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Visualized iodized oil-5-fluorouracil loaded polylactic acid microsphere preparation and preparation method thereof

A technology of fluorouracil polylactic acid and fluorouracil, which is applied in the field of medicine, can solve the problems of large toxic and side effects, short half-life of 5-fluorouracil, short drug action time, etc., and achieves large drug load, reduced physical damage and economic burden, and stable drug release. Effect

Active Publication Date: 2011-02-16
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although this injection method of mixing the two medicines before use has a good therapeutic effect, because both are liquid, they have strong fluidity and are easily washed away by the blood, resulting in a short drug action time at the lesion site. The half-life of 5-fluorouracil is short, and the effective treatment time usually only lasts for 3 to 4 hours, and after injection, the toxicity and side effects are also relatively large due to the high concentration of chemotherapy drugs in the early stage

Method used

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  • Visualized iodized oil-5-fluorouracil loaded polylactic acid microsphere preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1: adopt 2% polyvinyl alcohol to prepare microsphere preparation of the present invention

[0029] 1. Preparation of oil phase: Dissolve 60 mg of PLA in 2 ml of dichloromethane, add 0.06 ml of iodized oil injection, vortex for 3 minutes and mix evenly, as the oil phase, iodized oil injection is a commercially available drug, produced by GUERBET company in France Production (the same below);

[0030] 2. Prepare the inner water phase: use 1mol / L NaOH aqueous solution to prepare a 5-FU solution with a 50 g / L concentration of 5-FU as the inner water phase, and the purity of the anticancer drug 5-FU is not less than 95%;

[0031] 3. Preparation of colostrum: Take 0.4ml of the inner water phase solution and inject it into the above oil phase, and ultrasonicate with 400W power for 2 minutes under ice bath to form colostrum;

[0032] 4. Prepare the external water phase: use 2% polyvinyl alcohol (PVA) as the continuous phase to prepare a 5-FU saturated aqueous soluti...

Embodiment 2

[0035] Embodiment 2: adopt 2.5% polyvinyl alcohol to prepare microsphere preparation of the present invention

[0036] 1. Prepare the oil phase: Dissolve 60 mg of PLA in 2 ml of acetonitrile, add 0.06 ml of iodized oil injection, vortex for 3 minutes and mix well, as the oil phase;

[0037] 2. Prepare the inner water phase: use 1mol / L NaOH aqueous solution to prepare 5-FU with a 5-FU concentration of 60g / L as the inner water phase;

[0038] 3. Preparation of colostrum: the method is the same as in Example 1;

[0039] 4. Prepare the external water phase: use 2.5% polyvinyl alcohol (PVA) as the continuous phase to prepare a saturated aqueous solution of 5-FU, which is the external water phase;

[0040] 5. Prepare double milk: inject the above-mentioned colostrum into the 80ml external water phase with a syringe at a constant speed of 600r / min, and stir for 10 minutes to obtain double milk;

[0041] 6. Preparation of dry microsphere preparation: Same as Example 1.

Embodiment 3

[0042] Embodiment 3: adopt 3% polyvinyl alcohol to prepare microsphere preparation of the present invention

[0043] 1. Prepare oil phase: with embodiment 1;

[0044] 2. Prepare the inner water phase: use 1mol / L NaOH aqueous solution to prepare 5-FU with a concentration of 5-FU of 70g / L as the inner water phase;

[0045] 3. Preparation of colostrum: with embodiment 1;

[0046] 4. Prepare the external water phase: use 3% polyvinyl alcohol (PVA) as the continuous phase to prepare a 5-FU saturated aqueous solution, which is the external water phase;

[0047] 5. Preparation of double milk: inject the above-mentioned colostrum into the 80ml external water phase with a syringe at a constant speed of 600r / min, and stir for 10 minutes to obtain double milk;

[0048] 6. Preparation of dry microsphere preparation: Same as Example 1.

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Abstract

The invention belongs to the technical field of medicine, and discloses a visualized iodized oil-5-fluorouracil loaded polylactic acid microsphere preparation with a controlled-release effect and a preparation method thereof. The preparation comprises the main components of 5-fluorouracil, iodized oil injecta, polyvinyl alcohol and polylactic acid, and is characterized in that the preparation process is simple, the drug-loading rate is large, the drug release is stable and lasts for a long time, and the in-vitro continuous effective drug release time can be longer than 4 weeks. In the invention, the liquid preparation is prepared into solid microsphere preparation, thus compared with the traditional method, the invention has the advantages that controlled-release drug administration is realized; the toxic and side effect of chemotherapeutic drugs is reduced; the embolism time is prolonged; the microsphere preparation can durably act on focus; the drug therapy effect is enhanced; and the curative effect can be tracked according to the visualized position of the iodized oil in the later stage, thus waste of drugs can be reduced, and the physical damage and economic burden of patients can be lightened.

Description

technical field [0001] The invention relates to the technical field of medicine, and relates to a developable iodized oil-5-fluorouracil polylactic acid microsphere preparation with sustained release and a preparation method thereof. Background technique [0002] Iodized oil is a kind of organic iodine injection, which is viscous. Because it can be developed under X-ray, it is also called positive embolic agent. It is often used as Use of hepatic artery embolization agents. 5-Fluorouracil is a chemotherapy drug injection, which is a commonly used anticancer drug in clinic. It has the characteristics of a broad anticancer spectrum and is the drug of choice for the treatment of solid tumors. [0003] At present, the main usage in clinical interventional therapy is to directly inhale lipiodol and 5-fluorouracil (5-FU) into the same syringe and mix them, then inject the catheter through the femoral artery directly into the site of the lesion, and embolize it around the cancer c...

Claims

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Application Information

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IPC IPC(8): A61P35/00A61K47/34A61L31/16A61L31/06A61K9/16A61L31/18A61K31/513
Inventor 钟延强王新霞张国庆鲁莹
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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