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Slow release injection containing mtrosourea medicament and topoisomerase inhibitor

A technology of sustained-release injection and nitrosourea, which is applied in the field of medicine and can solve problems such as treatment failure and enhanced tolerance

Inactive Publication Date: 2007-08-08
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

[0113] Put 80, 80 and 80 mg of p(BHET-EOP / TC) (BHET-EOP: TC is 80: 20) copolymers into three containers of A, B and C respectively, and then add 100 ml of dichloromethane to each , after dissolving and mixing, add 20mg carmustine, 20mg camptothecin, 10mg carmustine and 10mg camptothecin respectively, shake up again and prepare 20% carmustine, 20% camptothecin with spray drying method Injection microspheres of thecine, and 10% carmustine and 10% camptothecin. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection. The release time of the sustained-release injection in physiological saline in vitro is 60-70 days, and the release time in mouse subcutaneous is more than 65 days.

Embodiment 2

[0115] The method step of being processed into sustained-release injection is the same as that of Example 1, but the difference is that the adjuvant used is p(BHET-EOP / TC) of 50:50, containing anticancer active ingredients and their weight percentages: 5-40% Combination of carmustine or nimustine with 1-20% camptothecin or hydroxycamptothecin.

Embodiment 3

[0117] Put 70 mg of p(LAEG-EOP) with a peak molecular weight of 10,000-25,000 into three containers of A, B, and C, respectively, and then add 100 ml of dichloromethane to each, dissolve and mix well, and pour into the three containers respectively Add 30mg carmustine, 30mg camptothecin, 25mg carmustine and 5mg camptothecin, re-shake and prepare 30% carmustine, 30% camptothecin, 25% carmustine by spray drying method Injectable microspheres of statin and 5% camptothecin. The dried microspheres are suspended in physiological saline containing 1.5% sodium carboxymethylcellulose to prepare the corresponding suspension-type sustained-release injection. The drug release time of the sustained release injection in physiological saline in vitro is 65-70 days, and the drug release time in mice subcutaneous is about 70 days.

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PUM

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Abstract

Disclosed is a slow release injection containing nitrosourea drugs and / or topoisomerase depressant, which comprises slow release microspheres and dissolvent, the slow release microspheres include nitrosourea drugs selected from Nimustine, Carmustine, and / or topoisomerase depressant anticancer active constituents and slow release auxiliary materials, the dissolvent being conventional dissolvent or specific dissolvent containing suspension adjuvant. The viscosity of the suspension adjuvant is 100-3000cp (at 20-30 deg C), and is selected from sodium carboxymethylcellulose, the slow release auxiliary materials are selected from polyphosphate ester copolymers such as p(LAEG-EOP), p(DAPG-EOP), copolymer or blend of polyphosphate ester with PLA, Polifeprosan, PLGA and poly(dodecanedioic acid-tetradecanedioic acid), the topoisomerase depressant is selected from camptothecine, monohydric camptothecine, Topotecan, Lartotecan, Irinotecan, Etoposide or Teniposide, the anticancer composition can also be prepared into slow release implanting agent for injection or placement in or around tumor with a period of effective concentration maintenance over 60 days, as well as the treatment effect of appreciably lowering general reaction of the drugs, and improving the treatment effect of the non-operative treatment methods such as chemotherapy.

Description

(1) Technical field [0001] The invention relates to a slow-release injection containing nitrosourea drugs and topoase inhibitors and a preparation method thereof, belonging to the technical field of medicines. (2) Background technology [0002] As a class of commonly used chemotherapeutic drugs, nitrosourea drugs have been widely used in the treatment of various malignant tumors, and the effect is relatively obvious. However, its significant toxicity greatly limits the wide application of this class of drugs. [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 camptothecin plus systemic camptothecin in the treatment of brain tumors in rats" "Journ...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K45/06A61K47/34A61P35/00
Inventor 孙宪君
Owner JINAN SHUAIHUA PHARMA TECH
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