Table 1.
Permeation properties of 6-β-naltrexol, hydroxybupropion, and the codrug, CB-NTXOL-BUPOH. Data is represented as mean (± S.D.). n =3 for the parent drugs and n = 4 for CB-NTXOL-BUPOH.
| Drug | Light mineral oil solubility
(mM)‡ |
Half-life in buffer, pH 7.4
(h) ‡ |
Guinea pig plasma half-life
(h) |
In vitro flux
(nmol cm-2 h-1) ‡ |
In vitro lag time
(h) ‡ |
|---|---|---|---|---|---|
| 6-β-naltrexol | 0.03 ± 0.01 | stable | stable | 0.36 ± 0.15 | 15.72 ± 1.76 |
| CB-NTXOL-BUPOH | 2.88 ± 0.09 | 28.875 | 8.72 | 1.34 ± 0.35 | 12.10 ± 0.77 |
| Hydroxybupropion | 4.04 ± 0.04 | stable | stable | 25.89 ± 6.01 | 7.83 ± 1.73 |
‡
Values obtained from (Kiptoo et al., 2006). Data are from human skin studies.