Superdisintegrants Effects: Development and Optimization of Febuxostat Tablets and Statistical Evaluation of Release Kinetics
LATIN AMERICAN JOURNAL OF PHARMACY
Authors: Qureshi, Saquib M.; Zafar, Farya; Ali, Huma; Shah, Shabana N.; Bushra, Rabia; Khan, Sohail; Khan, Maqsood A.; Mallick, Neelam
Abstract
the present study effects of two different superdisintegrants were assessed. For this purpose different formulations of Febuxostat 40 mg were developed using central composite rotatable design (CCRD). Batch I consists of nine different formulations (F1-F9) having (X-1) Crospovidone (1.964-9.035 %) and (X-2) Ludipress (35.857-64.142 %) with five levels and batch II consists of other nine formulations (FAFI) having (X-1) Ac-Di-Sol (1.171-6.828 %) and (X-2) Ludipress (35.857-64.142 %) with five levels were designed and evaluated. Powder blends of batch I and II were assessed for various micromeritic parameters and finally six formulations from each batch were selected for final compression stage. Chosen formulations were compressed by direct compression method. In all selected formulations dependant response variables were disintegration time (R-1) and hardness (R-2). Several quality assessments were carried out using compendial and non-compendial testing procedures and the results were found to be in the acceptable limits. On the basis of rapid disintegration time and excellent physico-chemical characteristics F8 (containing Crospovidone) and FD (containing Ac-Di-Sol) were selected as the best optimized formulations. Similarly, actual values were excellently correlated with the predicted values of hardness and disintegration time. Also, statistical model summary of response variables for batch I and II indicated that the results are within acceptable limits. Release profiles of all formulations were also assessed by several kinetic models. All the formulations followed Weibull kinetic model. Also reference formulations (F9 and FI) and tests formulations (F2, F4, F6, F7, F8 and FB, FD, FF, FG, FH) were compared using difference factor and similarity factor at several dissolution media. Results showed similar release profiles of tests and reference formulations. Release profiles of tests and reference formulations (batch I and II) were also assessed using one way ANOVA (Tukey's post hoc test) at three different dissolution media. Results demonstrated no variation between release pattern of test and reference formulations (batch I and II). In the present study optimized febuxostat formulations (batch I and II) were kept at accelerated conditions 40 +/- 2 degrees C and 75% RH +/- 5% RH in humidity chamber for 6 month. Results indicated that all the formulations have maintained their physico-chemical quality attributes indicating stability and compatibility of compound with excipients. Also, shelf lives of newly developed febuxostat formulations (batch I and II) were ranged of (23.51-26.65 months/weeks and 23.14-25.13 months/weeks).
QEEG - spectral power density of brain regions in predicting risk, resistance and resilience for bipolar disorder: A comparison of first degree relatives and unrelated healthy subjects
HELIYON
Authors: Kesebir, Sermin; Yosmaoglu, Ahmet
Abstract
Background: Temperament stems from the brain circuitry. Genetic differences among people are attributable to differences in neurophysiological function. Affective temperament is proposed endophenotype for bipolar affective disorder. QEEG spectral power density is thought to be an index of general affective and cognitive brain activity. The association of spectral power density with types of affective temperament may enlighten endo-phenotypes for bipolar affective disorder disposition. Method: TEMPS-A scale and rest QEEG were done on 25 euthymic patients, their healthy first degree relatives (n = 25) and 25 unrelated healthy control subjects. All patients were on lithium maintenance therapy. Results: F4 and T4 delta wave activity were similar between patients and first degree relatives, while Pz alpha activity was similar in first degree relatives and unrelated healthy subjects (p = 0.025, p = 0.001, p = 0.010). Cyclothymic and hyperthymic temperament scores were similar between patients and first degree relatives but higher than unrelated healthy subjects (p = 0.015, p = 0.010). F7 beta and F7-O2 high beta power were correlated with hyperthymic and irritable temperaments respectively in bipolar subject (r = 0.439, 0.387; 0.405, 0.364; 0.226, 0.351) T3-F4-T4 delta powers were correlated with cyclothymic temperament patients and their first degree relative (r = 0.443, 0.420, 505). Pz alpha power a hyperthymic temperament were inversely correlated in first degree rives and unrelated healthy subjects (r = 0.256 and -0.311). Conclusion: Medial temporal network may be associated with bipolar affective disorder heritability. On the other hand, left dorsolateral prefrontal beta and high beta activities may be a neural marker for disorder resistance together with right occipital high beta power.