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Publication Number
US-10098957-B2
Publication Date
2018-10-16
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 invention relates to reducing pain by administering to a wound a composition that includes a delivery system in the form of a semi-solid polymer formulation. The semi-solid polymer formulation comprises a polyorthoester, bupivacaine, and meloxicam, with bupivacaine and meloxicam present at a ratio ranging from about 15:1 to 50:1 and meloxicam present in an amount between about 0.005-0.75 wt %.
The polyorthoester is represented by Formula I, with R* as a C1-4 alkyl and n ranging from 5 to 400. Formula I also includes a diol component A with defined structural features and subunit representations as set forth in the claim.
The formulation is described as configured for controlled release, viscosity control, and sustained analgesia in vivo. The disclosure further describes extended release with measurable plasma drug levels over several days, and delivery-system refinements that tailor release profiles and support administration such as nerve block delivery.
Claims Coverage
The claims coverage centers on reducing pain by administering to a wound a semi-solid polymer formulation containing a polyorthoester defined by Formula I and a bupivacaine/meloxicam combination constrained by a specified ratio and meloxicam wt% range. Dependent claim refinements add specific classes of delivery-system components and further constrain delivery-system composition, polyorthoester molecular weight, and viscosity at 37°C.
Semi-solid polyorthoester formulation for reducing pain
Administering to a wound a composition comprised of a delivery system in the form of a semi-solid polymer formulation comprising a polyorthoester, bupivacaine, and meloxicam.
Bupivacaine-to-meloxicam ratio for wound pain reduction
Having bupivacaine and meloxicam present at a ratio ranging from about 15:1 to 50:1.
Meloxicam wt% concentration range in the wound composition
Having meloxicam present in the composition in an amount between about 0.005-0.75 wt %.
Polyorthoester defined by Formula I
Having the polyorthoester represented by Formula I with R* as a C1-4 alkyl and n ranging from 5 to 400, and A as a diol defined with specified substituent definitions as set forth in the claim.
Polar aprotic solvent and triglyceride viscosity reducing agent delivery-system components
Wherein the delivery system includes a polar aprotic solvent and a triglyceride viscosity reducing agent.
Named polar aprotic solvent selection
Wherein the polar aprotic solvent is selected from dimethyl sulfoxide, N-methyl pyrrolidone, or dimethyl acetamide.
Polyorthoester delivery system composition with dimethyl sulfoxide and triacetin
A delivery system composition including polyorthoester, dimethyl sulfoxide, and triacetin, with bupivacaine present at about 1-5 wt % and the polyorthoester present at 40-75 wt %.
Polyorthoester weight-average molecular weight range
Using a polyorthoester having a weight-average molecular weight between about 2,500 and about 10,000 Daltons.
Viscosity-limited delivery system at 37°C
Having a viscosity below 10000 mPa-s at 37°C when measured with a viscometer.
Overall, the claims coverage is directed to reducing pain by administering a semi-solid polymer formulation including a polyorthoester defined by Formula I and a bupivacaine/meloxicam combination constrained by a specified ratio and meloxicam wt% range. Dependent features add specific classes of delivery-system components and further constrain composition, polyorthoester molecular weight, and viscosity at 37°C.
Stated Advantages
Provides sustained analgesia in vivo.
Provides synergy versus either bupivacaine or meloxicam alone.
Provides extended release with measurable plasma drug levels over several days.
Tailors release profiles using delivery-system refinements.
Reduces delivery-system viscosity while largely preserving drug release kinetics/PK for injection/nerve block delivery.
Needle-administerable low-viscosity formulations enabled by viscosity control.
Documented Applications
Reducing pain by administering the composition to a wound.
Post-operative pain management in a porcine pain model, with sustained analgesia described using von Frey outcomes.
Nerve block application using a porcine sciatic nerve pain model with von Frey outcomes.
Perioperative pain management study concepts for herniorrhaphy pain.
Perioperative pain management study concepts for bunionectomy pain.
Providing long-acting pain-management for post-operative pain, including surgical-site instillation.
Perineural/nerve block administration for pain management.
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