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Optimising bioavailability of intra vitreally injectable steroids

A syringe, a technology for use in the field of optimization of steroid bioavailability for intravitreal injection

Inactive Publication Date: 2016-12-14
EYE CO PTY LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Despite its great potential, intravitreal triamcinolone acetonide c

Method used

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  • Optimising bioavailability of intra vitreally injectable steroids
  • Optimising bioavailability of intra vitreally injectable steroids
  • Optimising bioavailability of intra vitreally injectable steroids

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[0067] The invention relates to a pharmaceutical composition for treating eye diseases, including diabetic eye diseases and eye tumors, and a preparation method of the pharmaceutical composition.

[0068] The present invention is based, at least in part, on the unexpected discovery that compounds capable of modulating mineralocorticoid receptor and / or glucocorticoid receptor activity can be prepared so as to comprise one or more improved physicochemical properties. Such improved physicochemical properties may advantageously improve the desired course of treatment, eg, reduce the number of required intraocular injections or prolong the time between intraocular injections and / or increase the ease of injection.

[0069] In particular, the present invention relates to a process for the preparation of such pharmaceutical compositions and pharmaceutical compositions comprising one or both mineralocorticoids, wherein said composition comprises improved physicochemical properties, but ...

Embodiment

[0125] Water Solubility and Enhancement of Drug Solubility Using Cyclodextrins

[0126] We investigated the solubility enhancement of hydroxypropyl β-cyclodextrin (HP-βCD) on the solubility of MR compounds in saline with the aim of examining its potential use in suspension to increase the amount of drug in solution.

[0127] figure 1 It is shown that the addition of hydroxypropyl [beta]-cyclodextrin increases the solubility of MR compounds and TA in saline (data are presented as mean ± sd, n = 3). It is clearly shown that the solubility of FLU (fludrocortisone) and TA (triamcinolone acetonide) increases >30-fold compared to the solubility in saline and increases in both cases with cyclodextrin concentration increases linearly. The absolute solubility of TA is generally decreased. In aqueous suspensions, this will provide a higher proportion of drug in solution at the time of administration without the problem of reduced activity. The increase in concentration of DCS (desox...

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Abstract

The present invention relates to pharmaceutical compositions and a method for making a pharmaceutical composition comprising a therapeutically effective amount of one or more compounds capable of modulating an activity of a mineralocorticoid receptor and/or a glucocorticoid receptor, the method comprising formulating the composition to comprise one or more improved physicochemical properties. The receptor modulators are preferably chosen from triamcinolone acetonide, 11-desoxycortisone, fludrocortisone, deoxycorticosterone acetate, deoxycorticosterone, aldosterone, Cortisol, cortisone, prednisone, prednisolone, methylprednisolone, dexamethasone, betamethasone, triamcinolone, beclometasone fludrocortisone or a therapeutically active analogue, derivative, homolog, pharmaceutically acceptable salt or conjugate thereof. The improved physicochemical properties include solubility, porosity, electrokinetic potential (zeta potential), flocculation and particle size.

Description

technical field [0001] The invention described herein relates generally to pharmaceutical compositions and methods for the preparation of pharmaceutical compositions for the treatment of ocular diseases, including diabetic eye diseases and ocular tumors. In particular, the present invention relates to a method for the preparation of such pharmaceutical compositions and pharmaceutical compositions comprising one or more compounds capable of modulating mineralocorticoid receptor and / or glucocorticoid receptor activity , wherein the composition comprises improved physicochemical properties, although the scope of the invention is not necessarily limited thereto. Background technique [0002] Triamcinolone acetonide (TA) is a synthetic corticosteroid indicated for a variety of diabetic and neovascular retinopathy and inflammatory conditions unresponsive to topical corticosteroids. Triamcinolone acetonide has been used in monotherapy and combination therapy for a variety of fundu...

Claims

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Application Information

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IPC IPC(8): A61K31/573A61K31/58A61P27/02
CPCA61K9/0019A61K9/0048A61K9/10A61K31/573A61K31/58A61K47/38A61P27/02
Inventor P·L·彭福尔德
Owner EYE CO PTY LTD
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