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Pingyangmycin polyethylene glycol (PEG)-polycaprolactone (PCL)-polyethylene glycol (PEG) temperature-sensitive slow-release gel, as well as preparation method and application of same

A technology of pingyangmycin and sustained-release gel, which is applied in the fields of preparations, biology and new pharmaceutical dosage forms, can solve the problems of the treatment effect of arteriovenous malformation, difficulty in reaching effective drug concentration, short residence time of pingyangmycin, etc., and achieve Prolong half-life and action time, reduce systemic toxic and side effects, and significantly slow-release effect

Active Publication Date: 2012-12-26
WUHAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Vascular diseases with high flow rate, such as arteriovenous malformation, usually involve arteries, and surgical resection is difficult, and the flow rate in the tube is high. Pingyangmycin stays in the diseased blood vessel for a short time, and it is difficult to achieve and maintain effective drug concentration. Therefore, clinical Treatment of superior arteriovenous malformations still needs to be improved

Method used

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  • Pingyangmycin polyethylene glycol (PEG)-polycaprolactone (PCL)-polyethylene glycol (PEG) temperature-sensitive slow-release gel, as well as preparation method and application of same
  • Pingyangmycin polyethylene glycol (PEG)-polycaprolactone (PCL)-polyethylene glycol (PEG) temperature-sensitive slow-release gel, as well as preparation method and application of same
  • Pingyangmycin polyethylene glycol (PEG)-polycaprolactone (PCL)-polyethylene glycol (PEG) temperature-sensitive slow-release gel, as well as preparation method and application of same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] A kind of Pingyangmycin PEG-PCL-PEG temperature-sensitive slow-release gel, which is made of the following raw materials in parts by weight:

[0057]

[0058] A kind of pingyangmycin PEG-PCL-PEG temperature-sensitive slow-release gel, its preparation steps are as follows:

[0059] 11g (0.01mol) ε-caprolactam (Sigma, USA, analytically pure), 5.5g (0.01mol) ethyl glycolate (Sigma, USA, analytically pure, average molecular weight 550) and 0.08g stannous isooctanoate (Shanghai Sinopharm Chemical Reagent Co., Ltd., analytically pure, accounting for 0.5% of the total reaction system mass) was added to the reaction tube for mixing, placed in a dry nitrogen environment, and reacted at 130°C for 12 hours, then added 1.68g (0.01mol) of hexamethylene di Isocyanate (Sigma, USA, analytically pure) was continuously stirred at 80°C for 6h. After the above reaction was completed, gas was pumped for 1 h under a vacuum environment, and the obtained copolymer was cooled to room temper...

Embodiment 2

[0063] A kind of Pingyangmycin PEG-PCL-PEG temperature-sensitive slow-release gel, which is made of the following raw materials in parts by weight:

[0064]

[0065]

[0066] A kind of pingyangmycin PEG-PCL-PEG temperature-sensitive slow-release gel, its preparation steps are as follows:

[0067] 11g (0.01mol) ε-caprolactam (Sigma, USA, analytically pure), 5.5g (0.01mol) ethyl glycolate (Sigma, USA, analytically pure, average molecular weight 550) and 0.08g stannous isooctanoate (Shanghai Sinopharm Chemical Reagent Co., Ltd., analytically pure, accounting for 0.5% of the total reaction system mass) was added to the reaction tube for mixing, placed in a dry nitrogen environment, and reacted at 130°C for 12 hours, then added 1.68g (0.01mol) of hexamethylene di Isocyanate (Sigma, USA, analytically pure) was continuously stirred at 80°C for 6h. After the above reaction was completed, gas was pumped for 1 h under a vacuum environment, and the obtained copolymer was cooled to...

Embodiment 3

[0071] A kind of Pingyangmycin PEG-PCL-PEG temperature-sensitive slow-release gel, which is made of the following raw materials in parts by weight:

[0072]

[0073] A kind of pingyangmycin PEG-PCL-PEG temperature-sensitive slow-release gel, its preparation steps are as follows:

[0074]11g (0.01mol) ε-caprolactam (Sigma, USA, analytically pure), 5.5g (0.01mol) ethyl glycolate (Sigma, USA, analytically pure, average molecular weight 550) and 0.08g stannous isooctanoate (Shanghai Sinopharm Chemical Reagent Co., Ltd., analytically pure, accounting for 0.5% of the total reaction system mass) was added to the reaction tube for mixing, placed in a dry nitrogen environment, and reacted at 130°C for 12 hours, then added 1.68g (0.01mol) of hexamethylene di Isocyanate (Sigma, USA, analytically pure) was continuously stirred at 80°C for 6h. After the above reaction was completed, gas was pumped for 1 h under a vacuum environment, and the obtained copolymer was cooled to room tempera...

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Abstract

The invention discloses a pingyangmycin polyethylene glycol (PEG)-polycaprolactone (PCL)-polyethylene glycol (PEG) temperature-sensitive slow-release gel, as well as a preparation method and the application of the gel. The Pingyangmycin PEG-PCL-PEG temperature-sensitive slow-release gel mainly consists of two parts comprising PEG (polyethylene glycol)-PCL (polycaprolactone)-PEG (polyethylene glycol) co-polymer and Pingyangmycin, is liquid at room temperature, and is solid gel under the in vivo 37 DEG C condition; the gel system has significant slow-release effect, thereby having functions in prolonging the half-life period and the acting time of the Pingyangmycin, reducing drug concentration in plasma, and reducing systemic toxic and side effects. The gel can be formed in situ after the medicine is injected in a high-flow-speed vessel, and then location embolism is realized, and so as to realize the, and muscularization and closing of muscle is caused, so that the sclerotherapy and the interventional therapy are combined effectively, the gel has excellent biocompatibility and degradability, is beneficial for treating hemangiomas, vascular malformations and cancers, particularly, a new selection is provided to the treatment of the vein malformation and partial malformation of cancers.

Description

technical field [0001] The present invention relates to the technical field of new dosage forms and preparations of biology and medicine, more specifically to a pingyangmycin PEG-PCL-PEG temperature-sensitive slow-release gel, and also to a pingyangmycin PEG-PCL-PEG temperature-sensitive slow-release gel. The preparation method of the release gel is simple and easy to implement. It also relates to the application of a pingyangmycin PEG-PCL-PEG temperature-sensitive slow-release gel. The new dosage form of pingyangmycin prepared by the invention provides a new choice for the preparation of local chemotherapy drugs for treating arteriovenous malformations and malignant tumors. Background technique [0002] Vascular disease is the most common benign tumor or congenital malformation in human soft tissue, especially in infants and young children. It often invades the facial skin, causing facial deformity and dysfunction, and can cause secondary infection and bleeding, which is h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/14A61K47/34A61K9/06A61P9/00A61P35/00
Inventor 陈刚冯俊任建岗王华芬张伟贾俊孙志军
Owner WUHAN UNIV
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