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Tulobuterol transdermal patch and preparation method thereof

The technology of a transdermal patch and tulobuterol is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., which can solve the problem of poor skin permeability of drugs and the inability to maintain transdermal drug delivery , low drug loading and other issues, to achieve the effect of increasing the initial transdermal rate and enhancing the initial transdermal rate

Inactive Publication Date: 2021-06-25
苏州肌之究极医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The known tulobuterol transdermal patch technology uses synthetic rubber-based adhesives or acrylate adhesives, the drug has a low drug loading in synthetic rubber-based adhesives and acrylate adhesives, and has Poor skin permeability, unable to maintain 24-hour transdermal administration and other issues

Method used

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  • Tulobuterol transdermal patch and preparation method thereof
  • Tulobuterol transdermal patch and preparation method thereof
  • Tulobuterol transdermal patch and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0033] Such as figure 1 Described, a kind of tulobuterol transdermal patch, comprises drug-impermeable backing layer 2, drug storage layer 1 and anti-adhesive layer 3, contains in the described drug storage layer 1:

[0034] a first adhesive layer 1.1 comprising tulobuterol in amorphous form; and a second adhesive layer 1.1 provided under said first adhesive layer 1.1 so as to be in contact with said first adhesive layer 1.1 and comprising tulobuterol crystals Two adhesive layers 1.2; and the solubility of tulobuterol in the first adhesive layer 1.1 is 2 to 8 times that of tulobuterol in the second adhesive layer 1.2;

[0035] Wherein, the adhesive of the first adhesive layer 1.1 and the second adhesive layer 1.2 is a mixed matrix composed of polyacrylate pressure-sensitive adhesive and acrylate-rubber copolymer adhesive; in parts by weight, the The first adhesive layer 1.1 contains 65-95 parts of polyacrylate pressure-sensitive adhesive and 25-40 parts of acrylate-rubber cop...

Embodiment 2

[0043] Such as figure 2 As shown, a tulobuterol transdermal patch comprises a drug-impermeable backing layer 2, a drug reservoir layer 1 and an anti-adhesive layer 3, and the drug reservoir layer 1 contains:

[0044] A first adhesive layer 1.1 comprising tulobuterol in amorphous form; a second adhesive layer 1.1 provided below said first adhesive layer 1.1 in contact with said first adhesive layer 1.1 and comprising tulobuterol crystals an adhesive layer 1.2; and a tulobuterol-free rate controlling layer 1.3 provided under said first adhesive layer 1.1 and over said second adhesive layer 1.1 and controlling the rate of delivery of said tulobuterol and the solubility of the tulobuterol in the first adhesive layer 1.1 is 2 to 8 times that of the tulobuterol in the second adhesive layer 1.2; the second adhesive layer The solubility of tulobuterol in 1.2 is 1.5 to 5 times that of tulobuterol in rate control layer 1.3;

[0045] Wherein, the adhesive of the first adhesive layer 1...

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Abstract

The invention discloses a tulobuterol transdermal patch and a preparation method thereof. The patch comprises a medicine storage layer, the medicine storage layer comprises a first adhesive layer containing amorphous tulobuterol; and a second adhesive layer which is arranged below the first adhesive layer, is in contact with the first adhesive layer and comprises tulobuterol crystals, wherein the solubility of tulobuterol of the first adhesive layer is 2-8 times that of tulobuterol of the second adhesive layer. The medicine storage layer adopts a mixed matrix composed of a polyacrylate pressure-sensitive adhesive and an acrylate-rubber copolymer adhesive according to a specific content, the solubility of the tulobuterol medicine in the matrix can be enhanced, and the tulobuterol medicine exists in the first adhesive layer in an amorphous supersaturated state, so that the initial transdermal rate of the tulobuterol medicine can be remarkably enhanced; the tulobuterol crystals of the second adhesive layer are used for timely supplementing released medicines, so that the initial transdermal rate is remarkably improved, and meanwhile, long-time (48-72 hours) continuous approximate constant-speed transdermal administration is maintained.

Description

technical field [0001] The invention relates to the field of transdermal pharmaceutical preparations, in particular to a tulobuterol transdermal patch and a preparation method. Background technique [0002] Tulobuterol is a selective agonist acting on sympathetic β2 receptors, clinically used to relieve symptoms such as dyspnea caused by bronchial asthma, acute bronchitis, chronic bronchitis, emphysema and other airway obstructive diseases. [0003] Tulobuterol has a molecular weight of 227.7, a melting point of 91.6, and an oil-water partition coefficient of 1.03. It is relatively stable in solution without degradation products. The above physical and chemical properties just show that tulobuterol is a good percutaneous absorption drug, and is suitable for being prepared into a transdermal absorption patch. The known tulobuterol transdermal patch technology uses synthetic rubber-based adhesives or acrylate adhesives, the drug has a low drug loading in synthetic rubber-base...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K47/32A61K31/137A61P11/00A61P11/06
CPCA61K9/7053A61K31/137A61P11/00A61P11/06
Inventor 陈伟强
Owner 苏州肌之究极医药科技有限公司
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