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Publication Number
US-11642308-B2
Publication Date
2023-05-09
Expiration Date
Abstract
Disclosed herein is a ready-to-use liquid, injectable formulation comprising lidocaine and epinephrine. Also disclosed herein is a process for preparing a ready-to-use liquid formulation comprising lidocaine and epinephrine, as well as methods for using the ready-to-use liquid formulation.
Core Innovation
The invention relates to a ready-to-use liquid formulation comprising lidocaine hydrochloride and epinephrine, together with sodium chloride, sodium metabisulfite, EDTA sodium, citrate buffer, sterile water for injection, and a pH adjuster to obtain a pH that ranges from about 6.3 to about 6.5 or about 6.3 to about 6.4. Optional inclusion of N-acetyl-L-cysteine is also described, and the formulation is defined by specified concentrations of lidocaine hydrochloride and epinephrine.
A key aspect is epinephrine content retention after storage in a light protected environment for about 60 days to about 90 days at about 5°C. The document ties the retained epinephrine content to the formulation composition, including citrate buffer, EDTA sodium, sodium metabisulfite, and optionally N-acetyl-L-cysteine, along with the pH range of about 6.3 to about 6.5 or about 6.3 to about 6.4.
The description further characterizes formulation and packaging constraints for maintaining performance, including light transmission limits and evaluation of buffer systems, stabilizers/chelators, and antioxidants with respect to epinephrine degradation under refrigerated, light-protected storage. Preformulation studies and example batch formulations evaluate epinephrine potency and stability loss, and the examples report maintained potency over storage together with sterility and particulate matter checks.
Claims Coverage
The independent claims are directed to ready-to-use liquid formulations with specified concentrations of lidocaine hydrochloride and epinephrine, a defined excipient package, a pH range, and retained epinephrine content after light-protected refrigerated storage. Across the provided content, there are two pH variants and the same storage-related epinephrine retention feature.
Ready-to-use lidocaine hydrochloride and epinephrine formulation with citrate-buffered pH 6.3 to 6.5
A ready-to-use liquid formulation comprising lidocaine hydrochloride, epinephrine, sodium chloride, sodium metabisulfite, EDTA sodium, optionally N-acetyl-L-cysteine, citrate buffer, sterile water for injection, and a pH adjuster to obtain a pH that ranges from about 6.3 to about 6.5.
Epinephrine content retained after light-protected storage at 5°C
Epinephrine content ranges from about 9 mcg/mL to about 9.7 mcg/mL after storage in a light protected environment for about 60 days to about 90 days at a temperature of about 5°C.
Ready-to-use lidocaine hydrochloride and epinephrine formulation with citrate-buffered pH 6.3 to 6.4
A ready-to-use liquid formulation consisting of lidocaine hydrochloride, epinephrine, sodium chloride, sodium metabisulfite, EDTA sodium, optionally N-acetyl-L-cysteine, citrate buffer, sterile water for injection, and a pH adjuster to obtain a pH that ranges from about 6.3 to about 6.4.
Defined concentrations of lidocaine hydrochloride, epinephrine, and excipients
Lidocaine hydrochloride is present in an amount of about 5 mg/mL or about 10 mg/mL, epinephrine is present in an amount of about 10 mcg/mL to about 10.8 mcg/mL, sodium chloride is about 6 mg/mL to about 7 mg/mL, sodium metabisulfite is about 5 mcg/mL to about 5.6 mcg/mL, EDTA sodium is about 0.5 mg/mL to about 0.6 mg/mL, optionally N-acetyl-L-cysteine is about 10 mcg/mL to about 13 mcg/mL, and citrate buffer is about 1 to about 10 mM.
The claims cover ready-to-use lidocaine hydrochloride and epinephrine liquid formulations defined by a specified excipient system and pH range, together with a requirement for epinephrine retention after light-protected storage at about 5°C for about 60 to about 90 days.
Stated Advantages
Improved epinephrine stability versus prior art (e.g., Edge Pharma and Xylocaine MPF).
Maintenance of epinephrine content after light protected storage for about 60 days to about 90 days at a temperature of about 5°C.
Sterility (USP <71>) after 14 days is stated in the partial content.
Potency retention is stated for lidocaine and epinephrine after about 90 days at about 5°C.
Maintains epinephrine content within a defined range after storage in a light protected environment for about 60 days to about 90 days at about 5°C.
Documented Applications
Procedural analgesia associated with a venipuncture, shave removal, or a punch biopsy.
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