Evaluation of the Percutaneous Absorption of Ketamine HCl, Gabapentin, Clonidine HCl, and Baclofen, in Compounded Transdermal Pain Formulations, Using the Franz Finite Dose Modelmiércoles, 10 de octubre de 2018 0 Comentarios
Department of Research and Development, Professional Compounding Centers of America, 9901 South Wilcrest Dr., Houston, Texas, USA
Reprint requests to: Daniel Banov, RPh, Ms, Professional Compounding Centers of America (PCCA), 9901 South Wilcrest Drive, Houston, TX 77099, USA. Tel: 281-933-3248 ext.1166; Fax: 800-874-5760; E-mail: firstname.lastname@example.org.
Funding sources: The study was supported by Professional Compounding Centers of America, the manufacturer of Lipoderm and Lipoderm ActiveMax.
Objective. This study evaluates the ability of four commonly used analgesics (ketamine HCl, gaba-pentin, clonidine HCl, and baclofen), when incorpo-rated into two transdermal compounding bases, Lipoderm and Lipoderm ActiveMax, to penetrate human cadaver trunk skin in vitro, using the Franz finite dose model.
Design. In vitro experimental study
Methods. Ketamine HCl 5% w/w, gabapentin 10% w/ w, clonidine HCl 0.2% w/w, and baclofen 2% w/w were compounded into two transdermal bases, Lip-oderm and Lipoderm ActiveMax. Each compounded drug formulation was tested on skin from three dif-ferent donors and three replicate skin sections per donor. The Franz finite dose model was used in this study to evaluate the percutaneous absorption and distribution of drugs within each formulation.
Results Rapid penetration to peak flux was detected for gabapentin and baclofen at approxi-mately 1 hour after application. Clonidine HCl also had a rapid penetration to peak flux occurring approximately 1 hour after application and had a secondary peak at approximately 40 hours. Ketamine HCl exhibited higher overall absorption rates than the other drugs, and peaked at 6–10 hours. Similar patterns of drug distribution within the skin were also observed using both transdermal bases.
Conclusions. This study suggests that the combination of these 4 analgesic drugs can be success-fully delivered transdermally, using either Lipoderm or Lipoderm ActiveMax. Compounded transdermal drug preparations may then provide physicians with an alternative to traditional oral pain management regimens that can be personalized to the specific patient with the potential for enhanced pain control.
Key Words. Baclofen; Clonidine; Gabapentin; Keta-mine; Neuropathic Pain Management