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Trans-dermal drug administration type Cilnidipine paster for treating hypertension and preparation method thereof

A technology of dipine patch and cilnidipine, which is applied in pharmaceutical formulations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc., to reduce peak-to-valley changes, avoid liver first-pass effect and gastrointestinal tract Degradation of enzymes, the effect of prolonging blood pressure time

Active Publication Date: 2011-01-05
蚌埠丰原涂山制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Cilnidipine is a calcium antagonist with dual-channel blocking effects. In addition to the L-channel blocking effects of most calcium channel blockers, it can also act on the N-channels of peripheral nerves, so it will not cause posthypertensive reflexes Accelerated heart rate and the boosting response of baroreceptors to acute cold stimulation, thus becoming a new type of antihypertensive drug with unique pharmacological effects, but it has no antagonistic effect on P and Q channels

Method used

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  • Trans-dermal drug administration type Cilnidipine paster for treating hypertension and preparation method thereof
  • Trans-dermal drug administration type Cilnidipine paster for treating hypertension and preparation method thereof
  • Trans-dermal drug administration type Cilnidipine paster for treating hypertension and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] according to figure 2 The process flow shown for the preparation figure 1 Shown cilnidipine patch (note: the following examples are all the same), the specific preparation steps are as follows:

[0024] (1) Take 2g of azone, 6g of propylene glycol and 10g of absolute ethanol and stir evenly to make a skin penetration enhancer solution;

[0025] (2) Take by weighing 100g cilnidipine, pulverize it with a pulverizer to cross a 120 mesh sieve, add it to the solution prepared in step (1), and stir evenly; then pour it into 70g of acrylic pressure-sensitive adhesive, stir Until evenly, stir about 30 minutes, make medicine-containing pressure-sensitive adhesive (namely figure 1 Chinese medicine layer 3, the same below);

[0026] (3) The drug-containing pressure-sensitive adhesive prepared in step (2) is homogenized 3 times with a homogenizer at a pressure of 10 MPa; Release film coated with silicone polymer (i.e. figure 1 middle anti-adhesion layer 2, the same below) is ...

Embodiment 2

[0029] (1) Take 5g of azone, 8g of propylene glycol and 20g of absolute ethanol and stir evenly to make a skin penetration enhancer solution;

[0030] (2) Take by weighing 100g cilnidipine, pulverize it with a pulverizer to cross a 120 mesh sieve, add it to the solution prepared in step (1), and stir evenly; then pour it into 90g of acrylic pressure-sensitive adhesive, stir Until uniform, stir for about 30 minutes to prepare the drug-containing pressure-sensitive adhesive;

[0031] (3) The drug-containing pressure-sensitive adhesive prepared in step (2) is homogenized 3 times with a homogenizer at a pressure of 10 MPa; Dry on the anti-adhesive film coated with silicon polymer, the drying temperature is 60 ° C, the thickness is controlled to 45 μm, and then covered with aluminized film;

[0032] (4) Cut into discs with a diameter of 2 cm with a microtome, which are cilnidipine patches.

Embodiment 3

[0034] (1) Take 8g of azone, 15g of propylene glycol and 25g of absolute ethanol and stir evenly to make a skin penetration enhancer solution;

[0035] (2) Take 100g cilnidipine, pulverize it with a pulverizer to cross a 120 mesh sieve, add it to the solution prepared in step (1), and stir evenly; then pour it into 110g of acrylic pressure-sensitive adhesive, stir Until uniform, stir for about 30 minutes to prepare the drug-containing pressure-sensitive adhesive;

[0036] (3) The drug-containing pressure-sensitive adhesive prepared in step (2) is homogenized 3 times with a homogenizer at a pressure of 10 MPa; Dry on the anti-adhesive film coated with silicon polymer, the drying temperature is 65 ° C, the thickness is controlled to 50 μm, and then coated with aluminized film;

[0037] (4) Cut into discs with a diameter of 2 cm with a microtome, which are cilnidipine patches.

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Abstract

The invention provides a trans-dermal drug administration type Cilnidipine paster for treating hypertension, which is prepared by successively stacking a backing, a drug layer and an anti-adhesion layer into a whole, wherein the drug layer is prepared from Cilnidipine, a skin penetration enhancing agent and a pressure-sensitive adhesive by the weight ratio of 1:(0.08-0.23):(0.7-1.1). The Cilnidipine paster of the invention is preferentially pasted behind the neck or the parts with vena and arteries under the skin and belongs to a trans-dermal drug administration type, thereby reducing the change of the peak valley of blood concentration, avoiding the first-pass effect of livers and the degradation of gastrointestinal tract enzymes and reducing adverse reaction; and the release quantity of the drug is controlled to be slow by dissolving the drug in the pressure-sensitive adhesive, without a controlled release film structure, therefore, the structure of the Cilnidipine paster is simple, and the effects of slow and stable drug release and hypertension reduction time extension can be achieved.

Description

technical field [0001] The invention relates to the technical field of drug dosage form design, in particular to a transdermal cilnidipine patch for treating hypertension and a preparation method thereof. Background technique [0002] Cinidipine is a third-generation dual-channel dihydropyridine calcium channel blocker with good antihypertensive effect. Animal experiments have found that high-potential-activated calcium channels include five types, including N, P, Q, and R-type calcium channels in addition to L-type calcium channels; it is now believed that L-channel selective calcium channel blockers have reflex The effect of increasing heart rate, non-L channel selective calcium channel blockers have no such effect. Cilnidipine is a calcium antagonist with dual-channel blocking effects. In addition to the L-channel blocking effects of most calcium channel blockers, it can also act on the N-channels of peripheral nerves, so it will not cause posthypertensive reflexes Acce...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/4422A61K47/22A61K47/32A61P9/12
Inventor 陈鹏刘兆祥王超薛世静汪洪湖
Owner 蚌埠丰原涂山制药有限公司
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