Sustained and controlled-release transdermal patch containing lisinopril

A technology of transdermal patch and penetration enhancer, which is applied in the field of pharmaceutical preparations, can solve problems such as difficult control of process-related technical parameters, poor drug compliance, and unstable release rate, so as to avoid the first-pass effect and prolong blood drug production. Concentration stable period, the effect of improving drug safety

Active Publication Date: 2017-08-11
FERGUSON WUHAN BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

This patent can achieve a stable depressurization effect within 24 hours, but its process is complicated, the process-related technical parameters are not easy to control, th

Method used

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  • Sustained and controlled-release transdermal patch containing lisinopril
  • Sustained and controlled-release transdermal patch containing lisinopril
  • Sustained and controlled-release transdermal patch containing lisinopril

Examples

Experimental program
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Effect test

Embodiment 1

[0038] The embodiment of the present invention provides a sustained and controlled release transdermal patch containing lisinopril, comprising a drug reservoir layer, a backing layer and a protective layer, the drug reservoir layer is composed of lisinopril, reservoir matrix and Permeation enhancer composition, the sustained and controlled release transdermal patch containing lisinopril contained in each patch contains effective dose of lisinopril 80mg, by mass percentage, the drug reservoir layer contains 16 mg of lisinopril %, storage matrix 80%, penetration enhancer 4%, the content of the storage matrix in the drug storage layer is 100mg / cm 2 .

[0039] The drug reservoir layer of the transdermal patch in this example contains 80 g of lisinopril, 400 g of polyisobutylene pressure-sensitive adhesive, 10 g of lecithin, and 10 g of azone per 1000 patches. The backing layer is polyvinyl chloride and the protective layer is polyethylene.

Embodiment 2

[0041] The embodiment of the present invention provides a sustained and controlled release transdermal patch containing lisinopril, comprising a drug reservoir layer, a backing layer, a protective layer and an adhesive layer, the drug reservoir layer is composed of lisinopril, reservoir Reservoir matrix and permeation enhancer composition, the sustained and controlled release transdermal patch containing lisinopril contained in each paste contains effective dose of lisinopril 40mg, by mass percentage, the drug reservoir layer contains lisinopril 10% of Puli, 87.75% of reservoir matrix, 2.25% of penetration enhancer, the content of reservoir matrix in drug reservoir layer is 87.75mg / cm 2 .

[0042]Every 1000 pastes in the drug reservoir layer of the transdermal patch in this embodiment contain: lisinopril 40g, silicone pressure-sensitive adhesive 320g, carbomer 15g, triethanolamine 16g, lecithin 4.5g, azone 4.5g . The backing layer is non-woven fabric, the protective layer is...

Embodiment 3

[0044] The embodiment of the present invention provides a sustained and controlled release transdermal patch containing lisinopril, comprising a drug reservoir layer, a backing layer, and a protective layer, and the drug reservoir layer is composed of lisinopril, reservoir matrix and Penetration enhancer composition, the sustained and controlled release transdermal patch containing lisinopril described in each paste contains the lisinopril 80mg of effective dosage, by mass percentage, contains lisinopril 25mg in the described drug storage layer %, storage matrix 70%, penetration enhancer 5%, the content of the storage matrix in the drug storage layer is 50mg / cm 2 .

[0045] Every 1000 pastes in the drug reservoir layer of the transdermal patch in this embodiment contain: lisinopril 80g, silicone pressure-sensitive adhesive 287g, povidone 5g, methylcellulose 8g, lecithin 12g, azone 8g . The backing layer is polyester film, and the protective layer is polytetrachlorethylene fi...

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Abstract

The invention discloses a sustained and controlled-release transdermal patch containing lisinopril, and relates to the field of pharmaceutical preparations. The transdermal patch comprises a drug reservoir layer, a backing layer and a protective layer, wherein the drug reservoir layer is composed of the lisinopril, a reservoir substrate and a penetration enhancer. The drug reservoir layer of each dosage of the sustained and controlled-release transdermal patch consists of 10-80mg of the lisinopril in terms of effective dose; and in percentage by weight, the drug reservoir layer consists of 2.5-25% of the lisinopril, 70-97% of the reservoir substrate and 0.5-5% of the penetration enhancer. The sustained and controlled-release transdermal patch containing the lisinopril provided by the invention, in comparison with lisinopril normal tablets, capsules or oral sustained-release preparations on the current market, is uniform in drug release, concrete in curative effect and stable in quality.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a sustained and controlled release transdermal patch containing lisinopril. Background technique [0002] Lisinopril is a new generation of angiotensin-converting enzyme inhibitors, which mainly lowers blood pressure by inhibiting the adrenaline-angiotensin-aldosterone system, and is mainly used for the treatment of essential hypertension. Its structural formula is: [0003] [0004] Molecular formula: C 21 h 35 N 3 o 7 . [0005] At present, domestic lisinopril preparations are mainly film-coated oral tablets, 5-10 mg each time, once a day. After oral administration, the peak plasma concentration generally appears about 7 hours after taking the drug, but the time of peak plasma concentration in patients with acute myocardial infarction tends to lag slightly. Phase, but does not lead to drug accumulation. [0006] The onset of hypertensive patients has the ch...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K38/05A61K47/24A61K47/22A61P9/12
CPCA61K9/0002A61K9/7084A61K38/05A61K47/22A61K47/24
Inventor 赵小伟刘欣黄飞欧阳康乐
Owner FERGUSON WUHAN BIOTECH
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