Slow-releasing preparation containing metformin hydrochloride and glipizide and its preparation method

The technology of metformin hydrochloride and metformin acid is applied in the preparation field of the sustained-release preparation, which can solve the problem that the uniformity of blood drug concentration and release is not easy, the uniformity of drug release is not ideal, and the stability of the hypoglycemic process is affected. and other problems, to achieve the effect of convenient quality control and content determination, small incidence of adverse reactions, and good absorption effect

Inactive Publication Date: 2007-10-24
QIQIHAR MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The third problem is that the existing compound metformin hydrochloride and glipizide ordinary tablets do not maintain the blood drug concentration in the human body and the uniformity of drug release is not ideal, which affects the stability of the hypoglycemic process.
As a result, some people in China have launched sustained-release formulation designs for this type of compound drug, but judging from the specific content of these designs, some designs cannot play the role of drug sustained release in the current status quo, while others are designed directly. Made by mixing two drugs together with sustained-release materials
It is not easy to achieve a particularly ideal level of blood drug concentration and release uniformity in the human body after taking it.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] 1. Preparation of metformin hydrochloride pills

[0045] Weigh 210 g of metformin hydrochloride, 80 g of filler microcrystalline cellulose and 50 g of binder lactose, sieve metformin hydrochloride, microcrystalline cellulose and lactose and mix them evenly, according to the ratio of water to microcrystalline cellulose of 1.1:1 The appropriate amount of water is added in a proportion to make a suitable soft material, and the pellets are obtained by an extrusion spheronizer, and the extrusion speed is 50r·min -1 , the rounding speed is 1100r·min -1 , the spheronization time is 4min, and after spheronization, it is dried in an oven at 55° C. for 5h, and then sieved to take the pellets between 18 and 24 meshes for use.

[0046] 2. Preparation of metformin hydrochloride sustained-release pellets

[0047] Take 500g of the above metformin hydrochloride-containing pills, place them in a centrifuge chamber, start the main engine, adjust the position and angle of the baffle and...

Embodiment 2

[0055] 1. Preparation of blank pellets

[0056] The blank pellets were prepared by centrifugal granulation, and 500 g of microcrystalline cellulose was weighed and placed in a centrifugal granulator. The granulation conditions were jet pressure 0.3Mpa and blast flow 125L·min -1 , the centrifugal speed of the host is 550r·min -1 , the first 4min shotcrete flow is 8ml·min -1 , and then adjust the shotcrete flow to 6ml·min -1 , this process lasts for 4 minutes, and the final stage is the powder supply stage, and the rotation speed of the powder supply machine is 20r·min -1 , the shotcrete flow remains unchanged, and the machine is turned off when the parent nucleus grows to an appropriate size. After the end, open the discharge port, take out the finished product, dry at room temperature, and sieve and classify.

[0057] 2. Preparation of metformin hydrochloride pills

[0058] Take 80 g of 40-60 mesh microcrystalline cellulose blank pellet cores and put it in a centrifugal g...

example 3

[0066]This example is the animal pharmacozoological test of the product of the present invention. By establishing an HPLC method for measuring the concentration of metformin hydrochloride in dog plasma, taking the ordinary sustained-release tablet of metformin hydrochloride as the standard control, the area method was used to estimate the compound metformin hydrochloride sustained-release of the present invention. The relative bioavailability of the pellets was 97.9%. After taking 250 mg of metformin hydrochloride sustained-release pellets, the product of the present invention, the estimated terminal half-life was 10.97 ± 2.36 hours, the peak time and peak concentration were 5.8 ± 1.7 hours and 1114.37 ± 27.23 ng / ml, respectively; the average retention time was 11.54 ± 1.49 hours, the area under the curve was 1419.524 ± 246.5 ng / ml. When 10 mg of metformin hydrochloride ordinary sustained-release tablets were administered to dogs, the estimated terminal half-life was 2.09 ± 1....

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PUM

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Abstract

The invention discloses a diabecron and glipizide -containing slow-release agent and the method for preparing the same. The glipizide micro-pill takes blank micro-pill as carrier, and combines glipizide and other medical findings with it. The diabecron-containing slow-release micro-pill comprises diabetosan pill, slow-release coating membrane material or other medical findings. The method for preparing diabecron-containing slow-release micro-pill takes extrusion rolling method or blank micro-pill loading method. The product is characterized by safety, high efficient, low toxicity and convenient usage. It can be used to treat non-insulin-dependent diabetes mellitus.

Description

Technical field: [0001] The invention relates to a sustained-release preparation containing metformin hydrochloride and glipizide, and also relates to a preparation method of the sustained-release preparation. Background technique: [0002] At present, the main treatment methods for type II diabetes are insulin injection and oral hypoglycemic drugs such as sulfonylureas and biguanides. Due to the inconvenience of insulin dose control and inconvenience, biguanides and sulfonylureas are still used as first-line drugs for the treatment of type II diabetes in China. [0003] The hypoglycemic mechanism of metformin hydrochloride is mainly to increase aglycolysis, inhibit hepatic gluconeogenesis, reduce hepatic glucose output and increase the sensitivity of surrounding tissues to insulin. Symptomatic sulfonylurea failure and poor glycemic control of type I diabetes with insulin therapy. Because metformin does not stimulate insulin secretion, and can improve blood lipid metabolis...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4965A61K9/16A61K9/22A61K9/52A61K47/32A61K47/36A61K47/38A61K47/40A61P3/10A61J3/06A61K31/155
Inventor 刘吉成牛英才
Owner QIQIHAR MEDICAL UNIVERSITY
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