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Timolol maleate external preparation and preparation method thereof

A technology of timolol maleate and external preparation, applied in the field of timolol maleate external preparation and preparation thereof, can solve the problems of easy contamination, long sustained release time, short attack time, etc. The effect of improving stability and promoting hardening

Pending Publication Date: 2022-07-15
WUHAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Chinese patent application CN111374937A provides a gel for infantile hemangioma and its preparation method, its raw materials include timolol maleate, propranolol, glyceryl monostearate, sodium lauryl sulfate , glycerin, liquid paraffin, petrolatum, ethylparaben, purified water, NVP-maleic acid Guerbet alcohol monoester copolymer, overcomes the solution that exists easily when timolol maleate eye drops treat hemangioma Problems such as volatilization and short onset time
[0004] However, when the above-mentioned gels are applied to the skin of the affected part, although the gel has a good drug slow-release transdermal absorption effect, due to the long release time, reaching more than 4h, the gel is still basically half- Solid state, it is easy to be accidentally wiped off by clothing etc. when the patient is active, the surface of the gel is sticky, and it is easy to be contaminated with dirt

Method used

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  • Timolol maleate external preparation and preparation method thereof
  • Timolol maleate external preparation and preparation method thereof
  • Timolol maleate external preparation and preparation method thereof

Examples

Experimental program
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Embodiment approach

[0036] As a specific embodiment, the preparation method of the used nanofibers is:

[0037] (1) Clean wood, straw, cotton and linen fibers, remove impurities, dry to a moisture content of no more than 2%, and then simply grind and pulverize them into small segments no more than 3mm;

[0038] (2) adding a mixture of sodium hydroxide and dimethyl sulfoxide with a volume ratio of 1:10, stirring at a constant temperature of 25°C for 1 hour, and the mass ratio of fibers to the mixture is 1:10;

[0039] (3) Centrifuge to separate the fibers, wash and remove the residual mixture, add water to prepare a suspension with a concentration of 0.5%, first grind with a colloid mill to obtain small segments with a diameter of no more than 1 μm; then homogenize 3 times under a pressure of 1000-1200MPa ;

[0040](4) Centrifuge the suspension at high speed at 10,000 rpm for 5 minutes; remove the supernatant, and re-dry the product to a water content of no more than 1% to obtain nanofibers with ...

Embodiment 1

[0050] The timolol maleate topical preparation provided in this example, its raw materials are timolol maleate 6wt%, polylactic acid (weight average molecular weight of 100,000-200,000) 23wt%, nanofiber (cellulose mechanical grinding prepared by the method, the diameter is 5nm, the length is 5μm) 5wt%, gel matrix (poloxamer 940) 14wt%, soybean phospholipid 6wt%, surfactant (sodium deoxycholate) 1.5wt%, water retention agent ( Glycerol) 1 wt%, the remainder is deionized water.

Embodiment 2

[0052] The external preparation of timolol maleate provided in this example, its raw materials are 8wt% of timolol maleate, 18wt% of polylactic acid (weight average molecular weight of 100,000-200,000), nanofiber (cellulose mechanical grinding) prepared by the method, the diameter is 5nm, the length is 5μm) 8wt%, gel matrix (poloxamer 940) 15wt%, soybean lecithin 4wt%, surfactant (sodium deoxycholate) 1.5wt%, water retention agent ( Glycerol) 1 wt%, the remainder is deionized water.

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Abstract

The invention discloses a timolol maleate external preparation and a preparation method thereof. The timolol maleate external preparation is prepared from the following components in percentage by mass: 4 to 8 weight percent of timolol maleate, 18 to 25 weight percent of polylactic acid, 3 to 8 weight percent of nanofiber, 10 to 15 weight percent of gel matrix, 4 to 10 weight percent of phospholipid, 1 to 2 weight percent of surfactant, 0.8 to 1.2 weight percent of water-retaining agent and the balance of deionized water. The invention provides the timolol maleate external preparation in a gel form, a thin film can be formed on the surface of the external preparation after the external preparation is smeared, the external preparation is slowly hardened into a soft sheet, timolol maleate is gradually and slowly released in the hardening process, and the hardening time is basically matched with the effective drug release time; the external preparation is not easy to erase by clothes and the like, is easy to tear off after being hardened, and is convenient to use.

Description

technical field [0001] The invention relates to the technical field of timolol maleate external preparations, in particular to a timolol maleate external preparation and a preparation method thereof. Background technique [0002] Timolol maleate is a non-selective and potent β-receptor blocker, which has a blocking effect on β1 and β2 receptors; it is a white crystalline powder, odorless, bitter in taste, It is soluble in water or methanol, slightly soluble in ethanol, slightly soluble in chloroform, and almost insoluble in diethyl ether; its action strength is 8 times that of propranolol, and it can be made into external emulsions, gels, and patches. It is widely used in the treatment of glaucoma, essential hypertension, coronary heart disease, infantile hemangioma and other diseases. [0003] In the prior art, Chinese authorized patent CN106727278B provides a timolol maleate gel and a preparation method thereof, the raw materials of which include timolol maleate, carbomer...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/5377A61K47/34A61K47/36A61K47/38A61P9/10A61P9/12A61P27/06A61P35/00
CPCA61K31/5377A61K9/7015A61K47/34A61K47/38A61K47/36A61P27/06A61P9/12A61P9/10A61P35/00Y02A50/30
Inventor 蔡育王蓉周小程孙睿
Owner WUHAN UNIV
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