Formulations for treating eye disorders

A technology for mycophenolate sodium and ocular diseases, applied in the field of ocular solutions, can solve the problems of low bioavailability and intolerance, etc.

Inactive Publication Date: 2011-06-15
ASPREVA INT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, locally administered cyclosporine A (CsA) was shown to be poorly tolerated and has low bioavailability (Lallemand et al., 2003, Eur J Pharm Biopharm. 56( 3): 307-18)

Method used

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  • Formulations for treating eye disorders
  • Formulations for treating eye disorders
  • Formulations for treating eye disorders

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0065] Example 1: Preparation of NaMPA ophthalmic solution.

[0066] Ophthalmic Solution 1.4% MPA Ophthalmic Solution, Sodium Salt

[0067]

[0068] Preparation procedure. About 80% of the final volume of pure water was heated to about 80°C. Add glycerol and mycophenolic acid to water and mix to disperse. The heat was turned off and 10% NaOH was immediately added to the batch and mixed until the MPA was dissolved. Alternatively, pure water (approximately 80% final volume), 10% NaOH and glycerol were mixed and heated to approximately 80°C. The heat was turned off, then mycophenolic acid was added and mixed to dissolve. Pure water was added to about 95% of the batch volume, and the composition was mixed while cooling to room temperature. The pH was measured with a calibrated pH meter and adjusted with NaOH / HCl if necessary. Pure water was added to 100% of the batch volume and osmolarity was measured. Appropriate filters are used for clarification and sterilization.

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example 2

[0076] Example 2: Ophthalmic Formulations Containing EDTA

[0077] The table below provides various NaMPA ophthalmic formulations with additive EDTA and various levels of NaCl.

[0078] Table 1: Ophthalmic Solutions Containing EDTA

[0079]

[0080]

[0081] The table above shows the ophthalmic NaMPA formulations used in the animal studies including the efficacy studies described below. The first three ingredients (NaMPA, NaCl, and disodium edetate (EDTA)) are shown as % final concentration in weight per volume (w / v). The formulations were adjusted to the desired pH using NaOH or HCl as indicated, and to a final volume of 100 ml with purified water. Other volumes of ophthalmic NaMPA formulations can be prepared using the formulation outlined in Table 1. Under "NaMPA", the final concentration of MPA is shown in parentheses. For example, Formulation 3 refers to the 1% NaMPA formulation. The 1% NaMPA formulation contains 1% final concentration of MPA (active ingredient...

example 3

[0083] Example 3: Study of Tolerability and Ocular Tissue Penetration of MPA-Containing Formulations (Compared to Cyclosporine).

[0084] The purpose of this study was to evaluate the ocular tolerance and ocular tissue penetration of eight MPA formulations following one-day topical instillation eight times a day in the eyes of New Zealand White rabbits. Eight test article formulations, a negative control article (2.4% glycerol), and a positive control article are provided in Table 2 Manufactured by Allergan Inc., Irvine, CA, US (Allergan). The study was conducted in two phases, using four test articles and two control articles in each phase. Naive animals were used in both phases. Animals were placed in treatment groups as indicated in Tables 2, 3 and 4.

[0085] Table 2: Treatment Group Assignment: Phase 1

[0086]

[0087]

[0088] MPA = mycophenolic acid.

[0089] Table 3: Treatment Group Assignment: Phase 2

[0090]

[0091] MPA = mycophenolic acid.

[009...

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Abstract

Ocular delivery of drugs to the eyes is an ongoing challenge due to the unique anatomical and physiological properties of the eye. A solution of the immunosuppressant and anti-inflammatory compound mycophenolic acid with a pH from 6.0 to 8.5 has been demonstrated to exhibit improved bioavailability when topically applied to the eye. Specifically, topical application to the eye of such a solution is effective in penetrating anterior and posterior eye structures. Said solution is effective in treating a variety of inflammatory disorders, including uveitis, allergic conjunctivits, and keratoconjunctivitis sicca.

Description

[0001] Cross References to Related Applications [0002] This application claims the benefit of Application No. 61 / 079,413, filed July 9, 2008, under 35 U.S.C. § 119(e), the contents of which are incorporated herein by reference. Background technique [0003] Many inflammatory diseases of the eye are recurrent or occur as secondary complications of various systemic diseases such as autoimmune diseases or infections. Standard treatment, such as the use of topically applied steroids, is aimed at controlling the inflammatory symptoms of the eye. However, a complication of steroid therapy is that a significant percentage of treated individuals suffer from increased intraocular pressure, which can exacerbate ocular conditions such as glaucoma and cataracts. In some instances, ocular conditions are refractory to the action of topically applied steroids. [0004] In some instances, systemic therapy with anti-inflammatory steroids or other immunosuppressants will be used to treat o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61P27/02A61P27/14
CPCA61K9/0048A61K31/365A61P27/02A61P27/14
Inventor 爱德华·庄克莱夫·伯奇李·米泽恩
Owner ASPREVA INT
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