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Applying Different Techniques to Improve the Bioavailability of Candesartan Cilexetil Antihypertensive Drug.

ABSTRACT: Purpose:The objective of this study was to compare different techniques to enhance the solubility and dissolution rate, and hence the bioavailability of candesartan cilexetil. Methods:To achieve this target, various techniques were employed such as solid dispersions, inclusion complexes, and preparation of candesartan nanoparticles. Following the preparations, all samples were characterized for their physicochemical properties, and the samples of the best results were subjected to further bioavailability studies. Results:Results of dissolution studies revealed an increase in the dissolution rate of all samples. The highest dissolution rate was achieved using solid dispersion of the drug with PVP K-90 (1:4). Physicochemical investigations (XR, DSC, and FT-IR) suggested formation of hydrogen bonding and changing in the crystalline structure of the drug. Regarding the inclusion complexes, more stable complex was formed between HP-?-CD and CC compared to ?-CD, as indicated by phase solubility diagrams. Antisolvent method resulted in the preparation of stable nanoparticles, as indicated by ? potential, with average particle size of 238.9 ± 19.25 nm using PVP K-90 as a hydrophilic polymer. The best sample that gave the highest dissolution rate (CC/PVP K-90 1:4) was allowed for further pharmacokinetic studies using UPLC MS/MS assay of rabbit plasma. Results showed a significant increase in the bioavailability of CC from ~15% to ~48%. Conclusion:The bioavailability of CC was significantly improved from ~15% to ~48% when formulated as SDs with PVP K-90 with 1:4 drug:polymer ratio.

SUBMITTER: Aly UF

PROVIDER: S-EPMC7234962 | biostudies-literature | 2020

REPOSITORIES: biostudies-literature

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Applying Different Techniques to Improve the Bioavailability of Candesartan Cilexetil Antihypertensive Drug.

Aly Usama Farghaly UF Sarhan Hatem Abdel-Monsef HA Ali Taha F S TFS Sharkawy Hosny Abd El-Bakey HAE

Drug design, development and therapy 20200514

<h4>Purpose</h4>The objective of this study was to compare different techniques to enhance the solubility and dissolution rate, and hence the bioavailability of candesartan cilexetil.<h4>Methods</h4>To achieve this target, various techniques were employed such as solid dispersions, inclusion complexes, and preparation of candesartan nanoparticles. Following the preparations, all samples were characterized for their physicochemical properties, and the samples of the best results were subjected to ...[more]

PMID: 32523332

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Project description:BackgroundHyperbilirubinemia is emerging as an increasingly common problem in newborns due to a decreasing hospital length of stay after birth. Jaundice is the most common disease of the newborn and although being benign in most cases it can lead to severe neurological consequences if poorly evaluated. In different areas of medicine, data mining has contributed to improve the results obtained with other methodologies.Hence, the aim of this study was to improve the diagnosis of neonatal jaundice with the application of data mining techniques.MethodsThis study followed the different phases of the Cross Industry Standard Process for Data Mining model as its methodology.This observational study was performed at the Obstetrics Department of a central hospital (Centro Hospitalar Tâmega e Sousa--EPE), from February to March of 2011. A total of 227 healthy newborn infants with 35 or more weeks of gestation were enrolled in the study. Over 70 variables were collected and analyzed. Also, transcutaneous bilirubin levels were measured from birth to hospital discharge with maximum time intervals of 8 hours between measurements, using a noninvasive bilirubinometer.Different attribute subsets were used to train and test classification models using algorithms included in Weka data mining software, such as decision trees (J48) and neural networks (multilayer perceptron). The accuracy results were compared with the traditional methods for prediction of hyperbilirubinemia.ResultsThe application of different classification algorithms to the collected data allowed predicting subsequent hyperbilirubinemia with high accuracy. In particular, at 24 hours of life of newborns, the accuracy for the prediction of hyperbilirubinemia was 89%. The best results were obtained using the following algorithms: naive Bayes, multilayer perceptron and simple logistic.ConclusionsThe findings of our study sustain that, new approaches, such as data mining, may support medical decision, contributing to improve diagnosis in neonatal jaundice.

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Applying Different Techniques to Improve the Bioavailability of Candesartan Cilexetil Antihypertensive Drug.

Publications

Applying Different Techniques to Improve the Bioavailability of Candesartan Cilexetil Antihypertensive Drug.

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