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An anticancer sustained release injection carrying tumor drug resistance reversal agent and reversal agent synergist

A slow-release injection, drug resistance reversal technology, applied in the field of medicine, can solve the problems of many complications, poor curative effect, difficult operation and so on

Inactive Publication Date: 2006-12-13
JINAN KANGQUAN PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, solid sustained-release implants (Chinese Patent No. ZL96115937.5; ZL97107076.8) and existing sustained-release microspheres for the treatment of brain tumors (ZL00809160.9) or U.S. Patent (US5,651,986) all have inadequacies. Easy operation, poor curative effect, many complications, etc.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0095] Put 80mg of polyphenylpropane (p-CPP: 20:80 of sebacic acid (SA)) copolymer into a container, add 100ml of dichloromethane, dissolve and mix well, then add 10mg Hydroxycamptothecin and 10 mg nelarabine were re-shaken and spray-dried to prepare injection microspheres containing 10% hydroxycamptothecin and 10% nelarabine. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection with a viscosity of 220cp-460cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 10-15 days, and the drug release time in mice subcutaneous is about 20-30 days.

Embodiment 2

[0097] The method step of being processed into sustained-release injection is the same as in Example 1, but the difference is that the contained anticancer active ingredients and their weight percentages are:

[0098] (a) 2-40% of nelarabine, tipifarnib, ronafarib, valspodar, pemetrexed, raltitrexed or noratrexed;

[0099] (b) 2-40% hydroxycamptothecin, mitozolomide, 4-carboxytemozolomide, docetaxel, oxaliplatin, heptaplatin, ifosfamide, lomustine, estramustine , formustine, samustine, etoposide, teniposide, vinblastine, anastrozole, tamoxifen, fluorouracil, or mitomycin C; or

[0100] (c) 2-40% of nelarabine, tipifarnib, ronafarib, penspodar, pemetrexed, raltitrexed or noratrexed with 2-40% of hydroxycamptothecin Alkali, mitozolomide, 4-carboxytemozolomide, docetaxel, oxaliplatin, heptaplatin, ifosfamide, lomustine, estramustine, formustine, samustine, A combination of etoposide, teniposide, vinblastine, anastrozole, tamoxifen, fluorouracil, or mitomycin C.

Embodiment 3

[0102] Put 70 mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 65,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 15 mg of tipifarnib and 15 mg of lomustine, and re-shake Dry in vacuo to remove the organic solvent. Freezing and pulverizing the dried drug-containing solid composition to make micropowder containing 15% tipifarnib and 15% lomustine, and then suspending in physiological saline containing 1.5% carboxymethylcellulose sodium to obtain the corresponding Suspension-type sustained-release injection with a viscosity of 300cp-400cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 10-15 days, and the drug release time in mice subcutaneous is about 20-30 days.

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Abstract

Disclosed is an anticancer slow release injection carrying tumor drug resistance reversal agents and reversal agent synergistic agent, which comprises slow release micro-balloons and dissolvent, wherein the slow release micro-balloons use slow release auxiliary materials as the carrying agent, the dissolvent being specific dissolvent containing suspension adjuvant. The anticancer active ingredient in the micro-balloons is reversal agent synergistic agent selected from Tipifarnib, Ronafarnib, Valspodar, and / or selected from monohydric camptothecine, Mitozolomide, docetaxel, Oxaliplatin, Eptaplatin, Ifosfamide, Lomustine, Estramustine, Fotemustine, Samostine or Teniposide, the slow release auxiliary materials are selected from Polifeprosan, di-aliphatic acid and sebacylic acid copolymer, poly(erucic aciddipolymer-sebacylic acid), poly(fumaric acid-sebacylic acid) and EVAc.

Description

(1) Technical field [0001] The invention relates to an anticancer slow-release injection containing a tumor drug resistance reversal agent and a reversal agent synergist and a preparation method thereof, belonging to the technical field of medicines. Specifically, the present invention provides a slow-release preparation of anticancer drugs containing a tumor resistance reversal agent and / or a reversal agent synergist, mainly slow-release injections and slow-release implants. (2) Background technology [0002] As the expression product of Ras cancer gene, Ras protein exists in most tumors. Ras protein is a binding protein of guanosine triphosphate (GTP), which regulates cell mitosis. Ras protein plays an important role in cell proliferation and malignant transformation. Farnesyltransferase (FTase) is an essential enzyme closely related to the prenylation modification of Ras protein discovered in recent years. Inhibiting FTase activity and preventing the farnesylation of Ras...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K45/00A61K47/32A61K47/34A61K47/36A61K47/38A61K47/42A61K31/519A61K31/505A61P35/00A61K47/26
Inventor 孙忠厚
Owner JINAN KANGQUAN PHARMA TECH
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