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Trametinib microemulsion and application thereof

A technology of trametinib and microemulsion, which is applied to trametinib microemulsion and its application field, can solve the problems of lack of topical treatment preparations, insoluble trametinib, etc., and achieves an efficient, concise and controllable preparation process, and increases the Effect of patient compliance, avoidance of hepatic first-pass effect

Pending Publication Date: 2021-08-03
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the poor solubility of trametinib and the lack of topical formulations have not been resolved

Method used

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  • Trametinib microemulsion and application thereof
  • Trametinib microemulsion and application thereof
  • Trametinib microemulsion and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Embodiment 1 trametinib is in the mensuration of saturation solubility of different oil phases, surfactant, co-surfactant

[0041] Trametinib was added into different oil phases, surfactants and co-surfactants to investigate the solubility. Through the determination of saturation solubility, the optional prescription ingredients are determined for the next step of screening.

[0042] Experimental Materials:

[0043] Test items: oleic acid (OA), ethyl oleate (EO), isopropyl myristate (IPM), caprylic capric acid glyceride (ODO), vitamin E (Vit E), methyl salicylate ( MS), caprylic capric acid polyethylene glycol glyceride (Labrasol), polyoxyethylene castor oil EL (Cremophor EL), polyethylene glycol-15 hydroxystearate (SolutolHS15), Tween 80 (Tween 80), Polyethylene Glycol 400 (PEG 400), Diethylene Glycol Monoethyl Ether (Transcutol P), Ethanol (Ethanol), 1,2-Propanediol (PG).

[0044] Experimental method: Add excess trametinib to different oil phases, surfactants, and ...

Embodiment 2

[0046] The screening of embodiment 2 surfactants

[0047] The fixed oil phase is a mixture of caprylic capric acid glyceride, methyl salicylate, and vitamin E, and the co-surfactant is Transcutol P. Microemulsions are prepared by adding different surfactants, and the pseudo-ternary phase diagram is drawn. The best surfactant is determined by drawing the pseudo-ternary phase diagram.

[0048] Experimental Materials:

[0049] Test items: caprylic capric acid polyethylene glycol glyceride (Labrasol), polyoxyethylene castor oil EL (CremophorEL), polyethylene glycol-15 hydroxystearate (Solutol HS15).

[0050] Experimental method: the mixture of glyceryl capricate, methyl salicylate, and vitamin E was used as the oil phase, and Transcutol P was used as the co-surfactant to prepare microemulsions with Labrasol, Cremophor EL, and HS15 as surfactants. According to the titration The content of each component at the end point and draw the pseudo ternary phase diagram. Compare the area...

Embodiment 3

[0053] Embodiment 3 A kind of preparation of microemulsion

[0054] The microemulsion of the present embodiment comprises the following raw materials by mass percentage:

[0055]

[0056]

[0057] Preparation method of microemulsion:

[0058] A. According to the formula ratio, at room temperature, methyl salicylate, vitamin E and caprylic acid glyceride are mixed to form a transparent and clear solution;

[0059] B. Add Transcutol P to the solution described in A according to the formula ratio;

[0060] C. According to the formula ratio, add Cremophor EL to the solution described in B, and form a clear and transparent solution through a magnetic stirrer;

[0061] D. According to the formula ratio, at room temperature, slowly add water dropwise to the solution described in C, and pass it through a magnetic stirrer until a uniform, stable, transparent and clear solution is formed.

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Abstract

The invention discloses a trametinib microemulsion and application thereof. The microemulsion is prepared from trametinib, methyl salicylate, vitamin E, caprylic capric triglyceride, diethylene glycol monoethyl ether and polyoxyethylated castor oil EL. Compared with a trametinib water suspension, the trametinib microemulsion disclosed by the invention has the advantages that the retention volume is high; Compared with oral trametinib suspension, the trametinib microemulsion has more remarkable tumor inhibition efficacy, so that the trametinib micro-emulsion can effectively inhibit the melanoma and has more remarkable curative effect and advantages in the aspect of treating the melanoma. In addition, adopted instruments and equipment are simple and convenient, the preparation process is efficient, simple and controllable, and the method is suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a trametinib microemulsion and an application thereof. Background technique [0002] Melanoma is a highly aggressive and high-mortality skin cancer, accounting for 4% of skin cancers in incidence but 79% of skin cancers in mortality. The cancerous changes of melanoma cells occur at the base between the epidermis and dermis, and may migrate to other parts in advanced stages. UV exposure is a major cause of skin melanoma and can be hereditary. During the development of melanoma, the mitogen-activated protein kinase (MAPK) and phosphatidylinositol 3-kinase (PI3K) signaling pathways are often mutated. Studies have reported that up to 90% of melanomas show abnormal activation of the MAPK pathway. The BRAFV600 mutation was found in 40% to 50% of melanomas. Among them, activated BRAF leads to downstream activation of mitogen-activated protein kinase kinase (MEK...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/14A61K47/22A61K31/519A61P35/00
CPCA61K9/1075A61K9/0014A61K47/14A61K47/22A61K31/519A61P35/00
Inventor 徐月红王文秀
Owner SUN YAT SEN UNIV
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