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Metoprolol oral drug composite and preparation method thereof

A pharmacological and adhesive technology, which is applied in the field of sustained-release preparations containing metoprolol and its preparation, and can solve the problems of reduced in vitro release and poor stability

Inactive Publication Date: 2010-06-02
BEIJING D VENTUREPHARM TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The inventor purchased this preparation as a contrast preparation and found that its stability was poor, and after a long period of time, the in vitro release rate tended to decrease

Method used

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  • Metoprolol oral drug composite and preparation method thereof
  • Metoprolol oral drug composite and preparation method thereof
  • Metoprolol oral drug composite and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026]

[0027] Preparation method: Dissolve the prescription amount of metoprolol succinate and ethyl cellulose in an appropriate amount of ethanol to prepare a 50% by weight ethanol solution as a binder; combine the prescription amount of HPMC K100, hydrogen phosphate Calcium is sieved and mixed, wet granules are prepared with the above-mentioned binder, dried, magnesium stearate is added, and tablets are mixed evenly.

Embodiment 2

[0029]

[0030] Preparation method: mix prescription amounts of metoprolol succinate and glyceryl behenate, heat to melt them, and use them as adhesives; sieve and mix prescription amounts of HPMC 100LV and calcium sulfate, and use the above to bond Prepare wet granules from the agent, dry them, add magnesium stearate, and press tablets after mixing.

Embodiment 3

[0032]

[0033] Preparation process: mix prescription amounts of metoprolol succinate and glyceryl behenate, heat to melt them, and use them as adhesives; sieve and mix prescription amounts of HPMC K4M and aluminum hydroxide. The mixture is prepared as wet granules, dried, magnesium stearate is added, and tablets are compressed after mixing.

[0034] The in vitro release data of Examples 1, 2, 3 and the control formulations are shown in the following table:

[0035]

[0036] The accelerated 6-month in vitro release data of Examples 1, 2, 3 and the control formulations are shown in the following table:

[0037]

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PUM

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Abstract

The invention discloses an extended action tablet containing metoprolol and a preparation method thereof. The drug mainly contains metoprolol, a hydrophobic retarding agent and a gel-type retarding agent. The invention enables the drug to achieve 24-hour slow release effect by mainly adopting a mode of taking the hydrophobic retarding agent and metoprolol as a binding agent after being dissolved or melted together; then mixing the binding agent and the gel-type retarding agent, pelletizing and tabletting. The extended action tablet has simple preparation process and high stability and is mainly used for treating high blood pressure.

Description

Technical field [0001] The invention discloses a medicinal composition mainly used for the treatment of hypertension, in particular to a sustained-release preparation containing metoprolol and a preparation method thereof. Background technique [0002] At present, there are more than 100 million patients with hypertension in my country, and most of them have unknown causes and are a lifelong disease. Long-term effective implementation of antihypertensive drug therapy is one of the main ways to improve the quality of life and survival rate of hypertensive patients. The advantages of controlled-release products are well known in the field of pharmacy, including the ability to maintain blood drug concentration for a relatively long period of time, while being able to achieve the same concentration as required but reducing the number of administrations and increasing patient acceptance. Metoprolol is an effective drug for the treatment of hypertension. Making it into a long-acting o...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K31/138A61P9/12
Inventor 孟凡静
Owner BEIJING D VENTUREPHARM TECH DEV
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