Long-acting local anesthetic formulation
Inventors
Lalla, Rajesh V. • Burgess, Diane J. • Li, Tingting
Assignees
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Publication Number
US-12251378-B2
Publication Date
2025-03-18
Expiration Date
Abstract
Compositions that include a bupivacaine salt are provided. The compositions may include bupivacaine linoleate, bupivacaine linolenate or bupivacaine laurate, at least one thermosensitive polymer, and at least one mucoadhesive or dermoadhesive agent. Also provided are methods for the treatment of an inflammatory or ulcerative condition with the disclosed compositions.
Core Innovation
The disclosure provides an oral spray formulation for treating oral mucositis, aphthous stomatitis, pemphious vulgaris, or mucous membrane pemphigoid. The formulation comprises an anesthetic, at least one thermosensitive polymer, and a mucoadhesive or dermoadhesive agent, and the anesthetic comprises bupivacaine hydrochloride while the mucoadhesive or dermoadhesive agent comprises carboxymethylcellulose.
The thermosensitive polymer comprises poloxamer 407, poloxamer 188, or a combination thereof, and the formulation is defined by concentration ranges for bupivacaine hydrochloride, the thermosensitive polymer, and the mucoadhesive or dermoadhesive agent. The thermosensitive polymer is configured to form a thermosensitive, semi-solid gel behavior associated with temperature-dependent administration as an oral spray.
The method includes administering to a subject a therapeutically effective amount of the oral spray formulation. The thermosensitive behavior includes liquid at about 25°C and a semi-solid gel at about 37°C, with a defined gelation temperature range, and the formulation further provides anesthetic release over a period of about 2 hours to about 6 hours, including about 80% of the anesthetic released within 2 hours after administering.
Claims Coverage
The document provides one independent claim defining a method of treating specified oral conditions by administering an oral spray formulation with three functional components, with the inventive features centered on the particular anesthetic and mucoadhesive/dermoadhesive pairing, the thermosensitive polymer selection, and specific concentration ranges and thermosensitive release/gelation behaviors.
Treating oral mucositis and related oral diseases using an oral spray formulation
A method for treating a subject suffering from oral mucositis, aphthous stomatitis, pemphious vulgaris, or mucous membrane pemphigoid by administering a therapeutically effective amount of an oral spray formulation comprising an anesthetic, at least one thermosensitive polymer, and a mucoadhesive or dermoadhesive agent.
Bupivacaine hydrochloride with carboxymethylcellulose as the mucoadhesive/dermoadhesive agent
The anesthetic comprises bupivacaine hydrochloride and the mucoadhesive or dermoadhesive agent comprises carboxymethylcellulose.
Specified concentration ranges for bupivacaine hydrochloride, thermosensitive polymer, and mucoadhesive/dermoadhesive agent
The formulation concentrations are defined such that bupivacaine hydrochloride is about 0.05% w/v to about 5% w/v, at least one thermosensitive polymer is about 10% w/v to about 22% w/v, and the mucoadhesive or dermoadhesive agent is about 0.05% w/v to about 5% w/v of the formulation.
Thermosensitive polymer comprising poloxamer 407, poloxamer 188, or a combination thereof
The thermosensitive polymer comprises poloxamer 407, poloxamer 188, or a combination thereof.
Overall, the independent claim ties treatment of specified oral mucosal diseases to an oral spray formulation containing bupivacaine hydrochloride, carboxymethylcellulose, and a thermosensitive polymer selected from poloxamer 407 and poloxamer 188, with defined concentration ranges.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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