Pharmaceutical compositions for treating pain
Inventors
Davis, Brett Hale • Lade, Caleb Adrian • Erickson, Sierra Nichelle • Wojtalewicz, Susan Alice
Assignees
Publication Number
US-11918572-B2
Publication Date
2024-03-05
Expiration Date
2043-01-27
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Abstract
A pharmaceutical composition can include a lipophilic oil. The pharmaceutical composition can further include an analgesic agent, anesthetic agent, anti-inflammatory agent, or a mixture thereof dispersed in the lipophilic oil. The pharmaceutical composition can further include a structuring agent at least a portion of which is not dissolved in the lipophilic oil and forms a gel.
Core Innovation
The invention provides a pharmaceutical composition comprising a lipophilic oil, a therapeutic agent such as an analgesic, anesthetic, or anti-inflammatory agent dispersed in the lipophilic oil, and a structuring agent that is at least partially not dissolved in the lipophilic oil and forms a gel. This composition creates a semi-solid oleogel entrapping the drug-loaded lipophilic oil in a supramolecular network, enabling prolonged localized drug release and pain management.
The problem being addressed is the limited duration of current local anesthetics that cannot provide analgesia throughout the entire period patients experience severe postoperative pain. Existing anesthetics wear off quickly, necessitating opioid administration for several days. Additionally, current implantable anesthetic technologies are limited by their physical forms, and injectable formulations generally last less than 24 hours. The invention aims to deliver an injectable or implantable composition that is viscous enough to stay at the site of administration and provides sustained pain relief for 2 to 14 days.
The composition addresses these challenges by utilizing a lipophilic oil such as medium-chain triglycerides, possibly blended with castor oil or other oils, combined with a structuring agent that forms a gel network to modulate drug diffusion and extend release duration. The formulation is designed to be shear-thinning for ease of injection through standard needles and to retain high viscosity at rest to stay localized. Manufacturing methods include mixing components at elevated temperatures, filling into syringes, cooling to gel, and sterilizing to ensure safety and stability.
Claims Coverage
The patent contains 5 claims, including one independent composition claim, one kit claim, and additional method claims for manufacturing and application. The inventive features focus on the specific compositions, kit configurations, and methods that enable prolonged localized analgesia with controlled release and viscosity.
Injectable pharmaceutical composition with defined component ranges
The composition comprises bupivacaine at about 3 to 7 wt %, medium-chain triglyceride oil at about 39.5 to 46.5 wt %, castor oil at about 39.5 to 46.5 wt %, and tristearin at about 0.5 to 6 wt %, with the ratio of medium-chain triglyceride to castor oil approximately 50:50 and without rheological modifiers.
Nerve block composition configuration
The pharmaceutical composition is suitable for use as a nerve block agent for pain management.
Kit comprising syringe and the pharmaceutical composition
A kit includes a sealed syringe containing the injectable composition, with a needle sized about 15-30 gauge.
Method of manufacturing the pharmaceutical composition
The method involves mixing bupivacaine, medium-chain triglyceride oil, castor oil, and tristearin under stirring and heating above 25°C up to 150°C, filling into a sealed syringe, cooling to form a gel, and sterilizing the final product via gamma irradiation or electron beam.
Method of treating pain using the pharmaceutical composition
Administering the composition by injection through a needle sized about 18-30 gauge at or near surgical or injury sites, to provide extended local analgesia.
These inventive features enable the production of a stable, injectable, and prolonged-release analgesic composition with defined component ratios, compatible delivery devices, and practical manufacturing and administration methods to ensure effective, localized pain relief for 2 to 14 days.
Stated Advantages
Provides 2 to 14 days of robust pain relief with an injectable formulation that remains localized at the site of administration.
Shear-thinning properties facilitate injection through standard needles while maintaining high viscosity at rest to prevent dispersion.
Blending of lipophilic oils like medium-chain triglycerides and castor oil optimizes drug loading capacity and viscosity for injection.
The structuring agent forms a gel network that prolongs drug release, ensuring sustained analgesia while maintaining structural integrity at the site.
Documented Applications
Use for local, regional, and neuraxial anesthesia in human and veterinary care.
Postoperative management to reduce reliance on opioids by providing extended pain relief.
Application in treating procedural, injury, or wound-related pain, including local infiltration and management of myofascial pain.
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