Sustained release formulations for the treatment of intraocular pressure or glaucoma
Inventors
Wong, Vernon G. • Hu, Mae W. • Huang, Glenn T.
Assignees
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Publication Number
US-9636347-B2
Publication Date
2017-05-02
Expiration Date
Abstract
The present embodiments provide for methods of treating elevated intraocular pressure or glaucoma using a sustained release medicament consisting of prostaglandin in benzyl benzoate that is injected intraocularly no more frequently than once every two months.
Core Innovation
The disclosure provides a sustained-release liquid medicament for treating elevated intraocular pressure or glaucoma in a subject. The medicament consists of prostaglandin in benzyl benzoate, including prostaglandin such as latanoprost, and is configured to provide sustained release after ocular injection.
A monolithic, substantially clear liquid reservoir is formed after intravitreal injection into the vitreous or injection into the anterior chamber. The sustained release is described as lasting at least about 2 months and being kinetically detectable for up to more than about 6 months after a single injection.
The sustained release duration is correlated with prostaglandin concentration within benzyl benzoate and unit dose volume. The disclosure also describes dosing regimens that re-administer the medicament no more frequently than about once every two months, with schedules extending to longer intervals.
The disclosure includes supporting in vivo evidence in rabbits by detecting latanoprost acid in aqueous humour after single injections of latanoprost/benzyl benzoate formulations. The reduction of intraocular pressure relative to control is reported to persist for extended periods, and the document reports that toxic effects were not observed in the rabbit studies mentioned.
Claims Coverage
Two independent claims are present. Both claims are directed to sustained-release liquid medicaments/unit doses comprising prostaglandin in benzyl benzoate, with ocular administration by injection and constrained dosing intervals.
Liquid medicament comprising prostaglandin in benzyl benzoate with injection interval of no less than about two months
A liquid medicament for treating elevated intraocular pressure or glaucoma, the medicament consisting of prostaglandin in benzyl benzoate with the prostaglandin present at about 0.1% (w/w) to about 5% (w/w), inclusive, wherein about 5 μL to about 60 μL, inclusive, is injected into the anterior chamber or vitreous once per interval of no less than about two months.
Sustained release unit dose of latanoprost in benzyl benzoate administered by intravitreal injection with optional re-administration no more frequently than about every two months
A sustained release unit dose for treating elevated intraocular pressure or glaucoma, wherein the unit dose is a liquid consisting of latanoprost at a concentration of about 0.25% (w/w) to about 5% (w/w), inclusive, in benzyl benzoate, wherein the unit dose is about 5 μL to about 60 μL, inclusive, is administered by intravitreal injection, and optionally thereafter is re-administered no more frequently than once about every two months.
Overall claim coverage centers on sustained-release ocular liquid formulations of prostaglandin/benzyl benzoate and on injection-based dosing regimens that limit re-administration frequency.
Stated Advantages
Sustained release lasting at least about 2 months and kinetically detectable for up to more than about 6 months after a single injection.
Reduction of intraocular pressure relative to control persisting for extended periods after injection, as reported in the disclosed rabbit evidence.
Reported absence of toxic effects in the rabbit studies mentioned.
Documented Applications
Treatment of elevated intraocular pressure or glaucoma in a subject via injection of a sustained-release prostaglandin/benzyl benzoate liquid into the anterior chamber or vitreous, including intravitreal injection.
Use in rabbit in vivo studies to demonstrate sustained release by detection of latanoprost acid in aqueous humour and persistence of intraocular pressure reduction.
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