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Dermatan sulfate with low molecule and its preparing method

A dermatan sulfate, low-molecular technology, applied in the field of biomedicine, can solve the problems of low bioavailability, low bioavailability, complex process, etc., and achieve the goal of increasing the concentration of hydrogen peroxide, high bioavailability, and increasing the reaction temperature Effect

Inactive Publication Date: 2003-10-01
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
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Problems solved by technology

However, there are two major pharmacokinetic issues with dermatan sulfate: one is the short half-life and the other is low bioavailability when administered by subcutaneous and intramuscular routes
As the molecular weight of dermatan sulfate increases, its bioavailability decreases
Mascellani et al once reported the preparation of a low-molecular-weight dermatan sulfate in the U.S. Patent "Degraded dermatan sulfate with antithrombotic effect, fibrinolytic effect and anti-inflammatory activity and its pharmaceutical preparation components" (patent No. US4973580) method, this method uses heavy metal ions as a catalyst to degrade dermatan sulfate, has complex processes, low yield, and introduces the disadvantages of heavy metal ions harmful to human body

Method used

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Embodiment Construction

[0012] A best example of the practice of the present invention is given below.

[0013] The key to the preparation of low-molecular-weight dermatan sulfate is to control the molecular weight. This method adopts the hydrogen peroxide degradation method to obtain low-molecular-weight dermatan sulfate with a controllable degree of degradation.

[0014] (1) Preparation of low-molecular dermatan sulfate: make 1.0% solution of dermatan sulfate fine product with distilled water, adjust pH to 4-5, add 30% hydrogen peroxide dropwise to make the final concentration reach 2%, place in 70°C water bath Stir for 15 hours, adjust the pH to 7 with sodium hydroxide solution, and precipitate with 3 times the amount of methanol;

[0015] (2) Purification of low-molecular dermatan sulfate: the precipitate in step (1) is made into a 0.5% solution, and the membrane ultrafiltration with a molecular cut-off value of 8kD is used to collect the permeate, which is concentrated with a rotary evaporator a...

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Abstract

A low-molecular (3000-8000) dermatan sulfate is prepared from the dermatan sulfate through degradation by hydrogen peroxide, ultrafilter, and gel chromatography. Its advantages are sure thrombus-resistant and thrombolytic functions, easy absorption, long semi-life and high biologic utilization rate.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a low-molecular dermatan sulfate and a preparation method thereof. Background technique [0002] Dermatan sulfate is a kind of complex structure and sulfated glycosaminoglycans. The molecular weight of natural products is generally 15kD ~ 5kD, and it is widely found in animal tissues. Studies at home and abroad have shown that the anticoagulant activity of dermatan sulfate is lower than that of unfractionated heparin, but its antithrombotic activity is significantly higher than that of unfractionated heparin, and its bleeding side effects are significantly smaller than that of unfractionated heparin. . However, there are two major pharmacokinetic problems with dermatan sulfate: one is the short half-life, and the other is low bioavailability when administered by subcutaneous and intramuscular routes. As the molecular weight of dermatan sulfate increases, its bioavailabili...

Claims

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Application Information

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IPC IPC(8): A61P7/02C08B37/08
Inventor 姬胜利王凤山迟延青谢继青
Owner SHANDONG UNIV
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