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Glipizide sustained-release capsule formulation and preparation method thereof

A technology of glipizide and sustained-release capsules, applied in the field of glipizide sustained-release capsules and its preparation, can solve problems such as hypoglycemia and insufficient blood sugar control, achieve good blood sugar levels, good therapeutic effects, and reduce blood sugar fluctuations Effect

Active Publication Date: 2010-01-20
HANGZHOU CONBA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the constant changes in human blood sugar concentration, glipizide sustained-release and controlled-release preparations cannot solve the problem of blood sugar fluctuations well. The constant release of the drug may cause insufficient blood sugar control after meals in patients. Hypoglycemia occurs at low concentrations

Method used

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  • Glipizide sustained-release capsule formulation and preparation method thereof
  • Glipizide sustained-release capsule formulation and preparation method thereof
  • Glipizide sustained-release capsule formulation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Embodiment 1: Preparation of glipizide sustained-release pellets (Glipizide No. 1 pellets)

[0047] formula:

[0048] Glipizide 10g

[0049] Beta Cyclodextrin 3-6g

[0050] Starch 140g

[0051] NaCl fine powder 40g

[0052] Dextrin 20g

[0053] Ethyl cellulose 1.1~4.4g

[0054] Polyethylene glycol 6000 0.55~2.2g

[0055] Appropriate amount of 7.3% PVPK30 ethanol solution (50%)

[0056] Preparation Process:

[0057] Prepare blank pellets→prepare drug-containing pellets→prepare sustained-release pellets

[0058] Preparation:

[0059] I. Preparation of blank pellets

[0060] Fully mix 140g of starch, 20g of dextrin and 40g of sodium chloride fine powder, pass through an 80-mesh sieve, put in a coating granulator, and use 7.3% PVPK30 ethanol solution (50%) as a binder to make pellets. When spheronized to 28-20 mesh, take it out and dry at 60°C, select 28-20 mesh blank pellets, and set aside;

[0061] II. Preparation of drug-containing pellets

[0062] Get 10g of ...

Embodiment 2

[0067] Example 2 Determination of the release rate of glipizide sustained-release pellets

[0068] Get the embodiment 1 product of the present invention, according to the release assay method (Chinese Pharmacopoeia version two appendix XD first method in 1995), adopt the second method device of dissolution assay, be solvent with the artificial intestinal fluid 900ml not containing pancreatin, rotating speed is 50 rpm, operate according to the law, every 1 hour, take 8ml of the solution respectively, filter, take the filtrate as the test solution, and immediately add the same temperature and the same amount of the above solvent to the dissolution cup. Use high-performance liquid chromatography (model LC-10A, produced by Shimadzu Corporation of Japan) to measure release in Table 1:

[0069] Table 1 Example 1 of the present invention Glipizide sustained-release pellet release-time data table

[0070] time

[0071] Its release curve is shown in figure 1 .

Embodiment 3

[0072] Example 3 Preparation of Glipizide 4-hour Delayed-release Sustained-release Pellets (Glipizide No. 2 Pellets)

[0073] formula:

[0074] Glipizide Extended Release Pellets 200g

[0075] Ethyl cellulose 1-3g

[0076] Preparation:

[0077] 1. Get water-insoluble material ethyl cellulose (EC) 1g, dissolve with 10ml ethanol and make coating solution, set aside.

[0078] II. Put 80 g of the glipizide sustained-release pellets prepared according to Example 1 in a coating machine, and use an atomizing spray gun to spray the above-mentioned coating solution onto the glipizide pellets: adjust the nozzle pressure to make the coating solution spray To achieve the best atomization effect, blow in hot air, adjust the speed to achieve the best turning effect, spray into the coating solution, take it out and ventilate and dry at 60°C, select 30-20 mesh pellets and mix well to get glipizide 4 The sustained-release pellets are hourly delayed release, and the thickness of the coating...

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PUM

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Abstract

The invention relates to a glipizide sustained-release capsule formulation and a preparation method thereof. The glipizide sustained-release capsule formulation contains three glipizide sustained-release pillers with different release periods, wherein the glipizide sustained-release pillers respectively include conventional glipizide sustained-release pillers and glipizide time-delay sustained-release pillers in the following percentage by weight: 20-80 percent of the glipizide sustained-release pillers, 10-50 percent of glipizide 4-hour time-delay sustained-release pillers and 5-30 percent of glipizide 8-hour time-delay sustained-release pillers. A release curve of the glipizide sustained-release capsule formulation is more similar to a physiological change curve of the blood sugar concentration of human bodies, and release peaks of glipizide are respectively generated after the glipizide sustained-release capsule formulation is orally taken, 4 hours later and 8 hours later, corresponding to three meals a day, which are orally taken by ordinary people, thereby better controlling the blood sugar levels, reducing the blood sugar fluctuation of diabetics and bringing better treatment effect to patients.

Description

(1) Technical field: [0001] The invention relates to an oral chemical drug sustained-release preparation, in particular to a glipizide sustained-release capsule and a preparation method thereof. (two) background technology: [0002] Glipizide is a sulfonylurea oral hypoglycemic drug with the molecular formula C 21 h 27 N 5 o 4 S, molecular weight 445.55. The chemical name is 5-methyl-N-[2-[4-[[[(cyclohexylamino)carbonyl]amino]sulfonyl]phenyl]ethyl]-pyrazinecarboxamide. This product is white or off-white crystalline powder, slightly soluble in acetone, chloroform or dioxane, very slightly soluble in ethanol, almost insoluble in water. [0003] Glipizide is a second-generation sulfonylurea oral hypoglycemic agent. It mainly promotes the secretion of insulin by pancreatic β cells, especially the glucose-stimulated insulin secretion; it also enhances the action of insulin, thereby effectively reducing blood sugar concentration and glycosylated hemoglobin; and can improve h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/62A61K31/64A61K47/36A61K47/38A61K47/40A61P3/10
Inventor 胡江宁徐春玲叶剑锋徐秀卉陆振宇
Owner HANGZHOU CONBA PHARMA
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