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Timolol maleate liposome gel and preparation method thereof

A technology of timolol lipid and timolol maleate, which is applied in the field of timolol maleate liposome gel and its preparation, can solve the problems of cold limbs and irritability, Achieve the effects of increasing concentration, reducing systemic absorption, and increasing cumulative permeation

Pending Publication Date: 2021-08-13
周斌
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in recent years, studies have shown that adverse reactions often occur, such as superficial skin folds, diarrhea during medication, milk overflow, irritability, and cold limbs, etc.

Method used

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  • Timolol maleate liposome gel and preparation method thereof
  • Timolol maleate liposome gel and preparation method thereof
  • Timolol maleate liposome gel and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Ingredients ratio: timolol maleate 0.5%, azone 1.0%, transdermal short peptide 1x10-5%, propylene glycol 1.0%, DPPE 2.0%, cholesterol 0.25%, glycerol 2.5%, hydroxymethyl ethyl Base cellulose 0.5%, carbomer 0.15%, poloxamer P407 0.5%, caprylyl hydroxamic acid 0.1%, triethanolamine 0.125%, the balance is water

[0029] Preparation:

[0030] 1. Accurately weigh 0.5g of timolol maleate, 2.0g of hydrogenated phospholipid dipalmitoylphosphatidylethanolamine (DPPE), and 0.5g of cholesterol in a pear-shaped bottle, add 50ml of ethanol to dissolve it, and ultrasonic for 10 minutes, Remove the ethanol solvent by rotary evaporation under reduced pressure at 45°C, so that the phospholipids form a uniform film on the container wall, add 20mL of pH7.4PBS, rotate for 30 minutes, let it stand for 2 hours to make it fully hydrated, and sonicate for 25 minutes under ice bath conditions to obtain horse Timolol liposome solution; 3 batches of samples were prepared, and the average encapsu...

Embodiment 2

[0034] Ingredients ratio: timolol maleate 0.5%, azone 0.5%, transdermal short peptide 5x10-5%, propylene glycol 2.0%, DPPE 4.0%, cholesterol 0.45%, glycerol 4.5%, hydroxymethyl ethyl Base cellulose 0.35%, carbomer 0.25%, poloxamer P407 0.25%, caprylyl hydroxamic acid 0.1%, triethanolamine 0.25%, the balance is water

[0035] Preparation:

[0036] 1. Accurately weigh 0.5g of timolol maleate, 4.0g of hydrogenated phospholipid dipalmitoylphosphatidylethanolamine (DPPE), and 0.45g of cholesterol in a pear-shaped bottle, add 50ml of ethanol to dissolve it, and after ultrasonication for 10 minutes, Remove the ethanol solvent by rotary evaporation under reduced pressure at 40°C, so that the phospholipids form a uniform film on the container wall, add 20mL of pH7.4PBS, rotate for 30 minutes, let it stand for 2 hours to fully hydrate, and ultrasonicate for 30 minutes under ice bath conditions to obtain horse Timolol liposome solution; 3 batches of samples were prepared, and the average ...

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Abstract

The invention provides a timolol maleate liposome gel and a preparation method thereof. The gel is prepared from timolol maleate, a penetration enhancer, a humectant, a preservative, a liposome forming agent, a gel matrix, a pH regulator and medical purified water. The prepared timolol maleate liposome gel is uniform and delicate, suitable in viscosity and easy to spread, the drug release time is prolonged through the liposome technology, the concentration of the drug at the diseased region is kept, the gel is used for treating infantile hemangioma, drug administration is convenient, meanwhile, the first-pass effect of the liver is avoided, and meanwhile the gel is convenient to use, high in safety, simple in production process and good in application prospect.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a timolol maleate liposome gel and a preparation method thereof. Background technique [0002] Infantile hemangioma is a benign tumor that often occurs in infants and young children. The incidence rate is 8% -10% in infants and young children, and it is as high as 22% in premature or low birth weight newborns. parts. Hemangioma usually proliferates rapidly within 1 year of age, and then gradually enters a self-regression period, which lasts for 5-9 years. The incidence of hemangioma in infants and young children is high. Generally, those with mild symptoms and small tumors may subside on their own, but those that occur in special parts, such as the face, mouth, eyes, and respiratory tract, may cause disfigurement and functional damage. It can also be accompanied by complications such as ulcers and bleeding, which can even be life-threatening, so it must be t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K9/06A61K31/5377A61K47/22A61K47/10A61K47/42A61P35/00
CPCA61K9/127A61K9/06A61K9/0014A61K31/5377A61K47/22A61K47/10A61K47/42A61P35/00
Inventor 周斌韦祝罗勇奇树叶
Owner 周斌
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