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Publication Number
US-11413350-B2
Publication Date
2022-08-16
Expiration Date
Abstract
Compositions comprised of a delivery vehicle or delivery system and an active agent dispersed within the delivery vehicle or system, wherein the delivery vehicle or system contains a polyorthoester polymer and a polar aprotic solvent. Also disclosed are low viscosity delivery systems for administration of active agents. The low viscosity delivery systems have a polyorthoester polymer, a polar aprotic solvent and a solvent containing a triglyceride viscosity reducing agent. Compositions described include an amide- or anilide-type local anesthetic of the “caine” classification, and a non-steroidal anti-inflammatory drug (NSAID), along with related methods, e.g., for treatment of post-operative pain or for prophylactic treatment of pain. The compositions are suitable for delivery via, e.g., direct application and instillation, intradermal injection, subcutaneous injection, and nerve block (perineural).
Core Innovation
The disclosure addresses reducing postoperative pain and producing post-surgical analgesia using a pharmaceutical composition that includes an amide-type local anesthetic and an enolic-acid non-steroidal anti-inflammatory drug (NSAID) with a delivery vehicle. The approach is directed to extending the duration of pain relief beyond what is described for similar compositions lacking the enolic-acid NSAID or lacking specific delivery-vehicle features.
The disclosed combinations pair the amide-type local anesthetic with an enolic-acid NSAID such as meloxicam and other Oxicam-class NSAIDs. The disclosure emphasizes conversion of shorter-lasting anesthetic effects into long-lasting analgesia and describes synergistic pain-relief recovery, with extended measurable plasma presence of both agents.
The delivery vehicle is characterized as a sustained-release delivery vehicle and, in particular embodiments, a biodegradable polyorthoester-based semi-solid composition. Additional vehicle refinements include polyorthoester identity, inclusion of a polar aprotic solvent, and the use of a triglyceride viscosity reducing agent whose three fatty acid groups each independently comprise between 1-7 carbon atoms.
For extending and maintaining analgesia, the disclosure specifies performance-related aspects of the composition, including viscosity behavior and release and analytical timing windows. These include measurable plasma concentrations for at least 3 days and release metrics such as at least about 80% by weight of both a local anesthetic and an enolic-acid NSAID released over 5 days in an in vitro test at 37°C.
Claims Coverage
The document identifies five independent methods: reducing postoperative pain, producing post-surgical analgesia, and extending the duration of pain relief from a polyorthoester composition. Across these, the claims repeatedly combine an amide-type local anesthetic and an enolic-acid NSAID with a delivery vehicle, with further inventive feature constraints tied to vehicle composition and release or measurement windows.
Postoperative pain reduction composition with amide-type local anesthetic and enolic-acid NSAID in a delivery vehicle
Administering to a subject a composition comprising an amide-type local anesthetic, an enolic-acid NSAID, and a delivery vehicle.
Post-surgical analgesia production with amide-type local anesthetic and enolic-acid NSAID in a delivery vehicle
Administering to a subject a composition comprising an amide-type local anesthetic, an enolic-acid NSAID, and a delivery vehicle.
Postoperative pain reduction via semi-solid biodegradable polyorthoester composition with amide-type local anesthetic and enolic-acid NSAID
Administering to a subject a semi-solid composition comprising a biodegradable polyorthoester, an amide-type local anesthetic, and an enolic-acid NSAID.
Postoperative pain reduction using polyorthoester-based delivery vehicle with polar aprotic solvent and triglyceride viscosity reducing agent
Administering to a patient in need thereof a pharmaceutical composition comprising a first therapeutic agent and a delivery vehicle comprised of a polyorthoester, a polar aprotic solvent, and a triglyceride viscosity reducing agent, wherein the triglyceride viscosity reducing agent comprises three fatty acid groups each independently comprising between 1-7 carbon atoms.
Extending duration of pain relief by incorporating an enolic acid-NSAID into a polyorthoester composition containing an amide-type local anesthetic
Incorporating in the composition an enolic acid-NSAID in an amount effective to extend the duration of pain relief provided by the composition when compared to a similar composition lacking the effective amount of the enolic acid-NSAID.
Across the independent claims, the central inventive concept is administering a composition that combines an amide-type local anesthetic and an enolic-acid NSAID with a delivery vehicle, with additional claim sets focusing on semi-solid biodegradable polyorthoester formulations and specific delivery-vehicle composition constraints. Further independent coverage includes methods that extend the duration of pain relief by incorporating the enolic acid-NSAID in an amount effective to extend analgesia duration.
Stated Advantages
Synergistic pain-relief recovery.
Extended duration of analgesia relative to short-acting anesthetic formulations.
Extended measurable plasma presence of both agents.
Extending the duration of pain relief compared to a similar composition lacking the effective amount of the enolic acid-NSAID.
Measurable plasma concentrations for at least 3 days and in vitro release of at least about 80% by weight over 5 days at 37°C.
Reduction of postoperative pain.
Production of post-surgical analgesia for an extended period.
Documented Applications
Reducing postoperative pain in a subject or patient in need thereof.
Producing post-surgical analgesia by administering the disclosed composition to a subject.
Reducing pain after a surgical procedure for an extended period.
Extending duration of pain relief provided by a polyorthoester composition containing an amide-type local anesthetic by incorporating an enolic acid-NSAID.
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