Relative and absolute bioavailability of cibenzoline capsules and tablets in healthy subjects

Eighteen healthy adult volunteers completed an open-label, four-way crossover study designed to determine the bioequivalency of 160-mg cibenzoline [2-(2,2-diphenylcyclopropyl)-4,5-dihydro-1H-imidazole] capsules and tablets, their relative bioavailability compared with an oral solution of the drug, as well as the absolute bioavailability of these dosage forms compared with an intravenous infusion of the drug. Blood samples obtained at specified times after drug administration were assayed for cibenzoline by HPLC, and pharmacokinetic parameters were estimated from the resulting plasma concentration-time profiles. Comparisons were made between the tablet and capsule to assess bioequivalency, between the solid dosage forms and a solution to assess relative bioavailability, and between the oral forms and an intravenous infusion to assess absolute bioavailability. The pharmacokinetic parameters for each oral dosage form were similar and ratios of mean parameters indicated that the solid dosage forms were bioequivalent and completely bioavailable relative to an oral solution. The ratios of the area under the plasma concentration-time profiles (AUC) for the capsule, tablet, and oral solution to that of the intravenous infusion were 0.85, 0.83, and 0.86, respectively, indicating that orally administered cibenzoline has an absolute bioavailability of approximately 85%.     

单道感应式人工耳蜗装置的研制

感应式人工耳蜗装置将声音信息转变并处理为适当的电信号之后,采用电磁感应的方式将此信号送至植入全聋患者内耳耳蜗靠近听神经纤维的作用电极上,刺激神经发放冲动,使全聋患者恢复音感。本装置经临床全聋患者使用,取得较满意效果。     

Comparative study of oral conditions in schoolchildren of Strasbourg, France, 1974–85

A representative sample of 1650 children randomly selected in the 6-15-yr-old schoolchild population of Strasbourg was examined by well-calibrated examiners. The prevalence of caries was determined with the DMFT, DMFS and dft indices using bitewing radiographs. Plaque, calculus and gingival indices were also determined. The results obtained were compared with the initial study of 1974 performed in Strasbourg using the same epidemiologic methods. Whereas no important variations were observed in caries prevalence of primary teeth, a significant reduction of caries activity was observed in DMFT and DMFS indices in all age groups. There was a reduction of these two indices of respectively 32% and 33% in the 12-yr-old children. The reduction was the most significant on approximal surface lesions. A statistically significant decrease of the calculus and gingival indices was also observed between 1974 and 1984. A less significant decrease was observed for the plaque index.     

Haemodynamic effects of rectal methohexitone for induction of anaesthesia in children

Pulsed Doppler and two-dimensional echocardiography were used to determine the haemodynamic effects of rectal methohexitone in 12 children 32.4 +/- 3.8 months old and weighing 13.3 +/- 1.1 kg (mean +/- SEM). Heart rate, blood pressure and echocardiographic measurements of cardiac output, stroke volume and left ventricular end-diastolic and end-systolic volumes were obtained prior to the induction of anaesthesia. Anaesthesia was induced with 25 mg.kg-1 two per cent rectal methohexitone. Immediately following the onset of sleep all cardiovascular measurements were repeated. Following the induction of anaesthesia with rectal methohexitone there was a significant increase in heart rate. Blood pressure, cardiac index, stroke volume and ejection fraction were unchanged. It is concluded that rectal administration of two per cent methohexitone for the induction of anaesthesia in healthy paediatric patients has minimal haemodynamic effect.     

Alkaloidal components ofPanax ginseng

Over twelve alkaloids were delected in the roots ofPanax ginseng C.A. Meyer. Among them three alkaloids were isolated and were identified as N₉-formylharman, ethyl β-carboline-1-carboxylate and perlolyrine on the basis of spectroscopic studies.     

Effects of Ethanol on Arachidonic Acid Incorporation Into Lipids of a Plasma Membrane Fraction Isolated from Brain Cerebral Cortex

In the presence of ATP, MgCl2, and CoASH, somal plasma membranes isolated from rat cerebral cortex were active in transferring arachidonic acid to phosphatidylinositols, phosphatidylcholines, and triacylglycerols. Ethanol (350-525 mM) added to the incubation mixture inhibited arachidonic acid incorporation into phospholipids, while it enhanced the incorporation into triacylglycerols. Under these conditions, ethanol was found to react with arachidonic acid to form arachidonoyl ethyl ester. The incorporation of labeled arachidonic acid into glycerolipids as well as the synthesis of ethyl esters required the presence of ATP and CoASH for maximal activity. Nevertheless, each uptake process exhibited a unique pH profile. The esterification of arachidonic acid was not specific for ethanol as other aliphatic alcohols (e.g., propanol and butanol) were also able to react with labeled arachidonic acid to form the respective esters. Somal plasma membranes isolated from mice after chronic ethanol administration showed an increase in arachidonoyl transfer to both phospholipids and triacylglycerols. When these membranes were challenged with ethanol (325 mM), those isolated from the chronic ethanol group showed a greater increase in the labeling of triacylglycerols and ethyl esters than those from controls. Thus, different acyltransferases exhibite different responses to the effects of ethanol in vitro and in vivo.