Turkish Journal of Pharmaceutical Sciences最新文献

Objectives: The focus of this study was to design and optimize methylphenidate hydrochloride mouth dissolving film (MDF) that can be beneficial in an acute condition of attention deficit hyperactivity disorder (ADHD) and narcolepsy.

Materials and methods: Solvent casting method was used for the preparation of this film. Optimization of the effect of independent variables such as the number of polymers and active pharmaceutical ingredients [hydroxypropyl methyl cellulose (HPMC) E5, HPMC E15, and maltodextrin], % of drug release, disintegration time, and tensile strength of the film done using simplex centroid design. Complex formation of the film was tested using fourier-transform infrared spectroscopy and differential scanning calorimetry study. The multiple regression analysis was obtained from equations of the results that adequately describe influence of the independent variables on the selected responses. Polynomial regression analysis, contour plots, and 3-D surface plots were used to relate dependent and independent variables.

Results: Experimental results indicated that different polymer amounts had complex effects on % drug release from the film, disintegration time as well as the tensile strength of the film. The observed responses were in near alignment with expected values calculated from the developed regression equations as shown by percentage relative error. Final formulation showed more than 95% drug release within 2 min and was shown to disintegrate within a minute that had good tensile strength.

Conclusion: These findings suggest that MDF containing methylphenidate hydrochloride is likely to become a choice of methylphenidate hydrochloride preparations for treatment in ADHD and narcolepsy conditions.

Objectives: This study proves the protective effect of Apis dorsata honey against chronic monosodium glutamate (MSG)-induced testicular toxicity on the Leydig cell necrosis count and malondialdehyde (MDA) serum level in Mus musculus mice.

Materials and methods: In this study, 25 male mice were used and grouped into two large groups: The control group consisting of negative control (C-) and positive control (C+). C+ group was fed with 4 mg/g body weight (gBW) of MSG followed by distilled water. The treatment group consisted treatment 1, treatment 2, and treatment 3 groups with A. dorsata honey dosage 53.82 mg/20 g, 107.64 mg/20 g, 161.46 mg/20 g per os (p.o.), respectively, followed by MSG 4 mg/g BW of MSG p.o. For the difference analysis between the group used the one-way ANOVA test and Duncan test.

Results: The result of this study showed that there was a significant difference between the treatment group and control group (p<0.05) in the Leydig cell necrosis count and MDA levels. The highest Leydig cell necrosis count and MDA level were found in C+ with values 13.20 ± 2.05 cell and 37.08 ± 9.17 μmol/L compared to C-, while in the treatment group, T3 showed the lowest Leydig cell necrosis value and MDA level 4.64 ± 0.55 cell and 14.22 ± 2.01 μmol/L compared to the C+ group.

Conclusion: It can be concluded that A. dorsata honey could reduce the Leydig cell necrosis number and MDA level of mice (Mus musculus) exposed to MSG.

Objectives: Safflower oils, which are sold commercially, are in demand with food, cosmetics, and health-promoting claims. In this study, safflower oil samples belonging to 11 different brands were evaluated in terms of European Pharmacopoeia Criteria 7.0. Additionally, in vitro weight control potential of all samples was investigated.

Materials and methods: Samples to be analyzed were purchased from pharmacies, herbal, online, and cosmetics stores. Acid and peroxide values of 11 safflower samples and analysis of their fatty acids by gas chromatography-mass spectrometry (GC-MS) were carried out according to the "Carthami oleum raffinatum" monograph registered in the European Pharmacopeia 7.0. To test the effects of all samples on weight control, their inhibitory effects on carbohydrate-digesting enzymes (α-glucosidase and α-amylase) were evaluated using spectrophotometric methods.

Results: Out of 11 oil samples, only two of them had acid and peroxide values below the reference value. According to GC analysis, safflower oil samples are rich in monounsaturated fatty acids (oleic acid) and polyunsaturated fatty acids (linoleic acid) (67.10-99.53%) of total fatty acids in its content are oleic, linoleic, palmitic, and stearic acids. Saturated fatty acids were 0.58 to 12.18% of the total fatty acid methyl esters in oils. When evaluated in terms of the inhibition of α-amylase and α-glucosidase enzymes that hydrolyze carbohydrates, the results showed that safflower oil samples had no inhibitory activity on these enzymes.

Conclusion: It has been determined in this report that many safflower oil samples on the market do not meet the quality criteria recommended in European Pharmacopoeia 7.0. It was observed that safflower oil did not show any inhibitory effect on these two enzymes, which is considered a rational approach for weight control.

Objectives: Almond oil marketed for health benefits and cosmetic purposes should be in compliance with the European Pharmacopoeia (EP) criteria. Therefore, in this study, 17 almond oil samples sold in pharmacies, herbal shops, online, and cosmetics stores were analyzed in terms of "almond oil" monograph criteria, which have been mentioned in EP 7.0.

Materials and methods: In this study, 17 almond oil samples sold in pharmacies, herbal, online, and cosmetics stores were analyzed in terms of "almond oil" monograph criteria, which have been mentioned in EP 7.0. Appearance, acidity value, and peroxide value of each sample were determined and the ingredients were identified by thin layer chromatography. Fatty acids were analyzed by gas chromatographic method using flame ionization detector.

Results: It was determined that two of the 17 samples complied with EP 7.0 criteria.

Conclusion: Almond oil, which is currently marketed according to the manufacturer's own marketing and quality criteria, is excluded from the Turkish Food Codex Standards. Our research has shown that most of the products do not comply with the EP standards. For this reason, it should be ensured that almond oil is listed in this codex and urgent arrangements should be made for quality control analysis.

Objectives: This study aimed to identify the prevalence of potentially inappropriate medication use (PIMU) in adults above the age of 65 with chronic kidney disease (CKD) according to the American Geriatric Society Beers Criteria (Beers), Screening Tool of Older People's Potentially Inappropriate Prescriptions Criteria (STOPP) and medication appropriateness index (MAI) 30 criteria and to compare them to justify their use in this specific patient group.

Materials and methods: This was a retrospective and descriptive study conducted between October 1^st, 2019 and March 18^th, 2020 at Ibni Sina Hospital, Nephrology Department, Faculty of Medicine, Ankara University.

Results: Among 269 patients discharged from the hospital during the study period, 100 of them were eligible for the study. The mean age was 73.3 ± 6.9 years and 51.9% of them were male. The prevalence of 35 PIMU was 91%, 42%, and 70% according to the Beers, STOPP, and MAI criteria, respectively. There was a statistically significant difference in terms of prevalence among 3 criteria (p<0.001). Beer detected more PIMU (11.3% vs. 6.4%) and had higher sensitivity among older adults with CKD (0.97 vs. 0.56) compared to the STOPP criteria. Most patients had at least one drug-drug interaction (DDIs) in their discharge prescription (93%) and DDI was one of the main contributors of PIMU. Proton pump inhibitors were the most common medication associated with PIMU in all 3 criteria.

Conclusion: The prevalence of PIMU was high among older adults with CKD at discharge according to these criteria. To improve the prescriptions after hospital discharge, it is considered appropriate to use Beers criteria under guidance of a clinical pharmacist.

Objectives: Following the success of natural compounds for treating solid tumors, interest in applying such agents for treating hematologic malignancies has been fired up more strikingly. Thus far, anti-leukemic effects of several compounds have been examined in different leukemia cell lines, especially in acute lymphoblastic leukemia. The agent that has recently attracted tremendous attention is Britannin, which is derived from Inula aucheriana DC., a plant that grows in Iran (Azerbaijan) and Türkiye. In this study, we evaluated the effects of this compound in myeloid leukemia for the first time.

Materials and methods: We treated chronic myeloid leukemia (CML)-derived K562 and acute myeloid leukemia (AML)-derived U937 cells with different concentrations of britannin. We used several assays, including trypan blue, 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide, bromodeoxyuridine/5-bromo-2'-deoxyuridine, flow cytometry, and quantitative real-time polymerase chain reaction analysis, to study anti-leukemic effects of the compound.

Results: Our results show that while britannin remarkably reduced the survival of both cell lines in a concentrations-dependent manner, it had cytotoxic effects neither on mouse fibroblast-derived L929 cells nor on normal peripheral mononuclear cells. Moreover, among the tested cell lines, the viability of CML-derived K562 cells was inhibited at higher concentrations of the compound compared with AML-derived U937 cells. We found that britannin induced apoptotic cell death in both cell lines by altering the expression of anti- and pro-apoptotic genes. Britannin also hampered proliferative capacity of the cells in a p21/p27-dependent manner.

Conclusion: Overall, we suggest that based on the lack of toxicity on the normal cells and valuable anti-leukemic activities, britannin could be a promising agent in the treatment strategies of both CML and AML. However, further investigations must more precisely study this compound's mechanism of action and evaluate its safety profile.

Objectives: The concern for finding natural and curative agents without adverse side effects has prompted the interest in discovering hemostatic agents from plants. Therefore, in vitro activity of Aizoon hispanicum L. (Aizoaceae), Centaurea hyalolepis Boiss. (Asteraceae), Heliotropium maris-mortui Zohary. (Boraginaceae), Parietaria judaica L. (Urticaceae), Polygonum arenarium Waldst. & Kit. (Polygonaceae), and Verbascum sinuatum L. (Scrophulariaceae) on blood coagulation was estimated by two common tests, which are the prothrombin time test (PT) and the activated partial thromboplastin time test (aPTT).

Materials and methods: The extracted powders from the plants under this study were adjusted to be 50 mg/mL. Then, in vitro effect of these extracts on the platelet poor plasma samples was measured by an automated coagulation analyzer using PT and aPTT tests.

Results: Based on the obtained results, all plant extracts affected the coagulation cascade by rising either PT or aPTT or both, except for V. sinuatum extract, which reduced only aPTT value. Moreover, the recorded PT values showed that A. hispanicum, H. maris-mortui, and P. arenarium significantly prolonged the PT (p<0.05). Additionally, the results clearly showed that V. sinuatum acted as a coagulant agent based on aPTT values, while all other plants, in contrast, acted as strong anticoagulants. Among the plant species under study, A. hispanicum, H. maris-mortui, and P. arenarium extracts prolonged both PT and aPTT significantly (p<0.05). This could be referred to their additional effect on the common pathway. However, C. hyalolepis, P. judaica, and V. sinuatum showed no significant effect on PT values (p>0.05).

Conclusion: The positive recorded data from this research could serve as identification of new hemostatic remedies that could be used for the commercial economic purposes and for managing several cardiovascular diseases.

Objectives: Two optimized and validated high performance liquid chromatography (HPLC) and spectrophotometric methods are proposed. The developed methods were quantified with high sensitivity, accuracy, and precision at low concentrations to determine rufinamide (RUF) in active pharmaceutical ingredients (API) and pharmaceutical preparations.

Materials and methods: HPLC method was developed using a base deactivated silica Hypersil C₁₈ column and a combination of methanol: acetonitrile: water (15: 10: 75, v/v/v) as the mobile phase and detected at 210 nm. A reaction of RUF with sodium nitrite and hydrochloric acid occurred, absorbed maximally at 385 nm was extended to develop a ultraviolet (UV)-visible spectrophotometric method to determine RUF in API and pharmaceutical preparations.

Results: Different analytical validation parameters, including specificity, linearity, accuracy, precision, the limit of detection, quantification, ruggedness, and robustness, were determined as per International Conference on Harmonization guidelines. The linearity range of RUF was 0.15-3.5 and 10-100 μg/mL for HPLC and spectrophotometric methods, respectively.

Conclusion: The proposed investigations were valuable for drug monitoring and regular analysis of RUF in quality control and research laboratories. Moreover, the accuracy and precision obtained with the UV-visible spectrophotometer implied that it could be a cheap, easy, and alternative method, while HPLC could be sensitive to determine RUF at low concentration levels.

Objectives: Drugs that inhibit the reuptake of serotonin, norepinephrine, and/or dopamine are widely used for treating depressive disorders and have emerged as effective drugs for neuropathic pain. They have no substantial anti-nociceptive effects but are considered, with gabapentin/pregabalin, first-line drugs for neuropathic pain.

Materials and methods: In this study, three different antidepressant agents were used in different doses to investigate their anti-hyperalgesic effects in rat models of neuropathic pain using hot plate and tail flick methods. They have different mechanisms of action; vilazodone hydrochloride is a selective serotonin inhibitor and a 5-HT_1A partial agonist; talsupram hydrochloride is a selective noradrenaline inhibitor, and it has a high affinity for noradrenaline transporter (NET), whereas indatraline hydrochloride is a triple reuptake inhibitor that inhibits transporters for 5-HT (SERT), dopamine (DAT), and NET.

Results: All the drugs used in the experiment were found to have an anti-hyperalgesic effect in both tests compared to the sham group. When anti-hyperalgesic effects of the three agents were compared to each other, it was found that talsupram hydrochloride was significantly more effective than the two other drugs in hot plate test. However, there was no statistically significant difference in the tail flick test. Indatraline hydrochloride was more effective than vilazodone hydrochloride at the same doses in the tail flick test.

Conclusion: Our data suggest that three drugs are effective analgesics in rat models of neuropathic pain and inhibition of noradrenaline reuptake represents the cornerstone of analgesic mechanisms of effective antidepressants.