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77%

Due to the slow release mechanism of the bupivacaine liposome injectable suspension, the mean Cmax and T1/2 on day 1 were approximately 3 times lower and 3.5 times higher, respectively, compared with bupivacaine HCI.

Absorption

Following single subcutaneous doses of 9 mg/kg and 18 mg/kg bupivacaine liposome injectable suspension, the median time to reach Cmax was rapid (0.5 hr), but it was delayed significantly at a high dose of 30 mg/kg (60 hr).21 Following equivalent doses (9 mg/kg) of bupivacaine liposome injectable suspension and bupivacaine HCl solution, the mean bupivacaine AUC(0-72) and Tmax were comparable. However, due to the slow release mechanism of the bupivacaine liposome injectable suspension, the mean Cmax and T1/2 on day 1 were approximately 3 times lower and 3.5 times higher, respectively, compared with bupivacaine HCl. Of note, bupivacaine liposome injectable suspension can result in measurable systemic bupivacaine in plasma for up to 96 hours, but the systemic plasma levels do not necessarily correlate with local efficacy.24

21. NOCITA® [package insert]. Leawood, KS: Aratana Therapeutics, Inc.; 2016.

24. Richard BM, Ott LR, Haan D, et al. The safety and tolerability evaluation of DepoFoam bupivacaine (bupivacaine extended-release liposome injection) administered by incision wound infiltration in rabbits and dogs. Expert Opin Investig Drugs. 2011;20(10):1327-1341.