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Metroprolol succinate dropping pills and preparation method thereof

A technology of metoprolol succinate and toprolol dripping pills, which can be used in pill delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc. It can solve problems such as difficulty in control and fluctuation of blood drug concentration, and achieve low cost , good bioavailability, good effect

Inactive Publication Date: 2015-11-11
CHENGDU KECHUANG JIASI TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since metoprolol succinate sustained release is a non-constant release drug, the release and absorption rate of the drug is also affected by factors such as the gastrointestinal fluid in the patient's body, so its blood drug concentration still fluctuates greatly, which is difficult to control and predict , with some uncertainty

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] A kind of metoprolol succinate drop pill, is prepared by each raw material of following weight: metoprolol succinate 20g, beta-cyclodextrin 30g, glyceryl monostearate 40g, polyethylene glycol 600040g, Triethyl citrate 30g, disodium hydrogen phosphate 20g, liquid paraffin 20g.

[0025] The preparation method of the metoprolol succinate dropping pill described in the present embodiment comprises the following steps:

[0026] (1) Preparation of metoprolol succinate inclusion complex:

[0027] 1) In water or ethanol medium, react metoprolol succinate with β-cyclodextrin in proportion, filter the resulting solution through a microporous membrane until clear, and separate the clathrate from the mixture; or

[0028] 2) In solid form, metoprolol succinate combined with beta-cyclodextrin; or

[0029] 3) Metoprolol succinate reacts with β-cyclodextrin for high-energy grinding;

[0030] (2) Pass the metoprolol succinate inclusion compound prepared in step (1) through a 100-200 ...

Embodiment 2

[0033] Embodiment 2: The difference between this embodiment and embodiment 1 is only that polyethylene glycol 6000 is replaced by polyethylene glycol 4000.

Embodiment 3

[0034] Embodiment 3: The difference between this embodiment and embodiment 1 is that polyethylene glycol 6000 is replaced by polyethylene glycol 8000.

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PUM

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Abstract

The invention discloses metroprolol succinate dropping pills and a preparation method thereof. The metroprolol succinate dropping pills are prepared from the following raw materials in parts by weight: 1-3 parts of metroprolol succinate, 2-4 parts of beta-cyclodextrin, 8-18 parts of matrix, 1-3 parts of a stabilizer and 1-3 parts of condensate. According to the metroprolol succinate dropping pills and the preparation method thereof, provided by the invention, the prepared metroprolol succinate dropping pills can quickly release in vivo to achieve the therapeutic effect, and can further maintain a stable and lasting therapeutic effect; besides, the metroprolol succinate dropping pills are low in cost, good in effect and good in bioavailability.

Description

technical field [0001] The invention relates to a metoprolol succinate dropping pill and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] Metoprolol is a selective beta 1 Receptor blockers, first launched in Europe in 1975, are widely used in the treatment of hypertension, coronary heart disease, arrhythmia, etc., and are one of the first-choice antihypertensive drugs. In 1992, the United States launched the once-daily metoprolol succinate sustained-release tablets, which improved medication compliance and reduced adverse reactions to a certain extent. Since metoprolol succinate sustained release is a non-constant release drug, the release and absorption rate of the drug is also affected by factors such as the gastrointestinal fluid in the patient's body, so its blood drug concentration still fluctuates greatly, which is difficult to control and predict , with some uncertainty. Therefore, there is an urgent...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/135A61K47/48A61P9/12A61P9/10A61P9/06
Inventor 缪家戌
Owner CHENGDU KECHUANG JIASI TECH
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