The Effect of Administered Dose of Lipid-Based Formulations on the In Vitro and In Vivo Performance of Cinnarizine as a Model Poorly Water-Soluble Drug

Gastric Pre-Processing Is an Important Determinant of the Ability of Medium-Chain Lipid Solution Formulations to Enhance Oral Bioavailability in Rats

“…The bioavailability (∼17%) was comparable to that obtained for the 250 mg oral lipid solution formulation (18.9%, Table ). The low bioavailability of the ID bolus formulation was comparable to previously reported administration of CZ suspensions …”

“…Pharmacokinetic parameters C max and T max were determined from the normalised data for each formulation and the truncated area under the curve (AUC 0–12 h ) was calculated using the trapezoidal rule. Bioavailability was calculated by comparison of the dose‐normalised AUCs with normalised AUC data from intravenous administration of CZ, and expressed as percentage absolute bioavailability ( F %). SPSS for Windows (Version 19.0, SPSS, Chicago, Illinois) was used to statistically analyse differences in the data using independent samples t ‐test with statistical significance assumed when p ≤ 0.05.…”

“…and ID administration, as GI function is known to be altered by anaesthesia . Plasma profiles and bioavailability were compared with previous oral studies to assess the performance of the lipid solution formulations with the absence of gastric passage and gastric processing.…”

How relevant are assembled equilibrium samples in understanding structure formation during lipid digestion?

“…Simulated intestinal fluid was prepared using bile salt (BS, sodium taurodeoxycholate) and phospholipid (PL, DOPC) concentrations at a ratio of 5 mM:1.25 mM (fasted) and 20 mM:5 mM (fed), in digestion buffer pH 6.5 (50 mM Tris maleate, 150 mM NaCl, 5 mM CaCl 2 Á2H 2 O, 6 mM NaN 3 as an antibacterial agent) [10][11][12][13]. The mean values and 4:1 BS:PL ratio represent intestinal contents after digestion [14,15].…”

Assessment of the Mechanistic Role of Cinnarizine in Modulating Experimentally-Induced Bronchial Asthma in Rats

“…1). Drug doses were adjusted based on pilot trials guided with published literature doses of dexamethasone [17] and cinnarizine [18,19]. …”