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Epothilone freeze-drying composition

A technology of epothilone and its composition, which is applied in the field of epothilone freeze-dried composition and its preparation, can solve the problems of cumbersome and complicated operation, and achieve the effects of good solubility, stable quality and reduced side effects

Inactive Publication Date: 2009-05-06
ZHEJIANG HISUN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Patent applications CN99803672.2 and CN200480029613.2 disclose the recipe for preparing epothilone freeze-dried preparations, including preparing 30ml of epothilone B (epothilone B) and 1500mg of mannitol Aqueous solution, freeze-dried, because epothilone is insoluble in water, this technical scheme is impossible to realize in fact; However, with the in-depth understanding of cyclodextrin, its side effects as an excipient for injections have also attracted people's attention. Hydroxypropyl-β-cyclodextrin for injection can not only cause nephrotoxicity, but also Can cause hemolysis
[0005] The ZL02804090.2 patent discloses the use of tert-butanol-water to dissolve azaepothilone B to prepare a lyophilized stock solution. When the lyophilized product is reconstituted into a medicinal solution for intravenous injection, polyoxyethylene castor oil-free After the water and ethanol are dissolved, the lactic acid Grüner's solution is used to dilute. The whole operation is very cumbersome and complicated, and polyoxyethylene castor oil is also used. However, with the clinical occurrence of severe allergic reactions caused by polyoxyethylene castor oil excipients for injection At present, many newly developed insoluble drug injections do not use polyoxyethylene castor oil as an excipient for injection

Method used

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  • Epothilone freeze-drying composition
  • Epothilone freeze-drying composition
  • Epothilone freeze-drying composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Dissolve 5.0 mg of epothilone B in 500 mg of Solutol HS 15, then add 10 mM NaH, pH 7.0 2 PO4-Na 2 HPO 4 Buffer solution and 500 mg of mannitol were prepared into 5 ml of a clear solution. The solution was sterilized and filtered through a filter membrane with a pore size of 0.2 μm. The filtrate was filled into a vial with a volume of 10 ml under aseptic conditions, and lyophilized Rubber stopper, freeze-dried, after the freeze-drying is completed, aseptically inject sterile dry nitrogen gas to raise the pressure of the freeze-drying chamber to atmospheric pressure, compress the rubber stopper aseptically to provide an airtight aseptic seal, crimp the cap , Labeled, boxed and stored at 2-30°C.

[0036] Just before administration, it is reconstituted with 5ml of water for injection or other aqueous pharmaceutical media, and administered intravenously.

Embodiment 2

[0038] Dissolve 5.0 mg of epothilone B in 500 mg of Solutol HS 15, then add water for injection and 500 mg of mannitol to prepare 5 ml of a clear solution, pass the solution through a filter membrane with a pore size of 0.2 μm, and sterilize and filter the filtrate in a sterile Fill it into a vial with a volume of 10ml under the same conditions, add a freeze-dried rubber stopper under aseptic conditions, and freeze-dry. Aseptically compress the rubber stopper to provide an airtight aseptic seal, crimp the cap, label it, and pack it into a box for storage at 2-30°C.

[0039] Just before administration, reconstitute with 5ml of water for injection or other aqueous pharmaceutical media, and administer intravenously.

Embodiment 3-11

[0041] According to the method of Example 2, the lyophilized composition of the present invention was prepared with the prescription in Table 1.

[0042] Table 1

[0043] Example

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Abstract

The invention discloses an Epothilone freeze-dried compound which mainly contains the Epothilone, a solubilizer and a freeze-dried excipient; wherein, a preferable solubilizer is Carmowax 12-hydroxyl stearate. The product not only is simple in technique and is stable in quality, but also is low in side effect.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to an Epothilone freeze-dried composition and a preparation method thereof. Background technique [0002] Epothilone is a kind of microtubule-stabilizing cytotoxic substance, which belongs to 16-membered macrolide compound containing 7 chiral centers. Its anti-tumor mechanism is very similar to paclitaxel, and it is a new type of microtubule-stabilizing It has the effect of promoting guanosine triphosphate (GTP)-dependent tubulin polymerization to form microtubules, and has a stabilizing effect on microtubules, and inhibits the depolymerization of microtubules, abnormal arrangement of microtubules, The formation of stellate bodies can inhibit the formation of normal mitotic spindles, thereby inhibiting the growth of tumor cells and even inducing their death. Epothilone B (Patupilone, EPO906) developed by Novartis has entered clinical phase III research . [0003] Because epothi...

Claims

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Application Information

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IPC IPC(8): A61K31/427A61K9/19A61K47/34A61P35/00A61K47/14
Inventor 曹金全廖建维
Owner ZHEJIANG HISUN PHARMA CO LTD
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