Lasofoxifene tartrate emplastrum

A technology of lasoxifene tartrate and plaster, which is used in sheet delivery, sexual diseases, bone diseases, etc., can solve the problem that the dosage of microemulsion preparation is difficult to control, the transdermal effect cannot meet the requirements, and the drug is easy to wipe off. and other problems to achieve the effect of reducing the incidence of drug toxic and side reactions, avoiding the first pass effect, and facilitating production automation

Inactive Publication Date: 2014-06-04
崔书豪
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, external preparations need a longer administration time, and the exposure time of the drug site is too short, and the transdermal effect may not meet the requirements, and if it is covered with clothing, it is easy to wipe off the medicine and pollute the clothing; meanwhile, the microemulsion preparation It is also difficult to control the dosage of

Method used

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  • Lasofoxifene tartrate emplastrum
  • Lasofoxifene tartrate emplastrum
  • Lasofoxifene tartrate emplastrum

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036]

[0037]

[0038] Using this prescription, lasofoxifene tartrate microemulsion was prepared for future use. Heat the acceptable excipients to 140-160°C to melt, then lower the temperature to 90-100°C, add the adhesion enhancer and spare lasofoxifene tartrate microemulsion, mix well, and then pour the mixture while hot On the release film [release paper], cover with another layer of release film, pressurize both sides to form a film. After the above film is cooled to room temperature, the upper layer of peeling film is peeled off, and the non-woven fabric is covered on the adhesive layer and pressurized to make 1000 pieces.

Embodiment 2

[0040]

[0041] Using this prescription, lasofoxifene tartrate microemulsion was prepared for future use. Heat the acceptable excipients to 140-160°C to melt, then lower the temperature to 90-100°C, add the adhesion enhancer and spare lasofoxifene tartrate microemulsion, mix well, and then pour the mixture while hot On the release film [release paper], cover with another layer of release film, pressurize both sides to form a film. After the above film is cooled to room temperature, the upper layer of peeling film is peeled off, and the non-woven fabric is covered on the adhesive layer and pressurized to make 1000 pieces.

Embodiment 3

[0043]

[0044] Using this prescription, lasofoxifene tartrate microemulsion was prepared for future use. Heat the acceptable excipients to 140-160°C to melt, then lower the temperature to 90-100°C, add the adhesion enhancer and spare lasofoxifene tartrate microemulsion, mix well, and then pour the mixture while hot On the release film [release paper], cover with another layer of release film, pressurize both sides to form a film. After the above film is cooled to room temperature, the upper layer of peeling film is peeled off, and the non-woven fabric is covered on the adhesive layer and pressurized to make 1000 pieces.

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PUM

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Abstract

The invention discloses a lasofoxifene tartrate emplastrum preparation and a preparation method for the same. According to the preparation method disclosed by the invention, lasofoxifene tartrate micro-emulsion is prepared into a transdermal emplastrum, and the transdermal emplastrum is divided into four layers, that is, an anti-sticking layer, an adhesive layer, a backing layer and a medicine storage layer; the medicinal ingredient is lasofoxifene tartrate micro-emulsion, and is composed of lasofoxifene tartrate used as an active ingredient, polysorbate 80 used as a surfactant, propylene glycol used as a cosurfactant, pure water or distilled water and the like. Some non-polar polymers, a plasticizer, a tackifier, a transdermal accelerant and an antioxidant are further added in the emplastrum preparation disclosed by the invention besides the medicinal ingredients above. The lasofoxifene tartrate emplastrum preparation disclosed by the invention has the positive significance that compared with the existing dosage forms and tablets, the lasofoxifene tartrate emplastrum preparation has the prominent advantages of being lasting in efficacy, safe and low-toxicity, convenient, simple and sanitary to use, and accurate in medication dose.

Description

field of invention [0001] The invention relates to the field of chemical pharmacy, in particular to a lasofoxifene tartrate plaster. Background of the invention [0002] For more than half a century, improving the quality of life of postmenopausal women has attracted more and more attention. Hormone replacement therapy (HRT) has been widely used in perimenopausal and postmenopausal women. Although evidence from observational data has accumulated over the years, the benefits and harms of HRT in healthy postmenopausal women are still being explored. On the one hand, people are in-depth research on more scientific and reasonable HRT programs, and on the other hand, they are looking for more ideal drugs suitable for postmenopausal women. Selective estrogen receptor modulators (SERMS) are a class of synthetic drugs that play estrogen-like effects in some tissues and anti-estrogen-like effects in other tissues, and are expected to be used to prevent and treat menopause-related di...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K31/40A61P19/10A61P15/00
Inventor 崔书豪王志刚薛清佩陈洪瑜
Owner 崔书豪
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