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Controlled release formulation for anti entity tumour

A kind of technology of sustained-release preparation and sustained-release injection

Inactive Publication Date: 2007-05-09
JINAN KANGQUAN PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above factors greatly limit the effective diffusion of drugs into solid tumors and tumors, thus constituting the main obstacle to tumor chemotherapy.
[0007] Not only that, the blood vessels in the tumor stroma are not sensitive to conventional chemotherapy drugs, which often leads to the enhancement of tumor cell resistance to anticancer drugs, and the result is treatment failure

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0142] Put 80 mg of polylactic acid (PLGA, 50:50) with a peak molecular weight of 25,000-40,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 10 mg of collagenase and 10 mg of methotrexate, and re-shake Dry in vacuo to remove the organic solvent. The dried solid composition is shaped immediately, subpackaged and then sterilized by radiation to obtain the anti-cancer sustained release containing 10% collagenase and 10% methotrexate. All are percentages by weight. The drug release time of the anti-solid tumor pharmaceutical composition in physiological saline in vitro is 15-25 days, and the drug release time in mouse subcutaneous is 25-50 days.

Embodiment 2

[0144] As described in Example 1, the difference is that the peak molecular weight of polylactic acid is 35000-60000 (PLGA, 75:25), and the anticancer active ingredient and weight percentage are one of the following:

[0145] (1) 5% hyaluronidase and 10% epothilone, epothilone B, doxorubicin, epirubicin, mitomycin C, actinomycin D or dactinomycin combination; or

[0146] (2) 10% relaxin and 10% fluorouracil, 6-mercaptopurine, methotrexate, flumethorexate, calcium leucovorin, calcium folinate, carmofur, tegafur, and Youfudine , topotecan, a combination of topotecan hydrochloride, cytarabine, cyclocytidine, or hydroxyurea.

Embodiment 3

[0148] Put 80mg of polyphenylpropane (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) at 20:80) copolymer into a container, add 100ml of dichloromethane, dissolve and mix well, then add 10mg of pancreatic Protease and 10 mg fluorouracil were re-shaken and spray-dried to prepare microspheres for injection containing 10% trypsin and 10% fluorouracil. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection with a viscosity of 20cp-300cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 15-25 days, and the drug release time in mice subcutaneous is about 30-40 days.

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Abstract

A slow-release anticancer medicine in the form of injection or implant is disclosed. Said slow-release injection is composed of a special solvent containing suspending aid and the slow-release microballs consisting anticance medicine, iterstitial hydrolyte and slow-releasing auxiliary. Said anticancer medicine is chosen from antineoplastic antibiotic and antimetabolic medicine. Said interstitial hydrolyte is chosen from collagenase, relaxin, etc. Said slow-releasing auxiliary is chosen from polylactic acid copolymer, EVAc, polyethanediol, etc.

Description

(1) Technical field [0001] The invention relates to an anti-solid tumor slow-release agent, which belongs to the technical field of medicines. Specifically, the invention provides a sustained-release injection and a sustained-release implant containing an interstitial hydrolyzing agent. The anti-cancer slow-release agent can effectively inhibit or destroy the solid tumor stroma and tumor blood vessels, and can inhibit tumor angiogenesis, effectively reduce the tension in the tumor, interstitial pressure, and interstitial viscosity, thereby improving its interstitial fluid conduction. The rate is conducive to the effective diffusion of drugs into solid tumors and tumors. (2) Background technology [0002] Cancer treatment mainly includes surgery, radiotherapy and chemotherapy. Among them, surgical treatment cannot remove scattered tumor cells, so it often recurs or causes tumor cells to spread and metastasize due to surgical stimulation; radiotherapy and traditional chemoth...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K45/06A61K38/46A61K47/34A61P35/00A61K47/10A61K47/32
Inventor 刘玉燕邹会凤张红军张婕
Owner JINAN KANGQUAN PHARMA TECH