Turkish Journal of Pharmaceutical Sciences最新文献

Objectives: Drug information systems are commonly used by professionals to assist in the identification of drug interactions and to ensure the safe use of medications. Real-world evidence about the comparison of different drug interaction sources is scarce. We aimed to compare two drug interaction databases to identify interactions in a population-based survey.

Materials and methods: This is a cross-sectional study based on a previous survey performed in the city of Manaus, Brazil, in 2019. We included adults aged 18 years and over, who used two or more medicines 15 days before the interview. To assess potential drug interactions, we searched Micromedex and UpToDate databases. The primary outcome was the prevalence of potential drug interactions in each database. Weighted Kappa statistics were calculated to assess agreement on the presence of drug interaction, documentation and severity.

Results: A total of 752 participants were included in the study. The prevalence of drug interactions was 43.8% [95% confidence interval (CI): 40.2, 47.3%] in UpToDate and 30.2% (95% CI: 26.9, 33.5%), in Micromedex. The agreement related to drug interactions between the two databases was fair (Kappa: 0.631). For severity (Kappa: 0.398) and documentation (Kappa: 0.311), the agreement was poor.

Conclusion: Agreement among compared databases was sub-optimal. Better quality and transparency of evidence available in drug interaction sources are needed to support informed healthcare professionals' decision.

Objectives: Interferons (IFNs) are one of the most important components of innate immunity against viruses, especially those carrying the RNA genomes such as influenza viruses. Upon viral infection, the IFNs are rapidly secreted, inducing the expression of several genes in the target cells and establishing an antiviral state. In this study, the effects of proteins encoded by some IFN-related genes on influenza A virus RNA-dependent RNA polymerase enzyme were investigated. We evaluated the importance of these proteins in the pathogenesis of different influenza A virus types.

Materials and methods: The IFN-related genes were amplified by polymerase chain reaction from the HEK293 cDNA library and cloned into pCHA expression vector. The expression of genes and subcellular localizations of the proteins were determined by Western blotting and immunofluorescence staining, respectively. The effects of IFNs-related proteins on virus RdRP enzyme were determined by influenza A virus mini-replicons.

Results: The study revealed that the influenza A virus infections significantly altered the transcript level of the IFN-related CCL5, IFIT1, IFIT3, IFITM3, and OAS1 genes in HEK293 cells. It was determined that the alteration of the gene expression was also related to the virus type. The mini-replicon assays showed that the transient expression of CCL5, IFI27, OAS1, IFITM3, IFIT1, and IFIT3 have inhibitory effects on WSN and/or DkPen type virus RdRP enzymes. We observed that the proteins except OAS1 inhibited WSN type RdRP enzyme at a higher level than that of DkPen enzyme.

Conclusion: It was concluded that influenza A virus infection significantly alters the IFN-related gene expression in the cells. Most of the proteins encoded from these genes showed an inhibitory effect on the virus RdRP enzymes in the HEK293 cells. The inhibition of the influenza virus RdRP with IFN-related proteins may be the result of direct or indirect interactions between the host proteins and the viral enzyme subunits.

Objectives: Cancer diseases have been linked to a huge number of causes that led to deaths in this century along with cardiovascular and lung diseases. Most death-leading types of cancer are colon, lung, breast, and prostate cancers. Due to the remarkable properties of gold (Au) nanocarrier, they are used to deliver and improve tamoxifen (Tam) citrate activity in Caco-2 and MCF-7 cells.

Materials and methods: In this study, preparation of Au nanoparticles (NPs), zeta-potential and size, high resolution transient electron microscopy (HRTEM), high-performance liquid chromatography, ultraviolet-visible spectra, fluorescence microscopy, fourier infrared spectroscopy, and real-time cellular analysis xCELLigence technology were investigated.

Results: The zeta-average size of the Tam- β-cyclodextrin (β-CD)-hyaluronic acid (HA)-chitosan (Chi)-Au nanocomposite is 82.02 nm with a negative zeta potential of -23.6. Furthermore, HRTEM images showed that, successful formulation of polymer shell around Au core and the Au NP shape is mostly spherical, triangle and irregular. Furthermore, the fluorescence microscope image showed proper cellular uptake of the Tam-β-CD-HA-Chi-Au nanocomposite in MCF-7 and Caco-2 cells. Additionally, Tam-β-CD-HA-Chi-Au nanocomposite significantly improved the cytotoxic activity of Tam citrate on Caco-2 cells. IC₅₀ value of Tam reduced from 8.55 µM to 5.32 µM, after 48 h of incubation time (p value <0.00001).

Conclusion: This study showed that Tam-β-CD-HA-Chi-Au nanocomposite is a potential nanocarrier for delivering the drug to Caco-2 and MCF-7 cancer cells, since it has improved Tam citrate activity on colorectal cancer cells. After all, the developed formula showed more effect on Caco-2 than MCF-7. The prepared nanocomposite could be used to improve the cancer therapy in clinical trials.

Objectives: Racecadotril is an anti-diarrheal drug that has the indication to reduce the secretion of water and electrolytes into the intestine. It has an unpleasant taste, when administered orally. The presenting study developed a pharmaceutical racecadotril dispersible tablet, which masked the unpleasent taste using wet granulation method. For this reason, the effect of the number of ethylacrylate-methylmethacrylate copolymers (Eudragit^® NE 30D) in taste masking and in vitro dissolution of the finished product was investigated.

Materials and methods: Taste-masked racecadotril granules were prepared using Eudragit^® NE 30D and the ratio between the amounts of racecadotril and Eudragit^® NE 30D involved in the formulation was optimized. The products obtained in the dispersible tablet dosage form were evaluated in terms of taste and in vitro dissolution studies. In vitro dissolution profiles of the products obtained in this study were compared with reference product Tiorfan^® granules for oral suspension manufactured by Bioprojet Pharma (Paris, France). A method of apparatus II (paddle), 900 mL, pH 4.5 acetate buffer + 1% sodium dodecyl sulfate (SDS) and 100 rpm at 37.0 ± 0.5°C was adopted.

Results: Results of the studies have shown that the formulation should have Eudragit^® NE 30D higher than 1% by weight of racecadotril to satisfy the taste-masking ability and the formulation should have Eudragit^® NE 30D equal or lower than 10% by weight of racecadotril to have better release characteristic to be compatible with reference product.

Conclusion: Our results demonstrated that a chemically long-term stable racecadotril dispersible tablet product, whose taste is efficiently masked using wet granulation method with an acceptable release profile was obtained with Eudragit^® NE 30D ratio higher than 1% and equal or lower than 10% by weight of racecadotril. The developed formulation can increase patient compliance.

English oral delivery of drug was the commonly used modality because of patient compliance and ease of administration. After oral administration of any drug, its bioavailability is affected by its residence time in stomach. Recently, gastroretentive drug delivery systems (GRDDS) have gained wide acceptance for drugs with a narrow absorption window, decreased stability at high alkaline pH, and increased solubility at low pH. This approach develops a drug delivery system, which gets retained within gastric fluid, thereby releasing its active principles in the stomach. Some methods used to achieve gastric retention of drugs include the use of effervescence agents, mucoadhesive polymers, magnetic material, bouncy enhancing excipient, and techniques that form plug-like devices that resist gastric emptying. This review provides a concise account of various attributes of recently developed approaches for GRDDS.

Objectives: Datura stramonium L., D. stramonium var. tatula (L.) Torr., Hyoscyamus reticulatus L., H. niger L., and Atropa caucasica Kreyer naturally found in Azerbaijan and their seeds possess 17-35% of oils. This study aims to evaluate and determine fatty acids of these plants special to Azerbaijan climate and geography. The presented study is the first to research into fatty acids of A. caucasica, which is an endemic species of Caucasus.

Materials and methods: Fatty acid seed oils were derivatized to methyl esters and analyzed by gas chromatography equipped with a flame ionization detector, compared with a standard mixture of 37 fatty acid methyl esters.

Results: Linoleic (55-79%), oleic (11-26%), palmitic (4-12%), and stearic (2-3%) acids compose 97% of total fatty acids. Other minor compounds, including two trans-fatty acids, were determined in the samples. Significantly high concentration of a medicinally important polyunsaturated fatty acid, e.g. linoleic acid, was observed in all samples.

Conclusion: The results of this study showed that these oils are particularly valuable sources of linoleic and oleic acids, which have beneficial effects on cardiovascular diseases and are important compounds for the pharmaceutical and cosmetic industries in the manufacture of liposomes, nano- and microemulsions, soaps, etc.

Objectives: Atazanavir sulfate (AS), a Biosafety Cabinet (BCS) class II antiretroviral drug, shows dissolution rate-limited bioavailability, therefore, it is necessary to improve its solubility and oral bioavailability. The present investigation is intended to improve the aqueous solubility by developing AS-loaded nanoparticles (ASNPs). Additionally, the immediate release formulation of AS capsules has gastrointestinal side effects such as nausea and abdominal pain, cardiovascular side effect, e.g. abnormal cardiac conduction, toxic effects on kidney and liver such as nephrolithiasis, hyperbilirubinemia, and jaundice. Therefore, ASNPs were designed to release the drug slowly for 12 h, so that these side effects could be reduced.

Materials and methods: ASNPs were prepared using gamma-cyclodextrin (γ-CD) and the crosslinker dimethyl carbonate were characterized by differential scanning calorimetry (DSC) and X-ray diffraction (XRD) to check the crystal characteristics of AS upon entrapment in NPs. Entrapment efficiency (EE), particle size, morphology, solubility, and dissolution behavior were also determined.

Results: EE%, particle size, and zeta potential varied from 14.38 ± 0.16 to 75.97 ± 0.28%, 65.4 ± 1.25 nm to 439.6 ± 2.21 nm, and 28.3 ± 0.1 mV to 41.0 ± 0.3 mV, respectively. XRD and DSC confirmed the transformation of the crystalline AS to amorphous in NPs. There was 11.717 folds rise in AS solubility in water from NPs. The formulation having AS: γ-CD, 1:1 at 10 mg/mL, depicted 88.55 ± 0.58, 91.23 ± 0.80, and 86.8 ± 0.65% drug release in water, acid buffer, and phosphate buffer, respectively, in 12 h.

Conclusion: Solubility enhancement could be attributed to the decrease in crystallinity of atazanavir, when dispersed in NPs.

Objectives: Coronavirus Disease-2019 (COVID-19) pandemic has a massive impact on human health, causing sudden lifestyle changes. As it affects health, determining the lifestyles of university students related to smoking has gained importance. This study provides evidence of change in smoking behavior among university students in Türkiye during the ongoing COVID-19 pandemic.

Materials and methods: This cross-sectional survey study was conducted via an electronic questionnaire approximately 2020-2021 among university students in Türkiye. The study comprised a structured questionnaire that inquired about demographic information; and the Fagerström Test for Nicotine Dependence. The questionnaire was distributed randomly to university students; it required 6 min to complete.

Results: A total of 749 respondents were included in the study, aged between 19 and 35 years (54.8% females). Of 749 participants, 571 health science students (medicine, pharmacy, dentistry, etc.) completed the survey. The pre-pandemic and COVID-19 pandemic mean nicotine dependence scores were 3.03 and 2.97, respectively. A difference was seen pre-pandemic (p= 0.002) and during pandemic (p= 0.005) for those studying in health and other departments. Students who had middle socio-economical status had significantly higher nicotine dependence scores pre- COVID-19, compared to during the pandemic (p= 0.027). Compared to pre and during the pandemic, the mean score of dependence was significantly lower in students, whose parents were non-smokers during the pandemic.

Conclusion: In this study, we have provided the first data on the Turkish university student's nicotine dependence changes during the COVID-19 lockdown. The nicotine dependence level may change based on various factors including behavioral changes. Crucial times such as pandemics can affect individuals, thus, smoking addiction can increase. Behavioral support for quitting smoking such as digital platforms, internet, and television programs should also assist to support smokers quitting successfully during this supreme time.

Objectives: Pseudomonas aeruginosa has been globally implicated in healthcare-associated infection. The susceptibility pattern of clinical isolates of P. aeruginosa to anti-pseudomonal antibiotics is reported.

Materials and methods: Clinical samples, namely blood, urine, tracheal aspirate, cerebrospinal fluid (CSF), wound swabs, high vaginal swabs, eye, and ear exudates were obtained from patients, processed and identified using standard microbiological protocols. Antibiotic susceptibility testing was undertaken using the Kirby Bauer Disc diffusion method. Results were reported following the Clinical and Laboratory Standards Institute guidelines.

Results: Of 104 P. aeruginosa isolates identified, males (52.88%) had a higher incidence of infection than female (47.11%) patients. The highest prevalence was recorded from wound swabs [46 (44.23%)] followed by ear exudates [23 (22.12%)], urine [22 (21.15%)], while eye exudates and samples from the CSF yielded the least [1 (0.96% each)]. From the antibiogram, imipenem had the highest antibiotic activity (91.3%) followed by polymyxin B (84.6%). The isolates exhibited the highest resistance to ceftazidime (73.1%) and piperacillin-tazobactam (61.5%). The antibiotic susceptibility pattern of P. aeruginosa isolates revealed 7.69% susceptible, 26% resistant, 61% multidrug resistance (MDR), 5% extremely drug resistance (XDR), and an absence (0%) of pandrug-resistant phenotypes.

Conclusion: The study recorded alarmingly high cases of MDR and some XDR phenotypes of P. aeruginosa in University of Port Harcourt Teaching Hospital. It will help identify existing gaps in antimicrobial resistance surveillance and assist in improving public health policies regarding antibiotic stewardship, initiatives, and interventions.