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Dabrafenib transdermal preparation composition and preparation method of dabrafenib transdermal preparation

A technology for dabrafenib transdermal and transdermal preparations is applied in the field of preparation of dabrafenib transdermal preparation compositions and dabrafenib transdermal preparations, and can solve gastrointestinal irritation, poor specificity and low efficiency and other problems, to achieve the effect of high transdermal absorption rate and high specificity

Pending Publication Date: 2021-10-26
REYOUNG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The route of administration of dabrafenib that has been marketed is basically oral, and the side effects are relatively large after oral administration; oral administration is delivered to the lesion site, which not only has low efficiency and poor specificity, but also causes liver toxicity, gastrointestinal irritation, etc.
The transdermal absorption of drugs is affected by the nature of the drug and the skin barrier, resulting in a low absorption rate of transdermal preparations

Method used

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  • Dabrafenib transdermal preparation composition and preparation method of dabrafenib transdermal preparation
  • Dabrafenib transdermal preparation composition and preparation method of dabrafenib transdermal preparation
  • Dabrafenib transdermal preparation composition and preparation method of dabrafenib transdermal preparation

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Table 1 Prescription

[0029]

[0030]

[0031] making process:

[0032] (1) Dissolve 10 g of dabrafenib in 40 g of isopropanol.

[0033] (2) Heat 10g of glycerin, 10g of azone laurate, 7g of lecithin, 3g of sodium cholate, 1g of sodium benzoate, and 20g of stearin into a solution state, stir for 10 minutes using a high-speed homogenizer, and add isopropanol solution and continue stirring for 10 minutes.

[0034] (3) After static cooling, put it into the prepared composite hose and seal it. That is, dabrafenib cream.

[0035] Test results:

[0036] The transdermal absorption diffusion cell was used to detect the transmittance, and the results are shown in Table 2.

[0037] Table 2 Transmittance test results

[0038] time (hours) Dabrafenib Concentration (mg / mL) 3 0.015 6 0.033 12 0.043

Embodiment 2

[0040] Without adding lecithin, the more commonly used transdermal penetration enhancers azone laurate and oleic acid were used to prepare samples, and relevant transdermal tests were carried out.

[0041] Table 3 Prescription

[0042]

[0043] making process:

[0044] (1) Dissolve 10 g of dabrafenib in 40 g of isopropanol.

[0045] (2) Heat 10g of glycerin, 17g of azone or oleic acid, 3g of sodium cholate, 1g of sodium benzoate, and 20g of stearin into a solution state, use a high-speed homogenizer to stir for 10 minutes, and add isopropanol containing dabrafenib solution, stirring was continued for 10 minutes.

[0046] (3) After static cooling, put it into the prepared composite hose and seal it. That is, dabrafenib cream.

[0047] Test results:

[0048] The transdermal absorption diffusion cell was used to detect the transmittance, and the test results are shown in Table 4.

[0049] Table 4 Transmittance test results

[0050]

[0051] Conclusion: Without adding...

Embodiment 3

[0053] The test was carried out with azone laurate or lecithin, respectively.

[0054] Table 5 Prescription

[0055]

[0056] making process:

[0057] (1) Dissolve 10 g of dabrafenib in 40 g of isopropanol.

[0058] (2) Heat 10g of glycerin, 17g of azone laurate or lecithin, 10g of oleic acid, 3g of sodium cholate, 1g of sodium benzoate, and 20g of stearin into a solution state, stir for 10 minutes using a high-speed homogenizer, and add The isopropanol solution of Rafenib was stirred for an additional 10 minutes.

[0059] (3) After static cooling, put it into the prepared composite hose and seal it. That is, dabrafenib cream.

[0060] Test results:

[0061] The transdermal absorption diffusion cell was used to detect the transmittance, and the test results are shown in Table 6.

[0062] Table 6 Transmittance test results

[0063]

[0064] Conclusion: The penetration rate of dabrafenib is also significantly lower when acetrene laurate lecithin is used alone.

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Abstract

The invention relates to a dabrafenib transdermal preparation composition and a preparation method of a dabrafenib transdermal preparation, and belongs to the technical field of pharmaceutical preparations. The dabrafenib transdermal preparation composition disclosed by the invention is prepared from dabrafenib, a transdermal enhancer, a solvent and a solubilizer. The dabrafenib transdermal preparation composition disclosed by the invention is high in transdermal absorption rate and effectively avoids stimulation to gastrointestinal tracts. The invention also provides the simple and feasible preparation method of the dabrafenib transdermal preparation.

Description

technical field [0001] The invention relates to a dabrafenib transdermal preparation composition and a preparation method of the dabrafenib transdermal preparation, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Dabrafenib is an effective drug for the treatment of melanoma. It is a tyrosine kinase inhibitor targeting BRAF, which has inhibitory effects on BRAF V600E, BRAF V600K, and BRAF V600D. [0003] There are few relevant reports on dabrafenib-related drugs. CN201611112050.4 discloses a dabrafenib mesylate sustained-release tablet and a preparation method thereof, wherein the dabrafenib mesylate sustained-release tablet is prepared from the following raw materials: dabrafenib mesylate 1 part of nitric acid, 0.3-0.9 part of sustained-release framework material, 0.05-0.11 part of glidant, 1.1-3.1 parts of filler, 1-6 parts of adhesive, the dabrafenib mesylate prepared according to the present invention The main drug dabrafen...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K31/506A61K47/22A61K47/24A61P35/00
CPCA61K31/506A61K9/06A61K9/0014A61K47/22A61K47/24A61P35/00
Inventor 苗得足胡清文刘满广王向华杨书华
Owner REYOUNG PHARMA
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