Novel metformin hydrochloride sustained release pellets and preparation method thereof

A technology for metformin hydrochloride and sustained-release pellets, which is applied in the field of pharmaceutical preparations, can solve the problem that there is no metformin hydrochloride sustained-release pellets, etc., and achieves the effects of masking bad odor, enhancing drug stability, and improving bioavailability

Active Publication Date: 2013-04-17
GUANGZHOU PHARMACEUTICAL INDUSTRIAL RESEARCH INSTITUTE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The metformin hydrochloride sustained-release pellets reported in this paper are prepared by applying hot-melt coating technology. At prese

Method used

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  • Novel metformin hydrochloride sustained release pellets and preparation method thereof
  • Novel metformin hydrochloride sustained release pellets and preparation method thereof
  • Novel metformin hydrochloride sustained release pellets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0037] Example 1

[0038] The percentage in the prescription is the weight percentage of the component in the entire prescription, and the percentage of the lipid material is calculated based on the weight of the pill core. The following examples are the same.

[0039] (1) Components containing pill core:

[0040]

[0041] (2) The components of the sustained-release coating layer:

[0042] Glyceryl monostearate 10%-50%, preferably 15%-40%

[0043] Preparation of metformin hydrochloride sustained-release pellets:

[0044] Step 1: Mix metformin hydrochloride and lactose evenly, add a homogeneous solution of hypromellose and water, and make the powder into a moist, uniform soft material with certain plasticity;

[0045] Step 2: Put the soft material into an extruder and extrude the extrudate in a spheronizer, add an appropriate amount of talcum powder during the spheronization process, spheronize to form a pellet core, and dry to obtain a pill core;

[0046] Step 3: Put the pill-containing co...

Example Embodiment

[0053] Example 2

[0054] (1) Components containing pill core:

[0055]

[0056] (2) The components of the sustained-release coating layer:

[0057] Glyceryl tristearate 10%~50%, preferably 15%~40%

[0058] Preparation of metformin hydrochloride sustained-release pellets:

[0059] Step 1: Mix metformin hydrochloride and microcrystalline cellulose uniformly, add a homogeneous solution of starch and water, and make the powder into a moist, uniform soft material with certain plasticity;

[0060] Step 2: Put the soft material into an extruder and extrude the extrudate in a spheronizer, add an appropriate amount of talcum powder during the spheronization process, spheronize to form a pellet core, and dry to obtain a pill core;

[0061] Step 3: Place the pill-containing core in a fluidized bed coating machine, heat to melt the glyceryl tristearate, and then coat and dry, to obtain metformin hydrochloride sustained-release pellets.

[0062] Atomization pressure: 0.254mpa

[0063] Wind speed: 6~7m / ...

Example Embodiment

[0068] Example 3

[0069] (1) Components containing pill core:

[0070]

[0071] (2) The components of the sustained-release coating layer:

[0072] Glyceryl behenate 10%~50%, preferably 15%~40%

[0073] Preparation of metformin hydrochloride sustained-release pellets:

[0074] Step 1: Mix metformin hydrochloride and lactose evenly, add a homogeneous solution of polyvinylpyrrolidone and water, and make the powder into a soft, evenly moist material with certain plasticity;

[0075] Step 2: Place the soft material in an extruder to extrude, and the extrudate is placed in a spheronizer for spheronization, an appropriate amount of magnesium stearate is added in the spheronization process, spheronized to form a pellet core, and dried to obtain a pill-containing core;

[0076] Step 3: Put the pill-containing core in a fluidized bed coating machine, heat to melt the behenate glyceride and then coat and dry to obtain the metformin hydrochloride sustained-release pellets.

[0077] Atomization press...

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Abstract

The invention discloses novel metformin hydrochloride sustained release pellets and a preparation method thereof. The metformin hydrochloride is formed by coating a sustained release coating layer outside a medicament-containing pellet core, and the medicament-containing pellet core is prepared from the following components by weight percent: 5-50% of metformin hydrochloride, 50-95% of excipient, filler, adhesive, wetting agent and antisticking agent, wherein the filler, the adhesive, the wetting agent and the antisticking agent account for 20-80%, 2-20%, 10-60% and 1-20% of the total weight of the metformin hydrochloride and the excipient respectively; and the sustained release coating layer is prepared from the following component according to weight percentage: grease material which accounts for 10-50% of the total weight of the metformin hydrochloride and the excipient. The metformin hydrochloride sustained release pellets prepared by the method not only can effectively reduce the accumulation of medicaments and the toxic and side effects of the metformin hydrochloride, but also can reduce the release of the medicaments and improve the bioavailability.

Description

technical field [0001] The invention provides a novel metformin hydrochloride sustained-release pellet and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] [0003] Metformin hydrochloride (Metformin hydrochloride), chemical name 1,1-dimethylbiguanide hydrochloride, molecular formula C 4 h 11 N 5 ·HCl, molecular weight 165.63; white crystal or crystalline powder, odorless; easily soluble in water, soluble in methanol, slightly soluble in ethanol, insoluble in ether or chloroform; M.P.220~225℃; UV233nm. Metformin hydrochloride is a biguanide hypoglycemic drug, which is widely used in the treatment of type 2 diabetes due to its small adverse drug reactions. Metformin hydrochloride reduces glycogen output by inhibiting hepatic gluconeogenesis, and its main effect is to reduce fasting blood glucose concentration. It is a mixed therapy with biguanide as the main component. In clinical practice, repeated medi...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/155A61P3/10
Inventor 梁超峰应军陈桐楷孙湘陈玲黄良军黄春晖
Owner GUANGZHOU PHARMACEUTICAL INDUSTRIAL RESEARCH INSTITUTE
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