Slow release injection containing platinum compound and alkylating agent

A technology of sustained-release injections and compounds, applied in the field of medicine, can solve problems such as increased tolerance and treatment failure

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...

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0111] 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 cisplatin, 20mg carmustine, 10mg cisplatin and 10mg carmustine respectively, and prepare 20% cisplatin, 20% carmustine, And 10% cisplatin and 10% carmustine microspheres for injection. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection. The drug release time of the sustained release injection in the physiological saline in vitro is 60-65 days, and the drug release time in the mouse subcutaneous is more than 60 days.

Embodiment 2

[0113] The method step of being processed into slow-release injection is identical with embodiment 1, but difference is that the p(BHET-EOP / TC) that used adjuvant is 50: 50, containing anticancer active ingredient and weight percent thereof are:

[0114] (1) 2-30% carmustine or nimustine;

[0115] (2) 5-40% cisplatin, nedaplatin, or carboplatin; or

[0116] (3) Combination of 5-40% cisplatin, nedaplatin or carboplatin and 1-20% carmustine or nimustine.

Embodiment 3

[0118] 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 of cisplatin, 30mg of nimustine, 25mg of cisplatin and 5mg of nimustine, re-shake and use the spray drying method to prepare 30% cisplatin, 30% nimustine, 25% cisplatin and 5% Nimustine microspheres for injection. The dried microspheres are suspended in physiological saline 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 65-70 days, and the release time in mice subcutaneously is about 65 days.

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Abstract

Disclosed is a slow release injection containing platinum-group compounds and/or alkylating agents, which comprises slow release microspheres and dissolvent, the slow release microspheres include platinum-group compounds selected from Tegafur, Capecittabine, Pemetrexed, Carboplatin or Gemcitabine, and/or alkylating agent 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, poly(dodecanedioic acid-tetradecanedioic acid) or poly(fumaric acid-sebacylic acid). The alkylating agent is selected from Carmustine, Nimustine, Fotemustine, Lomustine or bendamustine. 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 sustained-release injection containing a platinum compound and / or an alkylating agent and a preparation method thereof, belonging to the technical field of medicines. (2) Background technology [0002] As a class of commonly used chemotherapeutic drugs, platinum compounds 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 carmustine plus systemic carmustine treatment of rat brain tumors" "Journal of Surgical O...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/282A61K31/555A61K45/06A61K47/34A61P35/00
Inventor 孙中先
Owner JINAN SHUAIHUA PHARMA TECH
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