Voriconazole slow-release suppository and preparation method thereof

A voriconazole sustained-release suppository, voriconazole technology, applied in suppository delivery, antifungal agents, pharmaceutical formulations, etc., can solve the problems of patient inconvenience and poor compliance, and achieve the effects of prolonging the action time, good antifungal effect, and reducing side effects

Active Publication Date: 2011-05-18
苏州特瑞药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The dosage forms of voriconazole include: freeze-dried powder injection, tablet, dry suspension, but the compliance of injection administration is poor, especially those drugs that require frequent administration, which is extremely inconvenient for patients, so it is necessary to administer voriconazole non-injection drug pathway research

Method used

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  • Voriconazole slow-release suppository and preparation method thereof
  • Voriconazole slow-release suppository and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] The preparation of voriconazole sustained-release suppository comprises the following steps:

[0040] 1. Preparation of voriconazole hydroxypropyl-β-cyclodextrin solution:

[0041] Heat the purified water to 80°C, add hydroxypropyl-β-cyclodextrin and stir to dissolve, configure a hydroxypropyl-β-cyclodextrin solution with a mass concentration of 19%, cool down to 70°C, add voriconazole and stir to dissolve, Stop heating, stir for 1.5h, and prepare a 20mg / ml voriconazole solution.

[0042] 2. Preparation of microspheres:

[0043] Weigh 0.3 g of chitosan and dissolve it ultrasonically with 10 ml of voriconazole solution. Take another beaker, add 30ml of liquid paraffin, stir magnetically, add about 2.5ml of Tween-80, after mixing evenly, add the above voriconazole solution containing chitosan, emulsify for 1.5h, adjust the pH value to 8 with 0.1mol / l NaOH , stirred, cross-linked for 1.5h, stopped stirring, centrifuged to separate the microspheres, and dried to obtain v...

Embodiment 2

[0072] The preparation of voriconazole sustained-release suppository comprises the following steps:

[0073] 1. Preparation of voriconazole hydroxypropyl-β-cyclodextrin solution:

[0074] Heat the purified water to 80°C, add hydroxypropyl-β-cyclodextrin and stir to dissolve, configure a hydroxypropyl-β-cyclodextrin solution with a mass concentration of 15%, cool down to 70°C, add voriconazole and stir to dissolve, Stop heating, stir for 1 h, and prepare a 5 mg / ml voriconazole solution;

[0075] 2. Preparation of microspheres:

[0076] Weigh 0.1 g of chitosan and dissolve it ultrasonically with 10 ml of voriconazole solution. Take another beaker, add 20ml of liquid paraffin, stir magnetically, add about 2.0ml of Span-80, after mixing evenly, add the above-mentioned voriconazole solution containing chitosan, emulsify for 1.5h, and adjust the pH value to 8 with 0.1mol / l NaOH , stirred, cross-linked for 1 hour, stopped stirring, centrifuged to separate microspheres, and dried t...

Embodiment 3

[0080] The preparation of voriconazole sustained-release suppository comprises the following steps:

[0081] 1. Preparation of voriconazole hydroxypropyl-β-cyclodextrin solution:

[0082] Heat the purified water to 80°C, add hydroxypropyl-β-cyclodextrin and stir to dissolve, configure a hydroxypropyl-β-cyclodextrin solution with a mass concentration of 18%, cool down to 70°C, then add voriconazole and stir to dissolve, Stop heating, stir for 1.5h, and prepare a 10mg / ml voriconazole solution.

[0083] 2. Preparation of microspheres:

[0084] Weigh 0.2g chitosan and dissolve it ultrasonically with 10ml voriconazole solution. Take another beaker, add 25ml of liquid paraffin, stir magnetically, add about 2.0ml of Tween-80, after mixing evenly, add the above voriconazole solution containing chitosan, emulsify for 1.5h, adjust the pH value to 8 with 0.1mol / l NaOH , stirred, cross-linked for 1.5h, stopped stirring, centrifuged to separate the microspheres, and dried to obtain vori...

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Abstract

The invention discloses a voriconazole slow-release suppository and a preparation method thereof. The voriconazole slow-release suppository disclosed by the invention is prepared from voriconazole, a solubilizer, a slow-release material, an emulsifier, a dispersing medium and an excipient; and the preparation method disclosed by the invention comprises the following steps of: preparing slow-release microspheres by solubilizing the extremely indissolvable voriconazole, carrying out cast pouring and cooling to obtain the voriconazole slow-release suppository. The preparation method disclosed bythe invention is simple, the prepared suppository has a slow-release characteristic, the first pass effect generated by oral administration and the toxic action of intravenous administration for the organs of a whole body are avoided, and particularly for the patients of intensive care units, the patients with serious fungous infection and child and senile patients, the pain brought to the patients by frequent administration is reduced, the administration compliance is improved, and the curative effect of medicaments is improved.

Description

technical field [0001] The invention relates to the field of medicines, in particular to a voriconazole sustained-release suppository and a preparation method thereof. Background technique [0002] Voriconazole (Voriconazole CAS NO.: 137234-62-9) was approved for marketing by the US FDA in May 2002. Its product name is "Vfend" and its Chinese name is "威芳". Its chemical structure is as follows: figure 1 . Voriconazole is a second-generation synthetic triazole antifungal drug, which has the advantages of broad antibacterial spectrum and strong antibacterial efficacy. It can treat invasive Aspergillus infection and severe invasive infection caused by fluconazole-resistant Candida krusei), for the treatment of serious infections caused by Actinomycetes and Fusarium species. This product is mainly used in the treatment of progressive, potentially life-threatening infections in immunocompromised patients. [0003] Fungal infections in immunocompromised patients have high morbid...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/02A61K31/506A61K47/44A61K47/42A61K47/40A61K47/36A61K47/34A61P31/10A61K47/10A61K47/26
Inventor 徐家军初虹王浩
Owner 苏州特瑞药业股份有限公司
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