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Timolol long-acting transdermal preparation and application thereof in hemangioma treatment

A technology of timolol and transdermal preparations, applied in long-acting timolol transdermal preparations and its application in hemangiomas, can solve the problems of large drug side effects, adverse reactions, and leftover scars, and achieve reduction The effect of dosage, improvement of treatment effect, and promotion of efficiency

Active Publication Date: 2015-01-14
BEIJING MERSON PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Traditional treatment methods such as oral corticosteroids, local injection of pingyangmycin, surgery, laser and freezing, etc., or because of the side effects of drugs, or because the treatment process is more painful, there may be a series of adverse effects such as scars and tissue atrophy in the later stage. Reaction, so that its clinical application is limited, the overall efficacy is not satisfactory
The application of Timolol is a revolutionary change in the treatment of hemangiomas. It is a β-adrenergic receptor antagonist. It was previously used to treat hypertension, angina pectoris, and tachycardia. It is completely clear that high-dose external application of timolol in the treatment of severe infantile hemangiomas has a rapid and obvious curative effect, is well tolerated by children, and can significantly shorten the course of hemangiomas, but there are still adverse reactions, including bradycardia and hypotension , bronchospasm, hypoglycemia, drowsiness or insomnia, nightmares, decreased appetite, sweating, etc.
In general, timolol may become the first-line drug for the treatment of severe and complicated infantile hemangiomas, but oral timolol has potential cardiotoxic side effects and adverse reactions

Method used

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  • Timolol long-acting transdermal preparation and application thereof in hemangioma treatment
  • Timolol long-acting transdermal preparation and application thereof in hemangioma treatment
  • Timolol long-acting transdermal preparation and application thereof in hemangioma treatment

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1 Preparation of timolol hydrogel long-acting transdermal preparation (1)

[0027] The small molecule drug timolol is prepared into a nano / micropowder hydrogel transdermal preparation, and the preparation process is as follows:

[0028] (1) Accurately weigh 10g of timolol and dissolve it in 100mL of water, then add 20g of porous silica nanoparticles, stir overnight to make timolol fully adsorbed in the silica particles, centrifuge to remove the supernatant, and then fully Washing, then freeze-drying to form timolol nano / micropowder medicine, the particle diameter of medicine is 20~100000 nanometers;

[0029] (2) Prepare a hydrogel solution with 12% by weight of polyvinyl alcohol (molecular weight: 40,000) and 1% by weight of polyethylene glycol (molecular weight: 400);

[0030] (3) Disperse the timolol nano / micropowder drug prepared in step (1) in the hydrogel solution prepared in step (2) according to the weight ratio of 1:1, and add benzene with a final wei...

Embodiment 2

[0047] Example 2 Preparation of timolol nano hydrogel long-acting transdermal preparation (2)

[0048] The small molecule drug timolol is prepared into a nano-hydrogel long-acting transdermal preparation, and the preparation process is as follows:

[0049] (1) Accurately weigh 0.2g of timolol and dissolve it in 10mL of water, then add 1g of porous hydroxyapatite nanoparticles, stir overnight to make timolol fully adsorbed in the hydroxyapatite particles, and centrifuge to remove the supernatant , fully washed, and then freeze-dried to form timolol nano-medicine, the particle size of the nano-medicine is 20-500 nanometers;

[0050] (2) Prepare a hydrogel solution with 4% by weight of polyvinyl alcohol (molecular weight: 40,000), 4% by weight of polyvinyl alcohol (molecular weight: 136,000), and 2% by weight of polyethylene glycol (molecular weight: 400) ;

[0051] (3) Disperse the timolol nanomedicine prepared in step (1) in the hydrogel solution prepared in step (2) accord...

Embodiment 3

[0057] Example 3 Preparation of timolol nano hydrogel long-acting transdermal preparation (3)

[0058] The small molecule drug timolol is prepared into a nano-hydrogel long-acting transdermal preparation, and the preparation process is as follows:

[0059] (1) Accurately weigh 10g of timolol and dissolve it in 100mL of water, then add 40g of porous silver nanoparticles, stir overnight to make timolol fully adsorbed in the silver nanoparticles, centrifuge to remove the supernatant, then fully wash, and then Freeze-drying to form timolol nano-medicine, the particle size of nano-medicine is 10-1000 nanometers;

[0060] (2) Prepare a hydrogel solution with 8% by weight of sodium carboxymethylcellulose, 5% by weight of polyvinyl alcohol (molecular weight: 100,000), and 1.5% by weight of polyethylene glycol (molecular weight: 400);

[0061] (3) Disperse the timolol nanomedicine prepared in step (1) in the hydrogel solution prepared in step (2) according to the weight ratio of 1:1...

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Abstract

The invention relates to a timolol long-acting transdermal preparation, comprising the following preparation processes: firstly preparing timolol into a timolol nano-drug or timolol micro-powder, and then preparing the timolol nano-drug or timolol micro-powder into a timolol hydrogel transdermal preparation, an ointment transdermal preparation or a micro-needle transdermal preparation. The invention also relates to an application of the drug in hemangioma treatment. When used for treating infantile hemangioma, the medicine disclosed by the invention is capable of improving the medicine absorption efficiency of the pathological cells, and therefore the treatment effect is improved, the dosage is lowered, and no adverse reactions are generated in the treatment process.

Description

Technical field [0001] The invention involves the field of pharmaceutical technology. Specifically, it is a long -acting dermatologist and its application in hemangioma. Background technique [0002] Infantile Hemangioma (IH) is the most common benign tumor in childhood. It is caused by a baby girl and premature infant.The incidence is characterized by the rapid hyperplasia and subsequent spontaneous consciousness in the early days of birth.After the natural disappearance, local erythema, pigmentation, capillary dilatation, atrophic scars, and fibrous fat tissues are often left with a beautiful.Because the existence of hemangioma can lead to severe appearance malformation and psychological disorders, most parents urgently require early treatment.From the perspective of plastic surgery, the treatment of hemangioma in infants and young children should be based on non -invasive, leaving no scarring and non -repellent damage. [0003] Traditional treatment methods such as oral glucoc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K9/00A61K31/5377A61P35/00
Inventor 袁伟恩郑家伟吴飞张凌
Owner BEIJING MERSON PHARMA CO LTD
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