Sustained release ocular implant for treating solid tumors

A slow-release implant, tumor technology, applied in the field of medicine, can solve the problems of unfavorable postoperative recurrence, difficult to control the maximum tolerated dose, and short release period of the sustained-release agent.

Inactive Publication Date: 2008-07-30
JINAN SHUAIHUA PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the existing sustained-release preparations have a short release period and obvious burst release phenomenon
Among them, the short drug release cycle is not conducive to the eradication of tumor cells entering the Go phase, so it is not conducive to effective control of postoperative recurrence; the obvious burst release phenomenon is not easy to control the maximum tolerated dose, and the toxicity is more obvious

Method used

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  • Sustained release ocular implant for treating solid tumors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0081] Put the weighed slow-release auxiliary material (molecular weight is 15000-25000 PLGA, 50:50) and slow-release modifier (mannitol) into different containers respectively, then add a certain amount of organic solvent to dissolve and mix well (to fully dissolve prevail) and then add different weights of nimustine, shake again and then vacuum dry to remove the organic solvent. The dried solid sustained-release implant was immediately shaped to obtain the following sustained-release implant:

[0082] (A) 1% Nimustine, containing 1mg Nimustine, 99mg PLGA

[0083] (a) 1% nimustine, containing 1mg nimustine, 95mgPLGA, 4mg mannitol;

[0084] (B) 5% nimustine, containing 5mg nimustine, 95mg PLGA;

[0085] (b) 5% nimustine, containing 5mg nimustine, 91mg PLGA, 4mg mannitol;

[0086] (C) 10% nimustine, containing 10mg nimustine, 90mg PLGA;

[0087] (c) 10% nimustine, containing 10mg nimustine, 80mg PLGA, 10mg mannitol;

[0088] (D) 15% Nimustine, containing 15mg Nimustine, 85...

Embodiment 2

[0093] 10 sustained-release implants in Example 1 were put into the dissolution apparatus respectively to measure the drug cumulative release amount (%) at different times, and it was found that in the sustained-release implants (A), (B), (C ), (D) and (E) five nimustine sustained-release implants that do not contain a sustained-release regulator (mannitol) have obvious burst release phenomena, and the burst release phenomenon mostly occurs on the 15th-20th day, Account for about 60-80% of the total drug content, while (a), (b), (c), (d) and (e) etc. contain sustained-release regulator (mannitol) nimustine sustained-release implants The sudden release phenomenon of the medicine is obviously not obvious, and the medicine is released slowly for 3-4 weeks.

Embodiment 3

[0095]Put the weighed sustained-release auxiliary material (PLGA with a molecular weight of 20000-30000, 75:25) and the sustained-release regulator (mannitol) into different containers respectively, then add a certain amount of organic solvent to dissolve and mix (to fully Dissolution prevails) and then add different weights of nimustine, shake again and then vacuum dry to remove the organic solvent. The dried solid sustained-release implant was immediately shaped to obtain the following sustained-release implant:

[0096] (A) 1% Nimustine, containing 1mg Nimustine, 99mg PLGA

[0097] (a) 1% nimustine, containing 1 mg nimustine, 95 mg PLGA and 4 mg sorbitol;

[0098] (B) 5% nimustine, containing 5mg nimustine, 95mg PLGA;

[0099] (b) 5% nimustine, containing 5 mg nimustine, 91 mg PLGA and 4 mg sorbitol;

[0100] (C) 10% nimustine, containing 10mg nimustine, 90mg PLGA;

[0101] (c) 10% nimustine, containing 10 mg nimustine, 80 mg PLGA and 10% sorbitol;

[0102] (D) 15% Nim...

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Abstract

A sustained release implant for treating solid cancer is characterized in that the sustained release implant comprises nimustine, sustained release excipients and a release regulator with an effective amount for anti-cancer. The sustained release excipients essentially include macromolecule polymer which has a biotic capacitability and can be degraded and absorbed, mainly relating to PLA, and PLGA; the release regulator is selected from one or combination of mannitol, sorbitol, xylitol, oligosaccharide, chitin, potassium salt, sodium salt, hyaluronic acid, collagen, chondroitin, gelatin and albumin. The sustained release implant can slowly release carmustine in partial knub during the process of degrading and absorbing; thereby being able to maintain effective medicine concentration on partial knub simultaneously when remarkably reducing the general toxicity reaction; consequently, the invention can be widely applied for the treatment of the solid knub in various stages by single or cooperated with non operative treatments like chemotherapy medicines and radiotherapy, which can not only selectively enhance medicine concentration on partial knub , but also enhance the curing effects of non operative treatments like medicine chemotherapy and radiotherapy.

Description

(1) Technical field [0001] The invention relates to a slow-release implant for treating solid tumors, belonging to the technical field of medicines. (2) Background technology [0002] Although the research on cancer has made great progress, its mortality rate is still in the forefront of various common causes of death. In my country, about 1.6 million people suffer from cancer every year, and nearly 1.3 million people die of cancer, accounting for one-fifth of the total death toll. The incidence of cancer is increasing year by year and tends to be younger. Statistics show that in less than 20 years, the incidence of cancer in my country has increased by 69%, and the mortality rate has increased by 29.4%. According to the latest statistics from the World Health Organization, the global cancer incidence rate will increase by 50% by 2020, and the number of patients will increase to 15 million. Therefore, exploring an effective method or drug for treating cancer has become a h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/505A61K47/34A61P35/00
Inventor 孙娟马玲君
Owner JINAN SHUAIHUA PHARMA TECH
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