Effect of structured diet with exercise education on anthropometry and lifestyle modification in patients with type 2 diabetes: A 12-month randomized clinical trial.

AIMS: Lifestyle modification involving active engagement of specialised dietitian with diet and exercise education, can be effective as first-line treatment for diabetes. METHODS: 192 patients were enrolled with diabetes in a randomised controlled trial and followed up for one year. Ninety-four patients in the intervention group participated in a comprehensive structured diet and exercise education conducted by a specialised dietitian at ambulatory centre in the United Arab Emirates. RESULTS: The mean difference in the change in body mass index between study groups at study exit and baseline was statistically significant (BMI difference = -1.86, 95 % CI -2.68 - -1.04, P < 0.01). The intervention group reported significant decrease in total carbohydrate and daily energy intake compared to baseline (173.7 g vs 221.1 g and 1828.5 kcal vs 2177.9 kcal, respectively). Moreover, the mean metabolic equivalents (METs) in the intervention group increased significantly at study exit from baseline compared to control group METs, with mean difference between all between-group differences after baseline of 0.63 (95 % 0.29 - 0.97, P < 0.01). CONCLUSIONS: Structured diet and exercise counselling by specialised dietitian in ambulatory settings significantly reduced carbohydrate and daily energy intake, with improved anthropometric measurements and physical activity.

Confidence, attitude, and practice of scientific research among health professions' students in the United Arab Emirates.

OBJECTIVE: This study aimed to assess the confidence, attitude, and scientific research practices of undergraduate students of different health profession specialties. METHODS: In this cross-sectional study, an online-based questionnaire was distributed as a Google Form via groups and pages of medical universities available on social media sites such as Facebook, WhatsApp, and Twitter to the second- to sixth-year students of different health profession specialties in different universities across the United Arab Emirates (UAE) in the period from October through December 2023 using the convenience sampling technique. The questionnaire included four parts that assessed socio-demographics and custom-designed research-related questions (6 items), perceived confidence (8 items), attitudes (14 items), and the practice in the context of scientific research and its implementation (9 items). Multivariate logistic regression analyses were conducted to explore the variables associated with the study outcomes, including confidence, attitudes, and practice levels. RESULTS: The study included 522 undergraduate students. The participants reported low confidence, a negative attitude, and low scientific research practice. Regression results revealed that individuals without prior research experiences were less likely to have high confidence and practice compared to those with previous research experience (OR = 0.634, 95% CI: 0.426-0.945, p = 0.025; and OR = 0.139, 95%Cl: 0.090-0.216, P<0.001, respectively). Additionally, participants who reported difficulty in differentiating between various literature resources were less likely to have high confidence and practice compared to those who reported the ability to differentiate (OR = 0.627, 95% CI: 0.42-0.935, p = 0.022, and OR = 0.370, 95%Cl: 0.237-0.579, p<0.001, respectively). Furthermore, individuals who had not taught research methods in their undergraduate studies were less likely to have high practice (OR = 0.505, 95%Cl: 0.309-0.823, p = 0.06). CONCLUSIONS: Undergraduates of different medical specialties in the UAE demonstrated acceptable levels of confidence and attitude toward scientific research, with several areas for practice improvement. Education and training courses focusing on various aspects of scientific research should be incorporated into the medical curricula in order to enhance students' confidence and practice of scientific research.

The Safety and Effectiveness of Apixaban in Patients with End-Stage Kidney Disease on Dialysis: A Retrospective Observational Study.

Background: Apixaban has been increasingly utilized for various FDA-approved indications, including stroke prevention and venous thromboembolism (VTE) treatment in patients with end stage kidney disease (ESKD) on hemodialysis. However, the safety and efficacy of its use in this population is not well established. Hence, the purpose of this study is to evaluate the safety and effectiveness of apixaban by examining outcomes in this population. Methods: This was a retrospective observational study that involved adults with ESKD who were on hemodialysis and prescribed apixaban from our hospital's outpatient pharmacy between 1 May 2015, and 31 March 2022. Demographics, apixaban indications, dose appropriateness, concomitant antiplatelet use, and comorbidities data were collected. Bleeding and thromboembolic events were also collected. Results: Sixty-six patients fulfilled the inclusion criteria, 50% of them males. Median age was 71 (63.5-82) years, and the median BMI 28.2 (59.5-86.25) kg/m2. The median follow-up time was 5 (1.9-12.3) months. Concomitant antiplatelet use (39.4%) and high medication adherence (84.8%) were observed. During follow-up, major bleeding events occurred in 15.2% of cases, with minor bleeding being more common (36.4%), and VTE and stroke events occurred in 4.5% of cases; appropriate dosing was prevalent (62.1%), and there was an overall all-cause mortality rate of 34.8%. Most patients received a 2.5 mg BID apixaban dose (56.1%), including both NVAF and VTE groups. Notably, the multivariate logistic regression analysis indicated that weight, and daily dose were insignificant predictors of bleeding events (p = 0.104, 0.591), however, the BMI was the main independent risk factor for bleeding in this population [OR = 0.9, 95% CI: 0.8-0.99; p = 0.023]. Conclusions: Our analysis of apixaban-treated ESKD patients highlights that the risk of bleeding is significant, and BMI was the main independent risk factor. A larger prospective study is needed to confirm our findings.

Effect of Hydration Forms and Polymer Grades on Theophylline Controlled-Release Tablet: An Assessment and Evaluation.

BACKGROUND: Drug release from controlled release delivery systems is influenced by various factors, including the polymer's grade and the drug's hydration form. This study aimed to investigate the impact of these factors on the controlled release of theophylline (THN). This research compares the monohydrate form found in branded products with the anhydrous form in generic equivalents, each formulated with different polymer grades. METHODS: Quality control assessment was conducted alongside in vitro evaluation, complemented by various analytical techniques such as X-ray diffraction (XRD) and scanning electron microscopy (SEM). Additionally, thermal analyses using differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) were employed. RESULTS: Quality control assessments demonstrated that the generic tablets exhibited lower average weight and resistance force compared to the branded ones. In vitro tests revealed that generic tablets released contents within 120 min, compared to 720 min for the branded counterpart. Characterization using XRD and SEM identified disparities in crystallinity and particle distribution between the three samples. Additionally, the thermal analysis indicated consistent endothermic peaks across all samples, albeit with minor variations in heat flow and decomposition temperatures between the two products. CONCLUSIONS: This study demonstrated that variations in polymer grade and hydration form significantly impact THN release.

Nanomedicines: Emerging Platforms in Smart Chemotherapy Treatment-A Recent Review.

Cancer continues to pose one of the most critical challenges in global healthcare. Despite the wide array of existing cancer drugs, the primary obstacle remains in selectively targeting and eliminating cancer cells while minimizing damage to healthy ones, thereby reducing treatment side effects. The revolutionary approach of utilizing nanomaterials for delivering cancer therapeutic agents has significantly enhanced the efficacy and safety of chemotherapeutic drugs. This crucial shift is attributed to the unique properties of nanomaterials, enabling nanocarriers to transport therapeutic agents to tumor sites in both passive and active modes, while minimizing drug elimination from delivery systems. Furthermore, these nanocarriers can be designed to respond to internal or external stimuli, thus facilitating controlled drug release. However, the production of nanomedications for cancer therapy encounters various challenges that can impede progress in this field. This review aims to provide a comprehensive overview of the current state of nanomedication in cancer treatment. It explores a variety of nanomaterials, focusing on their unique properties that are crucial for overcoming the limitations of conventional chemotherapy. Additionally, the review delves into the properties and functionalities of nanocarriers, highlighting their significant impact on the evolution of nanomedicine. It also critically assesses recent advancements in drug delivery systems, covering a range of innovative delivery methodologies. Finally, the review succinctly addresses the challenges encountered in developing nanomedications, offering insightful perspectives to guide future research in this field.

Preparation and Characterization of Theophylline Controlled Release Matrix System Incorporating Poloxamer 407, Stearyl Alcohol, and Hydroxypropyl Methylcellulose: A Novel Formulation and Development Study.

BACKGROUND: Theophylline (THN), a bronchodilator with potential applications in emerging conditions like COVID-19, requires a controlled-release delivery system due to its narrow therapeutic range and short half-life. This need is particularly crucial as some existing formulations demonstrate impaired functionality. This study aims to develop a new 12-h controlled-release matrix system (CRMS) in the form of a capsule to optimize dosing intervals. METHODS: CRMSs were developed using varying proportions of poloxamer 407 (P-407), stearyl alcohol (STA), and hydroxypropyl methylcellulose (HPMC) through the fusion technique. Their in vitro dissolution profiles were then compared with an FDA-approved THN drug across different pH media. The candidate formulation underwent characterization using X-ray diffraction, scanning electron microscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, and thermogravimetric analysis. Additionally, a comprehensive stability study was conducted. RESULTS: In vitro studies showed that adjusting the concentrations of excipients effectively controlled drug release. Notably, the CRMS formulation 15 (CRMS-F15), which was composed of 30% P-407, 30% STA, and 10% HPMC, closely matched the 12 h controlled-release profile of an FDA-approved drug across various pH media. Characterization techniques verified the successful dispersion of the drug within the matrix. Furthermore, CRMS-F15 maintained a consistent controlled drug release and demonstrated stability under a range of storage conditions. CONCLUSIONS: The newly developed CRMS-F15 achieved a 12 h controlled release, comparable to its FDA-approved counterpart.

Triple-Emulsion-Based Antibubbles: A Step Forward in Fabricating Novel Multi-Drug Delivery Systems.

Developing carriers capable of efficiently transporting both hydrophilic and lipophilic payloads is a captivating focus within the pharmaceutical and drug delivery research domain. Antibubbles, constituting an innovative encapsulation system designed for drug delivery purposes, have garnered scientific interest thanks to their distinctive water-in-air-in-water (W1/A/W2) structure. However, in contrast to their precursor, i.e., nanoparticle-stabilized W1/O/W2 double emulsion, traditional antibubbles lack the ability to accommodate a lipophilic payload, as the intermediary (volatile) oil layer of the emulsion is replaced by air during the antibubble fabrication process. Therefore, here, we report the fabrication of triple-emulsion-based antibubbles (O1/W1/A/W2), in which the inner aqueous phase was loaded with a nanoemulsion stabilized by various proteins, including whey, soy, or pea protein isolates. As model drugs, we employed the dyes Nile red in the oil phase and methylene blue in the aqueous phase. The produced antibubbles were characterized regarding their size distribution, entrapment efficiency, and stability. The produced antibubbles demonstrated substantial entrapment efficiencies for both lipophilic (ranging from 80% to 90%) and hydrophilic (ranging from 70% to 82%) components while also exhibiting an appreciable degree of stability during an extended rehydration period of two weeks. The observed variations among different antibubble variants were primarily attributed to differences in protein concentration rather than the type of protein used.

A review of pharmacogenomics studies assessing the knowledge and attitudes of physicians and pharmacists across the Arab and Middle Eastern Region

The principal goal of pharmacogenomics (PGx) is to achieve the highest drug efficacy while maintaining a low toxicity profile. Historically, health care systems used to target treatment for all individuals with the same diagnosis using a standardized medication or dose that fits all. However, a recent pattern in medicine has emerged focusing on personalized and precision medicine. For effective implementation of PGx, there is a need for more collaborations between all the stakeholders in the healthcare system to integrate the pharmacogenetics concept into practice. When it comes to the knowledge and attitudes towards pharmacogenomics, the majority of medical professionals, including pharmacists and physicians, appear to lack appropriate knowledge and training. Across the Middle East and Arab Region, only few studies have addressed this topic. The current review objective is to shed light on pharmacists’ and physicians’ knowledge and attitudes towards PGx practice in the UAE, Arab and the Middle East region as compared to the rest of the world. Moreover, highlighting the role of the pharmacists in the application of PGx services and the educational challenges that are faced. Proposed solutions to improve the knowledge gaps will also be discussed. We also aim to provide the international readers as well as the local researchers with a summary of the trends and distribution of the results across these countries. (AU)

Canagliflozin Ameliorates Oxidative Stress and Autistic-like Features in Valproic-Acid-Induced Autism in Rats: Comparison with Aripiprazole Action.

Based on their proven anti-inflammatory and antioxidant effects, recent studies have examined the therapeutic potential of the sodium-glucose cotransporter 2 (SGLT2) inhibitors in neurodevelopmental disorders such as autism spectrum disorder (ASD). Therefore, the aim of this study is to assess the effects of subchronic systemic treatment with intraperitoneal (i.p.) canagliflozin (20, 50, and 100 mg/kg) compared to aripiprazole (ARP) (3 mg/g, i.p.) in a valproic acid (VPA)-induced rat model of autism. The behavioral characteristics of ASD, oxidative stress, and acetylcholinesterase (AChE) activity in rats with ASD-like behaviors, which were induced by prenatal exposure to VPA, were evaluated. The behavioral assessment methods used for this study were the open field test (OFT), the marble-burying test (MBT), and the nestlet-shredding test (NST) to examine their exploratory, anxiety, and compulsiveness-like actions, while the biochemical assessment used for this study was an ELISA colorimetric assay to measure ASD biomarker activity in the hippocampus, prefrontal cortex, and cerebellum. Rats that were pretreated with 100 mg/kg of canagliflozin displayed a significantly lower percentage of shredding (1.12 ± 0.6%, p < 0.01) compared to the ARP group (3.52 ± 1.6%). Pretreatment with (20 mg/kg, 50 mg/kg, and 100 mg/kg) canagliflozin reversed anxiety levels and hyperactivity and reduced hyper-locomotor activity significantly (161 ± 34.9 s, p < 0.05; 154 ± 44.7 s, p < 0.05; 147 ± 33.6 s, p < 0.05) when compared with the VPA group (303 ± 140 s). Moreover, canagliflozin and ARP mitigated oxidative stress status by restoring levels of glutathione (GSH) and catalase (CAT) and increasing the levels of malondialdehyde (MDA) in all tested brain regions. The observed results propose repurposing of canagliflozin in the therapeutic management of ASD. However, further investigations are still required to verify the clinical relevance of canagliflozin in ASD.

Effect of Excipients on the Quality of Drug Formulation and Immediate Release of Generic Metformin HCl Tablets.

Generic medications are bioequivalent to brand-name medications, but the quality and purity of generic medications are still debatable. The aim of this study was to compare the generic product of metformin (MET) to its branded counterpart using pure MET powder as a reference. Quality control tablet assessment and in vitro evaluation of drug release were carried out in various pH media. Additionally, several analytical methods and thermal techniques were used, namely differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), X-ray diffraction (XRD), scanning electron microscopy (SEM), Fourier-transform infrared (FTIR), and confocal Raman microscopy. The results showed a significant difference between the two products. In terms of friability assessment, mean resistance force, and tablet disintegration, the generic MET product showed significant weight loss, higher mean resistance force, longer disintegration time, and a slower rate of drug release. In addition, DSC and TGA showed that the generic product had the lowest melting point and the least weight loss compared to the branded product and pure powder. XRD and SEM demonstrated some changes in the crystallinity structure of the molecule particles for the generic product. Additionally, FTIR and confocal Raman revealed the same peaks and band shifts in all samples, but with differences in the intensity for the generic tablet only. The observed differences could be due to the use of different excipients in the generic product. The possibility of forming a eutectic mixture between the polymeric excipient and metformin in the generic tablet was presumed, which might be attributed to alterations in the physicochemical properties of the drug molecule in the generic product. In conclusion, using different excipients might have a significant effect on the physicochemical properties of drugs in generic formulations, leading to significant changes in drug release behavior.

Enteric-coating film effect on the delayed drug release of pantoprazole gastro-resistant generic tablets.

Background: Enteric coating films in acidic labile tablets protect the drug molecule from the acidic environment of the stomach. However, variations in the excipients used in the coating formulation may affect their ability to provide adequate protection. This study is the first to investigate the potential effects of coating materials on the protective functionality of enteric coating films for pantoprazole (PNZ) generic tablets after their recall from the market. Methods: A comparative analysis was conducted between generic and branded PNZ products, using pure drug powder for identification. The in vitro release of the drug was evaluated in different pH media. The study also utilized various analytical and thermal techniques, including differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), X-ray diffraction (XRD), scanning electron microscopy (SEM), Fourier-transform infrared (FTIR), and confocal Raman microscopy. Results: The in vitro assessment results revealed significant variations in the release profile for the generic product in acidic media at 120 min. DSC and TGA thermal profile analyses showed slight variation between the two products. XRD analysis exhibited a noticeable difference in peak intensity for the generic sample, while SEM revealed smaller particle sizes in the generic product. The obtained spectra profile for the generic product displayed significant variation in peaks and band intensity, possibly due to impurities. These findings suggest that the excipients used in the enteric coating film of the generic product may have affected its protective functionality, leading to premature drug release in acidic media. Additionally, the presence of polysorbate 80 (P-80) in the brand product might improve the properties of the enteric coating film due to its multi-functionality. Conclusions: In conclusion, the excipients used in the brand product demonstrated superior functionality in effectively protecting the drug molecule from acidic media through the enteric coating film, as compared to the generic version.

Repurposing SGLT2 Inhibitors for Neurological Disorders: A Focus on the Autism Spectrum Disorder.

Autism spectrum disorder (ASD) is a neurodevelopmental disorder with a substantially increasing incidence rate. It is characterized by repetitive behavior, learning difficulties, deficits in social communication, and interactions. Numerous medications, dietary supplements, and behavioral treatments have been recommended for the management of this condition, however, there is no cure yet. Recent studies have examined the therapeutic potential of the sodium-glucose cotransporter 2 (SGLT2) inhibitors in neurodevelopmental diseases, based on their proved anti-inflammatory effects, such as downregulating the expression of several proteins, including the transforming growth factor beta (TGF-ß), interleukin-6 (IL-6), C-reactive protein (CRP), nuclear factor κB (NF-κB), tumor necrosis factor alpha (TNF-α), and the monocyte chemoattractant protein (MCP-1). Furthermore, numerous previous studies revealed the potential of the SGLT2 inhibitors to provide antioxidant effects, due to their ability to reduce the generation of free radicals and upregulating the antioxidant systems, such as glutathione (GSH) and superoxide dismutase (SOD), while crossing the blood brain barrier (BBB). These properties have led to significant improvements in the neurologic outcomes of multiple experimental disease models, including cerebral oxidative stress in diabetes mellitus and ischemic stroke, Alzheimer's disease (AD), Parkinson's disease (PD), and epilepsy. Such diseases have mutual biomarkers with ASD, which potentially could be a link to fill the gap of the literature studying the potential of repurposing the SGLT2 inhibitors' use in ameliorating the symptoms of ASD. This review will look at the impact of the SGLT2 inhibitors on neurodevelopmental disorders on the various models, including humans, rats, and mice, with a focus on the SGLT2 inhibitor canagliflozin. Furthermore, this review will discuss how SGLT2 inhibitors regulate the ASD biomarkers, based on the clinical evidence supporting their functions as antioxidant and anti-inflammatory agents capable of crossing the blood-brain barrier (BBB).

Translation and validation of the Arabic version of the Morisky, Green and Levine (MGL) adherence scale.

The Morisky Green Levine (MGL) adherence scale is a 4-item tool used for the detection of medication nonadherence among patients with chronic health conditions. Despite being widely used in Arabic-speaking research contexts, it has never been validated in Arabic language. The aim of this study was to translate and validate the MGL tool into Arabic. A standard forward-backward process was used to translate the questionnaire. Cronbach's alpha coefficient was measured to assess internal consistency of the scale. The test-retest reliability measured the consistency of participants' responses over time. Construct validity was evaluated by Explanatory factor analysis (EFA); Kaiser-Meyer-Olkin value and Bartlett's test of sphericity were determined. Convergent validity was assessed using a preexisting medications Arabic Adherence Assessment Tool (AAAT). The model fit was evaluated using confirmatory factor analysis (CFA). Associations between the MGL scale scores and the patient demographic/clinical characteristics were tested by linear regressions. A total of 201 participants were included into the study. The MGL scale categorization revealed that 20.9%, 59.2% and 19.9% of the participants had high, moderate and low levels of adherence respectively. Adequate internal consistency (alpha = 0.593) was observed. A significant strong ICC and Pearson's correlations were generated between responses at time 1 and time 2. EFA results elucidated the suitability of the data for factor analysis. Pearson's coefficient (r) revealed a significant strong correlation between MGL scale and AAAT. CFA results confirmed a good fit for the suggested model. Linear regression revealed higher number of medications, more frequent outpatient clinic visits and not experiencing medication adverse effect factors significantly associated with better adherence. The Arabic version of MLG scale is a reliable valid tool to assess adherence among Arabic-speaking communities. Implementing interventions targeting patients not compliant to regular clinic visits and those at higher risk of experiencing medication side effects can greatly enhance medication adherence.

Role of Brain Modulators in Neurodevelopment: Focus on Autism Spectrum Disorder and Associated Comorbidities.

Autism spectrum disorder (ASD) and associated neurodevelopmental disorders share similar pathogenesis and clinical features. Pathophysiological changes in these diseases are rooted in early neuronal stem cells in the uterus. Several genetic and environmental factors potentially perturb neurogenesis and synaptogenesis processes causing incomplete or altered maturation of the brain that precedes the symptomology later in life. In this review, the impact of several endogenous neuromodulators and pharmacological agents on the foetus during pregnancy, manifested on numerous aspects of neurodevelopment is discussed. Within this context, some possible insults that may alter these modulators and therefore alter their role in neurodevelopment are high-lighted. Sometimes, a particular insult could influence several neuromodulator systems as is supported by recent research in the field of ASD and associated disorders. Dopaminergic hy-pothesis prevailed on the table for discussion of the pathogenesis of schizophrenia (SCH), atten-tion-deficit hyperactivity disorder (ADHD) and ASD for a long time. However, recent cumulative evidence suggests otherwise. Indeed, the neuromodulators that are dysregulated in ASD and comorbid disorders are as diverse as the causes and symptoms of this disease. Additionally, these neuromodulators have roles in brain development, further complicating their involvement in comorbidity. This review will survey the current understanding of the neuromodulating systems to serve the pharmacological field during pregnancy and to minimize drug-related insults in pa-tients with ASD and associated comorbidity disorders, e.g., SCH or ADHD.

In Vitro and In Vivo Evaluation of Oral Controlled Release Formulation of BCS Class I Drug Using Polymer Matrix System.

Diltiazem hydrochloride is a calcium channel blocker, which belongs to the family of benzothiazepines. It is commonly used to treat hypertension and atrial fibrillation. Even though the drug has high solubility, its high permeability and rapid metabolism in the liver can limit the bioavailability and increase the dose frequencies for up to four times per day. This study focused on a polymer matrix system not only to control the drug release but also to prolong the duration of bioavailability. The polymer matrices were prepared using different ratios of poloxamer-188, hydroxypropyl methylcellulose, and stearyl alcohol. In vitro and in vivo assessments took place using 24 rabbits and the results were compared to commercially available product Tildiem® (60 mg tablet) as reference. Overall, the rate of drug release was sustained with the gradual increase of poloxamer-188 incorporated with hydroxypropyl methylcellulose and stearyl alcohol in the matrix system, achieving a maximum release period of 10 h. The oral bioavailability and pharmacokinetic parameters of diltiazem hydrochloride incorporated in polymer matrix system were similar to commercial reference Tildiem®. In conclusion, the combination of polymers can have a substantial effect on controlling and prolonging the drug release pattern. The outcomes showed that poloxamer-188 combined with hydroxypropyl methylcellulose and stearyl alcohol is a powerful matrix system for controlling release of diltiazem hydrochloride.

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

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.

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

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.

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

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.

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

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.

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