Pharmaceutical composition sustained-release implant containing caspofungin acetate and preparation thereof

A technology of caspofungin acetate and slow-release implants, which can be applied to medical preparations containing active ingredients, drug delivery, and pharmaceutical formulations, and can solve the problems of frequent and inconvenient administration

Inactive Publication Date: 2015-02-04
SHENZHEN JYMED TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The currently commercially available caspofungin acetate is a freeze-dried powder for injection. The administration metho

Method used

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  • Pharmaceutical composition sustained-release implant containing caspofungin acetate and preparation thereof
  • Pharmaceutical composition sustained-release implant containing caspofungin acetate and preparation thereof
  • Pharmaceutical composition sustained-release implant containing caspofungin acetate and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Weigh 120 g of caspofungin acetate and 30 g of amphotericin B, dissolve and disperse them in distilled water to obtain an inner water phase; weigh 300 g of PLGA and dissolve them in dichloromethane to obtain an oil phase. Preparation concentration is 200ml of polyvinyl alcohol solution of 0.5%. First move the main drug solution into the dichloromethane solution that is dissolved with PLGA, put it on the emulsification disperser at room temperature and emulsify it for 30 seconds with a rotating speed of 30000rpm, then transfer the obtained W / O emulsion to 200ml concentration of 0.5%. In the vinyl alcohol solution, put it on an emulsifying disperser at a speed of 5000rpm, and mix it evenly for 1 minute to obtain a W / O / W type double emulsion. , centrifuged, collected the microspheres obtained, washed several times with distilled water, then collected by centrifugation, added 10g of mannitol, and freeze-dried to obtain drug-containing sustained-release microspheres, the enc...

Embodiment 2

[0025] Weigh 80 g of caspofungin acetate and 20 g of fluconazole, dissolve and disperse them in distilled water to obtain an inner water phase; weigh 350 g of PLA and dissolve them in dichloromethane to obtain an oil phase. Preparation concentration is 200ml of polyvinyl alcohol solution of 0.5%. First move the main drug solution into the dichloromethane solution that is dissolved with PLA, put it on the emulsification disperser at room temperature and emulsify it with a rotating speed of 30000rpm for 30 seconds, then transfer the resulting W / O emulsion to 200ml concentration of 0.5% poly In the vinyl alcohol solution, put it on an emulsifying disperser at a speed of 5000rpm, and mix it evenly for 1 minute to obtain a W / O / W type double emulsion. , centrifuge, collect the gained microspheres, wash with distilled water several times, then centrifuge again, add 20g sorbitol, freeze-dry, obtain the drug-containing sustained-release microspheres, its encapsulation efficiency is 91....

Embodiment 3

[0030]Weigh 35g of caspofungin acetate, 7.5g of amphotericin B, and 7.5g of itraconazole, dissolve and disperse them in distilled water to obtain an inner water phase; weigh 400g of PGA and dissolve them in dichloromethane to obtain an oil phase. Preparation concentration is 200ml of polyvinyl alcohol solution of 0.5%. First move the main drug solution into the dichloromethane solution that is dissolved with PGA, put it on the emulsification disperser at room temperature and emulsify it for 30 seconds with a rotating speed of 30000rpm, then transfer the obtained W / O type emulsion to 200ml concentration of 0.5% poly In the vinyl alcohol solution, put it on an emulsifying disperser at a speed of 5000rpm, and homogenize it for 1 minute to obtain a W / O / W type double emulsion. phase, centrifuge, collect the obtained microspheres, wash with distilled water for several times, then collect by centrifugation, add 30g mannitol, and freeze-dry to obtain drug-containing sustained-release ...

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Abstract

The invention relates to a pharmaceutical composition sustained-release implant containing caspofungin acetate and a preparation method thereof. The pharmaceutical composition sustained-release implant is characterized in that the active ingredient of the medicine is echinocandins antifungal drug caspofungin acetate. In addition, the sustained-release implant also comprises polyene and triazole antifungal drugs with a synergistic effect with the caspofungin. The active ingredient of the medicine is coated in a high polymer material carrier with biodegradability and biocompatibility according to a certain ratio. The active ingredient is prepared into sustained-release microspheres to be directly pressed into tablets of a certain shape, and the tablets are used for implant, so that a long-acting sustained-release effect is achieved. The sustained-release period of the sustained-release implant lasts for several days or several months, the drug administration frequency is obviously reduced, the bioavailability is improved, the toxic and side effects are reduced, and thus the pharmaceutical composition sustained-release implant containing caspofungin acetate is beneficial for clinical treatment.

Description

Technical field: [0001] The invention relates to an antifungal slow-release implant, in particular to a pharmaceutical composition drug slow-release implant containing caspofungin acetate and a preparation method thereof. Background technique: [0002] With the increasing use of a large number of antibacterial drugs, antineoplastic drugs, corticosteroids and immunosuppressants, and the increasing incidence of organ transplantation, interventional surgery and acquired immunodeficiency syndrome, the incidence of deep fungal infection is also increasing year by year. Therefore, it is particularly important to develop new antifungal drugs and their preparations in the process of resisting fungal infections. So far, three main classes of drugs have been used for systemic antifungal therapy: polyenes, such as amphotericin B; triazoles, such as voriconazole, fluconazole, itraconazole, posaconazole; Steroids: These drugs play a very important role in the treatment of fungal infecti...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K45/06A61K38/12A61K47/34A61P31/10
Inventor 姚志勇李新宇舒遂智黄盛治曹演威黄秋霞
Owner SHENZHEN JYMED TECH
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