Preservative free pharmaceutical compositions for ophthalmic administration
Inventors
Karavas, Evangelos • Koutris, Efthimios • SAMARA, VASILIKI • Koutri, Ioanna • Kalaskani, Anastasia • KAKOURIS, ANDREAS • GOTZAMANIS, GEORGE
Assignees
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-10702471-B2
Publication Date
2020-07-07
Expiration Date
Abstract
The present invention relates to a preservative-free, aqueous solution in the form of eye drops packed in a container that ensures stability of the product, ideal eye drop volume and reduced drop volume variability and provides efficient dispensing.
Core Innovation
The invention relates to a multi-use ophthalmic kit that includes a container with an integral bacterial protection system and a dispensing tip, and an ophthalmic composition contained within the container and configured to be dispensed as drops from an orifice of the dispensing tip into an eye of a patient. The dispensing tip orifice geometry is constrained by an inner diameter to outer diameter ratio from 1:1 to 1:6, with defined ranges for the inner diameter and the outer diameter at the point a drop exits and at which the ophthalmic composition moves internally from the container to the tip.
The ophthalmic composition is a preservative-free aqueous solution of dorzolamide or timolol with pharmaceutically acceptable excipients selected to provide physical properties. The solution is specified to have a viscosity of less than 200 cP at 25°C as measured by European pharmacopoeia requirements, a surface tension of less than 22 mN/m and more than 10 mN/m at 25°C, and an osmolality value of 250 to 300 mOsm/Kg, and the ophthalmic composition is free of viscosity increasing agents.
The container’s integral bacterial protection system uses mechanical tip-seal technology to prevent bacterial contamination, where the mechanical tip-seal technology comprises a spring-loaded valve located directly below the dispensing tip orifice. In one dependent claim, the integral bacterial protection system further uses active silver in the dispensing tip orifice as a bactericide.
Claims Coverage
The document contains two independent claims, each covering a multi-use ophthalmic kit that combines integral bacterial protection system with mechanical tip-seal technology, constrained dispensing-tip orifice geometry, and a preservative-free aqueous solution formulation with defined physicochemical property limits, along with controlled dispensing performance at a 45° tip orientation and defined per-drop variability.
Orifice geometry for controlled drop delivery in a multi-use ophthalmic kit
A dispensing tip orifice geometry with an inner diameter to an outer diameter ratio from 1:1 to 1:6, wherein the inner diameter of the dispensing tip orifice is more than 0.3 mm and less than 2 mm and the outer diameter of the dispensing tip orifice is more than 1 mm and less than 4 mm, with the outer diameter defined at a point a drop exits the dispensing tip and the inner diameter defined at the point the drop exits the dispensing tip and to which internally the ophthalmic composition moves from the container to the tip.
Preservative-free aqueous formulation with defined physicochemical limits
A preservative-free aqueous solution of dorzolamide or timolol as an active ingredient with pharmaceutically acceptable excipients selected to provide viscosity of less than 200 cP at 25°C as measured by European pharmacopoeia requirements, surface tension of less than 22 mN/m and more than 10 mN/m at 25°C, and osmolality value of 250 to 300 mOsm/Kg, wherein the ophthalmic composition is free of viscosity increasing agents.
Mechanical tip-seal bacterial protection with spring-loaded valve
An integral bacterial protection system that uses mechanical tip-seal technology to prevent bacterial contamination, where the mechanical tip-seal technology comprises a spring-loaded valve located directly below the dispensing tip orifice.
Drop volume and variability at 45° dispensing orientation
A container configured to dispense drops of the ophthalmic composition having a volume of between 22 µL and 31 µL when the dispensing tip is oriented at an angle of 45° relative to a horizontal axis, wherein variability between each drop dispensed is ±7 µL.
Active silver bactericide within the dispensing tip orifice (dependent feature)
The integral bacterial protection system uses active silver in the dispensing tip orifice as a bactericide.
European pharmacopoeia pH range for the ophthalmic composition (dependent feature)
The ophthalmic composition has a pH between 5.5 and 7.5 measured according to European pharmacopoeia requirements.
Tighter osmolality range for the ophthalmic composition (dependent feature)
The ophthalmic composition is configured such that its osmolality value is within 266 to 296 mOsm/Kg to meet European pharmacopoeia requirements.
Tighter drop-to-drop variability (dependent feature)
The ophthalmic kit is configured so that the variability between each dispensed drop is ±7 µL.
Across the two independent claims, the core coverage is a multi-use ophthalmic kit that integrates mechanical tip-seal bacterial protection with a spring-loaded valve under the dispensing tip orifice, uses constrained dispensing-tip orifice dimensions, and requires a preservative-free aqueous formulation of dorzolamide or timolol with specified viscosity, surface tension, and osmolality limits and no viscosity increasing agents, while also constraining dispensed drop volume and variability at a 45° dispensing orientation. Dependent claims further specify pH, a narrower osmolality range, additional active silver bactericidal functionality, and quantified dispensing variability.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
Interested in licensing this patent?