Turkish journal of pharmaceutical sciences最新文献

Objectives: This study aimed to incorporate a pharmacy management course into pharmacy education and explore students' time management and career planning attitudes in relation to this course.

Materials and methods: This research, conducted between October 2, 2023, and January 12, 2024, employed a mixed-methods design, integrating both qualitative and quantitative research methodologies within a single study framework. Quantitative data were collected using the Sociodemographic Form, Career Futures Inventory (CFI), and Time Management Questionnaire (TMQ). A semi-structured interview form was employed to gather qualitative data. This study included 60 fifth-year pharmacy students. The experimental group (n=30) comprised volunteers enrolled in the "Management in Pharmacy" elective course, while the control group (n=30) consisted of randomly selected volunteers not enrolled in the course.

Results: In the intervention group, pre-test TMQ scores ranged from 56 to 117, yielding a mean score of 80.50±16.12. Post-test scores ranged from 55 to 112, with an average of 86.83±14.09. There was a significant difference in the change in the TMQ scores and Time Attitude scores between the control and intervention groups (p=0.003 and p=0.001, respectively). For the intervention group, pre-test CFI scores ranged from 63 to 116, yielding a mean score of 85.93±15.34. Post-test scores ranged from 68 to 111, with an average of 89.40±12.56. No significant difference was observed in the change in the CFI scores between the control and intervention groups (p=0.311). Student feedback provided insight into the necessity or usefulness, impact, and future suggestions concerning the delivery of this course.

Conclusion: The implementation of educational resources and methodologies aimed at fostering time management abilities and encouraging career planning attitudes from the initial phases of pharmacy education may result in greater outcomes.

Objectives: Lycopene is a powerful antioxidant with diverse health benefits. However, it belongs to the Biopharmaceutics Classification System II; thus, it depicts poor water solubility and dissolution. Its lipophilic nature hinders the bioavailability of this drug. To overcome these limitations, namely, poor solubility and bioavailability, several approaches have been tried so far, such as co-solvency, size reduction or micronization, complexation, adsorption on high surface area carriers, etc. The present research aimed to apply the liquisolid technique to prepare lycopene liquisolid compacts with an improved dissolution profile. The impact of parameters such as carrier and drug concentration percentage on drug dissolution was evaluated in liquisolid compacts.

Materials and methods: Lycopene was extracted by Soxhlet extractionand then characterized by ultraviolet spectroscopy, infrared spectroscopy, thin-layer chromatography, and melting point. Liquisolid compacts of lycopene were formulated by using excipients such as non-volatile solvent (glycerine), carrier (Avicel PH 101, Fujicalin, Neusilin US2), disintegrant (Croscarmellose sodium), and diluent (lactose). The different formulation batches of liquisolid compacts were formulated and evaluated based on different pre-compression and post-compression parameters.

Results: Powder X-ray Diffraction (PXRD) and Fourier transform infrared spectroscopy were utilized to analyze drug-excipient interaction; these studies showed no evidence of any physical or chemical interaction between the drug(s) and the excipients. The PXRD of lycopene showed sharp and intense peaks at diffraction angles (2θ) such as 12.563, 19.176, 19.636, 20.062, 21.283, 26.629, 29.479, 30.235, and 39.997, which indicates a crystallinestructure. The PXRD of the physical mixture of lycopene and excipients showed similar sharp peaks (12.582, 19.202, 19.634, 20.045, 21.304, 26.565, 29.474, 30.250, and 40.065), indicating thatthere is no drug-excipient interaction occurring. Lycopene was extracted and characterized. IR spectroscopy and PXRD showed no drug-excipient interaction. The lycopene liquisolid compacts passed both pre-compression and post-compression evaluations within acceptable limits.

Conclusion: The formulation batch F-7, formulated with Neusilin US2 as a carrier and 40% drug concentrationshowed 98% in vitro drug release and thus it was selected as the optimized formulation with improved dissolution.

Objectives: This study focused on synthesizing and characterizing novel thiosemicarbazide derivatives containing a 1,2,4-triazole moiety and evaluating their antimicrobial activity against several bacterial strains. The research aimed to identify key structural features that enhance antimicrobial efficacy through structure-activity relationship analysis and identify the minimum inhibitory concentration (MIC) of the most potent compounds to assess their potential for further development as antimicrobial agents.

Materials and methods: Nine novel thiosemicarbazide derivatives containing a 1,2,4-triazole moiety were synthesized by reacting 1,2,4-triazole derivatives with thiosemicarbazide precursors, and the products were characterized using infrared spectroscopy, proton nuclear magnetic resonance (¹H-NMR), carbon-13 nuclear magnetic resonance (¹³C-NMR) spectroscopy, and elemental analysis. The antimicrobial activity of these compounds (5a-i) was tested against Klebsiella pneumoniae (K. pneumoniae),Escherichia coli, Staphylococcus aureus, Enterococcus faecalis, and Pseudomonas aeruginosa (P. aeruginosa), using microdilution, disk diffusion, and broth microdilution methods. Dimethyl sulfoxide was used as a negative control, and Vancomycin and Meropenem were used as positive controls, with all results converted to µM for consistent analysis.

Results: The synthesized thiosemicarbazide derivatives (5a-i) were confirmed to be structurally correct through Fourier-transform infrared spectroscopy, ¹H-NMR, and ¹³C-NMR spectroscopy. Among the tested compounds, 5e (4-bromophenyl) and 5g (n-propyl) showed significant antimicrobial activity, with 5g exhibiting the strongest effects against S. aureus and P. aeruginosa. Other derivatives, such as 5b (4-NO₂Ph), 5c (4-FPh), and 5d (4-ClPh), showed moderate activity, while no significant activity was observed against K. pneumoniae or E. faecalis.

Conclusion: The study successfully synthesized a series of novel thiosemicarbazide derivatives with a 1,2,4-triazole moiety and evaluated their antimicrobial potential. Compounds 5e and 5g exhibited significant antibacterial activity, particularly against S. aureus and P. aeruginosa, with MIC values in the low micromolar range. These findings suggest that the compounds hold promise as potential antimicrobial agents, and further studies should focus on optimizing their efficacy and exploring their mechanism of action.

Objectives: Norvir^® oral powder [ritonavir (RTV)] employs polyvinylpyrrolidone/vinyl acetate as the polymer to formulate an amorphous solid dispersion. Its oral absolute bioavailability is 70% in the fasted state, and it has negative food effects. The aim of this study was to perform in vitro dissolution of Norvir^® powder and Wagner-Nelson deconvolution of in vivo data under fasted, moderate fat, and high fat conditions in order to elucidate the relevance of in vitro dissolution testing.

Materials and methods: In vitro dissolution of Norvir^® oral powder was conducted, and the human pharmacokinetic data of Norvir^® powder were obtained from literature, under fasted, moderate fat, and high fat conditions. Wagner-Nelson deconvolutions were performed. The absolute fraction absorbed (F_a) profiles were compared to the in vitro dissolution (F_d) profiles. Levy-Polli plot analysis was also conducted. For each pharmacokinetic condition, a scale factor was estimated to approximate the extent to which in vitro dissolution needed to be slowed down to mimic in vivo dissolution.

Results: Qualitatively, there was a large difference between in vitro and in vivo dissolution. In vitro dissolution showed 98% release in 5 minutes. Meanwhile, from Wagner-Nelson analysis, only 5.5% of the drug dissolved (and absorbed) in vivo in 5 min under fasted conditions. It was not until 2 hr that 49% of the RTV dose dissolved (and was absorbed) in vivo. In vivo, moderate fat and high fat conditions were even slower in producing a certain effect. The Levy-Polli plot exhibited a "reverse-L" profile. It was concluded that such rapid in vitro dissolution did not mimic the in vivo dissolution of RTV.

Conclusion: Biopharmaceutic consideration of in vitro dissolution, in vivo pharmacokinetics, and deconvolution analysis indicated that in vitro dissolution was "too rapid" to adequately mimic in vivo dissolution. Findings suggest greater inspection of in vitro methods for poorly water-soluble drugs, especially those drugs where in vivo absorption is expected to be rate-limited by dissolution.

Objectives: Corporate social responsibility (CSR) is defined as companies voluntarily taking action with their resources to help solve some of the social, economic, and environmental problems of the society in which they operate. This study aimed to reveal the current status of CSR projects in the pharmaceutical industry, which are strategically important on a global scale.

Materials and methods: The study was conducted between June and December 2019 using a structured online survey. The form included both multiple-choice and open-ended questions. This survey yielded both qualitative and quantitative data about the structure, size, and products of the companies, as well as details of CSR projects.

Results: A total of 60 companies participated in the study. Our survey results indicated that 83.33% of the pharmaceutical companies undertook CSR projects, and there was no statistically significant difference in the number of projects undertaken according to either the type of products the companies marketed or the companies' country of origin (p>0.05). It was found there were statistically significant differences with other factors such as project fields, the number of projects over the years, and the responsible department (p<0.05). When we examined the details of specific CSR projects, we observed that some companies, regardless of their national or multinational position, undertook sustainable projects that involved a broader array of stakeholders and appealed to various shareholder groups. Some companies undertook studies for patients, patient relatives, or society based on philanthropic activities or short-term social projects on local issues, instead of long-term projects within the scope of CSR initiatives.

Conclusion: Pharmaceutical companies carry out CSR projects as an important public relations activity in terms of reaching their stakeholders.

Objectives: Bortezomib (BTZ) functions as an androgen receptor signalling inhibitor, is used for the treatment of prostate cancer, and has been sanctioned by the United States Food and Drug Administration. The medicinal applications of BTZ are impeded by low solubility, first-pass metabolism, and restricted bioavailability. This study aimed to develop and enhance polylactic acid-co-glycolic acid (PLGA) nanobubbles (NBs) as a sustained-release mechanism for BTZ, thereby augmenting stability and bioavailability.

Materials and methods: Seventeen experimental runs were conducted to optimize drug-PLGA NBs using a three-factor, three-level Box-Behnken Design. The improved formulation comprised 30 mg of medication, 250 mg of PLGA, and 2.0% w/v polyvinyl alcohol as a stabilizing agent.

Results: The NBs exhibited a particle size of 186.9±13.9 nm, a polydispersity index of 0.146±0.042, and a zeta potential of -21.4±2.28 mV, along with an entrapment efficiency of 66.12±1.48%. Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction analysis verified the absence of drug-polymer interactions, whereas scanning electron microscopy demonstrated uniform spherical nanoparticles. In vitro experiments demonstrated superior drug release, and stability assessments indicated no major alterations after one month. Pharmacokinetic studies in rats demonstrated an elevated C_max (1.69) and area under the curve from time 0 to t (1.63), signifying enhanced sustained release and absorption. The results underscore the capability of BTZ-loaded PLGA NBs to augment drug kinetics and bioavailability, hence facilitating targeted distribution and enhanced therapeutic efficacy.

Conclusion: This investigation offered significant insights into the factors influencing oral absorption in NB formulations, which can guide future methods for oral medication development. BTZ-loaded PLGA nanobubbles showed promising results by enhancing oral absorption and improving pharmacokinetics in the study, which points to their potential use in sustained-release drug delivery. These findings offer a stepping stone toward nanomedicine via the oral route in future drug development.

Objectives: The study aimed to combine instant-release and mini-tablet methodologies to develop novel orally disintegrating mini-tablets (ODMTs) for a frequently pescribed antibiotic, cefixime trihydrate (CT), in paediatric patients.

Materials and methods: CT-loaded microcapsules were prepared using Eudragit^® EPO and Hydroxy Propyl Methyl Cellulose E50 by spray drying technique. The optimized microcapsules were mixed with co-processed ready-to-use tableting excipients, Ludiflash and Pearlitol 200SD, in different proportions and then compressed into ODMTs and evaluated.

Results: The particle size of CT microcapsules was found to be between 111.8 and 225.87 μm, suitable for oral delivery. The entrapment efficiency was found to be between 94.8% and 95.45%. Pre-compression and post-compression parameters indicated suitability for formulation. In vitro evaluation of ODMTs showed immediate disintegration within 15 seconds in the oral cavity as soon as they came in contact with saliva. Upon swallowing these microcapsules, the microcapsules completely dissolve in the gastrointestinal tract, releasing 100% of the drug (CT) within 15 minutes. The release kinetics of ODMTs were found to follow Hixson-Crowell kinetics for Eudragit^® EPO and Korsmeyer-Peppas kinetics for Hydroxy Propyl Methyl Cellulose E50 microcapsules. Scanning electron microscopy images demonstrated that the microcapsules were intact even after compression into ODMTs. Stability studies proved that the formulations were stable as per the International Council for Harmonisation guidelines.

Conclusion: A novel solid oral dosage form of CT ODMTs of 2 mm diameter was successfully developed using Eudragit^® EPO and Hydroxy Propyl Methyl Cellulose E50 in combination with co-processed ready-to-use tableting excipients such as Ludiflash and Pearlitol 200SD.

Objectives: It aimed to evaluate talent management practices in pharmaceutical companies according to different departments such as medical and marketing, and determine the effect of talent management on employee performance.

Materials and methods: The impact of talent management practices on employee performance was evaluated by applying survey to medical directors/regional medical directors and product managers/brand managers/brand specialists working in pharmaceutical companies. The Talent Management Practices Scale and the Employee Performance Scale were used. The online survey was applied to volunteer participants between March 2021 and March 2023. The data obtained from the participants were analyzed using SPSS ver 22.0. The effect of the sub-dimensions of talent management on employee performance was determined. In this research, Pearson characteristic test, regression test, Independent Groups t-test, and analysis of variance test were used to determine the relationship between variables.

Results: A total of 112 people, 51 female (45.5%) and 61 men (54.5%), participated in the study. The impact of talent management practices on employee performance, it varies depending on age, gender, education level, position in the company, the company's national or multinational status, and working period. This study revealed statistically significant differences in talent management perceptions based on gender (p<0.05), education level (p<0.05), age categories (p<0.05), and job categories (p<0.05), with job categories also significantly impacting employee performance (p<0.05). Correlation analyses indicated a statistically significant positive relationship between talent management's commitment (r=0.552; p<0.001) and retention (r=0.448; p<0.001) sub-dimensions and overall employee performance. Furthermore, a statistically significant regression model (F(7,104)=10.224; p<0.001) demonstrated that commitment, retention, and training aspects of talent management collectively explain 40.8% of the variance in employee performance. As a result of the analyses, it was determined that commitment and employee retention, which are subdimensions of talent management practices, has a positive relationship with employee performance.

Conclusion: According to survey results talent management affects employee performance. Evaluations of participants in the pharmaceutical industry revealed that the Attraction, Selection-Placement, Training, and Talent pool sub-dimensions of talent management practices implemented by businesses had a positive but weak effect on employee performance. The commitment and retention sub-dimensions were found to have a positive, moderate effect on employee performance.

Objectives: The skin is highly vulnerable to damage caused by free radicals, which disrupt biological components and accelerate aging. While endogenous antioxidants provide some protection, external sources are often needed. Rosella (Hibiscus sabdariffa L.) is a rich source of flavonoids and astaxanthin, proven antioxidants that inhibit matrix metalloproteinase-1, prevent collagen degradation, and reduce ultraviolet-induced damage. The aim of the study was to optimize the formulation of a peel-off mask, incorporating Rosella extract as an antioxidant.

Materials and methods: Rosella extract was analyzed using liquid chromatography-mass - mass spectrometry (LC-MS) to identify its antioxidant components. Freeze-dried Rosella powder was granulated and incorporated into a gel mask using polyvinyl alcohol (PVA) or gelatin as the base polymer. Formula optimization was conducted using simplex lattice design and evaluated for physical properties, antioxidant activity, and stability.

Results: LC-MS analysis detected astaxanthin, quercetin, rutin, and kaempferol in Rosella extract. Granulated Rosella exhibited good flowability and a particle size distribution of 250-425 μm. The optimized formula was PVA-based, containing 12.5% PVA and 7.5% propylene glycol. The product demonstrated desirable physical properties, including a drying time of 5.29 minutes, a pH of 5.32, a spreadability of 5.34 cm, an adhesivity of 6.86 seconds, and a viscosity of 30,658 cP. Stability tests confirmed the formula remained stable for 3 months, under room temperature, freeze-thaw cycles, and centrifugation. The final product, containing 15% Rosella, exhibited 45.33% antioxidant activity.

Conclusion: The PVA-based Rosella peel-off mask demonstrated optimal physical properties, stability, and antioxidant properties, offering a promising approach to incorporating antioxidants into cosmetic formulations.

Objectives: Michigan cancer foundation-7 (MCF-7) breast-cancer cells are recognized for their resilience against conventional chemotherapy drugs and apoptosis-triggering agents. Nanosponges (NSs) have emerged as promising drug-delivery systems in cancer therapy because of their ability to encapsulate and deliver therapeutic agents efficiently. The aim of this study was to establish the combined beneficial anticancer impacts of NSs alpha-amyrin (AMY) and higenamine (HGN) on MCF-7 breast-cancer cells.

Materials and methods: NSs were developed using a solvent-evaporation technique that used dichloromethane as the solvent and curdlan as the polymer. A comprehensive randomized 3² factorial design was employed to vary curdlan content (X₁) and stirring rate (revolutions per minute, X₂) and to investigate their influence on particle size (Y₁) and entrapment efficiency (EE, Y₂). The optimized formulation then underwent in-vitro investigations, encompassing apoptosis and cell-cycle studies with the MCF-7 breast-cancer cell line.

Results: The prepared NSs (F1-F9) exhibited optimal physical and chemical characteristics. Optimization produced formulation F10, which achieved a particle size of 280.9 nm and an EE of 63.00%. The model was established for all dependent variables, such as particle size and EE, at a significance level of p<0.05. In vitro studies of the prepared NSs demonstrated promising anticancer activity. The AMY + HGN combination showed synergistic effects versus AMY alone, significantly influencing the MCF-7 cell cycle, producing G1-phase arrest, and reducing cell propagation by flow-cytometry analysis.

Conclusion: The synergistic anticancer activity observed with AMY- and HGN-loaded NSs-combined with their sustained-release properties and cell-cycle modulation in MCF-7 cells-underscores the promise of this formulation as an effective cancer-treatment approach.