Atenolol sustained-release dropping pill and preparation method thereof

Abstract

The invention relates to a therapeutic drug for treating arrhythmia, angina and mild and moderate hypertension as well as the preparation method thereof. The therapeutic drug aims to supplement the deficiency of the prior art and provide a sustained-release atenolol dropping pill formulation. The sustained-release atenolol dropping pill is prepared by adding stabilize Vitamin E and a hydrophobic base to the ingredients accepted in the prior art, thereby effectively overcoming the defects in the prior art and guaranteeing no occurrence of an obvious change related to the substance content for the drug during the effective storage period and has the advantages of full release, controllable release time, low frequency of drug taking, long effective hours and high bioavailability simultaneously. The sustained-release atenolol dropping pill is suitable for clinical and family use.

Description

Technical field: [0001] The invention relates to the technical field of sustained-release pharmaceutical preparations, in particular to an oral atenolol sustained-release drop pill preparation and a preparation method thereof. Background technique: [0002] Atenolol is a selective β1 receptor blocker developed by the British ICI company in 1976 without sympathomimetic activity and membrane stability. In 1982, the US FDA approved it for the treatment of hypertension, angina pectoris, early acute myocardial infarction and arrhythmia. APIs, tablets and injections are listed in the British Pharmacopoeia and the US Pharmacopoeia. Among them, the injection has been listed in the United States, the United Kingdom, France, Canada, Switzerland and other countries, and has been included in the Pharmacopoeia. It is clinically used for the early treatment of arrhythmia and acute myocardial infarction. The 2000 edition of the Chinese Pharmacopoeia contains atenolol raw materials and ta...

AI Technical Summary

Problems solved by technology

Due to the preparation technology and other reasons, after taking the tablet, there are problems such as long dissolution time, low dissolution rate, poor absorption, many times of taking medicine, short effective time, hepatic and intestinal first pass effect and low bioavailability, etc. Efficacy, also directly affects the effect of treatment

[0004] Injections are often prone to allergic reactions or adverse reactions, etc., but also have the disadvantages of difficult operation, great pain for patients, high manufacturing and medical costs, and heavy economic burden for patients.

[0005] China Patent Office discloses a kind of Chinese invention patent atenolol dropping pills and its preparation method that the patent number is 200310113514.X. From its disclosed content and its preparation method, although it can obtain sufficient drug release and bioavailability It has the characteristics of high strength and low cost, but it has been proved by experiments that some unstable phenomena will occur in long-term storage, that is, aging phenomenon.

The analysis may be affected by factors such as the characteristics of the drug itself, the preparation method, and the external environment, which may cause variation in the structure of atenolol itself and the crystal form of the substance after forming the drop pill, thereby increasing the number of drug-related substances and making the drug release time longer. Out of control, the bioavailability decreases, therefore, to some extent offset the unique advantages of dripping pills