Controlled release transdermal patch for preventing and treating cardiovascular and cerebrovascular system diseases and preparation method thereof

Abstract

The invention relates to a controlled release transdermal patch for preventing and treating cardiovascular and cerebrovascular system diseases, which consists of a protectively layer, a medicine release layer, a medicine storage layer and a back lining layer through being sequentially overlapped, wherein the protectively layer is siliconized anti-sticking paper or a polyethylene film or a siliconized polyester film, the back lining layer is an aluminum foil, an aluminum foil and polyethylene composite film or a polyester composite film, the medicine releasing layer is prepared from 3 to 8 percent of cyclovimbuxine D, 60 to 70 percent of pressure sensitive adhesive substrates, 5 to 10 percent of composite transdermal penetrating agents, 20 to 30 percent of plasticizing agents and 1 to 3 percent of cross-linking agents, the medicine storage layer consists of 8 to 15 percent of the cyclovimbuxine D, 50 to 60 percent of the pressure sensitive adhesive substrates, 1 to 5 percent of composite transdermal penetrating agents, 20 to 30 percent of plasticizing agents and 1 to 3 percent of cross-linking agents. The patch of the invention is prepared by an organic solvent dispersing method, the preparation process is simple, the prepared patch has the exact curative effect, stable quality, high safety and convenient use, and is applicable to the long-time prevention and treatment of the cardiovascular and cerebrovascular diseases.

Description

technical field The invention relates to the field of medicine, in particular to a medicine for preventing and treating diseases of the cardiovascular system. Background technique Cardiovascular disease is the most serious disease that endangers people's life and health, and its morbidity and mortality rate account for the first among all kinds of diseases. Due to changes in eating habits and accelerated pace of life, the incidence of cardiovascular diseases is on the rise, which has a significant impact on the quality of life of patients. Cycloviral Buxillus D(C 26 h 46 N 2 O, Cyclovirobuxine D, whose structure is shown in formula 1) is a drug for treating cardiovascular diseases, which is recorded in "Chinese Pharmacopoeia" 2000 edition one, and has the following physical and chemical characteristics: the molecular weight is 402.364, and the melting point is 219-222 ℃, it is a colorless needle-like crystal, a fat-soluble alkaloid with a large oil-water partition coeff...

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Problems solved by technology

However, because Cyclovirbuxine D is fat-soluble, it is difficult to dissolve in a water-soluble matrix, so the use of a water-soluble matrix cannot provide an ideal transdermal rate; this patent also has a record of available non-water-soluble matrix, such as silicone, poly Traditional types of pressure-sensitive adhesives such as isobutylene and acrylates, although these matrices have been widely used in transdermal drug delivery systems, they still have many defects: (1) strong hydrophobicity, long-term use on the skin When sticking, there will be water accumulation and skin whitening; (2) the drug loading is low, when the drug concentration exceeds the saturation concentration, the performance of the pressure-sensitive adhesive will be completely changed, the viscosity will be greatly reduced, and drug crystals will be precipitated, thereby limiting (3) It takes a long time to completely swell in the solvent, which prolongs the production time. Because most of the organic solvents used are toxic, they will inevitably cause harm to the human body and cause potential safety hazards in large-scale industrial production. Hidden dangers, and the residual solvent and the rubber pressure-sensitive adhesive used will cause irritation and sensitization to the skin

In addition, the patch uses a controlled-release membrane to control the release of drugs, which increases production steps and costs, and the quality of the controlled-release membrane will directly affect the transdermal rate of Cyclovirubuxin D

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