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Novel atenolol slow-release drop pill and preparation method thereof

A technology for sustained-release dropping pills and angina pectoris, which is applied in pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc. It can solve the problem that injections are prone to allergic or adverse reactions, manufacturing and medical costs It can improve the left ventricular ejection fraction and exercise tolerance, reduce the incidence and save medical expenses.

Inactive Publication Date: 2019-05-03
ZHENGZHOU TAIFENG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to reasons such as preparation technology, there are problems such as long dissolution time, low dissolution rate, poor absorption, hepatic and intestinal first-pass effect and low bioavailability after taking tablets or capsules, which affect the efficacy of the drug and directly affect the outcome of the treatment
Although the atenolol dropping pill preparation produced by the prior art overcomes the defects produced by the above-mentioned dosage form, it has the advantages of quick effect, fast absorption, and high bioavailability, but there is uneven dispersion of medicine, unstable drug release, and Defects such as short action time
[0005] However, injections are often prone to allergic reactions or adverse reactions. At the same time, there are also disadvantages such as difficult operation, great pain for patients, high manufacturing and medical costs, and heavy economic burden for patients.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035]Based on the total weight of 100g, weigh the matrix PEG4000 35%, PEG6000 25%, PEG10000 10%, stearic acid 10%, glyceryl monostearate 6%, Tween-80 4%, raw material atenolol 10% Place the matrix in a heating container to heat and stir to melt, add atenolol in a corresponding proportion, stir well, then add Tween-80 and stir evenly, and then melt or mix the liquid medicine under heat preservation conditions Drop into the condensation column filled with dimethyl cinnamon oil, wherein the temperature when heated and melted is 80 ° C, the temperature of the upper part of the condensate is 25 ° C, and the temperature of the bottom is > 3 ° C; take it out after forming, and the obtained Product, the 2-hour cumulative release percentage is 35%-55%, the 6-hour cumulative release percentage is 56%-79%, the 10-hour cumulative release percentage is 80%-100%, and the roundness is better.

Embodiment 2

[0037] Based on the total weight of 100g, weigh the matrix PEG4000 20%, PEG6000 20%, PEG10000 3%, stearic acid 20%, glyceryl monostearate 10%, Tween-80 2%, raw material atenolol 25% Place the matrix in a heating container and heat it and stir it to melt, add the corresponding proportion of atenolol, stir well, then add Tween-80 and stir evenly, under the condition of heat preservation, put the melted or mixed medicine The liquid drops into the condensation column filled with simethicone oil, wherein the temperature when heated and melted is 60°C, the temperature of the upper part of the condensate is 35°C, and the temperature of the bottom is -2°C; take it out after forming, and the obtained The product has a cumulative release percentage of 28%-49% in 2 hours, a cumulative release percentage of 52%-65% in 6 hours, and a cumulative release percentage of 82%-92% in 10 hours, with good roundness.

Embodiment 3

[0039] Based on the total weight of 100g, weigh the matrix PEG4000 45%, PEG6000 10%, PEG10000 10%, stearic acid 10%, glyceryl monostearate 5%, Tween-80 2%, raw material atenolol 18% Place the matrix in a heating container to heat and stir to make it melt, add the corresponding proportion of atenolol, stir well, then add Tween-80 and stir evenly, under the condition of heat preservation, rub the melted or mixed medicine The liquid drops into the condensation column filled with simethicone oil, wherein the temperature during heating and melting is 70°C, the temperature of the upper part of the condensate is 20°C, and the temperature of the bottom is 0°C; take it out after forming, and the obtained Product, the 2-hour cumulative release percentage is 61%-72%, the 6-hour cumulative release percentage is 71%-85%, the 10-hour cumulative release percentage is 76%-100%, and the roundness is better.

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Abstract

Hypertension is recognized by the medical community at home and abroad as the "most ferocious killer" that threatens the human life, the mortality rate of hypertension is higher than that of any otherdisease, and hypertension seriously affects the human health. Atenolol tablets are administered twice per day, and the blood concentration fluctuates greatly, thereby being necessary to prepare the atenolol tablets into a slow-release preparation. The invention relates to an atenolol slow-release drop pill capable of quickly taking effect and slowly releasing drugs and used for treating hypertension and angina, performing maintenance treatment of myocardial infarction and treating arrhythmia, hyperthyroidism and the like, and a preparation method of the atenolol slow-release drop pill. In order to make up for the deficiencies of the prior art, the invention provides an atenolol slow-release drop pill preparation. The atenolol slow-release drop pill provided by the invention is characterized in that a hydrophobic skeleton capable of slowly releasing drugs and Tween-80 with a solubilizing effect are added on the basis of the existing drop pill technology, the deficiencies of the prior art are effectively overcome, and the atenolol slow-release drop pill has the advantages of uniform drug dispersion, sufficient drug release, long drug release time, reduced patient medication frequency and high bioavailability.

Description

technical field [0001] The present invention relates to a kind of atenolol sustained-release dripping pill capable of rapid effect and sustained release of medicine for the treatment of hypertension, angina pectoris, maintenance treatment after myocardial infarction, arrhythmia, hyperthyroidism and the like and a preparation method thereof. Background technique [0002] This product is a selective β1 adrenergic receptor blocker suitable for moderate and mild hypertension caused by various reasons, including senile hypertension and hypertension during pregnancy. It is a cardioselective β-receptor blocker with no membrane stabilizing effect and no endogenous sympathomimetic activity. Generally used for sinus tachycardia and premature beats, etc., can also be used for hypertension, angina pectoris and glaucoma. Oral absorption is about 50%, and small doses can pass through the blood-brain barrier. Protein binding 6 - 10%. The peak effect is reached 2-4 hours after taking it,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/165A61K47/10A61K47/14A61K47/26A61K47/38A61P9/10A61P9/12A61P9/06A61P5/16
Inventor 沙薇李映雪朱新科
Owner ZHENGZHOU TAIFENG PHARMA CO LTD
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