The <i>in vitro</i> release rate of methoxsalen from three commercially available tablets and an experimental tablet were evaluated at pH 2 and 7, using the USP dissolution test. The experimental tablet and one commercial product showed that 74% of the labeled amount is released in 1 h and almost completely released after 3 h at pH 2 and 7. Two products showed that only 12 and 10% of the labeled amount was released in 1 h and a maximum of 25 and 23% after 3 h at pH 2. At pH 7, the percent released from these two products were slightly higher. These results correlate with the reported clinical effectiveness of one of the products showing fast methoxsalen release. Since exposure to long-wave UV radiation is carried out 1–3 h following methoxsalen oral administration, delayed release might explain the failure of some products to give satisfactory clinical results.
Abstract An HPLC procedure for the detection and quantitative estimation of (-)-N-formylnorephedrine in rabbit plasma had been developed. The procedure involved the extraction of (-)-N-formylnorephedrine from plasma spiked with the internal standard (phenacetin), using ethyl acetate. The ethyl acetate extract is evaporated under nitrogen and the residue is reconstituted in water and injected onto the column. A u-Bondapak-C18 column 30 cm × 3.9 mm ID was used. The mobile phase is 20% acetonitrile in water; at a flow rate of 1.5 ml/min and uv detection at 256 nm. A linear relationship between concentration and peak height ratio (I/internal standard) was obtained (r = 1.00). The reported procedure allows the measurement of (-)-formylnorephedrine in concentrations as low as 150 ng/ml of plasma with total procedure time of about 10 min. The applicability of the procedure to pharmacokinetic studies is illustrated and metabolites are shown not to interfere with the assay procedure.
The clinical pharmacy component of Riyad College of Pharmacy curriculum was expanded from its present 4-credit h clinical pharmacy course to 18-credit h of clinical instructions in the pharmacy-core programme. In the final year of a 5-year programme, students may select clinical pharmacy as a professional option, thus receiving an additional 10-credit h of clinical instructions. The decision to expand the clinical component of the pharmacy curriculum was prompted by the need for patient-oriented pharmacy practitioners. The performance of graduates who had been rather briefly exposed to clinical pharmacy education led to this expansion.
Abstract The effect of diet on the absorption, metabolism, and elimination of salicylamide (SAM) in man was studied in five healthy male volunteers. In a three‐way cross‐over study, 300 mg SAM capsules were administered under fasting, carbohydrate, and lipid diet conditions. Total urinary salicylates, salicylamide glucuronide (SAMG), and salicylamide sulphate (SAMS) were determined at different time intervals. Diet was found to have no significant effect on the extent of SAM absorption or on its apparent elimination half‐life. A significant increase ( P < 0.001) in the fraction excreted as SAMS in the lipid diet trial compared to the fasting or carbohydrate trials is observed. In the lipid diet trial, the ratio ( R ) of the cumulative urinary SAMS/SAMG was found to be 1.5–3 times the ratio obtained under fasting or carbohydrate diet conditions. The equilibrium solubilities of SAM under physiologic conditions in water (W), simulated intestinal fluid (M), and corn oil (O) were 4.08, and 4.81, and 12.5mgml −1 , respectively. The equilibrium apparent distribution coefficients K O/W' K O/W , and K M/W were 3.1, 2.6, and 1.18, respectively. The increase in R is probably due to a decrease in free SAM concentration at the absorption site (intestinal mucosa) in the presence of lipids. A model for drug distribution in the gastrointestinal tract during lipid digestion is proposed and discussed.