Process for producing diabecron sustained release tablet

Abstract

The invention relates to a preparation method for metformin hydrochloride sustained-release tablets. The preparation method comprises the following steps: firstly, dissolving ethyl cellulose into ethanol solution, blending the ethyl cellulose with metformin hydrochloride to produce granules, and drying and sieving the granules at 45 to 55 DEG C; secondly, dissolving hydroxypropyl methylcellulose into ethanol solution to produce bonding agent, blending the granules prepared in step one, hydroxypropyl methylcellulose, ethyl cellulose and pore forming agent, adding the bonding agent, performing sieving and granulation, adding hydroxypropyl methylcellulose and lubricant, evenly blending, detecting the content, determining the tablet weight, and pressing into plain tablets; thirdly, dissolving film forming agent, plasticizer, masking agent and glidant for hydroxypropyl methylcellulose and ethyl cellulose into ethanol solution, completely stirring for more than 1 hour to produce sustained-release preparation coating solution, and finally obtaining the metformin hydrochloride sustained-release tablets by performing film coating to the plain tablets. The sustained-release preparation not only embodies the main characteristics of the sustained-release preparation for continuous sustained release of drug, but also presents high bioavailability.

Description

technical field [0001] The invention belongs to the field of preparation of drugs for treating hyperglycemia, in particular to a preparation method of metformin hydrochloride sustained-release tablets. Background technique [0002] Metformin Hydrochloride Sustained Release Tablets is a biguanide hypoglycemic drug listed under the trade name Glucophage XR by Bristol-Myers Squibb Company in the U.S. in October 2000. It is suitable for type II diabetes, especially obesity, high plasma insulin, secondary It is the drug of choice for obese type II diabetic patients who have failed to respond to sulfonylureas and whose blood sugar is not well controlled by insulin therapy for type I diabetes. Since the first domestic pharmaceutical factory was approved for this product, although more than ten pharmaceutical factories have obtained the new drug production approval for this product in the past two years, there are not many pharmaceutical factories that have achieved production and m...

AI Technical Summary

Problems solved by technology

[0003] At present, there are two major problems in preparing metformin hydrochloride into oral sustained-release preparations: 1. The water solubility of the main drug (metformin hydrochloride) is large: for oral sustained-release preparations, it is difficult to prepare drugs with high water solubility (such as greater than 100mg / ml) Oral sustained-release preparations, and the water solubility of metformin hydrochloride is very high (greater than 300mg / ml at 25°C), if the process technology is not adopted properly, its preparation products are prone to sudden release of the main drug

If the conventional hydrosol gel matrix slow-release technology is used to control the required release rate of the main drug, it may cause the main drug to be released too quickly and unstable from the initial stage of the sustained-release matrix; 2. The dosage specification of this product is relatively large ( 0.5 g / tablet): In order to reduce the release rate of the main drug from the preparation to a level consistent with the required blood concentration characteristics, a large amount of gel matrix material (cellulose polymer) needs to be selected. If the main drug dose is only A few milligrams will not be a problem, but for example, the dosage of metformin hydrochloride is 500 mg, which requires a large amount of high-viscosity polymers to prepare oral sustained-release tablets, which will bring great technical difficulties to the product production process

Moreover, the size of the preparation is too large, although it can promote the extension of the residence time of the drug preparation in the stomach and facilitate the absorption of the drug in the upper gastrointestinal tract, but the excessive volume expansion after absorbing liquid may lead to the degradation and erosion speed of the preparation in the body Delayed and prone to gastric or intestinal blockage