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In vivo slow-releasing anticancer medicinal composition

An anti-cancer drug and composition technology, which is applied in the directions of active ingredients of heterocyclic compounds, pharmaceutical formulations, and medical preparations containing active ingredients, etc., can solve the problem of difficulty in forming effective drug concentrations, and achieve the effect of strengthening the anti-cancer effect.

Inactive Publication Date: 2005-10-05
SHANDONG LANJIN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, further studies have found that the excessive expansion and hyperplasia of solid tumors has higher interstitial pressure, tissue elastic pressure, fluid pressure and interstitial viscosity than the surrounding normal tissue. Drug concentration (see Kong Q et al., "Intratumoral placement of cisplatin plus systemic carmustine in the treatment of rat brain tumors" "Journal of Surgical Oncology" 69 pages 76-82 (1998) (Kong Q et al., J Surg Oncol. 1998 Oct;69(2):76-82), simply increasing the dosage is limited by systemic reactions

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Put 90 mg of PLGA (copolymer of glycolic acid and glycolic acid, weight ratio 50:50) with a molecular weight of 10,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 10 mg of vinorelbine, and shake well again Dry in vacuo to remove the organic solvent. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain an anticancer drug composition containing 10% by weight of vinorelbine.

Embodiment 2

[0045] The method step of being processed into anticancer drug composition is identical with embodiment 1, and difference is that contained active ingredient is:

[0046] (a) 1-50% isovinblastine, vinblastine, vinblastine, vinblastine, podiazine, anhydrovinblastine tartrate, epoxy vinblastine tartrate, epoxy vinblastine, vinblastine tartrate, Torresine, Torrellactone or Vinpocetine; or

[0047] (b) 1-50% of tartaric acid, vinorelbine, vinorelbine ditartrate, vinorelbine tartrate, vincristate, vinosin, vinpocetone, vinblastin, vinblastin sulfate, vinblastin, Vinblastine, vinblastine, vinflunine, or vinpredine; or

[0048] (c) 1-50% vindesine, vinblastine, vinblastol, vinblastine, oxymatrine, harringtonine, deoxyharringtonine, homoharringtonine, hepatin or

[0049] (d) 1-50% Rubescensine A, Zhangzhou narcisine, pronarcisine hydrochloride, procarbazine, procarbazine hydrochloride, tangelonine, tangelonine, isosalphrine, waer Staphylline or bauffalline.

[0050] All the above...

Embodiment 3

[0052] Put 80 mg of pharmaceutical excipient ethylene vinyl acetate copolymer (EVAc) into a container, add 100 ml of dichloromethane to dissolve and mix well, add 20 mg of harringtonine, re-shake, and vacuum dry to remove the organic solvent. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain an anticancer drug composition containing 20% ​​by weight of harringtonine. The drug release time of the composition in physiological saline in vitro is 14-24 days, and the drug release time in mouse subcutaneous is 20-35 days.

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PUM

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Abstract

The present invention relates to an anti-cancer medicine composition which can be slowly-released in human body. Said composition comprises medicinal auxiliary material and plant alkaloids anti-cancer medicine, in white the plant alkaloids anti-cancer medicine can inhibit hyperplasia of tumor, and the medicinal auxiliary material mainly can be bio-compatible high-molecular polymer which can be degraded and absorbed, in the course of its degradation and absorption the plant alkaloid can be slowly released in tumor locality, so that at the same time of obviously reducing systematic toxic it can retain effective medicine concentration in tumor locality so as to obtain good therapeutic effect.

Description

(1) Technical field [0001] The invention relates to an anticancer pharmaceutical composition for slow release in vivo, belonging to the technical field of medicines. (2) Background technology [0002] The treatment of solid tumors mainly includes surgery, radiotherapy and chemotherapy. Among the various chemotherapeutic drugs used, plant alkaloid anticancer drugs have obvious effects and have been widely used in various malignant tumors. However, further studies have found that the excessive expansive hyperplasia of solid tumors has higher interstitial pressure, tissue elastic pressure, fluid pressure and interstitial viscosity than the surrounding normal tissue. Drug concentration (see Kong Qingzhong et al. "Intratumoral placement of cisplatin plus systemic carmustine in the treatment of rat brain tumors" "Journal of Surgical Oncology" 69 pages 76-82 (1998) (Kong Q et al., J Surg Oncol. 1998 Oct; 69(2):76-82), simply increasing the dosage is limited by systemic reactions....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/475A61K31/505A61K31/52A61K45/08
Inventor 孔庆忠
Owner SHANDONG LANJIN PHARMA
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