Water soluble anti-cancer medicine slow-release fiber preparation and preparing method therefor

A water-soluble, fiber-based technology, applied in drug combination, drug delivery, anti-tumor drugs, etc., can solve the problems of limiting drug loading performance, and achieve stable release, good body structure compatibility, and strong adaptability to implantation structures Effect

Inactive Publication Date: 2006-10-25
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the preparation method, because the drug must first be dissolved in water and needs to be prepared into an emulsion for spinning, the solubility of the drug in water compared with the water forming the emulsion greatly limits the drug-loading performance of this fiber preparation. The drug loading of fiber preparations prepared by this method is generally 2.3% (Evaluation of in Vitro Drug Release, pH Change, and Molecular Weight Degradation of Poly(L-lactic acid) and Poly(D, L-lactide-co-glycolide) Fibers [J]. Tissue Engineering. 2005; Volume 11, Number 7 / 8: 1077-1084.)

Method used

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  • Water soluble anti-cancer medicine slow-release fiber preparation and preparing method therefor
  • Water soluble anti-cancer medicine slow-release fiber preparation and preparing method therefor
  • Water soluble anti-cancer medicine slow-release fiber preparation and preparing method therefor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Add 0.32g of fluorouracil powder into 5ml of chloroform, and ultrasonically suspend; then add 0.75g of PLLA (L-lactic acid, viscosity-average molecular weight: 100,000), dissolve and stir evenly; then pass the mixed solution at a speed of 0.05ml / min through A 16-gauge flat-tipped needle is injected into the isopropanol curing agent, and the curing distance is 20cm. The solvent of the mixed solution diffuses in the curing agent, and the polymer and the drug are precipitated to form drug-loaded fibers; finally, the fibers are collected at the bottom of the curing agent container and removed by vacuum drying. Organic solvents, ie, see figure 1 . The resulting fiber diameter is 79.4 μm, the drug loading yield is 92.2%, and the drug can be released for 9 weeks, see figure 2 In vitro drug release profile, the release medium is NaN containing 0.1mg / ml 3 Phosphate buffer solution of pH 7.4, the release temperature is 37°C.

Embodiment 2

[0030] Add 0.125g of cisplatin powder into 5ml of chloroform, and ultrasonically suspend; then add 0.35g of PLLA (viscosity average molecular weight: 200,000), dissolve and stir evenly; then pass the mixed solution through a No. 16 flat head at a speed of 0.05ml / min Needle, injected into the isopropanol curing agent, the curing distance is 20cm, the solvent of the mixed solution diffuses in the curing agent, the polymer and the drug are precipitated to form drug-loaded fibers; finally, the fibers are collected at the bottom of the curing agent container, and the organic solvent is removed by vacuum drying. see image 3 . The resulting fiber diameter is 65.2 μm, the drug loading yield is 75.3%, and the drug can be released for 4 weeks, see Figure 4 In vitro release profile, the release medium is NaN containing 0.1mg / ml 3 Phosphate buffer solution of pH 7.4, the release temperature is 37°C.

Embodiment 3

[0032] Add 0.22g of nitrogen mustard powder into 5ml of dichloromethane, and ultrasonically suspend; then add 0.75g of PLA (polylactic acid, containing 3% D-type, with a viscosity average molecular weight of 50,000), dissolve and stir evenly; then mix the solution with At a speed of 0.07ml / min, through a No. 16 flat-tipped needle, inject into the petroleum ether curing agent, the curing distance is 20cm, the solvent of the mixed solution diffuses in the curing agent, and the polymer and the drug are precipitated to form drug-loaded fibers; The fibers are collected at the bottom, dried in vacuum to remove the organic solvent, and obtained. The diameter of the obtained fiber is 53.4 μm, the drug loading yield is 89.3%, and the drug can be released slowly for 20 days.

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Abstract

The present invention relates to the field of medicine preparation, in the concrete, it relates to a show-released fibre preparation of water-soluble anti-cancer medicine for body implantation and its preparation method. It is characterized by that the fibre carrier is oil-soluble biological degradable material. and the medicine is water-soluble anticancer medicine, its medicine content is up to 15-50%.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a slow-release fiber preparation of water-soluble anticancer drugs that can be implanted in a body and a preparation method thereof. Background technique [0002] Local chemotherapy, that is, the treatment method of directly delivering chemotherapy drugs to tumor tissue, has been considered as a good tumor treatment method with great development potential. Through local chemotherapy, anti-tumor drugs can be enriched and killed cancer cells at a high concentration in local tissues (ie, target tissues), while reducing the systemic side effects of administration. Theoretically, administering drugs directly to tumor tissue can kill cancer cells to the greatest extent and achieve a good curative effect; but in practice, this method will cause a large amount of local normal tissue necrosis on the one hand, and on the other hand, the action time is short and very short. Diffi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/10A61K31/704A61K45/00A61K47/34A61P35/00
Inventor 顾月清高昊平其能李清增顾鹏飞
Owner CHINA PHARM UNIV
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