Low pH pilocarpine and brimonidine compound formulations and related methods

• Main Authors: Shah, Mandar V, Subramanian, Ilango, Subramanian, Veerappan, Trehan, Aman
• Format: Patent
• Language: English
• Published: 30.04.2024
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

The present invention provides relatively low pH, stable, pharmaceutically acceptable and ophthalmologically suitable compositions comprising effective amounts of pilocarpine and brimonidine compounds for treating an ocular condition, wherein compositions demonstrate a significant difference in the amount or rate of one or more pharmaceutical ingredient(s) absorbed or retained by ocular tissue or compared to reference composition(s) with similar compositional characteristics but having a significantly higher pH. In aspects compositions are characterizable by other elements, e.g., the inclusion of benzalkonium chloride, a limited amount of sodium chloride, or both. In embodiments, compositions are free of both a borate and a citrate buffer. Compositions provided by the invention surprisingly demonstrate pharmaceutically acceptable stability when stored under controlled room temperature conditions for an extended period of time. Further, the invention provides methods of manufacturing such compositions in liquid (solution) and gel forms, and methods of their use in treating conditions such as presbyopia.