Advances in Pharmacological and Pharmaceutical Sciences

Background. Recently, there is a lack of studies comparing the renoprotective effects of sodium-glucose cotransporter-2 (SGLT-2) inhibitors and dipeptidyl peptidase-4 (DPP-4) inhibitors. This study therefore aimed to investigate the renoprotective effects of SGLT-2 inhibitors and DPP-4 inhibitors on Thai patients with type 2 diabetes mellitus. Methods. Patient medication records of all patients who used those two antidiabetic classes at Fort Wachirawut Hospital were reviewed. Renal function tests, blood glucose levels, and other baseline characteristics were collected. Continuous variables were compared within the group using the Wilcoxon signed-rank test and between groups using the Mann–Whitney U test. Results. There were 388 and 691 patients with SGLT-2 inhibitors and DPP-4 inhibitors, respectively. The mean estimated glomerular filtration rate (eGFR) of the SGLT-2 inhibitor group was significantly lower from baseline at 18 months of treatment, as well as the DPP-4 inhibitor group. However, the trend of eGFR reduction in patients with baseline eGFR <60 mL/min/1.73 m² was smaller than those with baseline eGFR ≥60 mL/min/1.73 m². In addition, the fasting blood sugar and haemoglobin A1c levels significantly decreased from baseline in both the groups. Conclusions. Both SGLT-2 inhibitors and DPP-4 inhibitors showed the same trends of eGFR reductions from baseline in Thai patients with type 2 diabetes mellitus. However, SGLT-2 inhibitors should be considered in patients with impaired renal function rather than in all T2DM patients.

Introduction. Limited aqueous solubility and subsequent poor absorption and low bioavailability are the main challenges in oral drug delivery. Solid dispersion is a widely used formulation strategy to overcome this problem. Despite their efficiency, drug crystallization tendency and poor physical stability limited their commercial use. To overcome this defect, ternary solid dispersions of glyburide: sodium lauryl sulfate (SLS) and polyethylene glycol 4000 (PEG), were developed using the fusion (F) and solvent evaporation (SE) techniques and subsequently evaluated and compared. Materials and Methods. Physicochemical and dissolution properties of the prepared ternary solid dispersions were evaluated using differential scanning calorimetry (DSC), infrared spectroscopy (FTIR), and dissolution test. Flow properties were also assessed using Carr’s index and Hausner’s ratio. The physical stability of the formulations was evaluated initially and after 12 months by comparing dissolution properties. Results. Formulations prepared by both methods similarly showed significant improvements in dissolution efficiency and mean dissolution time compared to the pure drug. However, formulations that were prepared by SE showed a greater dissolution rate during the initial phase of dissolution. Also, after a 12-month follow-up, no significant change was observed in the mentioned parameters. The results of the infrared spectroscopy indicated that there was no chemical interaction between the drug and the polymer. The absence of endotherms related to the pure drug from thermograms of the prepared formulations could be indicative of reduced crystallinity or the gradual dissolving of the drug in the molten polymer. Moreover, formulations prepared by the SE technique revealed superior flowability and compressibility in comparison with the pure drug and physical mixture (ANOVA, ). Conclusion. Efficient ternary solid dispersions of glyburide were successfully prepared by F and SE methods. Solid dispersions prepared by SE, in addition to increasing the dissolution properties and the possibility of improving the bioavailability of the drug, showed acceptable long-term physical stability with remarkably improved flowability and compressibility features.

Purpose. This study assessed the awareness, actions, and predictors of actions on adverse drug reaction reporting among patients attending a referral hospital in southern highland Tanzania. Methods. A hospital-based cross-sectional study was conducted from January to August 2022 at Mbeya Zonal Referral Hospital (MZRH) in Mbeya, Tanzania. A total of 792 adult patients with chronic conditions attending outpatient clinics at MZRH were recruited consecutively. A semistructured questionnaire was used to collect demographic characteristics, ADR awareness, and actions when encountering ADR. Data were analyzed using the statistical package for social sciences (SPSS) version 23 and results are summarized using frequency and percentages. Binary logistic regression was used to assess the predictors associated with reporting ADR among patients. value ≤0.05 was considered statistically significant. Results. Out of 792, 397 (50.1%) were males and 383 (48.6%) had a primary education level. Only 171 (21.6%) participants previously experienced ADR, and 111 (14.1%) were aware that ADR is an unexpected harm that occurs after medication use. The majority 597 (70.3%) of the participants said will report ADR to healthcare providers, 706 (88.9%) prefer reporting ADR to healthcare providers, and 558 (69.1%) said patients are not aware of the importance of reporting ADR. Patients aged below 65 years of age, unemployed ((AOR (95% CI) = 0.4 (0.18–0.87), self-employed ((AOR (95% CI) = 0.5 (0.32–0.83)), and those who ever encountered ADR ((AOR (95% CI) = 0.1 (0.05–0.11)) were more likely to report the ADR to HCPs compared to the rest. Conclusions. The majority of patients are not aware of what is ADR and the importance of ADR reporting. Most of the patients prefer to report ADR to healthcare providers. We recommend an awareness campaign to raise awareness of the patients on ADR and other methods of ADR reporting.

Amritotharanam Kashyam, a specific Ayurvedic drug, was the focus of the current inquiry to evaluate its efficacy. For liver and digestive-related issues, this medication is suggested. This was obtained from a standard Ayurvedic vendor in Chennai (India), and GC-MS analysis was carried out according to the standard procedure. A few critical biomolecules include benzoic acid, hexadecanoic acid, 6,9-octadecadienoic acid, 9-octadecenoic acid, methyl ester (E)-, heptadecanoic acid, 16-methyl, methyl ester, methyl 18-methylnonadecanoate, tetracosanoic acid, distearin, hexadecanoic acid, and 1-(hydroxymethyl)-1,2-ethanediol ester. The obtained biomolecules exhibited some significant therapeutic functions, including acidification, inhibition of arachidonic acid formation, increase in the aromatic amino acid decarboxylase, suppression of uric acid generation, inhibitors of catechol-O-methyltransferase, urine acidifiers, etc. The anticancer and antiviral potential of these phytocompounds were investigated using molecular docking and dynamics. The phytocompounds pharmacokinetic characteristics were investigated using ADME analysis. Through docking and dynamics simulation, in silico tests demonstrated the phytocompounds' inhibitory efficiency against the target proteins. These functions reasonably relate to the medicinal function of Amritotharanam Kashyam. The MTT assay findings demonstrated this medication’s anticancer effects. The ability to be an effective drug is demonstrated by its antioxidant, anti-inflammatory, and membrane-stabilizing properties.

Background. The use of Aspilia africana in traditional medicine for the management of ocular diseases has been reported in India and some indigenous communities of Africa. The aim of this study was to investigate the aqueous extract of the flowers of A. africana (AAE) as an anticataract remedy using murine models of diabetic and senile cataracts. Methods. Preliminary phytochemical screening of the extract, in vitro antioxidant assays, and in vitro aldose reductase inhibitory activity were performed. For anticataract investigations of the extracts, diabetic cataract was induced by galactose administration in 3-week-old Sprague Dawley rats. The evaluation of experimentally induced age-related cataract was performed by administering sodium selenite to 10-day-old rat pups. Results. The phytochemical analysis revealed the presence of alkaloids, tannins, flavonoids, glycosides, and saponins. In vitro aldose reductase inhibitory property of the extract on rat lenses revealed that the AAE inhibited the enzyme activity with IC₅₀ of 12.12 µg/ml. For the anticataract investigations, 30, 100, and 300 mg·kg⁻¹AAE-treated rats recorded significantly low () cataract scores compared to the negative control rats, indicating a delay in cataractogenesis from the second week of treatment in the galactose-induced cataractogenesis. Similarly, the treatment with AAE caused a significant reduction () in cataract scores compared to the negative control rats in the selenite-induced cataractogenesis. Markers of lens transparency, such as aquaporin 0, alpha-A crystallin, and total lens proteins and lens glutathione levels, were significantly preserved () in each cataract model after AAE treatment. Conclusion. The study established the anticataract potential of the aqueous extract of flowers of A. africana in murine models, hence giving scientific credence to its folkloric use in the management of cataract.

Medicinal plants are traditionally used in Gabon to treat several types of illnesses. The study’s purpose was to determine the toxic, antibacterial, and anti-inflammatory effects of Antrocaryon klaineanum Pierre extracts and to characterize their phytochemical compounds. Toxicity was evaluated on frog tadpoles (Phrynobatrachus africanus Hallowell). The microorganism susceptibility test was performed by the diffusion method, while minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were evaluated using the microdilution technique. Anti-inflammatory activity was tested through protein denaturation and membrane stabilization methods. Chromatography and molecular network techniques were used to characterize chemical compounds. The lethality test showed that the lethal concentration (LC₅₀) increased from 110.03 ± 1.25 to 15.86 ± 2.21 μg/mL after 24 and 96 hours of exposure. In tadpoles exposed to 7.81 μg/mL extract, the first mortalities (12.5%) were observed on the fifth day of exposure. A relative decrease in mature erythrocytes exposed to plant extracts was observed. The antibacterial activity shows that the Ak F₂, Ak F₃, and Ak F₄ fractions (from the water-ethanol crude extract) gave the greatest antibacterial activities compared to the other extracts. The water, water-acetone, and water-ethanol extracts showed good inhibition of denaturation. The haemolysis test shows that the extracts exhibited good anti-inflammatory activities. Phytochemical characterisation revealed four major compounds, including monogallate epicatechin and hydroxy-ergostadian. The molecular network revealed five main clusters. Our study shows that A. klaineanum Pierre could be a promising natural product for the isolation of molecules with potential biological activities.