Slow released injection containing satraplatin and its synergist

A technology of sustained-release injections and Satraplatin, which is applied in the field of sustained-release injections and its preparation, and can solve problems such as treatment failure and increased tolerance

Inactive Publication Date: 2006-11-08
JINAN KANGQUAN 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

[0115] 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 Scitraplatin and 10 mg camptothecin were re-shaken and spray-dried to prepare microspheres for injection containing 10% scitraplatin and 10% camptothecin. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection. The viscosity of the injection is 200cp-650cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 20-30 days, and the drug release time in mice subcutaneous is about 30-40 days.

Embodiment 2

[0117] 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:

[0118] (a) 2-40% satraplatin, cisplatin, carboplatin, heptaplatin, lobaplatin, nedaplatin or oxaliplatin; or

[0119] (b) 2-40% Satraplatin and 2-40% camptothecin, hydroxycamptothecin, letotecan, topotecan, irinotecan, etoposide, teniposide, ammonia Combinations of Rubicin, Erubicin, Rhodopyrin, Liurubicin or Zorubicin.

Embodiment 3

[0121] Put 70 mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 25,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, then add 15 mg of Satraplatin and 15 mg of hydroxycamptothecin, re-shake and vacuum Dry to remove organic solvent. The dried drug-containing solid composition was frozen and pulverized to make a micropowder containing 15% saterplatin and 15% hydroxycamptothecin, and then suspended in physiological saline containing 1.5% sodium carboxymethylcellulose to obtain the corresponding Suspension-type sustained-release injection. The viscosity of the injection is 300cp-650cp (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 30-35 days.

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PUM

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Abstract

The slow released anticancer injection containing both satraplatin and its synergist consists of slow released microsphere and solvent. The slow released microsphere includes effective anticancer component and slow releasing supplementary material carrier, and the solvent is special solvent containing suspending agent. The effective anticancer component includes satraplatin, Cisplatin, Carboplatin, etc and satraplatin synergist selected from antitumor antibiotic, toporase inhibitor and / or tetrazine compound. The slow releasing supplementary material is selected from difatty acid-sebacic acid copolymer, polylactic acid, etc. The suspending agent is carboxymethyl cellulose sodium, etc. and has viscosity of 100-3000 cp at 20-30 deg.c. The slow released microsphere may be also prepared into slow released implanting agent for use to raising chemotherapeutic and radiotherapeutic effect.

Description

(1) Technical field [0001] The invention relates to a sustained-release injection containing satetraplatin and / or its synergist and a preparation method thereof, belonging to the technical field of medicines. (2) Background technology [0002] Satrapiatin (JM-216) is a third-generation platinum complex antitumor drug with a cyclohexylamine structure developed by BMS. It has a certain effect on small cell lung cancer and non-small cell lung cancer, ovarian cancer, brain tumors and head and neck tumors. However, its unexpected neurotoxicity greatly limits the application of this drug. Blood vessels, connective tissue, matrix proteins, fibrin, and collagen in the tumor stroma not only provide scaffolds and essential nutrients for the growth of tumor cells, but also affect the penetration of chemotherapy drugs around the tumor and in the tumor tissue and diffusion (see Netti et al. "The influence of the status of the extracellular matrix on the movement of drugs in solid tumor...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/282A61K45/00A61K47/32A61K47/34A61K47/36A61K47/38A61K47/42A61P35/00
Inventor 孙娟
Owner JINAN KANGQUAN PHARMA TECH
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