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Transdermal penetration-promoting composition and application thereof in timolol preparation

A technology of timolol and composition, which is applied in the field of application of timolol preparations, can solve problems such as hemangiomas not appearing

Active Publication Date: 2021-03-05
WUHAN CONFORM PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, external application of timolol for IH is suitable for superficial and small lesions, and hemangiomas located deep in the subcutaneous area are not included in the recommendations for external application of timolol

Method used

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  • Transdermal penetration-promoting composition and application thereof in timolol preparation
  • Transdermal penetration-promoting composition and application thereof in timolol preparation
  • Transdermal penetration-promoting composition and application thereof in timolol preparation

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0039] 1. Preparation of Ex vivo Skin

[0040] Get the male piglet (age: 1 month), remove the hair from the abdomen with an electric razor, and apply the moisturizing agent glycerin solution to the skin at the depilated place. Execute before the test, take the hairless skin to remove the subcutaneous fat, rinse it with distilled water repeatedly until it is clean, and use filter paper to blot the remaining distilled water on the skin surface to obtain the final product.

[0041] 2. Ex vivo transdermal device and method

[0042] The improved Franz vertical diffusion cell was used for transdermal experiment. The stirrer was placed in the receiving tank, and the pig skin (pig abdomen skin) was placed between the supply chamber and the receiving tank. The dermis faced the receiving liquid and fixed. Use the receiving tank as the receiving solution, and then apply about 0.5g of the test product on the pigskin, the effective penetration area is 3.14cm 2 . Place the diffusion cell...

Embodiment 1

[0045] The transdermal effect contrast of embodiment 1 timolol maleate and timolol

[0046] Timolol maleate gel preparation process:

[0047] Weigh 2% of hypromellose and 15% of glycerin and mix well and add appropriate amount of water to form the gel matrix, and another 5% of timolol maleate is dissolved completely with appropriate amount of water (heated to 50°C and stirred) To obtain timolol maleate solution, add the dissolved timolol maleate solution to the gel matrix to obtain mixture A, weigh 2% laurocaprolactone and 5% propylene glycol and mix well and then add the mixture In A, stir evenly to obtain a timolol maleate gel sample.

[0048] Timolol ointment preparation process:

[0049] Weigh 5% white beeswax and 88% white petrolatum in a suitable container, heat in a water bath at 80°C to melt, and stir to mix evenly to obtain mixture A; after lowering the temperature of mixture A slightly, weigh 5% timolol Er and 2% laurocaprazine were added to the mixture A, stirred...

Embodiment 2

[0053] The transdermal effect contrast of embodiment 2 various timolol ointment prescriptions

[0054] As shown in Table 2, weigh light liquid paraffin, white vaseline and white beeswax in the prescribed amount in a suitable container, and put them in a water bath at 80°C until they are completely melted to obtain mixture A. Cool the mixture A to 65°C, keep it warm, weigh the prescribed amount of timolol and add it to the mixture A, stir for 6 minutes to dissolve completely, continue to stir and cool to room temperature to get final product.

[0055] Table 2 Various timolol ointment prescriptions

[0056]

[0057] The above-mentioned 6 prescription samples were subjected to transdermal test, and the influence of different prescriptions on drug transdermal behavior was investigated through piglet abdominal skin in vitro transdermal test. 4 mL of receiving solution was taken out at 1, 2, 4, 6 and 8 hours respectively, and at the same time Supplement with the same volume of b...

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Abstract

The invention provides a transdermal penetration-promoting composition for improving the transdermal absorption effect of timolol. The transdermal penetration-promoting composition is prepared from 65-98wt% of albolene and 2-35wt% of wax substances. The transdermal penetration-promoting composition can achieve the cumulative penetration amount of timolol of about 92.61 micrograms per square centimeter within 8 hours without additionally using other conventional transdermal penetration-promoting agents, the transdermal absorption promoting effect is remarkable, the skin irritation is low, and the safety is higher.

Description

technical field [0001] The invention relates to a transdermal penetration enhancer, in particular to a composition mainly composed of various substances, which is beneficial to drug transdermal absorption, and its application in timolol preparations. Background technique [0002] Infantile hemangiomas (IH) are one of the most common childhood benign tumors in the world. According to literature reports, the incidence rate of common neonatal hemangiomas is 1.1% to 2.6%, and premature infants can reach 10% or even higher. The incidence rate of girls is three times that of boys (Chinese Journal of Oral and Maxillofacial Surgery, 2011, 9(1): 61-67). Early literature reports that most infantile hemangiomas do not require treatment, but about 12% of high-risk patients may have to receive treatment due to the impact on organ function or even life-threatening. At present, in view of the potential harm of IH to children's physiology and psychology, especially the special site and spe...

Claims

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Application Information

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IPC IPC(8): A61K47/06A61K47/44A61K31/5377A61P35/00
CPCA61K47/06A61K47/44A61K31/5377A61P35/00A61K9/06A61K31/138A61K2300/00A61K35/64A61K35/06A61K9/0014A61K31/165A61K35/644
Inventor 周小顺牟东升童国富刘芝梅廖园贺容丽刘文双
Owner WUHAN CONFORM PHARMA CO LTD
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