Unlock instant, AI-driven research and patent intelligence for your innovation.

Anticancer sustained release agent containing clorfarabine and its synergist

A technology of sustained-release agent and synergist, applied in the field of sustained-release injection and its preparation, can solve the problems of treatment failure, enhanced tolerance and the like

Inactive Publication Date: 2006-12-13
JINAN KANGQUAN PHARMA TECH
View PDF10 Cites 0 Cited by
  • 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0130] 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 Clorabine and 10 mg camptothecin were re-shaken and spray-dried to prepare microspheres for injection containing 10% clorabine 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

[0132] 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:

[0133] (a) 2-40% clorabine and 2-40% camptothecin, hydroxycamptothecin, letotecan, topotecan, irinotecan, etoposide, teniposide, ammonia a combination of Rubicin, Erubicin, Rhodopyrin, Lyrubicin or Zorubicin; or

[0134] (b) 2-40% clorabine in combination with 2-40% procarbazine, mitozolomide, 4-carboxytemozolomide or temozolomide.

[0135] The excipients used are: racemic polylactic acid, racemic polylactic acid / glycolic acid copolymer, monomethyl polyethylene glycol / polylactic acid, monomethyl polyethylene glycol / polylactic acid copolymer, polyethylene glycol / polylactic acid, polyethylene glycol / polylactic acid copolymer, carboxyl-terminated polylactic acid or carboxyl-terminated polylactic acid / glycolic acid copolymer; the viscosity of the sustained-release injecti...

Embodiment 3

[0137] 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 clorabine and 15 mg of hydroxycamptothecin, re-shake and vacuum Dry to remove organic solvent. The dried drug-containing solid composition was frozen and pulverized to make micropowder containing 15% clorabine and 15% hydroxycamptothecin, and then suspended in physiological saline containing 1.5% sodium carboxymethylcellulose to obtain the corresponding Suspension-type sustained-release injection. 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.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
glass transition temperatureaaaaaaaaaa
melting pointaaaaaaaaaa
Login to View More

Abstract

Disclosed is a slow release agent containing clofarabine and synergistic agent, which comprises slow release microspheres and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents and slow release auxiliary materials, the dissolvent being specific dissolvent containing suspension adjuvant. The anticancer active constituents include clofarabine and combination with clofarabine synergistic agent selected topology enzyme inhibitor and / or tetrazine compounds, the slow release auxiliary materials are selected from Polifeprosan, sebacylic acid copolymer, EVAc, polylactic acid and copolymer, polyethylene glycol mono methyl and copolymer, polyethylene glycol and polylactic acid copolymer, PLA-COOH or PLA-COOH / glycollic acid copolymer or their combination. The viscosity of the suspension adjuvant is 100-3000cp and is selected from sodium carboxymethylcellulose.

Description

(1) Technical field [0001] The invention relates to a slow-release injection containing clorabine and / or its synergist and a preparation method thereof, belonging to the technical field of medicines. (2) Background technology [0002] Clofarabine, as a new class of chemotherapy drugs, has been widely used in the treatment of childhood acute myeloid leukemia (ALL), relapsed or resistant acute myeloid leukemia (AML), adult leukemia and solid tumors and other malignancies. Tumors, and the effect is more obvious. However, its obvious systemic toxicity greatly limits the application of this drug. [0003] In addition, 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 effect of chemotherapy drugs on the periphery of the tumor and in the tumor tissue. Penetration and diffusion (see Netti et al. "The influence of the condition of the extra...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K45/00A61K31/7076A61K47/34A61P35/00
Inventor 孔庆新
Owner JINAN KANGQUAN PHARMA TECH