Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-10213510-B2
Publication Date
2019-02-26
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 disclosed subject matter relates to semi-solid and pharmaceutical compositions that include a biodegradable polyorthoester delivery vehicle and bupivacaine and meloxicam. The polyorthoester is represented by Formula I, where R* is a C1-4 alkyl, n ranges from 5 to 400, and A is a diol where A is R1 and/or R3, with the fraction of A units of formula R1 between 0 and 25 mole percent.
The polyorthoester diol subunit A includes conditional structural definitions depending on whether A is R3 or A is R1. When A is R3, R3 is defined by the relationship in the formula where x is 2; when A is R1, R5 is H and R6 is defined, with the sum of p and q being 2 and s being 2, and the resulting component comprises the defined subunit.
The compositions combine the biodegradable polyorthoester with 1 wt % to 10 wt % bupivacaine and 0.01 wt % to 1 wt % meloxicam. In another composition, the delivery vehicle includes the polyorthoester together with a polar aprotic solvent and a triglyceride viscosity reducing agent having three fatty acid groups, each comprising between 1 and 7 carbon atoms.
Claims Coverage
Two independent claims are identified. The inventive coverage centers on a semi-solid or pharmaceutical composition with specified bupivacaine and meloxicam wt % ranges and a biodegradable polyorthoester defined by Formula I, with one claim further adding a polar aprotic solvent and a triglyceride viscosity reducing agent.
Semi-solid analgesic composition with defined polyorthoester formula I
A semi-solid composition comprising a biodegradable polyorthoester represented by Formula I, where R* is a C1-4 alkyl, n ranges from 5 to 400, and A is a diol where A is R1 and/or R3 with a fraction of A units of formula R1 between 0 and 25 mole percent, and where the semi-solid composition includes 1 wt % to 10 wt % bupivacaine and 0.01 wt % to 1 wt % meloxicam.
Delivery-vehicle formulation with polar aprotic solvent and triglyceride viscosity reducing agent plus defined polyorthoester formula I
A composition comprising 1 wt % to 10 wt % bupivacaine, 0.01 wt % to 1 wt % meloxicam, and a delivery vehicle comprised of a polyorthoester, a polar aprotic solvent and a triglyceride viscosity reducing agent, where the triglyceride viscosity reducing agent comprises three fatty acid groups each independently comprising between 1-7 carbon atoms, and where the polyorthoester is represented by Formula I with R* being a C1-4 alkyl, n ranging from 5 to 400, and A being a diol where A is R1 and/or R3 with the fraction of A units of formula R1 between 0 and 25 mole percent.
Overall claim coverage focuses on compositions that combine bupivacaine and meloxicam with a biodegradable polyorthoester defined by Formula I and constrained by R*, n, and A unit fraction. One independent claim is directed to a semi-solid composition where the polyorthoester is the biodegradable delivery vehicle, and the other independent claim further requires a delivery vehicle that includes a polar aprotic solvent and a triglyceride viscosity reducing agent with three fatty acid groups containing 1-7 carbon atoms.
Stated Advantages
Measurable plasma levels are produced.
Reduced viscosity does not substantially change drug release kinetics.
Lower-viscosity formulations maintain deeper and longer-lasting anesthesia in a sciatic-nerve peripheral nerve block model.
Granisetron release is comparable over a multi-day period despite viscosity reduction.
Provides extended bupivacaine release over a period of about 1 day to about 8 weeks.
Documented Applications
Extended pain relief treatment contexts including acute/chronic and prophylactic contexts are described in the partial content.
Peripheral nerve block performance is described in a porcine sciatic-nerve model with Von Frey testing.
Antiemetic therapy using granisetron is described in connection with viscosity-reducing formulations and in vitro release.
Managing pain in a subject by administering a composition as described.
Treatment of acute pain or chronic pain.
Administration by intramuscular, subcutaneous, perineural, or to a wound routes.
Interested in licensing this patent?