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Rubitecan containing formulation for injection

A technology of Rubicon and Rubicon, which is applied in the field of injection preparations and can solve the problems of expensive pharmaceutical excipients, high process conditions, etc.

Inactive Publication Date: 2005-07-06
QILU PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the preparation for injection is not a true solution, and the preparation requires higher process conditions and more expensive pharmaceutical excipients

Method used

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  • Rubitecan containing formulation for injection

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1: powder injection (freeze-dried formulation) containing Rubitol and its preparation

[0023] Specifications 1.0mg Rubicon is calculated as 1000 pieces

[0024] Ingredient Amount

[0025] Rubicon 1.0g

[0026] HP-β-CD 3000g

[0027] Water for injection 5700ml

[0028] Citric acid, sodium citrate amount

[0029] Dimethyl sulfoxide amount

[0030] preparation:

[0031] 1) Add 3000g HP-β-CD to 5700ml water, stir until completely dissolved, adjust the pH value to 3.2 with appropriate amount of citric acid and sodium citrate.

[0032] 2) Dissolve 1.0g of Rubicon with an appropriate amount of dimethyl sulfoxide and heat moderately.

[0033] 3) Add 2) into 1), and continue stirring for 30 minutes.

[0034] 4) Filtration, subpackaging, freeze-drying, inspection, and packaging.

Embodiment 2

[0035] Embodiment 2 powder injection (freeze-dried formulation) containing Rubicon and its preparation

[0036] Specifications: 0.5mg Rubicon is calculated as 1000 pieces

[0037] Ingredient Amount

[0038] Rubicon 0.5g

[0039] HP-β-CD 1500g

[0040] Water for injection 4100ml

[0041] Citric acid, sodium citrate amount

[0042] Dimethyl sulfoxide amount

[0043] 1) Add 1500g of HP-β-CD to 4100ml of water and stir until completely dissolved, and adjust the pH value to 3.8 with appropriate amount of sodium dihydrogen phosphate and disodium hydrogen phosphate.

[0044] 2) Dissolve 0.5g of Rubicon with an appropriate amount of dimethyl sulfoxide and heat moderately.

[0045] 3) Add 2) into 1), and continue stirring for 30 minutes.

[0046] 4) Filtration, subpackaging, freeze-drying, inspection, and packaging.

Embodiment 3

[0047] Embodiment 3 powder injection containing Rubicon and its preparation

[0048] Specification 0.3mg Rubitoran is calculated by 1000 pieces

[0049] Raw material name Feed amount

[0050] Rubicon 0.3g

[0051] HP-β-CD 750g

[0052] Mannitol aqueous solution for injection 500ml (containing mannitol 100g)

[0053] Water for injection 4000ml

[0054] Citric acid, sodium citrate amount

[0055] Dimethyl sulfoxide amount

[0056] a) Add 4000ml of water and 500ml of mannitol aqueous solution for injection to 750g of HP-β-CD and stir until completely dissolved, adjust the pH value to 3.4 with appropriate amount of sodium dihydrogen phosphate and disodium hydrogen phosphate.

[0057] b) Dissolve 0.3g of Rubicon with an appropriate amount of dimethyl sulfoxide and heat moderately.

[0058] c) Add 2) into 1) and continue stirring for 30 minutes.

[0059] d) Filtration, sub-packaging, freeze-drying, inspection, and packaging.

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Abstract

The invention relates to a Rubitecan containing formulation for injection which comprises Rubitecan and medical use cyclodextrin, the preparation by the invention may further includes auxiliary solvent, pH modifier and / or adjuvant for aqueous solvent for injection.

Description

field of invention [0001] The invention relates to a preparation for injection containing rubicol (9-nitro-camptothecin), which comprises rubicol and pharmaceutical cyclodextrin. The formulation of the present invention may further include cosolvents, pH regulators and / or auxiliary materials for water solvent injection. Background technique [0002] Rubicon is a known anticancer compound represented by the formula and its chemical name is 9-nitro-camptothecin [0003] [0004] Because rubiticol is a nearly water-insoluble compound, attempts have been made to administer it by injection. US Patent No. 6,509,027 discloses a colloidal solution for injection containing Rubitolone. The colloidal solution contains solid particles with a diameter of 0.05-10 μm, and the particles are covered with a film of 0.3 nm-3.0 μm. The film is composed of amphiphilic lipids. However, the preparation for injection is not a true solution, and its preparation requires relatively high process ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4745A61P35/00
Inventor 尹晓慧张桂婷张照珍王剑周英兰边红王晶翼张明会杨清敏韩作宏
Owner QILU PHARMA CO LTD