Triamcinolone acetonaide acetate nano controlled-release formulation, preparation method thereof and artificial lens containing same

A technology of triamcinolone acetonide acetate and intraocular lens, which is applied in the field of medicine, can solve the problems of low drug metabolism and elimination bioavailability, reduce patient tolerance, and short-term drug effect, so as to simplify the way of administration and prevent the turbidity of the posterior capsule , the effect of inhibiting cell proliferation

Inactive Publication Date: 2012-01-25
严宏 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, long-term systemic use of glucocorticoids will cause complications and side effects. When applied topically, due to rapid drug metabolism, low bioavailability, and short-term drug effect, multiple doses are often required.
May cause other complications due to multiple dosing in ophthalmic application and reduce patient tolerance

Method used

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  • Triamcinolone acetonaide acetate nano controlled-release formulation, preparation method thereof and artificial lens containing same
  • Triamcinolone acetonaide acetate nano controlled-release formulation, preparation method thereof and artificial lens containing same

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preparation example Construction

[0025] The invention provides a kind of preparation method of triamcinolone acetonide acetate nano-sustained-release agent, the method comprises:

[0026] 1) Prepare triamcinolone acetonide acetate-chloroform solution with triamcinolone acetonide acetate concentration of 1%-3% and lactic acid-glycolic acid copolymer PLGA-dichloromethane solution with 2%-5% lactic acid-glycolic acid copolymer PLGA concentration respectively Chloromethane solution;

[0027] 2) Triamcinolone acetonide acetate-chloroform solution and lactic acid-glycolic acid copolymer PLGA-dichloromethane solution are mixed in a volume ratio of 1:9 as the oil phase;

[0028] 3) Prepare 0.5%-1.5% polyvinyl alcohol PVA solution and use it as the water phase;

[0029] 4) Add the oil phase obtained in step 2) dropwise to the water phase obtained in step 3) in a volume ratio of 1:10 and stir to prepare a suspension of triamcinolone acetonide acetate and lactic acid-glycolic acid copolymer PLGA nanoparticles liquid: ...

Embodiment 1

[0037] Triamcinolone acetonide acetate 0.85g + chloroform 3ml (triamcinolone acetonide acetate concentration is 2%), PLGA 1.06g + dichloromethane 27ml (PLGA concentration is 2.5%) are mixed with 1:9 as oil phase (A), with 1 The % polyvinyl alcohol (PVA) solution is the liquid phase (B), placed in a flask and stirred (1000rpm), and the oil phase A is added to the water phase B in a ratio of 1:10 (A:B) (dropping speed is less than 3ml / min) , and then continue to stir for 5 minutes after complete addition, stir and volatilize the emulsion (A+B) at room temperature for 6 hours, then heat and volatilize for 40 minutes in a vacuum to obtain a nanoparticle suspension, centrifuge (16000rpm, 10min) twice at room temperature, and take the above Triamcinolone acetonide acetate-PLGA nanoparticle powder was obtained by freeze-drying. Take 10 mg of triamcinolone acetonide acetate-PLGA nanoparticle, dissolve it in 0.1ml distilled water, dissolve it in absolute ethanol solution, and volatilize...

Embodiment 2

[0039] Mix 0.51 g of triamcinolone acetonide acetate + 1.2 ml of chloroform (the concentration of triamcinolone acetonide acetate is 3%), PLGA 0.41 g + 10.3 ml of dichloromethane (the concentration of PLGA is 5%) at 1:9 as the oil phase (A), Use 1% polyvinyl alcohol (PVA) solution as the liquid phase (B), place in a flask and stir (1000rpm), add the oil phase A to the water phase B in a ratio of 1:10 (A:B) (dropping speed is less than 3ml / min), and then continue to stir for 5 min after complete addition, stir and volatilize the emulsion (A+B) at room temperature for 6 h, and then volatilize by vacuum heating for 40 min to obtain a nanoparticle suspension, which is centrifuged (16000 rpm, 10 min) twice at room temperature, Get the supernatant and make triamcinolone acetonide acetate-PLGA nanoparticle powder through freeze-drying, take triamcinolone acetonide-PLGA nanoparticle 10mg, be dissolved in 0.1ml distilled water, be dissolved in absolute ethanol solution and volatilize a...

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Abstract

The invention relates to a triamcinolone acetonaide acetate nano controlled-release formulation, a preparation method thereof and an artificial lens containing the same for preventing inflammation and late complication after cataract operation, wherein the triamcinolone acetonaide acetate nano controlled-release formulation is prepared from the triamcinolone acetonaide acetate-chloroform solution with the triamcinolone acetonaide acetate concentration of 1%-3%, the lactic acid-glycolic acid copolymer (PLGA)-dichloromethane solution with the lactic acid-glycolic acid copolymer (PLGA) concentration of 2%-5%, and the polyvinyl alcohol (PVA) with the concentration of 0.5%-1.5%. The invention provides the preparation method of the triamcinolone acetonaide acetate nano controlled-release formulation which can effectively prevent posterior capsular opacity, has simple preparation process, and is convenient to use and the artificial lens containing the triamcinolone acetonaide acetate nano controlled-release formulation.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a triamcinolone acetonide acetate nano-sustained-release agent for preventing inflammation and sequelae after cataract surgery, a preparation method thereof, and an intraocular lens containing the sustained-release agent. Background technique [0002] Cataract is the world's first blinding eye disease. Extracapsular cataract extraction combined with posterior chamber intraocular lens implantation has become the main means of cataract recovery. A complete posterior capsule not only supports the posterior chamber IOL, but also reduces the incidence of postoperative retinal detachment, cystoid macular edema, and endophthalmitis. However, postoperative opacity of the posterior lens capsule and posterior capsule opacity caused by fibrosis are the primary complications of extracapsular cataract extraction, and become the primary factor for long-term vision loss. Posterior capsule opacificationT...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/58A61L27/54A61P29/00A61P37/08
Inventor 严宏孙礼华
Owner 严宏
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