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Article

Development and In Vitro Evaluation of Controlled Release Viagra® Containing Poloxamer-188 Using Gastroplus PBPK Modeling Software for In Vivo Predictions and Pharmacokinetic Assessments

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College of Pharmacy, Al Ain University, Al Ain P.O. Box 64141, United Arab Emirates
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Department of Pharmacology and Therapeutics, College of Medicine and Health Sciences, United Arab Emirates University, Al Ain P.O. Box 17666, United Arab Emirates
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Department of Biopharmaceutics and Clinical Pharmacy, School of Pharmacy, The University of Jordan, Amman 11942, Jordan
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Author to whom correspondence should be addressed.
Academic Editors: Jung-woo Chae and In-hwan Baek
Pharmaceuticals 2021, 14(5), 479; https://0-doi-org.brum.beds.ac.uk/10.3390/ph14050479
Received: 11 April 2021 / Revised: 5 May 2021 / Accepted: 14 May 2021 / Published: 18 May 2021
Sildenafil is the active substance in Viagra® tablets, which is approved by the FDA to treat sexual dysfunction in men. Poor solubility and short half-life, however, can limit the span of its effectiveness. Therefore, this study focused on an oral controlled release matrix system with the aim to improve solubility, control the drug release, and sustain the duration of drug activity. The controlled release matrices were prepared with poloxamer-188, hydroxypropyl methylcellulose, and magnesium stearate. Various formulations of different ratios were developed, evaluated in vitro, and assessed in silico. Poloxamer-188 appeared to have a remarkable influence on the release profile of sildenafil citrate. In general, the rate of drug release decreased as the amount of polymer was gradually increased in the matrix system, achieving a maximum release period over 12 h. The in silico assessment by using the GastroPlus™ PBPK modeling software predicted a significant variation in Cmax, tmax, t1/2, and AUC0-t among the formulations. In conclusion, the combination of polymers in matrix systems can have substantial impact on controlling and modifying the drug release pattern. View Full-Text
Keywords: sildenafil citrate; poloxamer-188; matrix system; polymer; controlled release sildenafil citrate; poloxamer-188; matrix system; polymer; controlled release
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MDPI and ACS Style

Arafat, M.; Sarfraz, M.; AbuRuz, S. Development and In Vitro Evaluation of Controlled Release Viagra® Containing Poloxamer-188 Using Gastroplus PBPK Modeling Software for In Vivo Predictions and Pharmacokinetic Assessments. Pharmaceuticals 2021, 14, 479. https://0-doi-org.brum.beds.ac.uk/10.3390/ph14050479

AMA Style

Arafat M, Sarfraz M, AbuRuz S. Development and In Vitro Evaluation of Controlled Release Viagra® Containing Poloxamer-188 Using Gastroplus PBPK Modeling Software for In Vivo Predictions and Pharmacokinetic Assessments. Pharmaceuticals. 2021; 14(5):479. https://0-doi-org.brum.beds.ac.uk/10.3390/ph14050479

Chicago/Turabian Style

Arafat, Mosab, Muhammad Sarfraz, and Salahdein AbuRuz. 2021. "Development and In Vitro Evaluation of Controlled Release Viagra® Containing Poloxamer-188 Using Gastroplus PBPK Modeling Software for In Vivo Predictions and Pharmacokinetic Assessments" Pharmaceuticals 14, no. 5: 479. https://0-doi-org.brum.beds.ac.uk/10.3390/ph14050479

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