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Anti-cancer slow release injection comprising plant alkaloid

A technology of sustained-release injections and plant alkaloids, which is applied in the field of medicine and can solve problems such as complicated operations, limited dosage, and large trauma

Inactive Publication Date: 2007-03-07
孔庆忠
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, further studies have found that inappropriate drug administration often leads to the development of tolerance, which eventually leads to the failure of treatment
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 brain tumors in rats", "Journal of Surgical Oncology", 1998, 69, pages 76-82 (Kong Q et al., J Surg Oncol.1998 Oct; 69 (2) :76-82), simply increasing the dosage is limited by systemic reactions
Drug implantation may solve the problem of drug concentration to some extent. However, the operation of drug implantation is more complicated and traumatic. In addition to easily causing various complications such as bleeding, infection, and decreased immunity, it can also cause or accelerate tumor spread and metastasis

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Put 80 mg of PLGA (copolymer of glycolic acid and glycolic acid, weight ratio 70:30) as a pharmaceutical excipient of 20,000 into the container, add 100 ml of dichloromethane to dissolve and mix well, add 20 mg of vinorelbine, and shake well again Dry in vacuo to remove the organic solvent. The dried solid composition is melted to prepare slow-release pellets containing 20% ​​by weight of vinorelbine, which are subpackaged and sterilized by radiation. The sustained-release pellets are suspended in water for injection containing 1.5% sodium carboxymethylcellulose to prepare the corresponding suspension-type sustained-release injection. The release time of the slow-release injection in physiological saline in vitro is 14-24 days, and the release time in mouse liver cancer is 20-35 days.

Embodiment 2

[0042] As described in Example 1, the difference is that the contained active ingredients are 30% by weight (sulfuric acid) vincristine, vinblastine, isovinblastine, vinpoindole, vinca mustard, oxyvinblastine, podophyllum Hydrazine, Dehydrated Vinblastine Tartrate, Epoxy Vinblastine Tartrate, Epoxy Vinblastine, Vinblastine Tartrate, Hainan Crude Torresine, Hainan Crude Torrellactone, Vinpocetine, Bitartrate, Vinorelbine, Vinorelbine Bitartrate, vinorelbine tartrate, vinblastate, vinblastol, vinblastol, vinblastin, vinblastine sulfate, vinblastine, vinblastine, vinblastine, vinblastine, vinblastine, vinblast Dixin, vinblastine, vinblastine, vinblastine, oxymatrine, harringtonine, deoxyharringtonine, homoharringtonine, pearl cyst shellin, monocrotaline, metansin , erythrocetium, total alkaloids of camels, heart chrysanthemum lactone, medensine, oridonin, Zhangzhou narcissine, pronarcisine hydrochloride, procarbazine, procarbazine hydrochloride, tangsongine, tangsong Staclitine,...

Embodiment 3

[0044] 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 prepared by a melting method to obtain slow-release pellets containing 20% ​​by weight of harringtonine, which are subpackaged and sterilized by radiation. The sustained-release pellets are suspended in water for injection containing 1.5% sodium carboxymethylcellulose and 15% mannitol to prepare the corresponding suspension-type sustained-release injection. The release time of the slow-release injection in physiological saline in vitro is 14-24 days, and the release time in mouse lung cancer is 20-35 days.

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PUM

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Abstract

Disclosed is an anticancer slow release injection containing plant alkaloids, wherein the constituents include anti-cancer drugs, slow release auxiliary materials, suspending agent and / or dissolvent. The anti-cancer drugs include leurocristine, Vinblastine, procarbazine, leurosidine or vinorelbine, the slow release auxiliary materials can be selected from polylactic acid, glycolic acid and glycolic acid copolymer, ethylene-vinylacetate copolymer or their combination. The suspending agent is selected from sodium carboxymethylcellulose and mannitol. The dissolvent is selected from distilled water, water for injection, physiological lotion, absolute ethyl alcohol, microcosmic salt or carbonates cushioning liquid. The anticancer slow release injection can be administered through subcutaneous, intracavity, intra-tumor, tumor-surrounding, intra- lymph gland or bone marrow channels, the whole body toxicity reaction of the anti-cancer medicament can be lowered, the tumor local medicinal concentration can also be selectively increased and maintained, and the treatment effect of the non-operative treatment methods such as chemotherapy, medicament and radiation can also be improved.

Description

(1) Technical field [0001] The invention relates to an anticancer sustained-release injection containing plant alkaloids, which belongs to the technical field of medicines. (2) Background technology [0002] Plant alkaloid anticancer drugs, as commonly used chemotherapy drugs, have been widely used in the treatment of various malignant tumors, and have achieved relatively obvious effects. However, further studies have found that inappropriate drug administration often leads to the generation of tolerance, which eventually leads to the failure of treatment. 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 treatme...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K9/00A61P35/00
Inventor 孔庆忠孙娟孔令栋张红军
Owner 孔庆忠
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