Pharmacological in vivo test to evaluate the bioavailability of some St John's Wort innovative oral preparations.
In this study, the optimisation of biopharmaceutical properties of a dried commercial extract of St John's Wort were evaluated employing the in vivo forced swimming test (FST). Three new dosage forms containing beta-cyclodextrin and surfactants (SDS, ASC8) were compared in the FST with the commercial extract. The commercial extract showed antidepressant activity in mice after 60 min at a dosage of 100 mg/kg. The same antidepressant activity appeared in 30 min with a micellar solution of SDS containing the same quantity of extract (100 mg/kg), while with micelles of ASC8 the effect appeared at 15 min and with a dosage of 30 mg/kg. In the case of beta-cyclodextrin the best results were obtained at 30 min, administering 60 mg/kg of the extract. Finally, the influence of the formulations on the water solubility of the constituents of the extract is reported. The tensides dramatically enhanced solubility, in particular that of the more lipophilic compounds, in the case of beta-cyclodextrin this effect was very pronounced for flavonoids and biapigenin, lower for hypericins and practically insignificant for hyperforins.
Isacchi
B
B
Department of Pharmaceutical Sciences, University of Florence, Italy.
Galeotti
N
N
Bergonzi
M C
MC
Ghelardini
C
C
Bilia
A R
AR
Vincieri
F F
FF
D000284:Administration, Oral; D000818:Animals; D000928:Antidepressive Agents / Q000493:pharmacokinetics*; D001682:Biological Availability; D004305:Dose-Response Relationship, Drug; D004355:Drug Stability; D005079:Excipients / Q000494:pharmacology; D020902:Hypericum / Q000737:chemistry*; D008297:Male; D051379:Mice; D008823:Micelles; D010936:Plant Extracts / Q000493:pharmacokinetics*; D010946:Plants, Medicinal; D012967:Sodium Dodecyl Sulfate / Q000494:pharmacology; D012995:Solubility; D013550:Swimming; D047392:beta-Cyclodextrins / Q000494:pharmacology
D000928:Antidepressive Agents; D005079:Excipients; D008823:Micelles; D010936:Plant Extracts; D047392:beta-Cyclodextrins; D012967:Sodium Dodecyl Sulfate