Metformin hydrochloride sustained release tablets and preparation method thereof

Abstract

The invention discloses metformin hydrochloride sustained release tablets and a preparation method thereof. The metformin hydrochloride sustained release tablets are prepared through direct tabletting after uniform mixing of drug-containing particles and pharmaceutically acceptable auxiliary accessories, wherein the drug-containing particles are obtained by adding a metformin aqueous solution into an ethanol solution of ethyl cellulose to form a suspension, then heating, drying through distillation, and then screening. The preparation disclosed by the invention reduces the dosage of sustained release materials, the coating and granulation of the particles are finished through one step, and the drug release is stable, so that the metformin hydrochloride sustained release tablets are suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a metformin hydrochloride sustained-release tablet and a preparation method thereof. Background technique [0002] Metformin hydrochloride is a biguanide hypoglycemic drug that can be taken orally and is widely used. It is the only oral biguanide antihyperglycemic drug still used in developed countries in the world. And postprandial plasma glucose concentration, the mechanism of action is different from other antidiabetic drugs. Metformin hydrochloride reduces glycogen production, reduces the absorption of sugar in the small intestine, and improves insulin resistance by increasing the uptake and utilization of peripheral sugar. In normal people and patients with type 2 diabetes, neither hypoglycemia nor hyperinsulinemia occurs. Metformin hydrochloride currently used clinically is common tablets and capsules, etc., and the usual dosage is 1.5g per...

AI Technical Summary

Problems solved by technology

Therefore, the time of taking the medicine must be regularly spaced to ensure that the blood drug concentration maintains the therapeutic level, and there are disadvantages such as inconvenience for patients to take, easy to forget to take, missed dose, and large fluctuations in blood drug concentration.

[0003] Because metformin hydrochloride is a kind of medicine with good water solubility, and the dose is relatively large, therefore, it is very difficult to make sustained-release tablets. Currently, common sustained-release materials such as hydroxypropyl methylcellulose and carboxymethylcellulose are used Sodium, etc., the use of sustained-release materials is too large, resulting in heavy tablets, and the sustained-release indicators cannot meet the quality requirements in the USP32 standard. It is more difficult to achieve a good therapeutic effect

[0004] The disclosed metformin hydrochloride slow-release tablet of CN1391890A is to adopt common pharmaceutically commonly used polymer materials such as hydroxypropyl methylcellulose, ethyl cellulose, sodium carboxymethylcellulose, to form the slow-release agent of gel type, Moreover, it is very inconvenient to use organic carboxylic acid or alcohol to granulate under the molten state of 50-60°C, and the preparation is also difficult to achieve the purpose of controlling the steady release of the drug at a certain speed.

[0005] The disclosed metformin hydrochloride sustained-release tablet of CN1543937C adopts hydroxypropyl methylcellulose and micropowder ethylcellulose to make sustained-release material, and this sustained-release material consumption is less, and after metformin dissolves, the hydration that slow-release material forms "Erosion holes" are generated in the gel layer, which affects the sustained release effect, and it is difficult to achieve the ideal smooth release purpose, and the quality index cannot meet the requirements of the drug quality standard of the USP32 edition of the United States Pharmacopoeia

Sustained-release tablets prepared by this mechanism use a large amount of skeleton polymer materials, resulting in excessive tablet weight and tablet shape

The weight of the tablet of "Glucophage XR" product is 1g, and the active drug is 0.5g. When taking it, it needs to be swallowed whole, not crushed, so it is very inconvenient to have to swallow a tablet that is too heavy, especially for the elderly People are more inconvenient

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