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Anticancer composition containing Sirolimus and its application

A technology of rapamycin and composition, which is applied in the field of rapamycin-containing compositions, can solve the problems of anticancer drug resistance enhancement and treatment failure, and achieve the improvement of interstitial fluid conductivity, promotion of penetration and Diffusion and tension-reducing effects

Inactive Publication Date: 2007-06-06
SHANDONG LANJIN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Not only that, the blood vessels in the tumor stroma are not sensitive to conventional chemotherapy drugs, especially single-drug chemotherapy, which often leads to enhanced resistance of tumor cells to anticancer drugs, resulting in treatment failure

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0123] Put 80 parts of polylactic acid (PLGA, 50:50) with a peak molecular weight of 10000-25000 into a container, add an appropriate amount of dichloromethane to dissolve and mix well, add 10 parts of rapamycin and 10 parts of gemcitabine, and re-shake Dry in vacuo to remove the organic solvent. The dried solid composition is formed immediately, subpackaged and then sterilized by radiation to obtain the anti-cancer sustained release containing 10% rapamycin and 10% gemcitabine. All are percentages by weight. The drug release time of the anti-solid tumor pharmaceutical composition in physiological saline in vitro is 18-24 days, and the drug release time in mouse subcutaneous is 21-25 days.

Embodiment 2

[0125] As described in Example 1, the difference is that the auxiliary material is polylactic acid (PLGA, 75:25) with a peak molecular weight of 25000-45000, and the anticancer active ingredients and weight percentages are: 0.005%-20% rapamycin and 2%-40% pemetrexed, pemetrexed disodium, lumitrexed, carmofur, tegafur, temozolomide, zalcitabine, emtricitabine, galocitabine, ibata Bine, Ancitabine, Decitabine, Flucitabine, Enoxitabine, Mizotabine, Capecitabine, Gemcitabine, Fazarabine, Fludarabine, Cladribine, Pentoside, Ray A combination of tetrozine, raltitrexed, dexrazoxane, cladribine, acivexin, triptorelin, edoxifene, or noratrexed.

Embodiment 3

[0127] Put 70 parts of polyphenylene propane (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) at 20:80) copolymer into a container, add an appropriate amount of dichloromethane to dissolve and mix well, then add 10 parts Rapamycin and 20 parts of doxorubicin were re-shaken and spray-dried to prepare microspheres for injection containing 10% rapamycin and 20% doxorubicin. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection with a viscosity of 200cp-300cp (at 20°C-30°C). The drug release time of the sustained release injection in the physiological saline in vitro is 20-25 days, and the drug release time in the mouse subcutaneous is about 20-30 days.

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PUM

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Abstract

The anticancer composition containing sirolimus is one kind of slow releasing injection comprising slow released microsphere and solvent. The slow released microsphere includes effective anticancer component and slow releasing supplementary material. The solvent is special solvent containing suspending agent. The effective anticancer component is composition of sirolimus, antitumor antiseptic and / or antimetabolite. The slow releasing supplementary material is selected from polylactic acid, lactic acid copolymer, polifeprosan, etc; the suspending agent has viscosity of 100cp-3000cp. The slow released microsphere may be also prepared into slow releasing implant. The slow releasing injection and the slow releasing implant may release medicine locally for about 40 days, and can inhibit tumor growth effectively, destroy tumor blood vessel and increase the sensitivity of tumor on anticancer medicine.

Description

(1) Technical field [0001] The invention relates to a composition containing rapamycin and belongs to the technical field of medicines. Specifically, the invention provides a sustained-release injection and a sustained-release implant containing rapamycin. (2) Background technology [0002] Traditional chemotherapy is not selective, and it is difficult to form an effective drug concentration or therapeutic dose locally in the tumor. The effect is poor and the toxicity is high. Simply increasing the drug or radiation dose is limited by systemic toxicity. See Kong et al. "Intratumoral placement of cisplatin plus systemic carmustine to treat brain tumors in rats" "Journal of Surgical Oncology" 69 pages 76-82, 1998 (Kong Q et al., J SurgOncol.1998 Oct; 69( 2): 76-82). [0003] Low-dose anticancer drug treatment can not only increase the drug resistance of cancer cells, but also promote their invasive growth", see Liang et al. "Anticancer drug pulse screening increases the drug...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/436A61K45/06A61K47/34A61P35/00
Inventor 孔庆忠贺润平
Owner SHANDONG LANJIN PHARMA