Ophthalmic compositions comprising calcineurin inhibitors or mTOR inhibitors

A technology of phosphatase inhibitors and compositions, which is applied in the field of ophthalmic compositions, can solve problems such as difficulty in target tissues, treatment limitations of posterior segment diseases, etc.

Active Publication Date: 2010-12-15
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

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 formulation

[0109] In order to prepare formulations with drug concentrations of 0.02, 0.2, 0.4, 0.5 and 1.0 wt%, the following scheme was adopted. The basic pharmaceutical preparations were prepared according to the ratio shown in Table 1. In the first scheme, for example, calculate the calcineurin inhibitor and vitamin ETPGS required for 50 mL, weigh, and then mix into 5 mL 95% ethanol until a clear solution is obtained. Evaporate the ethanol solution under vacuum to obtain a film-like near solid. Mix 25 mL of deionized water and octoxynol-40, add the solution to the film-like near-solid material, and ultrasonically treat it for about 20 minutes to ensure complete formation of mixed micelles. Store the prepared 2X formulation at room temperature. Or, in the second scheme, calculate the amount of the drug, vitamin E TPGS and octoxynol-40 required for 50mL, weigh it, and then mix it into 5mL of 95% ethanol and evaporate u...

Embodiment 2

[0112] Example 2. General preparation method of the formulation

[0113] The basic 2X formulation shown in Table 1 was prepared as described in the second protocol in Example 1. A basic preparation is prepared, wherein the calcineurin or mTOR inhibitor is vorosporin, cyclosporin A, sirolimus and tacrolimus. In a preparation method of a 50 mL formulation, a buffer mixture was prepared by dissolving a certain amount of components shown in Table 2 in 25 mL of deionized water to prepare a 2X buffer. The 2X buffer mixture is prepared with and without preservatives.

[0114] Table 2 Buffer mixture

[0115] Component

[0116] N.A.=Not joined

[0117] Disperse the required amount of polymer excipients shown in Table 3A in 2.5 mL of 2X buffer mixture and vortex gently to obtain a clear solution. Add an equal volume of the basic 2X formulation and mix to obtain a homogeneous solution. Adjust the pH of the solution to a target of about 6.8 with NaOH or HCl. NaCl was used to adjust the o...

Embodiment 3

[0137] Example 3. Determination of drug content

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

Invention field [0001] The embodiments disclosed herein relate to stable ophthalmic compositions comprising calcineurininhibitor or mTOR inhibitors, and more specifically, to methods of using the disclosed compositions to treat ocular diseases and / or disorders. Background technique [0002] In the United States, diseases and injuries on the front surface of the eye are the main reasons for seeking medical care from a physician. These diseases and injuries are among the most painful eye conditions and can lead to disability and blindness. The main clinical problems of the ocular surface include dry ocular surface, abnormal tear film and related complications; ocular surface trauma that leads to pathology and scarring; corneal dysfunction dystrophy and genetic diseases; inflammatory diseases; and External ocular infections. Ocular diseases and injuries can range from itching, runny eyes to impaired vision. Therefore, it is important to solve eye problems immediately, because cer...

Claims

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Application Information

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IPC IPC(8): A61K38/00
CPCA61K9/0048A61K38/13A61K9/1075A61K31/436A61K31/355A61K47/32A61K31/56A61P27/02A61P27/04A61P27/14A61P29/00A61P31/04A61P37/06A61P9/10
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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