Transdermal drug delivery system of high-solubility ibuprofen or structural analog of ibuprofen

A drug delivery system and a technology similar in structure, applied in the field of transdermal drug delivery systems of high-solubility ibuprofen or its structural analogs, can solve the problems of large patch area, unpracticalability, low content and the like

Active Publication Date: 2019-03-01
DEMOTECH INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

A variety of ibuprofen transdermal administration methods have been publicly reported in the literature at present, but due to the relatively low content, the area of ​​the patch is too large, and the practical purpose cannot be achieved

Method used

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  • Transdermal drug delivery system of high-solubility ibuprofen or structural analog of ibuprofen
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  • Transdermal drug delivery system of high-solubility ibuprofen or structural analog of ibuprofen

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0090] A transdermal drug delivery system for ibuprofen with high solubility, comprising a polymer matrix layer, the polymer matrix layer comprising active ingredient ibuprofen, HPMCAS, a second polymer compound and a pressure-sensitive adhesive; the second The polymer compound is a pharmaceutically acceptable fat-soluble polymer and / or amphiphilic polymer.

[0091] Further, the ibuprofen transdermal drug delivery system of this embodiment also includes a backing layer and a protective layer; the polymer matrix layer is located between the backing layer and the protective layer.

[0092] In this embodiment, the weight content of ibuprofen in the polymer matrix layer is 30%, the weight content of the pressure-sensitive adhesive is 35%, the weight content of HPMCAS is 15%, and the weight content of the second polymer compound is 15%; Pharmaceutically acceptable excipients (such as talcum powder, colloidal SiO 2 , montmorillonite, vitamin E, etc.).

[0093] In this embodiment, ...

experiment example 1

[0101] Experimental Example 1 Stability Experiment

[0102] The ibuprofen delivery system (patch) prepared in Comparative Example 1 and Example 4 is placed under the same storage conditions (30 ± 2° C., 60% ± 10% RH), and the polymer matrix is ​​regularly observed by an electron microscope The surface condition, the observation results see figure 1 .

[0103] Continuous observation results show that both Comparative Example 1 and Example 4 can be stored stably. The types of polymers contained in the polymer matrix are different, and the morphology of the polymer matrix is ​​also different. In Comparative Example 1 where only HPMCAS is contained in the polymer matrix, the surface of the polymer matrix is ​​uniformly distributed, while in Example 4 where both HPMCAS and ethylcellulose EC are contained in the polymer matrix, the polymer matrix appears as clusters. Different types and different proportions of polymers lead to different aggregation states of the polymer matrix, ...

experiment example 2

[0104] Experimental example 2 in vitro release test

[0105] In vitro release is a basic performance index of the patch, reflecting the interaction between the active ingredient and other components in the polymer matrix. The overall properties of the polymer matrix, the interactions between ibuprofen and the polymer and other components such as hydrogen bonds, ion pairs, van der Waals forces, etc., lead to different behaviors of ibuprofen flowing in the polymer matrix. In vitro release is the basis of transdermal absorption, and only appropriate release capacity can meet specific transdermal absorption requirements.

[0106]Dissolution determination method (Chinese Pharmacopoeia 2015 Edition 4th General Rule 0931 4th Method - paddle-disc method), using PBS as the dissolution medium, the temperature is 32°C, 50 rpm, and it is operated according to the law. Take 10ml samples at 0.1h, 0.2h, 0.3h, 0.8h, 1.0h, 2.0h, 3.0h, 4.0h, 5.0h, 6.0h, 7.0h and 8.0h, filter; and accurately we...

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Abstract

The invention discloses a transdermal drug delivery system of high-solubility ibuprofen or a structural analog of the ibuprofen. The transdermal drug delivery system comprises a polymer matrix layer,and the polymer matrix layer contain active ingredients, pressure sensitive adhesive and compounds for regulating and controlling the solubility of the active ingredients, wherein the compounds comprise first polymer hyrdroxypropyl methylcellulose acetate succinate (HPMCAS) and a second polymer compound; and the second polymer compound comprises pharmaceutically acceptable fat-soluble polymers and / or amphiphilic polymers. According to the transdermal drug delivery system, by selecting the types, the using amount and the proportion of the first polymer HPMCAS and the second polymer compound, the solubility, the releasing speed and the transdermal diffusion rate of the ibuprofen or the structural analog of the ibuprofen in the transdermal drug delivery system can be selectively regulated andcontrolled; through joint action of the HPMCAS and the second polymer compound, the soluble state of the ibuprofen or the structural analog of the ibuprofen in a polymer matrix can be maintained, crystallization of the ibuprofen or the structural analog of the ibuprofen can be inhibited, and the ibuprofen or the structural analog of the ibuprofen can be preserved stably for a long term; and a production process is easy, convenient, controllable and economical.

Description

technical field [0001] The invention belongs to the technical field of transdermal drug delivery, in particular to a transdermal drug delivery system of ibuprofen with high solubility or structural analogues thereof. The invention utilizes the first polymer HPMCAS and the second polymer compound to selectively regulate the solubility, dissolution rate and transdermal diffusion rate of the ibuprofen or its analogs in a transdermal drug delivery system. The first polymer HPMCAS and the second polymer compound can inhibit the crystallization of ibuprofen or its analogues, and can be stored stably for a long time. Background technique [0002] Phenylpropionic acid derivatives are a kind of non-steroidal anti-inflammatory drug (NSAID, non-steroidal anti-inflammatory drug). Among them, ibuprofen has been widely used due to its good safety and effectiveness since it was first listed in the UK in 1969, and has been approved as an OTC drug in the UK, the United States and other coun...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K47/38A61K47/32A61K31/192A61P29/00
CPCA61K47/32A61K47/38A61P29/00A61K9/7061A61K31/192
Inventor 谢文委律嵩何双江程楠
Owner DEMOTECH INC
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