SPL Set ID: 0af296bb-1599-4b35-b66b-994924d3e898

Bupivacaine liposome injectable suspension is a sterile, non-pyrogenic white to off-white preservative-free aqueous suspension consisting of multivesicular liposomes containing bupivacaine for infiltration and interscalene brachial plexus nerve block. Bupivacaine is present at a concentration of 13.3 mg/mL. After injection of bupivacaine liposome injectable suspension, bupivacaine is released from the multivesicular liposomes. Bupivacaine liposome injectable suspension is for infiltration or perineural use. Active Ingredient Bupivacaine is related chemically and pharmacologically to the amide-type local anesthetics. It is a homologue of mepivacaine and is related chemically to lidocaine. All three of these anesthetics contain an amide linkage between the aromatic nucleus and the amino, or piperidine group. They differ in this respect from the procaine-type local anesthetics, which have an ester linkage. Chemically, bupivacaine is 1-butyl-N-(2,6-dimethylphenyl)-2-piperidinecarboxamide with a molecular weight of 288.4. Bupivacaine has the following structural formula: Bupivacaine Liposome Injectable Suspension The median diameter of the liposome particles in bupivacaine liposome injectable suspension ranges from 22 to 30 μm. The liposomes are suspended in a 0.9% Sodium Chloride Injection. Each vial contains bupivacaine at a nominal concentration of 13.3 mg/mL. Inactive ingredients and their nominal concentrations are: cholesterol, 4.7 mg/mL; 1, 2-dipalmitoyl-sn-glycero-3 phospho-rac-(1-glycerol) sodium salt (DPPG), 0.9 mg/mL; tricaprylin, 2.0 mg/mL; 1, 2-dierucoylphosphatidylcholine (DEPC), 8.2 mg/mL; and phosphoric acid to adjust pH. The pH of bupivacaine liposome injectable suspension is in the range of 5.8 to 7.4. Bupivacaine in bupivacaine liposome injectable suspension has different functional properties relative to those of the unencapsulated or nonlipid-associated bupivacaine products. Bupivacaine that is released from bupivacaine liposome injectable suspension has a different pharmacokinetic and systemic profile relative to other bupivacaine products. In addition, the nominal weight percent concentration of bupivacaine in bupivacaine liposome injectable suspension is based on bupivacaine free base rather than bupivacaine HCl (100 mg of bupivacaine HCl contains 88.6 mg of bupivacaine free base) [ see Dosage and Administration ( 2.1 ) ]. structure