Anticancer sustained release injection containing tumor drug resistance reversal agent and cytotoxic drug

A slow-release injection and drug resistance reversal technology, applied in the field of medicine, can solve problems such as complicated operation, accelerated tumor spread and metastasis, cost impact on effective implementation, etc.

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

[0003] Due to the excessive expansion and hyperplasia of solid tumors, the interstitial pressure, tissue elastic pressure, fluid pressure and interstitial viscosity are all higher than those of the surrounding normal tissues. Therefore, it is difficult for conventional chemotherapy to form an effective drug concentration in the tumor. See Kong Qingzhong "Intratumoral placement of cisplatin plus systemic carmustine in the treatment of rat brain tumors" "Journal of Surgical Oncology" 69 pages 76-82 (1998) (KongQ et al., J Surg Oncol.1998 Oct; 69 (2 ):76-82), simply increasing the dosage is limited by systemic reactions
Local application of drugs may solve the problem of drug concentration to some extent. However, surgical operations such as drug implantation are more complicated and traumatic. In addition to easily leading to various complications such as bleeding, infection, and decreased immunity, it may also cause or Accelerate tumor spread and metastasis
In addition, the preparation and expensive costs before and after the operation often affect its effective implementation.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0097] 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 Paclitaxel and 10 mg of pemetrexed were re-shaken to prepare microspheres for injection containing 10% paclitaxel and 10% pemetrexed by a spray-drying method. 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

[0099] 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:

[0100] (1) 2-40% camptothecin, procarbazine, paclitaxel, cisplatin, carboplatin, tumor canning, cyclophosphamide, carmustine, nimustine, irinotecan, vincristine Alkaline, leuprolide, colchicine, aminotriazole, butylthionine, O6-benzylguanine, or O4-benzylfolate;

[0101] (2) 2-40% of nelarabine, tipifarnib, ronafarib, valspodar, noratrexed, pemetrexed, or raltitrexed; or

[0102] (3) 2-40% camptothecin, procarbazine, paclitaxel, cisplatin, carboplatin, tumor canning, cyclophosphamide, carmustine, nimustine, irinotecan, vincristine Alkaline, leuprolide, colchicine, aminotriazole, butylthionine thioxime, O6-benzylguanine, O4-benzyl folic acid and 2-40% nelarabine, tipifarnib, Luo A combination of nafarnib, penspodar, noratrexed, pemetrexed, or raltitrexed.

Embodiment 3

[0104] 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 raltitrexed and 15 mg of nimustine, 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% raltitrexed and 15% nimustine, and then suspending in physiological saline containing 1.5% carboxymethylcellulose sodium to prepare 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 containing tumor drug resistance reversal agents and cytotoxic drugs, which comprises slow release micro-balloons 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 nelarabine, Tipifarnib, Ronafarnib, Valspodar, and / or selected from cytotoxic drugs including Cyclophosphamide, Carmustine, Nimustine, camptothecine, Paclitaxel, cisplatin, Carboplatin, Vincristine, O6-benzylguanine, or O6-benzylfolacin. The slow release auxiliary materials are selected from Polifeprosan, di-aliphatic acid and sebacylic acid copolymer, polylactic acid copolymer and EVAc. The viscosity of the suspension adjuvant is 100-3000cp (at 25-30 deg C) and can be sodium carboxymethylcellulose.

Description

(1) Technical field [0001] The invention relates to an anticancer sustained-release injection containing a tumor drug resistance reversal agent and a cytotoxic drug 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 cytotoxic drug, mainly slow-release injections and slow-release implants. (2) Background technology [0002] As one of the routine cancer treatment methods, drug chemotherapy has been widely used in the treatment of various malignant tumors, and the effect is more obvious. However, its obvious systemic toxicity and the development of drug resistance greatly limit the application of this drug. Among them, the resistance of tumor cells to chemotherapy drugs is an important reason for the failure of clinical chemotherapy. Therefore, finding resistance reversal agents (RRAs) is one of the impor...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K45/00A61K47/32A61K47/34A61K47/36A61K47/38A61K47/42A61K31/517A61K31/505A61P35/00A61K47/26
Inventor 高化兰
Owner JINAN KANGQUAN PHARMA TECH
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