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Slow-release medicament release system as well as preparation method and application thereof

A technology of releasing system and slow-release medicine, applied in the field of medicine releasing system and its preparation, can solve the problem of leaving carrier foreign bodies, etc., and achieve the effects of less toxic and side effects, lower drug concentration, and longer drug effect time

Inactive Publication Date: 2010-05-26
于美丽 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The earliest polymer used was vinyl acetate-ethylene copolymer (ethylene-vinyl acetate EVAc). Although it has been proved to be a good drug carrier in the laboratory, since it is a non-biodegradable polymer, the drug can be dispersed in the body after injection. The way to gradually release the drug, but will leave the carrier foreign matter

Method used

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  • Slow-release medicament release system as well as preparation method and application thereof
  • Slow-release medicament release system as well as preparation method and application thereof
  • Slow-release medicament release system as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Preparation of pirarubicin-p-carboxyphenoxypropane and sebacic acid copolymer slow-release implants by melt casting:

[0031] Fully mix p-carboxyphenoxypropane and sebacic acid copolymer and pirarubicin raw material medicine in an agate mortar and dissolve in dichloromethane, pour it into a film tool and set it in a desiccator at 4°C to form a film. The finally processed p-carboxyphenoxypropane and sebacic acid copolymer-pirarubicin sustained-release implant has a circular size, 6 mm in diameter, 2 mm in thickness, and a mass of (20.0 ± 0.2) mg. The injection contains 5.0 mg of pirarubicin, and the content of pirarubicin is 25%. The slow-release implant is sealed, sterilized by Co-60 irradiation, and the irradiation dose is 20 kGy, and stored at -20°C for future use.

[0032] (The release rate of 1 tablet of pirarubicin in physiological saline in vitro is about 8-10 μg / d. The non-enzymatic hydrolytic release can be maintained for more than 100 days.)

Embodiment 2

[0034] Birubicin-p-carboxyphenoxypropane and sebacic acid copolymer sustained-release microsphere injection preparation prepared by freeze-drying with emulsified solvent evaporation:

[0035] Accurately weigh 1000 mg of medical p-carboxyphenoxypropane and sebacic acid copolymer and 250 mg of pirarubicin powder, and dissolve them in 50 ml of acetone-ethanol solution. ) The birubicin-polyanhydride-acetone-ethanol solution is slowly injected into the polyvinyl alcohol (PVA) aqueous solution with a syringe, emulsified by a stirrer to form an oil-in-water emulsion, and stirred under normal pressure in a fume hood until completely removed Organic solvent, then centrifuged at 20,000r / min for 20min with an ultracentrifuge, precipitated, washed with distilled water and centrifuged 3 times to remove free birubicin and PVA, freeze-dried, and stored at 4°C.

[0036] Collect all supernatants simultaneously in centrifugation and washing process, be used for detecting the content of free pir...

Embodiment 3

[0038] Preparation of paclitaxel-poly-β-hydroxybutyrate sustained-release implants by melt casting:

[0039] The poly-β-hydroxybutyrate and paclitaxel raw materials are fully mixed in an agate mortar and dissolved in methylene chloride, cast in a film tool and placed in a desiccator at 4°C to form a film, and finally processed into paclitaxel-poly β-Hydroxybutyrate slow-release implant, the specification is round, 6mm in diameter, 2mm thick, mass (20.0±0.2)mg, each implant contains 5.0mg of paclitaxel, and the content of paclitaxel is 25%; The implant is sealed, sterilized by Co-60 irradiation at a dose of 20 kGy, and stored at -20°C for future use.

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Abstract

The invention relates to a slow-release medicament release system as well as a preparation method and an application thereof. The slow-release medicament release system is a targeted slow-release preparation of antineoplastic drugs encapsulated by biodegradable high molecular materials, is prepared by the antineoplastic drugs encapsulated by the biodegradable high molecular materials, and has wide application prospects on preparing the antineoplastic drugs. The medicament is directly sent to nidus positions by in-vivo implantation, injection or other mode by the slow-release medicament release system. In the release process of the medicament, polymer substrates gradually degrades, thereby avoiding being removed by a second operation and also avoiding the phenomena of the wave peaks and wave troughs of blood concentration of common prepartions. The local persistent-effect slow-release preparation has long drug efficacy, and can enable cancer cells at different cell cycles to stand a chance to be killed by the chemotherapy medicament, thereby achieving the advantages of high bioavailability of the medicament, small toxic and side effects and favorable tumor inhibition effect.

Description

technical field [0001] The invention relates to a drug release system and its preparation method and application, especially a slow-release drug release system and its preparation method and application. Background technique [0002] Malignant tumors do great harm to human health and life, especially bladder cancer is the most common and recurring malignant tumor, 70%-80% of which are superficial bladder cancers. 50%-70% of superficial bladder tumors tend to recur after surgery, and 30%-40% of the recurrence cases are accompanied by increased malignancy or enhanced infiltration. The remarkable feature of bladder cancer is that most of them are superficial papillomas at the first onset, but the recurrence rate after simple tumor resection is high. Multiple recurrences not only cause pain and economic burden to patients, but also increase the pathological grade every time they recur. Eventually develop into invasive carcinoma. Therefore, preventing tumor recurrence after sur...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/16A61K47/34A61K47/36A61K47/42A61P35/00
Inventor 于美丽杜智
Owner 于美丽
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