[Computational approach to the prediction of blood-brain partitioning of basic drug candidates using mixed micellar liquid chromatography]

Background and Objective: The blood-brain barrier [BBB] is considered to be the main barrier to drug transport into the central nervous system. In this study, the capability of biopartitioning micellar chromatography [BMC] using the mixed micellar system of Brij-35/sodium dodecyl sulfate [Brij-35/SDS, 85:15 mol/mol] has been studied to predict pharmacokinetic parameter [BBB penetration ability] of 14 basic drugs

Methods: In this descriptive-analytical study, the potential of BMC using mixed micellar system [Brij-35/SDS, 85:15 mol/mol] in 0.04 M at physiological pH 7.4 was evaluated to predict pharmacokinetic parameter [BBB penetration ability] of 14 basic drugs. The regression model for the prediction of blood-brain distribution coefficient is derived from the multiple linear regression analysis using the training set in mixed micellar mobile phase. Also, the predictive ability of model was evaluated for a prediction set of 5 compounds [Chlorpromazine, Mianserin, Propranolol, Cimetidine, and Thioridazine]. The fair R2 indicates good stability and predictive ability of the developed model for the drugs not included in modeling

Results: The relationship between the BMC retention data of 14 basic drugs and their log BB parameter showed a good statistically model [R2=0.822, F=25.42, SE=0.225, R2CV=0.781]

Conclusion: This study points out the usefulness of mixed micellar solution of Brij-35/SDS, 85:15 [mol/mol] in BMC as a high-throughput primary screening tool that can provide key information about the blood-brain distribution of basic drugs in a simple and economical way

[Effect of swimming training and fenugreek seed extract on plasma glucose and antioxidant activity in heart tissue of streptozotocine - induced diabetic rats]

Free radical production andsubsqunt oxidative steress can be due to hyperglycemia and its oxidation. This study was done to evaluate the effect of swimming training test and Fenugreek seed extract on plasma glucose and antioxidant activity in heart tissue of streptozotocine - induced diabetic rats. In this experimental study, 50 male wistar rats were allocated into five groups; diabetic [DC, n=10], healthy control [HC, n=10], swimming training [S, n=10], swimming training + Fenugreek seed extract [1.74 g/kg/bw] [SF1, n=10], and swimming training + Fenugreek seed extract [0.87 g/kg/bw] [SF2, n=10]. Streptozotocine [60 mg/kg/bw] was used for induction of diabetes in DC, S, SF1 and SF2 groups. Serum glucose and the rat heart tissue antioxidant enzymes activities of superoxide dismutase, Catalase and Glutation peroxidase were determined. Body weight in all groups were significantly reduced in comparsion with healthy control group [P<0.05]. Plasma glucose level significantly reduced in SF1 and HC groups compared to diabetic group [P<0.05]. Cardiac antioxidant enzymes in swimming training, SF1 and SF2 groups significantly increased in compare to diabetic group [P<0.05]. The combination of endurance swimming training and fenugreek seed extract can reduce plasma glucose and increase cardiac antioxidant enzymes in streptozotocine - induced diabetic rats

Treatment of thyroid hot nodules by percutaneous ethanol injection

Twenty-eight patients with autonomously functioning thyroid nodules of 2-6 cm diameter were selected. Fifteen patients were clinically and biochemically hyperthyroid. Depending on the nodule size, 2-4 ml of 95% ethanol was injected into the nodules. There were no major complications. Thyroid scans were done at two-month intervals and repeated injections were done only if the hot nodules were still present. 71.4% needed only one, 25% needed two, and 3.6% needed three injections for complete ablation of the hot nodules. On follow-up examination all nodules had shrunken in size and those patients with hyperthyroidism showed improvement of their symptoms. The hormone levels also returned to normal range.Repeated thyroid scans showed disappearance of the hot nodule and gradual resumption of function of the previously suppressed thyroid tissue. This study shows that percutaneous ethanol injection is a safe and cheap alternative to surgical and radioiodine ablation of AFTN's and this can be achieved in most cases in one or two sessions. Importantly, with this method, the chance of future hypothyroidism will be nil

Massive osteolysis with chylothorax: a case report and review of literature

A case of massive osteolysis in a young man with complaints of chest pain and respiratory difficulty is presented. The patient was found to have destruction of several ribs and bilateral chylothorax. Massive osteolysis is discussed and relevant medical literature is reviewed