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Sustained release tablet of glibenclamide and preparation process thereof

A technology of glyburide and sustained-release tablets, applied in the field of medicine, can solve the problems of short half-life, difficult to maintain hypoglycemic effect, hypoglycemia, etc., and achieve the effects of reducing side effects, prolonging elimination half-life, and reducing the number of times of taking

Inactive Publication Date: 2007-05-23
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the short half-life of glibenclamide in the body, which is 3-6 hours, the release of common clinical oral preparations is too fast to cause hypoglycemia after taking the medicine, and it is difficult for ordinary tablets to maintain a continuous and gentle hypoglycemic effect for one day. It is difficult to estimate the change of blood sugar in the body after drug administration, and the blood sugar concentration must be monitored all the time, which brings a lot of inconvenience to the patient. In order to maintain effective blood concentration, it is necessary to develop its once-a-day slow-release preparation to obtain a sustained and gentle release. Drug effect, to avoid the side effects of hypoglycemia brought by the release peak

Method used

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  • Sustained release tablet of glibenclamide and preparation process thereof
  • Sustained release tablet of glibenclamide and preparation process thereof
  • Sustained release tablet of glibenclamide and preparation process thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] This example is a non-constant-rate-release glibenclamide ordinary sustained-release tablet, wherein each component and its weight ratio are as follows:

[0044] 1 part of glibenclamide, 125 parts of hydroxypropylmethylcellulose (K4M), 25 parts of ethyl cellulose, 40 parts of microcrystalline cellulose, 9 parts of talcum powder, appropriate amount of PVP (made into 10% ethanol solution for viscose) mixture).

[0045] The preparation method of this embodiment is as follows:

[0046] Weigh the glibenclamide, hydroxypropylmethylcellulose, ethylcellulose and microcrystalline cellulose in the stated amount, mix them evenly, and pass through an 80-120 mesh sieve after being evenly pulverized; add an appropriate amount of PVP10% ethanol solution, and use Wet granulation, use 18-mesh sieve to granulate, dry at 40-60°C for 1-3 hours, take out; add the stated amount of talcum powder, mix well, test the content of the main ingredient in the mixed powder, and then press it with a ...

Embodiment 2

[0048] This example is a non-constant-rate-release glibenclamide ordinary sustained-release tablet, wherein each component and its weight ratio are as follows:

[0049] 2.5 parts of glibenclamide, 110 parts of hydroxypropylmethylcellulose (K4M), 35 parts of methylcellulose, 35 parts of microcrystalline cellulose, 5 parts of talcum powder, appropriate amount of hydroxypropylmethylcellulose (made into 5% aqueous solution as a binder).

[0050] The preparation method of this embodiment is as follows:

[0051] Weigh the glibenclamide, hypromellose (K4M), methylcellulose and microcrystalline cellulose in the stated amount, mix them evenly, and pass through a 80-120 mesh sieve after being evenly crushed; add an appropriate amount of hypromellose Base cellulose 5% aqueous solution to make wet granules, granulate with 18 mesh sieve, dry at 40-60°C for 2-4 hours and take out; add the stated amount of talcum powder, mix well, and test the content of the main ingredient in the mixed pow...

Embodiment 3

[0053] This example is a non-constant-rate-release glibenclamide ordinary sustained-release tablet, wherein each component and its weight ratio are as follows:

[0054] Glibenclamide 5 parts, carnauba wax 75 parts, hydrogenated vegetable oil 10 parts, calcium sulfate 20 parts, mannitol 12 parts, ethyl cellulose 50 parts, magnesium lauryl sulfate 12 parts, magnesium stearate 15 parts , an appropriate amount of sodium alginate (dubbed a 5% aqueous solution as a binder).

[0055] The preparation method of this embodiment is as follows:

[0056] Glibenclamide, carnauba wax, hydrogenated vegetable oil, calcium sulfate, mannitol, sodium alginate, ethyl cellulose, magnesium lauryl sulfate and magnesium stearate were weighed, and the glibenclamide Add it to the mixture of melted carnauba wax and hydrogenated castor oil, let it cool after stirring, grind it finely, and pass through an 80 mesh sieve; add calcium sulfate, mannitol, magnesium stearate, ethyl cellulose, mix well, and use ...

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Abstract

The invention relates to a Glibenclamide slow release tablet preparation which comprises effective dose of main constituent of Glibenclamide and medicinal auxiliary materials, the constituents include (by weight portion) Glibenclamide 0.5-5.0 parts, slow release material 20.0-170.0 parts, filling agent 5-100 parts, lubricating agent 5.0-30.0 parts, and right amount of binding agent. The invention also discloses the process for preparing the tablet preparation.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a slow-release tablet preparation for treating diabetes and a preparation method thereof. Background technique [0002] Diabetes is a systemic chronic metabolic disease determined by genetics. Due to the relative or absolute deficiency of insulin in the body, it causes the disorder of sugar, fat and protein metabolism; its main features are hyperglycemia and glycosuria, and it is often accompanied by serious complications. diseases such as hypertension and coronary heart disease. In recent years, the prevalence of diabetes in my country has been increasing year by year, but the age of patients has declined. Seriously affect people's quality of life, more and more harmful to people's physical and mental health, is the second killer in modern diseases, and the harm to human body is second only to cancer. [0003] Diet therapy is the basic treatment for various types of diabetes....

Claims

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Application Information

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IPC IPC(8): A61K31/17A61K9/22A61K47/00A61P3/10
Inventor 尹宗宁王怡鑫
Owner SICHUAN UNIV
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