Publications by authors named "Salahdein AbuRuz"

5 Publications

  • Page 1 of 1

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 (Basel) 2021 May 18;14(5). Epub 2021 May 18.

Department of Pharmacology and Therapeutics, College of Medicine and Health Sciences, United Arab Emirates University, Al Ain P.O. Box 17666, United Arab Emirates.

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 C t, t, and AUC among the formulations. In conclusion, the combination of polymers in matrix systems can have substantial impact on controlling and modifying the drug release pattern.
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http://dx.doi.org/10.3390/ph14050479DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8158482PMC
May 2021

Comparison between Branded and Generic Furosemide 40 mg Tablets Using Thermal Gravimetric Analysis and Fourier Transform Infrared Spectroscopy.

J Pharm Bioallied Sci 2020 Oct-Dec;12(4):489-498. Epub 2020 Oct 8.

College of Medicine and Health Sciences, The United Arab Emirates University, Al Ain, UAE.

Background And Purpose: There has been a long-standing belief that generic drugs are of lower value in comparison to their branded name counterparts. They are in particular under scrutiny due to their low market price. Even though the reduction in costs is largely based on skipping expensive preclinical studies and clinical trials for generic drugs, the purity and quality of the raw materials in the production of generic drugs is debatable. Thus, the objective of the study was to analyze and assess the quality comparability of generic furosemide 40 mg (FSD) tablets to branded product available in the market.

Materials And Methods: Quality control tests, in vitro drug release assessments, and thermal analysis investigations for both analog products of FSD were performed. Various physical parameters related to the tablet quality, such as hardness, weight variation, and friability tests, were examined. In vitro drug release behavior evaluations were conducted according to United States Pharmacopeia (USP) specifications and guidelines, whereas thermal analysis was carried out using thermal gravimetric analysis (TGA), and tablets were further evaluated by Fourier transform infrared (FTIR) spectroscopy.

Results: The results indicated a significant variation between the two products in terms of hardness, weight variation, and friability. This could be correlated to variation appeared in thermal and spectroscopic spectra between the two products using TGA and FTIR. Drug release of FSD was slightly different between both products following incubation in different pH media (1.2, 3.0, and 6.5; 120 min), however, this was in accordance with USP dissolution requirements as < 80% of drug release was obtained within the first 30 min from each product.

Conclusion: This study is a useful example for the independent investigations using thermal and spectroscopic analysis to confirm potential hidden variations between generic and branded products that could not be obtained by the bioequivalence studies.
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http://dx.doi.org/10.4103/jpbs.JPBS_365_19DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7909057PMC
October 2020

The Large Action of Chlorpromazine: Translational and Transdisciplinary Considerations in the Face of COVID-19.

Front Pharmacol 2020 16;11:577678. Epub 2020 Dec 16.

Department of Medical Microbiology and Immunology, College of Medicine and Health Science, United Arab Emirates University, Al Ain, United Arab Emirates.

Coronavirus disease 2019 (COVID-19) is a severe acute respiratory syndrome (SARS) in humans that is caused by SARS-associated coronavirus type 2 (SARS-CoV-2). In the context of COVID-19, several aspects of the relations between psychiatry and the pandemic due to the coronavirus have been described. Some drugs used as antiviral medication have neuropsychiatric side effects, and conversely some psychotropic drugs have antiviral properties. Chlorpromazine (CPZ, Largactil) is a well-established antipsychotic medication that has recently been proposed to have antiviral activity against SARS-CoV-2. This review aims to 1) inform health care professionals and scientists about the history of CPZ use in psychiatry and its potential anti- SARS-CoV-2 activities 2) inform psychiatrists about its potential anti-SARS-CoV-2 activities, and 3) propose a research protocol for investigating the use of CPZ in the treatment of COVID-19 during the potential second wave. The history of CPZ's discovery and development is described in addition to the review of literature from published studies within the discipline of virology related to CPZ. The early stages of infection with coronavirus are critical events in the course of the viral cycle. In particular, viral entry is the first step in the interaction between the virus and the cell that can initiate, maintain, and spread the infection. The possible mechanism of action of CPZ is related to virus cell entry via clathrin-mediated endocytosis. Therefore, CPZ could be useful to treat COVID-19 patients provided that its efficacy is evaluated in adequate and well-conducted clinical trials. Interestingly, clinical trials of very good quality are in progress. However, more information is still needed about the appropriate dosage regimen. In short, CPZ repositioning is defined as a new use beyond the field of psychiatry.
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http://dx.doi.org/10.3389/fphar.2020.577678DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7772402PMC
December 2020

Bioavailability of Beclometasone From Two HFA-BDP Formulations With a Spacer.

Respir Care 2019 Oct 28;64(10):1222-1230. Epub 2019 May 28.

Inhalation Consultancy Limited, Leeds, United Kingdom.

Background: The drug delivery characteristics of each inhaler/spacer combination are unique. The spacer size as well as the presence of electrostatic charge greatly influence the inhaler dose emission and in vivo delivery. Using a previously developed urinary pharmacokinetic method, we have measured the relative lung and systemic bioavailability of beclometasone dipropionate (BDP) after inhalation from 2 hydrofluroalkane-beclometasone dipropionate (HFA-BDP) formulations when used with a spacer.

Methods: 12 healthy volunteers received 8 randomized doses, separated by 7 d, of inhaled of BDP with either the Clenil pressurized metered-dose inhaler (pMDI; 250 μg) or the breath-actuated Qvar Easi-Breathe inhaler (100 μg), used alone or with a spacer. The urinary amounts of BDP excreted and retained in the spacer were assayed using a liquid chromatographic mass spectrometer. The spacer was assessed after washing with a detergent solution that was either rinsed or not rinsed with water. In addition, the aerodynamic characterization of each inhaler/spacer combination was assessed using the Andersen Cascade Impactor operated at 28 L/min using a 4-L inhalation volume. The amount of BDP deposited in the induction port, spacer, and various Anderson Cascade Impactor stages were determined.

Results: The in vivo 30-min urinary excretion and the in vitro fine particle dose results were only slightly affected by adding the spacer to the Clenil pMDI or the Qvar Easi-Breathe inhaler. However, the spacer significantly reduced drug particle impaction in the oropharynx and minimized deposition in the gastrointestinal tract. Therefore, using spacers with BDP inhalers is associated with a more favorable therapeutic ratio because it has little effect on lung dose, but it significantly reduced throat deposition. An improved lung deposition was achieved with non-rinsed spacers compared to spacers rinsed with water.

Conclusion: The difference in the BDP particle size between formulations as well as spacer size greatly affected drug deposition in different regions of the respiratory tract.
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http://dx.doi.org/10.4187/respcare.06689DOI Listing
October 2019

Comparison of the application of treatment Panel III and American College of Cardiology/American heart Association guidelines for blood cholesterol treatment in Saudi Arabia.

J Saudi Heart Assoc 2018 Oct 24;30(4):349-355. Epub 2018 Aug 24.

Department of Pharmacy Practice, College of Pharmacy, King Saud bin Abdulaziz University for Health Sciences, Riyadh, Saudi ArabiaSaudi Arabia.

Background: One of the major risk factors for cardiovascular diseases is hyperlipidemia. The primary aim of this study was to estimate the proportion of individuals between 40-75 years old that would be eligible for statin therapy based on ACC/AHA guideline as compared to ATP-III guideline in a population of patients in Saudi Arabia. We also intended to extrapolate the results to the entire Saudi population, and estimate the cost implications of the ACC/AHA treatment guideline.

Methods: This study was a retrospective, observational study involving adult patients aged between 40-75 years old. The study was conducted at the primary health care clinics at King Abdul-Aziz Medical/Riyadh. The eligibility for statins use was assessed and compared for each patient based on both the recent 2013 ACC-AHA guideline and the 2002 ATP-III guideline. The cost implication of applying the ACC/AHA treatment guideline was estimated based on the average cost for 40 mg Atorvastatin in the Saudi Market.

Results: A total of 1005 patients were included in the study. Using the ATP-III guideline, there were 139 male (43.7%) and 279 female (40.6%) eligible to receive statin therapy. Based on the 2013 ACC/AHA guideline, treatment is recommended in 315 males (99.1%) and 564 females (82.1%). On the other hand, high-intensity statin was recommended in 302 male (95%) and 400 female (58.2%). Only 74 (10.5%) patients were prescribed high-intensity statin of the 702 eligible patients. Extrapolating the results to the entire Saudi population, 2.369 million additional patients would be eligible for statin therapy when applying the ACC/AHA guideline. Applying the new guideline would result in a cost increase of at least 4.318 billion SR per year.

Conclusions: The eligibility for statin therapy was much higher when applying the ACC/AHA guideline as compared to ATP-III guideline. Applying the recent ACC/AHA dyslipidemia guideline increased the number of patients eligible for statin therapy to approximately two folds. This would be associated with a substantial increase in cost and possibly side effects. The concerns surrounding the ACC/AHA guideline should be addressed at the national level.
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http://dx.doi.org/10.1016/j.jsha.2018.08.003DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6140824PMC
October 2018
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