Topical drug delivery systems for ophthalmic use

A water eye and eye drop technology, which is applied in the direction of drug delivery, drug combination, powder delivery, etc., can solve the problems of increasing tissue damage and infection

Inactive Publication Date: 2012-05-16
AURINIA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Not only is this regimen difficult for the patient to tolerate, but it also carries an increased risk of tissue damage and infection

Method used

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  • Topical drug delivery systems for ophthalmic use
  • Topical drug delivery systems for ophthalmic use
  • Topical drug delivery systems for ophthalmic use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0085] Preparation of mixed nanomicelle formulations

[0086] The mixed nanomicelle formulations of the present invention with drug concentrations of 0.02 wt%, 0.2 wt%, 0.4 wt%, 0.5 wt% and 1.0 wt% were prepared as follows. Base 2X drug formulations were prepared in the proportions shown in Table 1. In one protocol, for example, the required calcineurin inhibitor and vitamin E TPGS are calculated for about 50 mL, weighed, and then mixed in about 5 mL of 95% ethanol until a clear solution is obtained. The ethanol solution was evaporated under vacuum to obtain a thin film near solid. About 25 mL of deionized water and octoxynol-40 were mixed, and the solution was added to the film-like near-solid substance, and ultrasonicated for about 20 minutes to ensure complete formation of mixed micelles. Store the prepared 2X drug formulation at room temperature. Alternatively, the amount of drug, vitamin E TPGS, and octoxynol-40 required for 50 mL was calculated, weighed, then mixed in...

Embodiment 2

[0108] After surface application of 0.2wt% / volume voclosporin nanomicelle formulation (LX214) 14 Ocular distribution and pharmacokinetics of C-voclosporin

[0109] NZW rabbits (30 females / 8 males) were used in single dose (SD) and 7-day repeat dose (RD) studies (Table 5A). DB rabbits (16 females) were used in the single dose study (Table 5B). Animals received no treatment (control) or single dose or daily ocular topical application for 7 days (35 μL of 0.2% 14 C-LX214 solution). At indicated time points, blood and ocular tissue radioactivity levels were assessed by burning followed by liquid scintillation counting. Blood voclosporin concentrations were also measured using a validated liquid chromatography method coupled to air pressure ionization mass spectrometry (LC-API / MS / MS).

[0110] Table 5A

[0111]

[0112]

[0113] a Topical formulation containing 0.2% voclosporin. A target dose of ~3 μCi / 35 μL and 70 ng of voclosporin

[0114] b was used as the pre-admin...

Embodiment 3

[0137] Preparation of Dexamethasone Mixed Nanomicelle Preparation

[0138] The aqueous solubility of corticosteroids such as dexamethasone is about 0.159 mg / mL. In this example, the solubility of the drug dexamethasone was increased about 6.2 times (1 mg / mL). In one embodiment, to prepare a composition having a drug (dexamethasone) concentration of 0.1 wt%, the following protocol was used. Pharmaceutical base formulations were prepared according to the ratios shown in Table 9. In this protocol, the dexamethasone, vitamin E TPGS, and octoxynol-40 required for a final 50 mL formulation were calculated, weighed, and then mixed in approximately 6 mL of 95% ethanol until a clear solution was obtained. The ethanol solution was evaporated under vacuum to give a thin film near solid. 25 mL of deionized water was added to the film-like near-solid substance, and ultrasonic treatment was performed for about 20 minutes to ensure complete formation of mixed micelles. The prepared 2X fo...

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Abstract

Topical drug delivery systems for ophthalmic use including mixed nanomicellar formulations of water-insoluble drugs and methods of treating diseases affecting the posterior ocular segments are disclosed. In an embodiment, an aqueous ophthalmic solution includes nanomicelles in a physiologically acceptable buffer, having a pH of 5.0 to 8.0, wherein a corticosteroid at a concentration from about 0.01 % w/v to about 1.00 % w/v is solubilized through entrapment in a mixed micellar hydrophobic core with a corona composed of hydrophilic chains extending from the hydrophobic core, wherein the nanomicelles comprise vitamin E TPGS at a concentration ranging from about 3.0 % w/v to about 5.0 % w/v stabilized with octoxynol-40 at a concentration ranging from about 1.0 % w/v to about 3.0 % w/v.

Description

field of invention [0001] Embodiments disclosed herein relate to topical drug delivery systems, more particularly to mixed nanomicelle formulations of corticosteroids, and methods of treating diseases affecting the posterior segment of the eye. Background technique [0002] Ophthalmic conditions include conditions in the front of the eye, such as glaucoma, where medications can be delivered using eye drops and other conventional ophthalmic formulations, and retinal diseases that affect the vitreous or the back of the eye, such as age-related macular degeneration (AMD) and diabetic macular edema (DME), which is the leading cause of vision loss in Western countries. [0003] Disease and injury of the front surface are the leading reasons for visits to physicians for ophthalmic medical care in the United States. These diseases and injuries are among the most painful ocular conditions and can lead to disability and blindness. Major clinical problems of the ocular surface inclu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14
CPCA61K9/107A61K31/436A61K47/10A61K47/22A61K9/0048A61K31/573A61K31/14A61P27/02A61K9/1075
Inventor 阿希姆·K·米特拉普纳姆·R·韦拉加莱蒂乌尔里希·M·格罗
Owner AURINIA PHARMA
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