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Application of timolol butyryl in preparation of medicine for treating superficial, mixed or deep hemangioma

A butyryl timolol and mixed technology, which is applied in the field of medicinal chemistry, can solve the problems of special parts or deep hemangiomas that are difficult to cure, and achieve the effects of strong adipogenic ability, high skin penetration and high drug concentration

Active Publication Date: 2021-06-11
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the ointment can promote the hydration of the skin and enhance part of the transdermal function, if the lesion is thicker, the drug may not penetrate to a certain depth
It is difficult for drugs to penetrate into all parts of the tumor, so it is difficult to completely cure special parts or deep hemangiomas

Method used

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  • Application of timolol butyryl in preparation of medicine for treating superficial, mixed or deep hemangioma
  • Application of timolol butyryl in preparation of medicine for treating superficial, mixed or deep hemangioma
  • Application of timolol butyryl in preparation of medicine for treating superficial, mixed or deep hemangioma

Examples

Experimental program
Comparison scheme
Effect test

experiment Embodiment 1

[0022] Experimental Example 1. In vitro transdermal test of butyryl timolol

[0023] In this experimental example, 8-week-old female nude mice were used, and their skin was sacrificed for in vitro transdermal test.

[0024] (1) The mice used in the test were killed by neck breaking, the hair on the back of the mouse was cut off with scissors, and a piece of skin on the back of the mouse was cut;

[0025] (2) Remove the subcutaneous fat tissue with scissors, and rinse the skin with distilled water and saline;

[0026] (3) Dry the water stains on the surface of the skin with filter paper, stick it on the surface of the skin with tape, remove the tape after gently pressing, and repeat 20 times to remove the cuticle of the skin;

[0027] (4) Place the treated skin in a double-chamber osmotic diffusion device, including a diffusion pool, a receiving pool and a constant temperature water bath system. The solution in the receiving pool is 75% phosphate buffer / ethanol, the volume of...

experiment Embodiment 2

[0032] Experimental example two, in vivo transdermal test of butyryl timolol

[0033] In this experimental example, nine 3-week-old rats were used and divided into three groups, and the drugs treated were normal saline, 0.5% timolol maleate, and 0.5% timolol butyryl timolol for in vivo transdermal test.

[0034] (1) The hair on the back of the rat was cut off with scissors, and the cuticle was pasted repeatedly with adhesive tape;

[0035] (2) Soak the gauze with the three kinds of drugs respectively, stick it on the back of the rat, and cover the outside with a layer of plastic wrap to keep it moist;

[0036] (3) After 0.5, 1, 2, 4, and 8 hours, respectively, the blood of the rat was sampled once, and the skin was removed after 8 hours, fully washed with normal saline and distilled water, and then homogenized;

[0037] (4) The blood sample and skin homogenate were quickly frozen in a -80°C refrigerator for mass spectrometry detection.

[0038] The in vivo transdermal exper...

experiment Embodiment 3

[0041]Experimental Example 3. Comparison of adipogenic and apoptotic functions of timolol maleate and timolol butyryl in hemangioma endothelial cells and stem cells

[0042] In this experimental example, infantile hemangioma endothelial cells (Hemangioma derived endothelial cells, HemECs) and stem cells (Hemangioma derived stem cells, HemSCs) were used. The isolation of HemECs and HemSCs from tissues was performed by CD31- and CD133-labeled magnetic beads, respectively. Infantile hemangioma samples were obtained from proliferative hemangiomas resected by reconstructive surgery at the Ninth People's Hospital Affiliated to Shanghai Jiaotong University School of Medicine. The specimens were put into 50ml centrifuge tubes, shaken and washed twice with PBS, stored at room temperature with 5% BSA, and transported to the laboratory. Put 5ml in a Petri dish containing 3mM CaCl 2 HBSS (CaCl-free 2 and MgSO 4 ) solution, put it into the specimen, remove the epidermis and subcutaneou...

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Abstract

The invention relates to an application of butyryl timolol in preparation of a medicine for treating superficial, mixed or deep infant hemangioma.

Description

technical field [0001] The application relates to the field of medicinal chemistry, in particular to the use of butyryl timolol in the preparation of medicines for treating superficial, mixed or deep hemangiomas. Background technique [0002] Infantile hemangioma is one of the most common benign tumors in infants. The incidence rate in Caucasians is as high as 10-12%, and the incidence rate in newborns in my country is as high as 1%. twenty million. About 10% of children will have serious complications such as ulcers, infection, pain, and even blindness and suffocation during the course of the disease. Even if there are no such complications, there will still be residual fatty fibrous tissue or (and ) surface skin texture changes, leading to secondary deformities, coupled with the characteristics of its prone to occur in the head and face, which has to be repaired by plastic surgery in the later stage, so early intervention in the treatment of hemangiomas becomes particularl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/5377A61P35/00
CPCA61K31/5377A61P35/00Y02A50/30
Inventor 黄永焯林晓曦仇雅璟王慧媛陈彬马刚陈辉金云波杨希
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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