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Slow released injection containing blood vessel inhibitor and its synergist

A technology of vascular inhibitors and sustained-release injections, which is applied in the field of sustained-release injections and its preparation, and can solve problems such as increased tolerance and treatment failure

Inactive Publication Date: 2006-11-08
JINAN SHUAIHUA PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The latter often leads to increased resistance of tumor cells to anticancer drugs, with consequent treatment failure

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0117] 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 Gefitinib and 10 mg camptothecin were re-shaken and spray-dried to prepare microspheres for injection containing 10% gefitinib and 10% camptothecin. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection. The viscosity of the injection is 200cp-650cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 20-30 days, and the drug release time in mice subcutaneous is about 30-40 days.

Embodiment 2

[0119] 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:

[0120] (a) 2-40% camptothecin, hydroxycamptothecin, 9-nitrocamptothecin, podophyllotoxin, trihydroxyisoflavones, letotecan, topotecan, irinotecan Poside, teniposide, 14-hydroxydaunorubicin, amrubicin, erubicin, detorubicin, esorubicin, rhodorubicin, rhrubicin, or zorubicin ;

[0121] (b) 2-40% of gefitinib, erlotinib, lapatinib, vatalanib, peritinib, carboxyaminotriazole, thalidomide, ranolamid, angiostatin, endostatin , endostatin, imatinib mesylate, semazinil, dasatinib, Avastin, canertinib, sorafenib, sunitinib, Teosta, or penito horse; or

[0122] (c) 2-40% of gefitinib, erlotinib, lapatinib, vatalanib, peritinib, carboxyaminotriazole, thalidomide, ranolamid, angiostatin, endostatin , endostatin, imatinib mesylate, semazinil, dasatinib, Avastin, canertinib, sora...

Embodiment 3

[0124] Put 70 mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 25,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 15 mg of erlotinib and 15 mg of hydroxycamptothecin, and re-shake Dry in vacuo to remove the organic solvent. The dried drug-containing solid composition was frozen and pulverized to make micropowder containing 15% erlotinib and 15% hydroxycamptothecin, and then suspended in physiological saline containing 1.5% sodium carboxymethylcellulose to obtain the corresponding Suspension-type sustained-release injections. The viscosity of the injection is 300cp-650cp (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 30-35 days.

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Abstract

The slow released injection containing blood vessel inhibitor and its synergist consists of slow released microsphere and solvent. The slow released microsphere includes effective anticancer component and slow releasing supplementary material, and the solvent is special solvent containing suspending agent. The effective anticancer component is blood vessel inhibitor carboxyl amino triazole, Irotinat, Lapatinat, etc and / or blood vessel inhibitor synergist selected from toporase inhibitor and tetrazin compound. The slow releasing supplementary material is one of difatty acid-sebacic acid copolymer, poly(erucic acid dipolymer-sebacic acid), poly(fumaric acid-sebacic acid), polylactic acid, etc or their composition. The suspending agent is carboxymethyl cellulose, etc. and has viscosity of 100-3000 cp at 20-30 deg.c. The slow released microsphere may be also prepared into slow released implanting agent for improving the treating effect of chemotherapeutic and / or radiotherapeutic medicine.

Description

(1) Technical field [0001] The invention relates to a slow-release injection containing a blood vessel inhibitor and / or its synergist and a preparation method thereof, belonging to the technical field of medicines. (2) Background technology [0002] As a commonly used chemotherapeutic drug, vascular inhibitors have been widely used in the treatment of various malignant tumors, and the effect is more obvious. However, its unexpected neurotoxicity greatly limits the application of this drug. Blood vessels, connective tissue, matrix proteins, fibrin, and collagen in the tumor stroma not only provide scaffolds and essential nutrients for the growth of tumor cells, but also affect the penetration of chemotherapy drugs around the tumor and in the tumor tissue and diffusion (see Netti et al. "The influence of the status of the extracellular matrix on the delivery of drugs in solid tumors" "Cancer Research" 60 pp. 2497-503 (2000) (Netti PA, Cancer Res.2000, 60 (9) : 2497-503)). D...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/505A61K45/00A61K47/26A61K47/32A61K47/34A61K47/36A61K47/38A61K47/42A61P35/00
Inventor 孔庆霞
Owner JINAN SHUAIHUA PHARMA TECH
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