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Publication Number
US-10898575-B2
Publication Date
2021-01-26
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 describes long-acting polyorthoester-based drug delivery systems. The systems use a polyorthoester polymer combined with a polar aprotic solvent and, in low-viscosity embodiments, a triglyceride viscosity reducing agent to form a single-phase composition in which an active agent is dispersed or solubilized. The polyorthoester formulations are associated with controlled release profiles over extended periods.
The compositions combine an amide local anesthetic with an enolic-acid non-steroidal anti-inflammatory drug (NSAID), and the enolic-acid NSAID is the sole NSAID comprised in the composition. The combination is stated to provide extended local anesthesia/analgesia and is described in relation to pain management, including post-operative or prophylactic pain and emesis.
The disclosure also states that the triglyceride viscosity reducing agent lowers viscosity without altering release or pharmacokinetics. It further states that inclusion of the enolic-acid NSAID, as compared to other NSAID classes, restores and/or extends analgesic efficacy and can produce synergistic pain relief beyond additive effects.
Claims Coverage
The independent claims comprise 4 claims, directed to compositions and a method combining an amide local anesthetic with an enolic-acid NSAID while requiring that the enolic-acid NSAID is the sole NSAID. The claims distinguish delivery/formulation frameworks, including delivery-vehicle-inclusive compositions, semi-solid biodegradable polyorthoester compositions, and polyorthoester/polar aprotic solvent/triglyceride-viscosity-reducing-agent compositions.
Pain-relief composition with sole enolic-acid NSAID
A composition comprising an amide local anesthetic, an enolic-acid non-steroidal anti-inflammatory drug (NSAID), and a delivery vehicle, wherein the enolic-acid non-steroidal NSAID is the sole NSAID comprised in the composition.
Semi-solid polyorthoester composition with sole enolic-acid NSAID
A semi-solid composition comprising a biodegradable polyorthoester, an amide local anesthetic, and an enolic-acid non-steroidal anti-inflammatory drug (NSAID), wherein the enolic-acid non-steroidal NSAID is the sole NSAID comprised in the composition.
Polyorthoester, polar aprotic solvent, triglyceride viscosity agent, and sole enolic-acid NSAID
A composition comprising an amide local anesthetic, an enolic-acid non-steroidal anti-inflammatory drug (NSAID), 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, and wherein the enolic-acid non-steroidal NSAID is the sole NSAID comprised in the composition.
Method for extending duration of pain relief by incorporating enolic acid-nsaid
A method for extending duration of pain relief of a polyorthoester composition comprising an amide-type local anesthetic, comprising 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.
Overall claim coverage centers on compositions and a method that combine an amide local anesthetic with an enolic-acid NSAID while requiring that the enolic-acid NSAID is the sole NSAID. The independent claims distinguish delivery-vehicle-inclusive compositions, semi-solid biodegradable polyorthoester compositions, and polyorthoester/polar aprotic solvent/triglyceride-viscosity-reducing-agent compositions with a defined triglyceride fatty-acid group carbon count.
Stated Advantages
Extends duration of pain relief compared to a similar composition lacking the effective amount of the enolic acid-NSAID.
Provides low-viscosity delivery systems via inclusion of a polar aprotic solvent and a triglyceride viscosity reducing agent with specified properties.
Supports extended release and pain-relief/efficacy over time, as supported by in vitro release and in vivo pharmacokinetic/pharmacodynamic findings described in the document.
Triglyceride solvent lowers viscosity without altering release or pharmacokinetics.
Inclusion of enolic-acid NSAIDs (vs other NSAID classes) restores and/or extends analgesic efficacy.
Enolic-acid NSAID inclusion can produce synergistic pain relief beyond additive effects.
Documented Applications
Pain relief and extended-duration pain relief using polyorthoester compositions comprising an amide-type local anesthetic and an enolic acid-NSAID.
Administration routes/locations for pain management, including intramuscular, subcutaneous, perineural, in a nerve, in the epidural space, intrathecally, or directly to a surgical site or wound, as described in the dependents.
Nerve-block studies and related in vivo performance for pain relief described in the document.
Pain-management compositions providing extended local anesthesia/analgesia, including post-operative or prophylactic pain and emesis contexts.
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