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Publication Number
US-11083730-B2
Publication Date
2021-08-10
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 is directed to sustained-release pharmaceutical compositions that deliver an amide-type local anesthetic together with meloxicam. The compositions include a delivery system and specify an amide local anesthetic:meloxicam ratio ranging from about 10:1 to 50:1, while containing no additional active agents. The delivery system is described in multiple forms, including liposomes, microspheres, implantable osmotic, mechanical, or electromechanical devices, non-polymeric sucrose acetate isobutyrate/benzyl alcohol liquids, and polymeric depots using bioerodible polymers.
The long-acting delivery system is described as forming a miscible single phase and enabling controlled release over durations from about 1 day to about 8 weeks. Drug release and stability are related to delivery-system properties such as lipid fluidity/rigidity for liposomes and polymer matrix characteristics for microspheres and microparticles, with the amide local anesthetic and meloxicam entrapped within a polymer matrix or localized in an aqueous space and/or a lipid layer. The compositions are also described as being configured to provide controlled release behavior over time, including release timeframes and related pharmacokinetic and analgesic outcomes.
A central component is the use of bioerodible polymer depots, including polyorthoesters. The document provides structural guidance for polyorthoesters using alternating diketene acetal/diol residues and latent acid subunits derived from glycolide and/or lactide, with specified mole percentage ranges, and describes polyorthoester Formula I to IV embodiments with variable substituent identities and integer ranges for structural elements.
Claims Coverage
The document includes one independent claim, which covers a pharmaceutical composition comprising a delivery system, an amide local anesthetic, and meloxicam, with specified ratio limits and an explicit restriction on additional active agents.
Delivery system with amide local anesthetic and meloxicam ratio
A pharmaceutical composition comprising a delivery system, an amide local anesthetic, and meloxicam wherein the amide local anesthetic and meloxicam are present in the composition at a ratio ranging from about 10:1 to 50:1.
No additional active agents
The composition contains no additional active agents.
Polyorthoester defined by formulas I to IV and structural-variable ranges
A polyorthoester selected from polyorthoesters defined by formulas I, II, III, and IV with specified structural-variable ranges and substituent definitions.
Entrapment in liposome compartment or microsphere
In a liposome delivery system, the amide local anesthetic and meloxicam are entrapped in an aqueous space or in a lipid layer of the liposome, or are entrapped in the microsphere.
Delivery system viscosity threshold at 37 C
The delivery system has a viscosity less than 10000 mPa-s when measured at 37 C using a viscometer.
Overall claim coverage is centered on a delivery-system-based pharmaceutical composition containing an amide local anesthetic and meloxicam at a specified ratio, explicitly excluding any additional active agents. Dependent claim coverage further specifies delivery-system types and drug incorporation, and introduces quantitative constraints and polyorthoester structural parameters.
Stated Advantages
Extended pain relief is asserted.
Synergistic analgesia is asserted.
Controlled release over durations from about 1 day to about 8 weeks is described.
Measurable plasma concentrations are asserted.
Lower delivery-system viscosity is described via viscosity thresholds at 37°C intended for room-temperature needle administration.
Documented Applications
Pain management using the composition in perineural injection/nerve block contexts is described, with pain assessed using von Frey fibers and Pain Numeric Rating Scale (PNRS) and Pain Visual Analog Scale (VAS).
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