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Nanoemulsion of trabectedin and preparing method thereof

Active Publication Date: 2017-06-23
JIANGSU HENGRUI MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, some patients are resistant to lactose during practical application, and this invention does not provide a new method to solve the problems of poor solubility and unstable properties of ET-743 in water
In addition, these formulations still showed substantial active ingredient degradation when stored under accelerated conditions of 40°C / 70%RH for 3 months, suggesting that the formulations are still less stable if stored for a long time
[0008] Need to provide a kind of composition, solve the problem that existing preparation and preparation method can't reach or can't solve completely, comprise the stability and solubility of trabectedine, the embodiment of trabectedine preparation should preferably show favorable Freeze Drying Properties

Method used

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  • Nanoemulsion of trabectedin and preparing method thereof
  • Nanoemulsion of trabectedin and preparing method thereof
  • Nanoemulsion of trabectedin and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Prepared with soybean oil for injection and medium-chain glyceride as solubilizer, 15-hydroxystearic acid-polyethylene glycol as emulsifier, disodium hydrogen phosphate as pH buffer, and sodium chloride as osmotic pressure regulator Trabectedine nanoemulsion, and using mannitol as another excipient, prepares its freeze-dried preparation, and the prescription composition and dosage are as follows:

[0047]

[0048] Preparation:

[0049] 1. Add 15-hydroxystearic acid-polyethylene glycol ester, medium-chain glyceride and soybean oil into a 7mL vial, heat to 60±5°C, and stir at a certain stirring speed until the mixture is uniform.

[0050] 2. Take 10mL of water for injection and put it in beaker 2, and cool it down to 45°C for later use.

[0051] 3. Take about 2.4 mL (15%) of cooled water for injection and pour it into vial 1, stir at 400 rpm for 10 min until micelles are formed, and maintain 45°C.

[0052] 4. Take 2 mg of trabectedin powder, put it in a 7 mL vial, ad...

Embodiment 2

[0063] Trabectedin nanoemulsion was prepared with olive oil for injection and medium-chain glyceride as solubilizer, lecithin as emulsifier, disodium hydrogen phosphate as buffer, sodium chloride as osmotic pressure regulator, and sucrose as Freeze-dried protective agent, prepare its freeze-dried preparation, prescription composition and dosage are as follows:

[0064]

[0065] Preparation:

[0066] 1. Add lecithin E80, medium-chain glycerides and olive oil into a 7mL vial, heat to 60±5°C, and stir at a certain speed until they are evenly mixed.

[0067] 2. Take 10mL of water for injection and put it in beaker 2, and cool it down to 45°C for later use.

[0068] 3. Take about 2.4 mL (15%) of cooled water for injection and pour it into vial 1, stir at 400 rpm for 10 min until micelles are formed, and maintain 45°C.

[0069] 4. Take 2 mg of trabectedin powder, put it in a 7 mL vial, add 160 μL of 45°C water for injection to moisten the API, and add it to beaker 1, then add 1...

Embodiment 3

[0081] Coconut oil and medium-chain glycerides were used as solubilizers, poloxamer 188 was used as emulsifier, disodium hydrogen phosphate was used as buffer, sodium chloride was used as osmotic pressure regulator to prepare trabectedin nanoemulsion, and sucrose As another excipient, prepare its freeze-dried preparation, the composition and dosage of the prescription are as follows:

[0082]

[0083] Preparation:

[0084] 1. Add Poloxamer 188, medium-chain glycerides and coconut oil into a 7mL vial, heat to 60±5°C, and stir at a certain speed until they are evenly mixed.

[0085] 2. Take 10mL of water for injection and put it in beaker 2, and cool it down to 45°C for later use.

[0086] 3. Take about 2.4 mL (15%) of cooled water for injection and pour it into vial 1, stir at 400 rpm for 10 min until micelles are formed, and maintain 45°C.

[0087] 4. Take 2 mg of trabectedin powder, put it in a 7 mL vial, add 160 μL of 45°C water for injection to moisten the API, and add...

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Abstract

The invention relates to nanoemulsion of trabectedin and a preparing method thereof. Specifically, the nanoemulsion of trabectedin comprises a solubilizer and an emulgator. The nanoemulsion improves the stability of trabectedin during preparation and storage of pharmaceutic preparations.

Description

technical field [0001] The invention relates to a trabectedin nanoemulsion and a preparation method thereof. Background technique [0002] Trabectedin (Eid-743, abbreviated as ET-743 or ET743) is a tetrahydroisoquinoline alkaloid isolated from marine tunicates, and its specific structure is as follows. Its anti-tumor activity is mainly achieved by alkylating DNA by itself forming iminium ions or similar intermediates (Chem. Rev. 2002, 102, 1669). , colon cancer, kidney cancer, ovarian cancer, endometrial cancer, melanoma, osteosarcoma and prostate cancer have inhibitory activity, and it is a novel anticancer drug that can bind to DNA. Haiscidin-743 was developed by PharmMar, Spain, and was approved in the European Union in 2007 as a rare drug for the treatment of soft tissue sarcoma. It is used to treat patients with advanced soft tissue sarcoma who are ineffective in traditional chemotherapy. [0003] [0004] ET-743 is a complex compound with limited water solubility,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K9/19A61K31/4995A61K47/44A61K47/14A61K47/24A61K47/10A61K47/26A61P35/00
CPCA61K9/1075A61K9/19A61K31/4995A61K47/10A61K47/14A61K47/24A61K47/26A61K47/44
Inventor 孙琼邵长丽简彤刘凯史海贤
Owner JIANGSU HENGRUI MEDICINE CO LTD
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