Impact of acacia arabica topical gel on skin wound healing: An experimental study

Aim of the study: To estimate the influence of Acacia Arabica gel abstract on skin wound healing. Material and method: 28male adult rabbits were included, 2 incisions of 1cm length were made on the skin of the rabbit’s back, one is treated by acacia gel while another left for normal healing, histopathological examination was done at 24h, 3, 7 and 14 days intervals. Results: The inflammatory reactions showed no significant results for both the control group and the study group during the study intervals. Granulation tissue in the control group was absent after 24h but increased to become profound after 7 days then become moderate, while the study group showed scanty granulation tissue from the first day and increased through study intervals. Re-epithelialization mean scores in the study group were higher than control one. Conclusions: Acacia arabica has the efficacy of hastening the wound healing process.

Study of the dissolution kinetics of drugs in solid dosage form with lisinopril and atorvastatin and intestinal permeability to assess their equivalence in vitro

Atorvastatin and lisinopril are a successful combination for the treatment of patients with chronic heart failure and hypertension. Study of the dissolution kinetics of drugs in solid dosage form with lisinopril and atorvastatin and intestinal permeability to assess their equivalence in vitro were described. In medium with hydrochloric acid pH 1.2, in the medium of acetate buffer solution with a pH of 4.5 and in the medium phosphate buffer solution with a pH of 6.8 for 15 min more than 85% of the active substance passes into solution, hence the dissolution profiles these drugs in these environments are similar, and the drugs in them are “very quickly soluble”. Among the in vitro models that make it possible to assess the degree of absorption of API, the most widely used culture of adenocarcinoma cells of the colon – Caco-2. The development of the analytical methodology and its validation is the final stage of both the dissolution study and the Caco-2 test, as well as the biowaver procedure. It plays the most important role in the reliability of the results for all the above procedures and tests. To study permeability, method LC-MS/MS was developed. According to the obtained results, atorvastatin and lisinopril showed low permeability. The values ​​of recovery of transport of test and control substances through the monolayer of cells of the Caco-2 line indicate that the results of the experiment can be considered reliable. The equivalence of the drugs “Lisinopril”, tablets of 10 mg and “Atorvastatin”, tablets of 10 mg, belongs to class III BCS proven by in vitro studies.

Analysis of amino acids content in the plant components of the antidiabetic herbal mixture by GC-MS

Medicinal plants and their combinations due to the wide range of biologically active substances can influence on various links of the pathogenetic mechanism of development of DM type 2 and its complications. One of such combinations is an antidiabetic herbal mixture (Urticae folia, Rosae fructus, Myrtilli folia, Menthae folia and Taraxaci radices) with established hypoglycaemic, hypolipidemic, antioxidant, hepatoprotective, pancreatoprotective activity in previous pharmacological studies in vivo and in vitro and defined phytochemical composition. Thus, the aim of this study was to identify and establish the content of amino acids in the plant components of antidiabetic herbal mixture. The amino acids were separated by GC-MS method with pre-column derivatization. The calibration curves of twenty CRS of amino acids were linear (R2 > 0.98) over the range of 1–100 µg/mL, the LODs and the LOQs were in the range of 0.01–0.07 µg/mL and 0.02–0.20 µg/mL, respectively. The results of analysis showed that the predominant essential amino acid was L-proline in Taraxaci radices, Urticae folia, Rosae fructus and Menthae folia, its total content was 101.46 mg/g, 25.31 mg/g, 23.04 mg/g and 19.30 mg/g, respectively. In addition, it was established total content of essential amino acid – L-leucine that can stimulate insulin secretion in β-cells of the pancreas. Its total content was 58.51 mg/g in Taraxaci radices, 9.58 mg/g in Myrtilli folia, 4.68 mg/g in Rosae fructus, 2.99 mg/g in Urticae folia and 0.79 mg/g in Menthae folia. Chromatographic examination also revealed L-phenylalanine, an essential amino acid important for antidiabetic therapy that can increase insulin secretion, stimulate proliferation and neogenesis of β-cells of the pancreas and reduce insulin resistance. Its total content was 13.42 mg/g in Myrtilli folia, 2.23 mg/g in Rosae fructus, 1.478 mg/g in Urticae folia, 1.46 mg/g in Taraxaci radices and 0.52 mg/g in Menthae folia. This phytochemical study shows, which plant material forms the amino acid composition and content in the finished herbal mixture and due to which biologically active substances the antidiabetic activity of this phytocomposition is manifested.

Investigating matrix interference in the pharmacopeial limit test for aluminum in citric acid: a re-examination, for revision of the method

In many pharmacopoeias, the limit test used for determining the level of aluminum in citric acid labeled for use in the manufacture of dialysate, is based on solvent extraction using 8-hydroxyquinoline and measurement of fluorescence. However, the fluorescence intensity (F.I.) readout from the extract of citric acid samples has been found to be highly dubious, showing low value, and even lower than that of a blank solution. The aim of this work therefore was to examine what effects the matrix has on the test. The comparison of the two standard curves of aluminum solutions in water, against those prepared in citric acid solutions revealed that they differed greatly in terms of slope and y-intercept. In addition, the F.I. values on the plot of the citric acid solution were much lower than that prepared in the water. In another experiment, a decrease in the F.I. of aluminum solution was clearly seen when the co-existing concentration of citric acid was increased. The results inferred that citric acid interfered with the test due to its acidity and metal-chelating capabilities. Based on this evidence, the pharmacopeial limit test for aluminum in citric acid should be revised; otherwise, it could yield results that underestimate aluminum levels and lead to inaccurate conclusions

HPLC determination of Escitalopram in tablet dosage forms

Purpose: A simple, specific, precise, and accurate reversed phase liquid chromatographic (RP-LC) method has been developed for the determination of Escitalopram in tablet dosage form. Methods: The chromatographic separation was achieved on a LiChrosorb C18, 250 mm x 4.6 mm, 5 μm column at a detector wavelength of 270 nm and a flow rate of 1.0 ml/min. The mobile phase was composed of methanol, acetonitrile (70:30 v/v). The retention time of Escitalopram was 5.49 min. The method was validated for the parameters like specificity, linearity, precision, accuracy, limit of quantitation and limit of detection. Results: The method was found to be specific as no other peaks of impurities and excipients were observed. The square of correlation coefficient (R2) was 0.9999 while relative standard deviations were found to be <2.0%. Conclusion: The proposed RP-LC method can be applied for the routine analysis of commercially available formulations of Escitalopram.

Comparative assessment of clinical trials, indications, pharmacokinetic parameters and side effects of approved platinum drugs

Platinum complexes are among the most commonly applied anticancer agents. The aim of current work is collection, analysing and comparative estimation of clinical trials and pharmacological indications of currently approved for application platinum detivatives: Cisplatin, Carboplatin, Oxaliplatin, Nedaplatin (Japan), Lobaplatin (China), Heptaplatin (North Korea), and Satraplatin. The other aim of the study includes the summarizing of the hystoric data for the stages of the developlement of these drugs, and the comparison of pharmacokimetic parameters, side effecs and the dose-liniting factors of the drugs. The observational study on pharmacokinetic parameters shows that protein binding decreases in order: 95% (Cisplatn); 90% (Oxaliplatin); 50% (Nedaplatin); low (Carboplatin). For every of Cisplatin, Carboplatin, Oxaliplatin have been reported more than 1000 clinical trials; for Lobaplatin, Nedaplatin, Satraplatin - about 10 trials. The differenses in dose-limiting effects are: neuro-, nephro-, ototoxicity (Cisplatin); neurotoxicity (Oxaliplatin); nephrotoxicity (Heptaplatin); myelosuppression: thrombocytopenia, neutropenia, leukopenia (Carboplatin, Nedaplatin, Satraplatin).

Repurposing – second life for drugs

Drug repurposing refers to finding new indications for existing drugs. The paradigm shift from traditional drug discovery to drug repurposing is driven by the fact that new drug pipelines are getting dried up because of mounting Research & Development (R&D) costs, long timeline for new drug development, low success rate for new molecular entities, regulatory hurdles coupled with revenue loss from patent expiry and competition from generics. Anaemic drug pipelines along with increasing demand for newer effective, cheaper, safer drugs and unmet medical needs call for new strategies of drug discovery and, drug repurposing seems to be a promising avenue for such endeavours. Drug repurposing strategies have progressed over years from simple serendipitous observations to more complex computational methods in parallel with our ever-growing knowledge on drugs, diseases, protein targets and signalling pathways but still the knowledge is far from complete. Repurposed drugs too have to face many obstacles, although lesser than new drugs, before being successful.

Improvement of in vitro antioxidant activity of kaempferol by encapsulation in copolymer micelles

Antioxidant capacity of poorly soluble natural antioxidant kaempferol, in particular free or loaded in two types of cationic micelles, was studied on non-enzyme induced lipid peroxidation (LPO) in vitro. The micelles were based on triblock copolymers - poly(2-(dimethylamino)ethyl methacrylate-b-poly(propylene oxide)-b-poly(2-(dimethylamino)ethyl methacrylate (PDMAEMA-PPO-PDMAEMA) and poly(2-(dimethylamino)ethyl methacrylate-b-poly(ε-caprolactone)-b-poly(2-(dimethylamino)ethyl methacrylate (PDMAEMA-PCL-PDMAEMA). The lipid peroxidation was induced by incubating of rat liver microsomes with iron sulphate and ascorbic acid (Fe2+/AA). The effect of free and micellar kaempferol (at concentrations 25, 50 and 75 μg/ml) was assessed after 20 min incubation time. In the non-enzyme lipid peroxidation model, the kaempferol-loaded micelles significantly decreased the formation of malondialdehyde (MDA). The effect of kaempferol loaded in PDMAEMA-PCL-PDMAEMA micelles was more pronounced, showing an improved antioxidant activity in the conditions of oxidative stress and lipid peroxidation in vitro.

Specialized nutrition for athletes: evaluation of ergogenic action using the principles of evidence-based medicine

The aim is to form a balanced position regarding the ergogenic characteristics of new sports food products in the modern practice of training highly qualified athletes on the basis of clinical-experimental evaluation of the effectiveness of special purpose real food additives. Materials and methods. Studies were carried out on laboratory animals (36 Wistar rats at the age of 3 months weighing 150–200 g and 16 Svetlogorsk mini-pigs) as well as on 102 high-qualified representatives of cyclic sports (all men aged 19–26) − members of national teams such as swimming (25), cross-country athletics (53), and skiing (24). As a control group, we studied 25 athletes of the same gender (all men), age and qualifications who received a placebo (starch capsules) for a long time during exercise. Placebo-controlled studies have been conducted on laboratory animals and athletes in compliance with the principles of bioethics. Results. It has been established that in the experiment the application of a new specialized food product MioActiv has a positive effect on the physical performance of animals and delays the onset of fatigue, which significantly exceeds the corresponding characteristics in the placebo group. Athletes also showed an increase in speed when passing competitive distances by 18.7–21.4% (p < 0,05), as well as a significant increase in mental endurance indicators (p < 0,05). The approbation of the innovative pre-workout pharmacological nutrient complex Pre-Fuse also showed the high efficacy and safety of this product with a positive effect of increasing the performance and endurance of animals, as well as the parameters of mental performance of athletes in the main groups, in contrast to the data in the placebo control groups. Conclusions. An analysis of the prescription components of new types of ergogenic sports nutrition and the presented results of preclinical and clinical studies conducted on the basis of the evidence-based medicine paradigm regarding the effectiveness of specialized products indicate the complex action of these funds on various aspects of both physical and mental performance. From the materials presented in the article, it can be seen that specialized sports nutrition products of an ergogenic orientation can provide significant assistance in increasing sports results.

Development of new HPLC method for identification of metabolic degradation of N-pyrrolylhydrazide hydrazones with determined MAO- B activity in cellular cultures

In this research, a new rapid PR- HPLC method was developed for the determination of metabolites in isolated rat hapatocytes. The chromatographic parameters, including the stationary and mobile phases, outlet pressure, temperature and flow rate, were optimized. The method identified two initial from the synthesis molecules in higher concentration and one new unidentified structure as products of the hepatocytic processing of the evaluated analyte. The results identified as first step of metabolism the hydrolysis of the hydrazone group. Further investigations should be aimed into determining the next metabolic transformations, predicted by the in silico application of the web server SMARTCyp.