Echinocandin antifungal pharmaceutical composition sustained release microsphere preparation and preparation method thereof

A technology for sustained-release microsphere preparations and antifungal drugs, which can be used in antifungal agents, pharmaceutical formulations, medical preparations containing active ingredients, etc., and can solve problems such as potential changes and visual disturbances.

Active Publication Date: 2014-07-30
南京星银药业集团有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The use of azole drugs is also limited due to the side effects on the kidney and retina, and the interaction with other drugs. For example, voriconazole can cause 100% of users to have retinal potential changes, and 33% may have temporary visual impairment; For example, fluconazole and voriconazole have a 50% chance of cross-resistance

Method used

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  • Echinocandin antifungal pharmaceutical composition sustained release microsphere preparation and preparation method thereof
  • Echinocandin antifungal pharmaceutical composition sustained release microsphere preparation and preparation method thereof
  • Echinocandin antifungal pharmaceutical composition sustained release microsphere preparation and preparation method thereof

Examples

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Effect test

Embodiment 1

[0018] Weigh 10g caspofungin acetate, 10g amphotericin B, 20g gelatin, 20g glycerin, 20ml 0.5% polyvinyl alcohol solution, 20ml absolute ethanol and dissolve in distilled water to obtain the internal aqueous phase; weigh 800g polylactide Dissolve in dichloromethane to get oily phase. First move the water phase into the oil phase, place it on an emulsifying disperser at 30000 rpm at room temperature, and homogenize for 30 seconds, then transfer the resulting W / O emulsion to an aqueous solution of polyvinyl alcohol and place it on the emulsifying disperser at 5000 rpm. Rotate and homogenize for 1 minute to obtain W / O / W double emulsion. Stir at low speed at 500 rpm for 2 hours at room temperature, remove organic solvent, ultracentrifuge, collect the resulting microspheres, wash with distilled water several times, and then centrifuge to collect , Adding 90g sorbitol, freeze-drying, and distributing into a echinocandin antifungal sustained-release microsphere preparation with an act...

Embodiment 2

[0027] Weigh 60g caspofungin acetate, 20g fluconazole, 30g gelatin, 30g glycerin, 20ml 0.5% polyvinyl alcohol solution, 30ml propylene glycol and dissolve in distilled water to obtain the internal water phase; weigh 720g polyglycolide to dissolve In dichloromethane, the oily phase is obtained. First move the water phase into the oil phase, place it on an emulsification disperser at a rotation speed of 30,000 rpm, and homogenize for 30 seconds, then transfer the obtained W / O type emulsion to 50 ml of purified water, and place it on the emulsification disperser at a rotation speed of 5000 rpm. Homogenize the milk for 1 minute to obtain a W / O / W double emulsion, place it on a mechanical stirrer, stir at 500 rpm at low speed for 2 hours at room temperature, centrifuge, collect the resulting microspheres, wash with distilled water several times, and then centrifuge to collect , Adding 70g of mannitol, freeze-drying, and distributing it into a echinocandin antifungal sustained-release...

Embodiment 3

[0036] Weigh 110g caspofungin acetate, 30g itraconazole, 40g gelatin, 40g glycerin, 20ml 0.5% polyvinyl alcohol solution, 40ml absolute ethanol and dissolve in distilled water to obtain the internal aqueous phase; weigh 700g polylactide -Glycolide is dissolved in dichloromethane to obtain an oil phase. Prepare 50ml of polyvinyl alcohol solution with a concentration of 5%. First move the water phase into the oil phase, place it on an emulsifying disperser at room temperature at 30000 rpm and homogenize for 30 seconds, then transfer the resulting W / O emulsion to 50 ml of a 5% polyvinyl alcohol solution and place On the emulsifying and dispersing machine at 5000 rpm, the milk is homogenized for 1 minute to obtain W / O / W double emulsion, placed on a mechanical stirrer, stirred at 500 rpm at low speed for 2 hours at room temperature, centrifuged, collected the resulting microspheres, and used distilled water Wash it several times, then collect by centrifugation, add 40g of mannitol,...

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Abstract

The invention belongs to the field of pharmaceutical preparations and relates to an echinocandin antifungal pharmaceutical composition sustained release microsphere preparation and a preparation method thereof. The pharmaceutical active ingredients of the echinocandin antifungal pharmaceutical composition comprises caspofungin acetate and antifungal agents respectively being polyenes and triazoles; and the sustained release microsphere comprises the following materials in percentage by total weight of microsphere: 0.1%-30% (w/w) of active ingredients, 60%-99.9% daltonian biodegradable and biocompatible high polymer material with molecular weights of 5,000-200,000 and 0%-10% of pharmaceutically acceptable other auxiliary materials. The average grain diameter of the sustained release microsphere is 5-20 microns, and the encapsulation efficiency is more than 85%. The sustained release period of the sustained release microsphere is up to 50 days, the drug use frequency is significantly reduced, the bioavailability is improved, and the toxic and side effects of the drug are reduced, thus being beneficial to clinical treatment. The product is good in reproducibility of production technology and good in feasibility.

Description

Technical field [0001] The invention relates to the technical field of sustained-release microsphere preparations, in particular to a echinocandin antifungal drug sustained-release microsphere preparation and a preparation method. Background technique [0002] With the widespread use of a large number of antibacterial drugs and antitumor drugs, the development of organ transplantation and interventional technology, the increase in the use of corticosteroids and immunosuppressive agents, and the incidence of acquired immunodeficiency syndrome has increased year by year, fungal infections have gradually increased, and antifungal The clinical use of drugs has also increased significantly. Therefore, the development of new antifungal drugs is the first choice for the treatment of fungal infections. So far, there are mainly three drugs that can be used for systemic antifungal treatment: polyenes, such as amphotericin B and its liposomes; triazoles, Such as voriconazole, fluconazole, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/12A61K9/16A61P31/10A61K31/7048A61K31/4196A61K31/496A61K31/506
Inventor 付玉清马洪季张建松徐洲文
Owner 南京星银药业集团有限公司
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