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Freeze-drying composition of posaconazole prodrug and preparation method and application of freeze-drying composition of posaconazole prodrug

A prodrug, posaconazole technology, applied in the direction of freeze-drying delivery, powder delivery, antifungal agents, etc., to achieve stable performance, easy large-scale industrial production, and high quality effects

Inactive Publication Date: 2016-02-03
HC SYNTHETIC PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is reported in the literature that this excipient has certain hemolytic, nephrotoxic and carcinogenic properties, and there may be more serious side effects that are not known to us, so its use should be more cautious

Method used

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  • Freeze-drying composition of posaconazole prodrug and preparation method and application of freeze-drying composition of posaconazole prodrug
  • Freeze-drying composition of posaconazole prodrug and preparation method and application of freeze-drying composition of posaconazole prodrug
  • Freeze-drying composition of posaconazole prodrug and preparation method and application of freeze-drying composition of posaconazole prodrug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1: the preparation of posaconazole phosphate for injection

[0023] Prescription: posaconazole phosphate 200g

[0024] Water for injection 2000ml

[0025]

[0026] Makes 1000 bottles

[0027] Add 1500ml of water for injection into the liquid preparation container, add posaconazole phosphate in the exact prescription amount, stir to dissolve, slowly add sodium hydroxide, adjust the pH to 8.0, add water to the full amount, and then add 0.05% (W / V) medicinal charcoal, stirred for 20 minutes, decarbonized by coarse filtration with a sand filter, and finely filtered with a 0.22 μm microporous membrane until the clarity was qualified; Put a half stopper in the bottle, pre-freeze the sample at -40°C for 4 hours, vacuumize, keep the vacuum at 10-30Pa, slowly raise the temperature to -20°C, and keep it for 12 hours; then slowly raise the temperature to 20°C, keep it for 4 hours, control the moisture 2%, cork and cap.

Embodiment 2

[0028] Embodiment 2: the preparation of posaconazole phosphate disodium for injection

[0029] Prescription: Posaconazole Phosphate Disodium 200g

[0030] Water for injection 2000ml

[0031]

[0032] Makes 1000 bottles

[0033] Add 1500ml of water for injection into the liquid preparation container, add posaconazole disodium phosphate disodium phosphate in the exact prescription amount, stir to dissolve, slowly add acetic acid, adjust the pH to 8.5, add water to the full amount, and then add 0.05% (W / V) medicinal charcoal, stirred for 60 minutes, decarbonized by coarse filtration with a sand filter rod, and finely filtered with a 0.22 μm microporous membrane until the clarity was qualified; Put a half stopper in the bottle, pre-freeze the sample at -45°C for 4 hours, vacuumize, keep the vacuum at 10-30Pa, slowly raise the temperature to -20°C, and keep it for 12 hours; then slowly raise the temperature to 0°C, keep it for 6 hours, and then slowly Raise the temperature t...

Embodiment 3

[0034] Embodiment 3: the preparation of posaconazole phosphate disodium pentahydrate for injection

[0035] Prescription: Posaconazole Phosphate Disodium Pentahydrate 200g

[0036] Mannitol 2g

[0037] Water for injection 2500ml

[0038]

[0039] Makes 1000 bottles

[0040] Add 2000ml of water for injection into the liquid preparation container, add the exact prescription amount of posaconazole phosphate disodium pentahydrate, 2g of mannitol, stir, slowly add sodium carbonate, adjust the pH to 9.0, add water to the full amount, Then add 0.1% (W / V) medicinal charcoal, stir for 10 minutes, decarbonize by coarse filtration with a sand filter, and fine filter with a 0.22 μm microporous membrane until the clarity is qualified; after the determination of the intermediate content is qualified, set the Measure and pack in vials, add half stopper, pre-freeze the sample at -40°C for 4 hours, vacuumize, keep the vacuum at 10-30Pa, slowly raise the temperature to -20°C, and keep it ...

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Abstract

The invention relates to a freeze-drying composition of a posaconazole prodrug and a preparation method and application of the freeze-drying composition of the posaconazole prodrug. The freeze-drying composition has the advantages that the freeze-drying composition is high in water solubility, and safety of the freeze-drying composition is guaranteed due to the fact that cyclodextrins auxiliary materials need not to be added during the preparation of the freeze-drying composition; the freeze-drying composition is suitable for being used for treating various amphotericin-intolerant or refractory adult invasive fungal infections; the freeze-drying composition is used as a preventive drug for high-risk patients, the freeze-drying composition is applicable to patients above 13 years old and with impaired immunity and especially applicable to patients who have graft versus host disease (GVHD) after hematopoietic stem cell transplant, patients with leukemia and patients with long-term leukopenia due to chemotherapy; compared with control drugs such as fluconazole and itraconazole, the freeze-drying composition can effectively prevent invasive aspergillosis and can lower the mortality related to the invasive fungal infections.

Description

technical field [0001] The invention relates to a composition, in particular to a posaconazole prodrug freeze-dried composition and a preparation method and application thereof. Background technique [0002] Posaconazole (Posaconazolc), molecular formula: C 37 h 42 f 2 N 8 o 4 . Posaconazole is a derivative of itraconazole, a second-generation triazole antifungal drug launched in 2006. Broad antibacterial spectrum, for Candida, histoplasma capsulata, Sedosporum, bipolar zygomycetes, Fusarium, yeast. Including fluconazole-resistant non-albicans strains, Cryptococcus neoformans and Aspergillus have strong inhibitory activity; especially against relatively rare but life-threatening fungal diseases (zygomycosis, fusarium and coccidioidomycosis, etc. ) also works. This product is suitable for the treatment of a variety of adult invasive fungal infections that are intolerant or refractory to amphotericin; it is used as a prophylactic drug for high-risk patients, and it is ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/496A61P31/10
Inventor 张起愿刘飞张丽芳
Owner HC SYNTHETIC PHARMA CO LTD
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