Compound control-released percutaneous medicine plaster for treating high blood pressure and its preparation method

A high blood pressure and drug technology, which is applied in the field of compound transdermal controlled-release patches for the treatment of high blood pressure drugs and their preparation, can solve the problem of large individual differences in drug absorption and in vivo metabolism, inaccurate curative effects, and increased incidence of adverse reactions, etc. It can avoid the peak and valley phenomenon of blood drug concentration, improve the treatment efficiency and safety, and facilitate the individualized administration of dosage.

Inactive Publication Date: 2005-07-06
王睿 +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] (1) A single drug can generally only control the blood pressure of 40% to 60% or even less patients, and the effect of severe hypertension is even worse;
[0015] (2) The dose-response curve of commonly used drugs is low and flat, and the effect is not good. When the dose is increased, the curative effect will not increase much, and the side effects will increase logarithmically;
[0020] (3) Concomitant use of drugs can inactivate counter-regulation and mutually limit the adverse compensation induced by another drug;
[0023] However, the medicines currently on the market for the treatment of hypertension are all unilateral pharmaceutical preparations, and the general dosage forms are oral tablets, injections, etc., and as mentioned above, the ideal antihypertensive effect cannot be achieved when the unilateral use is used, although clinicians can treat according to the needs of patients A combination of two or more different medicines is prescribed, but the following treatment defects still exist:
[0024] (1) Quite a few of the above-mentioned drugs for the treatment of hypertension have a large hepatic first-pass effect, and oral administration requires a large dose to achieve effective blood drug concentration, which increases the cost of treatment, but the treatment efficiency is low;
[0025] (2) Oral administration, drug absorption is greatly affected by gastrointestinal factors, drug absorption and metabolism in the body vary greatly among individuals, and the curative effect is uncertain and uncontrollable;
[0026] (3) Frequent administration is required, and the treatment of hypertension is a long-term behavior, which usually requires life-long medication, so the treatment is inconvenient for patients and the compliance is low;
[0027] (4) Based on the above reasons, the dosage of drugs is usually increased to achieve an effective therapeutic effect, but this usually causes relatively large toxic and side effects and increases the incidence of adverse reactions
Because the drug is administered orally, it is often difficult to reverse the toxic and side effects caused by the drug, which will also increase the risk and cost of treatment;
[0028] (5) From the perspective of pharmacoeconomics, the treatment cost of increasing the dose of a single drug is much greater than that of a combination of small doses of drugs
However, oral administration still has some shortcomings such as large dosage, low bioavailability, uncertain curative effect, high incidence of adverse reactions, inconvenient treatment for patients, and poor compliance.

Method used

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  • Compound control-released percutaneous medicine plaster for treating high blood pressure and its preparation method
  • Compound control-released percutaneous medicine plaster for treating high blood pressure and its preparation method

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preparation example Construction

[0080] The steps of the embodiment of the preparation method of the present invention include:

[0081] (1) Weigh the compound drug and compound transdermal penetration enhancer in proportion, dissolve them in absolute ethanol, stir at 1500-3000rpm for 20min, and form a clear solution, slowly add dibutyl sebacate dropwise in the above solution as a plasticizer agent, succinic acid as the cross-linking agent, stirring at 1500-3000rpm for 30min to make a clear solution;

[0082] (2) Add absolute ethanol to the required composite polymer material, swell naturally for 6 hours to form a transparent colloidal solution, combine the solutions of (1) and (2), and stir at 1500-3000rpm for 30min to form a clear solution containing Drug pressure sensitive adhesive reservoir viscose;

[0083] (3) apply the drug-containing pressure-sensitive adhesive reservoir viscose on the backing film with a coating machine to form a film with uniform thickness;

[0084] (4) Put the film into a blast d...

Embodiment 1

[0098] Embodiment 1: its composition structure is as figure 1 As shown, wherein: the backing film 1 adopts aluminum foil composite polyethylene film, and its thickness is about 0.05mm; 10; the mass ratio w / w accounting for the composite polymer material is 25%) and the composite transdermal penetration enhancer azone, propylene glycol, oleic acid and terpenoid turpentine (accounting for the mass ratio w / w of the composite polymer material is 25%) 3%) and the mixture of E, RS type polyacrylic resin and ethylene / vinyl acetate copolymer (EVA), its thickness is 1.6mm, protective film 5 adopts aluminum foil composite polyethylene film, and its thickness is about 0.05mm.

[0099] If it is necessary to better control the drug release rate and quickly reach the required blood drug concentration after the first administration, a rate-controlled release film and an immediate-release drug-containing pressure-sensitive adhesive layer can be sequentially added to the pressure-sensitive adh...

Embodiment 2

[0100] Embodiment 2: its composition structure is as figure 1 As shown, wherein: the backing film 1 adopts cellulose acetate film, and its thickness is about 0.1mm; Accounting for the mass ratio w / w of the composite polymer material is 15%) and composite transdermal penetration enhancer azone, propylene glycol, monolauric acid and terpenoid lemon essential oil (accounting for the mass ratio w / w of the composite polymer material is 5%) and the mixture of polyisobutylene and polyvinyl alcohol (PVA), its thickness is 1.4mm, can add protective film 5 now.

[0101] If it is necessary to better control the drug release rate and quickly reach the required blood drug concentration after the first administration, the rate-controlled release film and the immediate-release drug-containing pressure-sensitive adhesive layer can be sequentially added to the pressure-sensitive adhesive skeleton-type drug-containing reservoir layer, Such as figure 2 As shown, wherein: the rate-controlled r...

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Abstract

The invention relates to a compound control-released percutaneous medicine plaster for treating high blood pressure and its preparation method, wherein the paste comprises laminated back lining layer, a pressure-sensitive adhesive framework form medicament-containing layer and a protective film, wherein the compound medicament comprises diuretics, central alpha-acceptor excitant and cirumferential alpha-receptor blocking agent, beta-receptor blocking agent, calcium antagonist and any two of the five categories of medicament for influencing angiotensin II formation and treating high blood pressure. The invention may realize medicine administration once in front of chest or behind the ears, wherein homeostasis blood concentration can be reached.

Description

technical field [0001] The invention belongs to the technical field of drug dosage form design, in particular to a compound transdermal controlled-release patch for treating hypertension and a preparation method thereof. Background technique [0002] At present, there are more than 100 million hypertensive patients in my country, most of which have unknown causes and are a lifelong disease. Long-term and effective implementation of antihypertensive drug therapy is one of the main ways to improve the quality of life and survival rate of hypertensive patients. It has become a consensus in the academic community that hypertensive patients need to use antihypertensive drugs for life. Good control of blood pressure mainly depends on drug effects, adverse drug reactions, patient compliance, and treatment costs. The above aspects are directly related to the success or failure of treatment and the survival of patients. [0003] At present, several types of drugs commonly used in c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K45/06A61P9/12
Inventor 王睿恽榴红周筱青王文刚柴栋段澜波刘仲春
Owner 王睿
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