[0044] ③Mix the drug-loaded granules with the prescribed amount of mannitol (passed through a 100-mesh sieve) and magnesium stearate evenly, and press into tablets, Φ9mm punched tablets, and control the hardness within the range of 40-60N.

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Abstract

The invention discloses gliclazide sustained-release tablets, which are prepared by evenly mixing drug-loading particles with pharmaceutically acceptable adjuvant materials and tabletting the obtained mixture; a preparation method of the drug-loading particles comprises the following steps: heating glyceryl behenate up to 65-70 DEG C for melting, then adding meglumine and evenly stirring in a heat preservation process, adding gliclazide and stirring until the mixture is molten, cooling for solidifying, and pelletizing, wherein the mass ratio of the gliclazide to the glyceryl behenate to the meglumine is equal to 1 to (1.5-4.5) to (0.1-0.3). The gliclazide sustained-release tablets are stable in drug release speed, better in drug stability, high in bioavailability, simple in preparation technology and suitable for industrial mass production.

Description

technical field [0001] The invention belongs to the technical field of western medicine preparations, and in particular relates to a gliclazide sustained-release tablet and a preparation method thereof. Background technique [0002] Diabetes mellitus (DM, Diabetes Mellitus) is a metabolic disease with multiple etiologies, characterized by chronic hyperglycemia, accompanied by disorders of sugar, fat and protein metabolism caused by defects in insulin (Insulin) secretion and / or action. Gliclazide was first successfully developed by the French Servier pharmaceutical company, and its trade name is Diamicron. Diamicron has been registered and sold in more than 130 countries in the world. After the drug entered China, it received unanimous praise from doctors and experts, and now it has become the first-line oral hypoglycemic drug in my country. [0003] The chemical name of Gliclazide is 1-(3-azabicyclo[3.3.0]octyl)-3-p-toluenesulfonylurea, which is white or off-white crystalli...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K31/64A61K47/14A61K47/18A61P3/10
Inventor 冯荣权邵良碧
Owner 浙江康德药业集团股份有限公司
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