Implant capable of releasing doxorubicin continuously for long term, and preparation method thereof

A technology of doxorubicin and implants, which can be applied to non-active ingredients medical preparations, medical preparations containing active ingredients, and pharmaceutical formulas, etc., can solve the problems of low release degree, reduced systemic toxicity, and high tumor concentration.

Active Publication Date: 2017-05-24
ANHUI ZHONGREN TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Some of these implants release rapidly, some have severe burst release, some release too slowly, some have low release degree, and some have secondary release. Continued long-term administration to kill tumor cells, the curative effect is limited
[0012] In order to overcome the deficiencies of the prior art, the present invention provides an implant for sustained long-term release of doxorubicin and a preparation method thereof, which solves the problem that the existing doxorubicin PLGA implant cannot last for a long time, uniformly or relatively uniformly, completely Or compare the problem of complete release of doxorubicin, and provide safe and high-quality doxorubicin implants for the clinic. After the implant is implanted in the tumor area, it will release doxorubicin for a long time until it is completely released. The concentration of the tumor site is high and the action time is long. Long-term, significant curative effect; at the same time, the blood concentration is extremely low, and the systemic toxicity is greatly reduced; once administered, it is effective for dozens of days, especially suitable for the treatment of solid tumors

Method used

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  • Implant capable of releasing doxorubicin continuously for long term, and preparation method thereof
  • Implant capable of releasing doxorubicin continuously for long term, and preparation method thereof
  • Implant capable of releasing doxorubicin continuously for long term, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0133] Example 1 Doxorubicin implant A, B, C

[0134] (1) For prescription, see Table 1.

[0135] Table 1 Doxorubicin implant A, B, C components and weight ratio

[0136]

[0137] (2) Preparation

[0138] ① Pulverize the materials in Table 1 respectively and pass through a 120-mesh drug sieve to obtain adriamycin hydrochloride fine powder and PLGA fine powder;

[0139] ② Mix the fine powder of ① according to the ratio in the above table 1, and make implant A, B, C mixed powder respectively;

[0140] ③ Dry the mixed powder of ② in a vacuum drying oven at a temperature of 22°C and a pressure of 9KPa, so that the content of water and volatile components in the mixed powder is less than 0.1%, and the mixed powder of dry implants A, B, and C is obtained;

[0141] ④ Place each dry mixed powder of ③ in a stainless steel container and melt at 110°C for 9 minutes, pour it into a mold (diameter of the mold hole is 0.9mm, length 4mm) for molding, cooling, demoulding, and sterili...

Embodiment 2

[0142] Example 2 Doxorubicin implants D, E, F, G

[0143] (1) For prescription, see Table 2.

[0144] Table 2 Doxorubicin implant D, E, F, G components and weight ratio

[0145]

[0146] (2) preparation

[0147] ① Pulverize the materials in Table 2 respectively and pass through a 120-mesh drug sieve to obtain adriamycin hydrochloride fine powder and PLGA fine powder;

[0148] ② Mix the fine powder of ① according to the ratio in the above table 2, and make implant D, E, F, G mixed powder respectively;

[0149] ③Dry the mixed powder of ② in a vacuum drying oven at a temperature of 26°C and a pressure of 11KPa, so that the content of water and volatile components in the mixed powder is less than 0.1%, and the mixed powders of dry implants D, E, F, and G are prepared ;

[0150] ④ Place the mixed powder of each dry implant in ③ into a stainless steel container and melt at 130°C for 9 minutes, inject it into a mold (diameter of the mold hole is 0.9mm, length 4mm) for moldi...

Embodiment 3

[0151] Example 3 In vitro release test

[0152] (1) Determine the content of doxorubicin implants A, B, C, D, E, F, and G by spectrophotometry;

[0153] (2) Take 3 doxorubicin implants A, weigh them accurately, put each into a 10mL clean test tube with stopper, add 5mL purified water (pH=7.0) to each test tube, and make the implant The particles are immersed in water and kept in a water bath at (37±0.5)°C to keep warm, which is the in vitro release device for doxorubicin implant A.

[0154] (3) Make the in vitro release devices of doxorubicin implants B, C, D, E, F, and G in the same way.

[0155] (4) Take out all the liquid in each test tube every day, add the same volume of fresh purified water at the same time, and put it in a water bath at (37±0.5 )°C to keep warm;

[0156] (5) Use spectrophotometry to detect the amount of doxorubicin hydrochloride in the liquid taken out every day, and calculate the release rate according to the input amount and release amount. The ...

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Abstract

The invention relates to an implant capable of releasing doxorubicin continuously for a long term, and a preparation method thereof. The implant is composed of doxorubicin hydrochloride, a glycolide-lactide copolymer, and polyethylene glycol. According to the preparation method, melting method is adopted to prepare the cylindrical implant with a diameter ranging from 0.3 to 1.6mm and a length ranging from 0.8 to 5mm; in in-vivo test, 5 to 21% of the coated drug is released in one day, 25 to 51% of the coated drug is released in 5 days, 35 to 63% of the coated drug is released in 10 days, and 80 to 100% of the coated drug is released in 30 days. The surface of the implant is smooth; the implant can be implanted in tumor, or tumor surrounding tissue, or administration places using a drug implanting needle via percutaneous puncture; the implant is suitable for treatment of solid tumor; the preparation process is simple; quality control is convenient to realize; cost is low; no pollution is caused; and the preparation method is convenient for industrialization.

Description

technical field [0001] The invention relates to a doxorubicin sustained-release implant and a preparation method thereof, in particular to the composition, shape, size, strength, drug release performance and preparation method of the doxorubicin sustained-release implant, belonging to the technical field of medicines . Background technique [0002] Doxorubicin is a broad-spectrum anti-tumor drug with strong anti-cancer pharmacological activity. It can directly act on DNA, insert DNA double helix strands, untie the latter, change the template properties of DNA, and inhibit DNA polymerase. Inhibits DNA synthesis and also inhibits RNA synthesis. In addition, doxorubicin has the function of forming superoxide radicals, and has a special effect of destroying the membrane structure and function of cells. As a cycle non-specific anticancer chemotherapy drug, it has effects on cells in all phases and is suitable for Acute leukemia, malignant lymphoma, breast cancer, bronchial lung...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/704A61K47/34A61P35/00
Inventor 王世亮杜坤田艳芝韦芳芳周春霞
Owner ANHUI ZHONGREN TECH
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