An-Najah Staff

BACKGROUND AND THE PURPOSE OF THE STUDY: Partition coefficients (log D and log P) and molecular surface area (PSA) are potential predictors of the intestinal permeability of drugs. The aim of this investigation was to evaluate and compare these intestinal permeability indicators.
METHODS:Aqueous solubility data were obtained from literature or calculated using ACD/Labs and ALOGPS. Permeability data were predicted based on log P, log D at pH 6.0 (log D(6.0)), and PSA.
RESULTS:Metoprolol's log P, log D(6.0,) and a PSA of <65 Å correctly predicted 55.9%, 50.8% and 54.2% of permeability classes, respectively. Labetalol's log P, log D(6.0) and PSA correctly predicted 54.2%, 64.4% and 61% of permeability classes, respectively. Log D(6.0) correlated well (81%) with Caco-2 permeability (P(app)). Of the list of national essential medicines, 135 orally administered drugs were classified into biopharmaceutical classification system (BCS). Of these, 57 (42.2%), 28 (20.7%), 44 (32.6%), and 6 (4.4%) were class I, II, III and IV respectively.
CONCLUSION:Log D(6.0) showed better prediction capability than log P. Metoprolol as permeability internal standard was more conservative than labetalol.

Objeetive: To evaluate the diagnostic value of prostate specific antigen (PSA) and its derivatives in detecting prostate cancer at biopsies. Materials and methods: Between July 2004 and March 2005, 1,05patients who underwent transrectal ultrasound-guided (TRUSO) systemic sextant core biopsies were included. All patients had PSA values 4-20 ng/ml ± abnormal digital rectal examinations (DRE) findings. PSA density (PSAD) and PSA density of the transition zone(TZPSAD) were calculated for each patient. Comparison between the clinical variables of patients with prostate cancer and benign prostatic hyperplasia (BPH) in terms of TPSA, total volume, TPSAD, TZPSAD, TRUS findings and DRE findings, "vas done. The diagnostic value of TRUS and DRE were also evaluated. Results: Out of 105 patients 11 had prostatic cancer (10.47%). There was no significant difference between subjects with BPH and subjects with prostate cancer in terms of total prostate volume, TPSA values, TRUS findings and DRE findings. However the values ofTPSAD and TZPSAD for patients with BPH differs significantly from that of patients with prostate cancer (P = 0.0001, P = 0.009 respectively). The accuracy ofDRE and TRUSO were 59.04% and 50.470/0respectively, both of them are poor predictors with insignificant difference (P= 0.25). Conclusion: Total PSA is of no diagnostic value in detecting prostate cancer in Egyptian patients with PSA < 20 ng/ml. However TPSAD and TZPSAD could be considered as accurate parameters with clinical significant for prostate cancer prediction in patients with PSA below 20 ng/ml. TRUS and DRE are poor predictor of prostate cancer with no significant difference.