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Ophthalmic compositions comprising calcineurin inhibitors or mTOR inhibitors

A technology of phosphatase inhibitor and composition, applied in the field of ophthalmic composition, can solve the problems of difficulty in target tissue, limitation of treatment of posterior segment diseases, etc.

Active Publication Date: 2014-11-26
AURINIA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently, the treatment of posterior segment diseases is significantly limited due to the difficulty in delivering effective doses of drugs to target tissues in the back of the eye

Method used

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  • Ophthalmic compositions comprising calcineurin inhibitors or mTOR inhibitors
  • Ophthalmic compositions comprising calcineurin inhibitors or mTOR inhibitors
  • Ophthalmic compositions comprising calcineurin inhibitors or mTOR inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0108] Example 1. General preparation method of basic preparation

[0109] To prepare formulations with drug concentrations of 0.02, 0.2, 0.4, 0.5 and 1.0 wt%, the following protocol was used. The basic pharmaceutical preparations were prepared according to the ratios shown in Table 1. In the first protocol, for example, the calcineurin inhibitor and vitamin ETPGS required for 50 mL are calculated, weighed, and then mixed into 5 mL of 95% ethanol until a clear solution is obtained. The ethanol solution was evaporated under vacuum to give a thin film near solid. Mix 25 mL of deionized water and octoxynol-40, add the solution to the film-like near-solid substance, and perform ultrasonic treatment for about 20 minutes to ensure complete formation of mixed micelles. The prepared 2X formulation was stored at room temperature. Alternatively, in the second protocol, calculate the amount of drug, vitamin E TPGS, and octoxynol-40 required for 50 mL, weigh, then mix into 5 mL of 95...

Embodiment 2

[0112] Example 2. General preparation method of preparation

[0113] The base 2X formulations shown in Table 1 were prepared as described in the second protocol in Example 1. A base formulation was prepared wherein the calcineurin or mTOR inhibitors were voclosporin, cyclosporin A, sirolimus and tacrolimus. In one preparation of the 50 mL formulation, a buffer mixture was prepared by dissolving the amounts of the components shown in Table 2 in 25 mL of deionized water to make a 2X buffer. The 2X buffer mixture was prepared with and without preservatives.

[0114] Table 2 Buffer mix

[0115] components

[0116] N.A. = not included

[0117] The required amount of polymeric excipient indicated in Table 3A was dispersed in 2.5 mL of 2X buffer mixture and vortexed gently to obtain a clear solution. An equal volume of base 2X formulation was added and mixed to obtain a homogeneous solution. The pH of the solution was adjusted to a target of approximately 6.8 with Na...

Embodiment 3

[0137] Embodiment 3. The mensuration of drug content

[0138] The drug content of each formulation was analyzed by HPLC. The composition of the HPLC mobile phase was acetonitrile / water / trifluoroacetic acid (75:25:0.1, v / v / v) at a flow rate of 1 mL / min, washed from a reversed-phase phenyl column (5 μm, 15×4.6 mm) off target compound. The absorbance of the drug was measured at 210 nm with a UV detector and compared to a standard curve of different known concentrations of the target drug. The observed peak elution of voclosporin was about 5.5 minutes.

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Abstract

The embodiments disclosed herein relate to ophthalmic compositions comprising calcineurin inhibitors or mTOR inhibitors, and more particularly to methods for treating an ocular disease and / or condition using the disclosed compositions. According to aspects illustrated herein, there is provided a pharmaceutical composition that includes a calcineurin inhibitor or an mTOR inhibitor; a first surfactant with an HLB index greater than about 10; and a second surfactant with an HLB index of greater than about 13, wherein an absolute difference between the HLB index of the first surfactant and the HLB index of the second surfactant is greater than about 3, and wherein the composition forms mixed micelles.

Description

field of invention [0001] Embodiments disclosed herein relate to stable ophthalmic compositions comprising calcineurin inhibitors or mTOR inhibitors, and more particularly, to methods of treating ocular diseases and / or disorders using the disclosed compositions. Background technique [0002] Diseases and injuries of the anterior surface of the eye are the leading cause of visits to physicians for ophthalmic medical care in the United States. These diseases and injuries are among the most painful eye conditions and can lead to disability and blindness. Major clinical problems of the ocular surface include ocular surface dryness, tear film abnormalities, and associated complications; ocular surface trauma leading to morbidity and scarring; corneal dysfunction dystrophy and genetic disorders; inflammatory disorders; and External ocular infections. Eye diseases and injuries can range from itching, runny eyes to impaired vision. Therefore, it is important to address eye proble...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K45/00A61K9/00A61K9/10A61K9/107A61K45/06
CPCA61K31/436A61K47/32A61K38/13A61K9/1075A61K31/355A61K31/56A61K9/0048A61P27/02A61P27/04A61P27/14A61P29/00A61P31/04A61P37/06A61P9/10
Inventor 阿希姆·K·米特拉普纳姆·R·瓦拉加莱蒂苏布拉马尼安·纳特桑
Owner AURINIA PHARMA
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