Abstract:
:Nalbuphine is a semi-synthetic opioid indicated for the relief of moderate to severe pain. Dinalbuphine sebacate (DNS) is a prodrug of nalbuphine for which we have developed long-acting lipophilic formulations in a benzyl benzoate/sesame oil mixture for intramuscular (IM) injection. In this study, we found that the in vitro release profile of DNS could be affected by adjusting the weight ratio of benzyl benzoate to sesame oil (the solvent/oil ratio). A longer release period could be attained by increasing the solvent/oil ratio in the formulation. A pharmacokinetic study was conducted in beagle dogs to verify the relationship between the in vitro release and the drug release from the formulations in vivo. The pharmacokinetic study confirmed that the formulation with a higher benzyl benzoate to oil ratio exhibits a longer drug release profile with a lower maximum concentration (Cmax) and a longer time to peak blood concentration level (Tmax) than the formulation with a lower benzyl benzoate to oil ratio.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Li CJ,Ku MY,Lu CY,Tien YE,Chern WH,Huang JDdoi
10.1016/j.ijpharm.2017.08.083subject
Has Abstractpub_date
2017-10-05 00:00:00pages
306-312issue
1eissn
0378-5173issn
1873-3476pii
S0378-5173(17)30801-3journal_volume
531pub_type
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