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Ophthalmic compositions of rifamycins and uses thereof

a technology of ophthalmic compositions and rifamycin, which is applied in the field of pharmaceutically acceptable compositions, can solve the problems of loss of visual acuity, loss of vision in the center of the visual field (the macula), and difficulty or inability to read or recognize faces

Inactive Publication Date: 2017-07-20
SERIZAWA HIROAKI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This patent describes the use of ophthalmic pharmaceutical compositions containing rifamycin compounds, such as rifampicin, to treat ocular diseases and conditions. The invention relates to methods of treating ocular neovascularization, age-related macular degeneration, and reducing retina thickness. The patent also provides formulations for eye drops and injectables, as well as pH and physiological salt concentration ranges. The technical effects of the invention include improved treatment outcomes and reduced side effects.

Problems solved by technology

Loss of visual acuity is a common problem associated with aging and with various diseases of the eye such as macular degeneration, ocular histoplasmosis syndrome, myopia, diabetic retinopathy and inflammatory diseases all of which result from neovascularization in the cornea, retina or choroid.
Age-Related Macular Degeneration (AMD) is a common eye condition which usually affects older adults and results in a loss of vision in the center of the visual field (the macula) due to retinal damage.
Although some peripheral vision remains, it is difficult or impossible to read or recognize faces.
AMD is a leading cause of blindness among people older than 65 years and is caused by abnormal development of blood vessels behind retina.
However, intravitreal injection is a process that requires great precision, because it is performed with the help of a needle under local anesthesia.

Method used

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  • Ophthalmic compositions of rifamycins and uses thereof
  • Ophthalmic compositions of rifamycins and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

example 1

Eye Drop Formulation of Rifamycin Compounds

[0084]The active ingredient, i.e. rifamipicin, rifabutin, rifapentine, rifalazil or rifaximin is dissolved in saline or water and a surfactant such as polysorbate 80, tween 80 or tween 20 is added and mixed. Further, various additives such as glycerin, xanthan gum, hydroxypropylmethylcellulose (HPMC), cyclodextrin derivatives such as hydroxypropyl-β-cyclodextrin, isotonic agents such as such as sodium chloride, potassium chloride or sodium bisulfate, preservative such as disodium EDTA or methylparaben, anti-oxidant such as ascorbic acid are optionally added and mixed to form a clear solution. The solution is optionally filtered to remove particulate matter and the pH is adjusted by adding an acid such as hydrochloric acid or a base such as sodium chloride to obtain the desired pH.

example 2

[0085]16 different formulations were prepared for topical eye drop application of rifampicin, as disclosed in Tables 1-3. The formulations of Example 1A and Example 6A were used in the following studies.

[0086]The following eye drop formulations were prepared at room temperature (Tables 1 and 2), and Rifampicin was added to the eye drop formulations to the final concentrations listed:

TABLE 1ExampleExampleExampleExampleExample1A2A3A4A5ApH of input bufferpH8.7pH8.7(50 mM Boric Acid-Borax)pH of input bufferpH8.3pH8.3pH8.3(100 mM Boric Acid-NaOH)Final concentrations10mM10mM20mM25mM25mMof input buffersFinal pH detected afterpH7.64pH7.37pH8.01pH8.30addition of RifampicinNaCl*150mM150mM0.9%0.9%0.9%Tween 80*0.5%0.5%0.5%0.5%0.5%EDTA*0.1%0.1%0.1%0.1%0.1%Benzalkonium chloride*0.01% 0.01% 0.01% 0.01% 0.01% Rifampicin*0.25% 0.5%0.5% 1%0.5%*Final concentrations

TABLE 2ExampleExampleExampleExampleExample6A7A8A9A10ApH of input bufferpH8.7pH8.7pH8.5pH8.5pH8.3(50 mM Boric Acid-Borax)Final concentration...

example 3

[0090]Rifampicin was delivered to retina by topical eye drop application. 0.25% rifampicin eye drop formulation was used for the studies. It showed good delivery efficiency, and retina tissue got micro gram concentrations of rifampicin per g of tissue by the eye drop application.

[0091]Four male Sprague-Dawley rats (250-300 g) were used to determine retina exposure levels of rifampicin following applications of eye drops. Two rats received 3 drops of an eye drop formulation (0.25% Rifampicin) which is presented as Example lA listed in Table 1 in each eye under isoflurane sedation. The remaining two rats received the same applications, but 10 drops, to each eye under isoflurane sedation. A single drop contained 5 micro L of the formulation, and applications of each drop had 30 min interval. After the eye drop application, retinas were extracted under a dissection microscope. In addition, “Non-treatment” negative control was taken, and retina was extracted from two rats without any tre...

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Abstract

Provided herein are ophthalmic pharmaceutical formulations comprising a rifamycin compound. Also provided herein are methods of treating ocular diseases or disorders by administering such ophthalmic formulations. This invention relates generally to pharmaceutical compositions or formulations suitable for administration to an eye. In some aspects, this invention relates to ophthalmic pharmaceutical compositions or formulations comprising one or more rifamycin compounds selected from the group consisting of rifampicin, rifabutin, rifapentine. In one aspect, the invention relates to methods of treating an ocular disease, disorder or condition comprising administering to a patient in need thereof an ophthalmic composition comprising an effective amount of a rifamycin compound selected from the group consisting of rifampicin, rifabutin, rifapentine, and rifaximin.

Description

REFERENCE TO RELATED APPLICATIONS[0001]This application claims priority to U.S. Provisional Application Ser. Nos. 62 / 027,189 filed Jul. 21, 2014, 62 / 136,222 filed Mar. 20, 2015, and 62 / 174,884 filed Jun. 12, 2015, the content of each of which is incorporated herein in its entirety by reference.FIELD OF THE INVENTION[0002]Provided herein are pharmaceutically acceptable compositions or compositions suitable for topical administration to an eye, the composition comprising a therapeutically-effective amount of an antimicrobial agent, which, in a preferred embodiment comprises a rifamycin derivative, methods for their preparation, and methods for their use in treating various disorders.BACKGROUND[0003]Loss of visual acuity is a common problem associated with aging and with various diseases of the eye such as macular degeneration, ocular histoplasmosis syndrome, myopia, diabetic retinopathy and inflammatory diseases all of which result from neovascularization in the cornea, retina or chor...

Claims

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Application Information

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IPC IPC(8): A61K31/5383A61K9/00A61K31/435A61K9/08A61K47/10A61K47/02A61K47/18A61K47/14A61K31/496A61K47/26
CPCA61K31/5383A61K31/496A61K9/0048A61K31/435A61K9/08A61K47/10A61K47/02A61K47/183A61K47/14A61K47/26A61K9/0019A61P25/00A61P27/02
Inventor SERIZAWA, HIROAKI
Owner SERIZAWA HIROAKI
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