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A low-molecular-weight heparin sustained-release preparation and its preparation method and application

A low-molecular-weight heparin and sustained-release preparation technology, applied in the field of medicine, can solve the problems affecting the in vivo stability and therapeutic efficiency of the preparation, the rapid and mass release of low-molecular-weight heparin, poor biocompatibility, etc., and achieve prolonging blood half-life and in vivo stability. Excellent performance and improved compliance

Active Publication Date: 2018-04-13
INST OF PROCESS ENG CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, chitosan can only dissolve under strong acidic conditions, and its solubility is low under physiological conditions. At the same time, chitosan has high toxicity and poor biocompatibility, which seriously limit its application in vivo
In addition, the complexes and preparations formed by chitosan and its derivatives and low-molecular-weight heparin do not use cross-linking means to solidify the nanoparticles. Under the intervention of physiological media, the particles are likely to cause rapid and large-scale release of low-molecular-weight heparin, which is likely to affect the preparation. In vivo stability and therapeutic efficiency

Method used

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  • A low-molecular-weight heparin sustained-release preparation and its preparation method and application
  • A low-molecular-weight heparin sustained-release preparation and its preparation method and application
  • A low-molecular-weight heparin sustained-release preparation and its preparation method and application

Examples

Experimental program
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Effect test

Embodiment 1

[0052] In this embodiment, low molecular weight heparin sustained-release preparations are prepared by the following method, which includes the following steps:

[0053] Weigh 100mg polylysine (PLL, M W =13000Da) into a centrifuge tube, add 5mL of 5% glucose solution, and mix by ultrasonic; Measure 5mL of 15mg / mL PLL solution in a centrifuge tube, then add 5mL of 6mg / mL Traut's reagent, add a magnet, and place under a magnetic force Stir on the stirrer for 2h to carry out mercaptolation to prepare a mercaptolated PLL (PLL-SH) solution; add 60 mL of 5% glucose solution to the mercaptolated PLL (PLL-SH) solution and mix evenly, and quickly add to the mixed solution Add 100mL of 20mg / mL sodium heparin (LMWH) solution, mix well, homogenize, age for 24h to stabilize the nanoparticles, freeze-dry, and the reconstituted preparation solution is used for subsequent characterization.

[0054] The nanoparticles prepared in this embodiment were characterized by scanning electron microsco...

Embodiment 2

[0056] The difference between this example and Example 1 is that the mass ratio of PLL to low molecular weight heparin is adjusted to 5:6, and the rest of the preparation methods and conditions are the same as in Example 1. The prepared low molecular weight heparin sustained-release preparation nanoparticles The particle size and potential of nanoparticles were determined by dynamic light scattering technique (DLS).

[0057] The result is shown in Figure 2, where Figure 2A is the particle size distribution diagram of the low molecular weight heparin sustained-release preparation, as can be seen from the figure, the average particle size is about 105nm; Figure 2B It is the surface potential map of low molecular weight heparin sustained-release preparation; as shown in the figure, the surface potential is about -16mV.

Embodiment 3

[0059] In this embodiment, low molecular weight heparin sustained-release preparations are prepared by the following method, which includes the following steps:

[0060] Weigh 100mg polyhistidine (M W =1000Da) into a centrifuge tube, add 5mL of 5% glucose solution, and mix by ultrasonic; Measure 5mL of 20mg / mL PLL solution in a centrifuge tube, then add 0.1mg / mL Traut's reagent 10mL, add magnets, place Stir on a magnetic stirrer for 2 hours to carry out mercaptolation to obtain a mercaptolylated polyhistidine solution; add 50 mL of 5% glucose solution to the mercaptolylated polyhistidine solution and mix well, and quickly add 5 mL of 30 mg / mL dalteparin sodium (LMWH) solution, homogenized after mixing, aged for 24 h to stabilize the nanoparticles, and freeze-dried to prepare low molecular weight heparin sustained-release preparations.

[0061] Characterized by scanning electron microscopy and dynamic light scattering, the low molecular weight heparin sustained-release prepar...

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Abstract

The present invention provides a low-molecular-weight heparin sustained-release preparation, a preparation method and application thereof, wherein the low-molecular-weight heparin sustained-release preparation comprises nanoparticles formed by polypeptides and low molecular weight heparin, and the polypeptides are cross-linked through chemical bonds. The present invention adopts any one or a combination of at least two of self-assembly technology, freeze-drying technology, homogenization technology, emulsification technology, embedding technology or spray-drying technology to prepare low molecular weight heparin sustained-release preparation. The low-molecular-weight heparin sustained-release preparation of the invention has a release rate of only about 20% within 500 hours under in vitro conditions, has a sustained-release effect, can effectively prolong its blood half-life, avoid the "peak-to-valley fluctuation" of the drug, and reduce the dosage of the low-molecular-weight heparin solution. The risk of hemorrhage when the dose is used, the toxic and side effects of the drug are reduced, the compliance of patients is improved, and the treatment efficiency of the disease is improved, and can be used for the prevention and treatment of thrombosis diseases. The preparation method of the invention is simple and has broad application prospects.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a slow-release preparation of low-molecular-weight heparin, a preparation method and application thereof. Background technique [0002] my country has entered an aging society, and the number of elderly people is gradually increasing. Thrombosis is one of the most common diseases in the elderly population, with a high incidence and a wide patient population. The sequelae of thrombosis seriously affect the patient's ability to work and even become disabled. [0003] Among the antithrombotic drugs, heparin drugs have attracted much attention because of their biological components derived from the living body, good therapeutic effect, biocompatibility, and safety. Among the heparin drugs, low molecular weight heparin (LMWH) has anticoagulant, antithrombotic, and blood lipid-regulating effects. Widely used in the field of cardiovascular disease prevention and treatment. LMWH is a l...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K47/42A61K31/727A61P7/02
Inventor 闫学海陈成军李淑坤张宁马光辉
Owner INST OF PROCESS ENG CHINESE ACAD OF SCI
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