Stable tulobuterol percutaneous absorption preparation

A technology of tulobuterol and preparations, which can be applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, respiratory diseases, etc. Low, unable to maintain good efficacy and other problems, to achieve the effect of reducing discomfort, superior adhesion, and simple structure

Active Publication Date: 2021-05-25
BEIJING TIDE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This patented technology allows small area pads that are easy to use with drugs like tacrolimod or salicylic acid to be effective over an extended period without causing sweating or other negative side effect from prolonged exposure. These tiny areas help reduce pain while still being able to deliver their medications effectively through this route into deeper layers within your body.

Problems solved by technology

The technical problem addressed in this patents relates to improving the stability and efficiency of administering tulocycleroside through traditional ways such as applying an ointment containing medicines directly onto the patient's back without any issues associated therewith including poor stickiness during application process and reduced effective delivery rate when applied at different locations along the entire length of therapy period.

Method used

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  • Stable tulobuterol percutaneous absorption preparation
  • Stable tulobuterol percutaneous absorption preparation
  • Stable tulobuterol percutaneous absorption preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1－5

[0029] Embodiment 1-5, comparative example 1-4

[0030] Uniformly mix 39 parts by weight of 2-ethylhexyl methacrylate, 6.5 parts by weight of dodecyl methacrylate, 4.5 parts by weight of 2-ethylhexyl acrylate and 30 parts by weight of ethyl acetate, add azobisiso After 0.6 parts by weight of butyronitrile, a polymerization reaction was carried out under a nitrogen flow environment at 65° C. to prepare an alkyl (meth)acrylate polymer (referred to as binder A). A drug-containing coating solution is prepared by adding a quantitative amount of tulobuterol and an amine compound (ammonia water, diethanolamine, ethylenediamine, ammonium acetate, ammonium chloride) into a quantitative polymer ethyl acetate solution. Coat the coating solution on the release film, and dry it at 70°C for 8 minutes to make the thickness of the adhesive layer reach about 46 μm. A polyethylene terephthalate film is compounded on the surface of the adhesive layer to obtain the percutaneous absorption prepar...

Embodiment 6－10

[0041] Examples 6-10, Comparative Example 5 and Reference Example (marketed product)

[0042] Add 4.0 to 4.8 parts by weight of tulobuterol, 0.05 parts by weight of ammonia water, 1.0 parts by weight of Span 80 and 3.0 parts by weight of DL-α-tocopherol in the quantitative binder A ethyl acetate solution, Mix to obtain the drug-containing coating solution. Apply the coating solution on the surface of the release film, and dry it at 70°C for 8 minutes to make the thickness of the adhesive layer reach about 46 μm. A polyethylene terephthalate film is compounded on the surface of the adhesive layer, namely the percutaneous absorption preparation of dertulobuterol. As a comparative example, a tulobuterol percutaneous absorption preparation was prepared using a carboxyl group-containing acrylic binder. Tables 4 and 5 are the formulations (by weight) of Examples 6-10 and Comparative Example 5.

[0043] 【Table 4】

[0044]

[0045] 【table 5】

[0046]

[0047] A transdermal ...

Embodiment 8

[0061] Embodiment 8: There is no residual glue phenomenon in the sticking part, there is no peeling off around the patch, and the peeling strength is weak;

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Abstract

The invention relates to a tulobuterol transdermally absorbed preparation, which has good application properties, has little change in adhesive force after application, and is capable of maintaining a certain drug release rate over a long period of time. According to the invention, an amine compound is added into an adhesive layer, so that the stability of tulobuterol is effectively improved, the precipitation of tulobuterol medicine crystals is inhibited, a small amount of medicine in the tulobuterol patch can be fully absorbed into the body, and the medicine absorbability and bioavailability are improved.

Description

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Claims

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Application Information

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Owner BEIJING TIDE PHARMA
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