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Bazedoxifene acetate emplastrum

A technology of bazedoxifene acetate and plaster, which is applied in the directions of bone diseases, antitumor drugs, sheet delivery, etc., can solve the problem that the dosage of microemulsion preparation is difficult to control, the transdermal effect cannot meet the requirements, and it is easy to wipe off. Drugs and other problems, to avoid the peak and valley phenomenon of blood drug concentration, facilitate production automation and aseptic operation, and avoid the effect of first-pass effect

Inactive Publication Date: 2014-06-18
王志刚
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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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  • Bazedoxifene acetate emplastrum

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Bazedoxifene Acetate 20g

[0035] Propylene glycol 300g

[0036] Polysorbate 150g

[0037] Oleic acid 30g

[0038] Add pure or distilled water to 1000g

[0039] Using this prescription, the bazedoxifene acetate microemulsion was prepared for subsequent use. Heat the acceptable excipients to 140-160°C to melt, lower the temperature to 90-100°C, add the adhesion enhancer and spare bazedoxifene acetate 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

[0041] Bazedoxifene Acetate 20g

[0042] Propylene glycol 300g

[0043] Polysorbate 300g

[0044] Oleic acid 50g

[0045] Carbomer 94050g

[0046] Add pure or distilled water to 1000g

[0047] Using this prescription, the bazedoxifene acetate microemulsion was prepared for subsequent use. Heat the acceptable excipients to 140-160°C to melt, lower the temperature to 90-100°C, add the adhesion enhancer and spare bazedoxifene acetate 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

[0049] Bazedoxifene Acetate 20g

[0050] Propylene glycol 300g

[0051] Polysorbate 200g

[0052] Oleic acid 30g

[0053] Polyvinyl alcohol 100g

[0054] Add pure or distilled water to 1000g

[0055] Using this prescription, the bazedoxifene acetate microemulsion was prepared for subsequent use. Heat the acceptable excipients to 140-160°C to melt, lower the temperature to 90-100°C, add the adhesion enhancer and spare bazedoxifene acetate 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 bazedoxifene acetate emplastrum preparation and a preparation method thereof. According to the preparation method, transdermal emplastrum is prepared from bazedoxifene acetate micro-emulsion, and is divided into four layers, namely an anti-adhesive layer, an adhesive layer, a lining layer and a drug-storage layer, wherein the effective component is bazedoxifene acetate micro-emulsion, and is prepared from bazedoxifene acetate serving as an active component, polysorbate 80 serving as a surfactant, propylene glycol serving as a cosurfactant, purified water or distilled water and the like. Except the effective component, the emplastrum also comprises a non-polar polymer, a plasticizer, a tackifier, a transdermal enhancer and an antioxidant. Compared with the existing preparations, such as tablets, the bazedoxifene acetate emplastrum has the prominent advantages of durable drug effect, safety and low toxicity and accurate administration dosage, is convenient to use, and is simple and sanitary.

Description

field of invention [0001] The invention relates to the field of chemical pharmacy, in particular to a bazedoxifene acetate plaster preparation. 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...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/55A61K47/34A61P19/10A61P35/00
Inventor 王志刚崔书豪陈洪瑜薛清佩
Owner 王志刚
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