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Trabectedin medicinal composition and preparation method thereof.

A technology of trabectedin and composition, which is applied in the direction of drug combination, pharmaceutical formulation, drug delivery, etc., can solve the problems of unusable, unstable and unstable in long-term storage, and achieve improved stability and easy large-scale production , The effect of solubility increase

Active Publication Date: 2017-06-16
JIANGSU HENGRUI MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this formulation is unstable for long-term storage in the refrigerator and at room temperature and must be stored at -15 to -25°C in the dark
CN102018714A discloses a ET-743 freeze-dried preparation containing disaccharides selected from lactose, sucrose, etc., which may not be available for some lactose-intolerant patients. In addition, these preparations are stored under accelerated conditions of 40°C / 70%RH3 Still showed substantial degradation of the active ingredient at 3 months, suggesting that the formulation is still less stable if stored for long periods of time

Method used

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  • Trabectedin medicinal composition and preparation method thereof.
  • Trabectedin medicinal composition and preparation method thereof.
  • Trabectedin medicinal composition and preparation method thereof.

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] The trabectedin inclusion compound was prepared with sulfobutyl-β cyclodextrin as the main molecule, wherein the concentration of sulfobutyl-β cyclodextrin was 30%, and the solution prescription and method before freeze-drying were as follows:

[0034] composition effect batch size 6mL dosage Trabectedin active ingredient 0.25mg / mL 1.5mg Phosphoric acid, 0.1N Dissolution / pH adjustment 0.043mg / mL 0.258mL Sulfobutyl-β-cyclodextrin Principal Molecule 300mg / mL 0.18g Potassium dihydrogen phosphate pH adjustment 6.8mg / mL 40.8mg Phosphoric acid, 1N / potassium hydroxide, 0.1M pH adjustment pH5.5 Appropriate amount Water for Injection solvent Appropriate to volume Appropriate to volume

[0035] Preparation:

[0036] 1. Take 1.5 mg of trabectedin, add 0.258 mL of 0.1N phosphoric acid solution, and stir to completely dissolve the drug;

[0037] 2. Take 0.18g of sulfobutyl-β cyclodextrin and 40.8mg ...

Embodiment 2

[0048] The inclusion compound of trabectedin was prepared with sulfobutyl-β cyclodextrin as the main molecule, wherein the concentration of sulfobutyl-β cyclodextrin was 10%, and the solution prescription and method before freeze-drying were as follows:

[0049] composition effect batch size 6mL dosage Trabectedin active ingredient 0.25mg / mL 1.5mg Phosphoric acid, 0.1N Dissolution / pH adjustment 0.043mg / mL 0.258mL Sulfobutyl-β-cyclodextrin Principal Molecule 100mg / mL 0.06g Potassium dihydrogen phosphate pH adjustment 6.8mg / mL 40.8mg Phosphoric acid, 1N / potassium hydroxide, 0.1M pH adjustment pH6.5 Appropriate amount Water for Injection solvent Appropriate to volume Appropriate to volume

[0050] Preparation:

[0051] 1. Take 1.5 mg of trabectedin, add 0.258 mL of 0.1N phosphoric acid solution, and stir to completely dissolve the drug;

[0052] 2. Take 0.06g of sulfobutyl-β cyclodextrin and 40.8...

Embodiment 3

[0063] The trabectedin inclusion complex was prepared with sulfobutyl-β cyclodextrin as the main molecule, wherein the concentration of sulfobutyl-β cyclodextrin was 3%, and the solution prescription and method before freeze-drying were as follows:

[0064] composition effect batch size 6mL dosage Trabectedin active ingredient 0.25mg / mL 1.5mg Sulfobutyl-β-cyclodextrin Principal Molecule 20mg / mL 0.12g Water for Injection solvent Appropriate to volume Appropriate to volume

[0065] Preparation:

[0066] 1. Take 1.5mg trabectedin and add a small amount of water for injection to moisten;

[0067] 2. Take 0.12g of sulfobutyl-β cyclodextrin and add 4mL of water for injection, stir to dissolve;

[0068] 3. Add the solution in 1 to 2, mix well, stir at room temperature for 0.5-2 hours, and prepare the solution before lyophilization;

[0069] 4. Filter the solution before freeze-drying, freeze-dry after filling and half stoppering. ...

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Abstract

The present invention relates to a trabectedin medicinal composition and a preparation method thereof, and concretely relates to a composition formed by trabectedin and a cyclodextrin derivative, and a preparation method thereof. Trabectedin in the composition is included as a guest molecule by the cyclodextrin derivative, so the solubility is increased, and the stability is improved. The invention also discloses a lyophilized preparation containing the above inclusion compound. The trabectedin composition has the advantages of good solubility, stable quality, and facilitation of clinical application.

Description

technical field [0001] The invention relates to a trabectedin composition, in particular to a prescription, a freeze-dried preparation, a preparation method and a process of the trabectedin composition. The invention belongs to the technical field of medicine. 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 advanc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K9/19A61K9/08A61K31/4995A61P35/00
CPCA61K9/0019A61K9/08A61K9/19A61K31/4995
Inventor 孙琼邵长丽刘凯周晓丹简彤
Owner JIANGSU HENGRUI MEDICINE CO LTD
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