European Pharmaceutical Journal最新文献

{"title":"51st Conference Synthesis and Analysis of Drugs (SAD 2023)","authors":"L. Habala","doi":"10.2478/afpuc-2023-0021","DOIUrl":"https://doi.org/10.2478/afpuc-2023-0021","url":null,"abstract":"","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-11-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139224397","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A Randomized, Two-Treatments, Two-Periods, Crossover, Open label, Laboratory-Blind, Single Dose Bioequivalence Study between Vildagliptin/Metformin 50 mg/1000 mg Film Coated Tablets (Sensityn^®) and Galvusmet^® 50 mg/1000 mg Film Coated Tablets in healthy adults under fed conditions","authors":"J. Shiekmydeen, T. Siddiqi, K. Chakraborty, S. Khalaf, M. Albarazi, I. Eqtefan, J. Sliva","doi":"10.2478/afpuc-2023-0019","DOIUrl":"https://doi.org/10.2478/afpuc-2023-0019","url":null,"abstract":"Abstract Aim Vildagliptin/metformin 50 mg/1000 mg film coated tablets (Sensityn ® ) is being developed for the treatment of type 2 diabetes mellitus. An open label, crossover, bioequivalence study (phase I) was conducted to assess the bioequivalence between Sensityn ® Film Coated Tablets (Test Product/Alpha Pharma Industries, a subsidiary of Cigalah Healthcare LLC, KAEC, Saudi Arabia) and Galvusmet ® Film Coated Tablets (Reference product/Novartis Pharma, Switzerland), in healthy adults under fed conditions. Safety and tolerance were evaluated as secondary endpoints. Materials and methods A randomized study with two treatments, two periods, crossover, open-label, laboratory-blind, single dose, with a washout period of seven days under fed conditions in 36 healthy male subjects. These were administered medicinal drug product (Sensityn ® ) or the reference medicinal product (Galvusmet ® ); both as a single 50 mg/1000 mg oral dose, under fed conditions. Blood samples were collected for pharmacokinetic analysis before treatment and until 24.00h post-dosing in each study period. ANOVA analysis (test sequence, subjects’ nested within sequence, product and period effect) was performed using a 5% significance level for logarithmic and untransformed data for C max AUC 0-t and AUC 0-∞ and for untransformed data for T max , K elimination (λz) and half-life. Results The results showed that C max , AUC 0-t , and AUC 0-∞ have passed the 90% CI acceptance limits of 80.00%–125.00% for vildagliptin and metformin. Consequently, the bioequivalence of Sensityn ® and Galvusmet ® film coated tablets was demonstrated under fed conditions. Treatment emergent adverse events were reported by 3 subjects and 1 subject following the administration of Sensityn ® and the Galvusmet ® , respectively. Conclusion The present findings confirmed that Sensityn ® , the test medicinal product is bioequivalent to Galvusmet ® , the reference medicinal product, in the rate and extent of absorption. Also, it has comparable safety profile. These findings support the continued development of vildagliptin/metformin 50 mg/1000 mg film coated tablets (Sensityn ® ) for use in patients with type 2 diabetes mellitus.","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135570039","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Formulation and Evaluation of Gastroretentive <i>In Situ</i> Gelling System of Ketoprofen","authors":"AR. Shabaraya, T. T Ashwini, K. Vineetha","doi":"10.2478/afpuc-2023-0018","DOIUrl":"https://doi.org/10.2478/afpuc-2023-0018","url":null,"abstract":"Abstract A revolutionary concept for achieving long-term medication release is the gastroretentive in situ gelling system. The goal of this research was to formulate and test a gastroretentive in situ gel for ketoprofen delivery to targeted site to increase the residence and delivery time. Ketoprofen gastroretentive in situ gels were synthesized using a cation-driven gelation approach using various combinations and concentrations of polymers such as gellan gum, sodium alginate, and hydroxypropyl methylcellulose (HPMC) K100M. Visual appearance, pH, viscosity, in vitro gelation, in vitro buoyancy, drug content, density measurement, gel strength measurement, water uptake, and in vitro drug release were all evaluated. The total floating time was more than 12 h, with a floating lag time of less than 2 min. The formulations showed pH ranging from 6.89 to 7.61 and drug content ranging from 82.01% to 95.53%. For 11 h, the percent cumulative drug release of formulations F5 and F14, which contained a greater concentration of polymer sodium alginate (1.5%) and a combination of gellan gum and HPMC K100M (0.175% and 0.2%), was 84.10% and 85.49%, respectively. In vitro dissolution experiments and stability investigations both revealed no significant changes in drug content. The findings revealed that the formulated in situ gels aided in extending gastric residence duration, allowing the drug to be released in the stomach.","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135252072","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Role of raloxifene in the management of postmenopausal osteoporosis of rheumatoid arthritis patients","authors":"M. Sahebary, M. Sarafraz, M. Salari, T. Asadi Sakhmarresi","doi":"10.2478/afpuc-2023-0003","DOIUrl":"https://doi.org/10.2478/afpuc-2023-0003","url":null,"abstract":"Abstract Objective Due to the severe side effects of long-term treatment using hormone replacement therapy, Raloxifene (RLX) is introduced with beneficial effects on rheumatoid arthritis (RA) for postmenopausal women. This review was conducted to collect data from the available literature on RLX for the management of postmenopausal women suffering from RA. Method All studies published up to 2019 were searched in four databases, including Google Scholar, PubMed, Scopus, and Medline. All articles were searched using several keywords, including “Raloxifene” or “Evista” in combination with “Rheumatoid Arthritis” or “Autoimmunity”. Finally, six studies were selected for the review analysis of this study. In all studies, 60 mg/day RLX was administered for postmenopausal subjects. The majority of the studies showed that the use of RLX was effective in postmenopausal women who underwent corticosteroid therapy. No severe complications were reported after RLX therapy in patients with RA. Result Based on the obtained results, RLX is a selective estrogen receptor modulator that its short-term anti-arthritic effects are proven in the treatment of postmenopausal osteoporosis. It was well tolerated without serious adverse events. Conclusion It seems that RLX is a promising treatment candidate in postmenopausal RA due to its anti-arthritic and anti-osteoporotic effects and based on the outcomes of experimental postmenopausal arthritis in animal and human studies.","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136341762","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Experimental evaluation of the nonselective and selective TMEM16 family calcium-activated chloride channel blockers in the airways","authors":"J. Mažerik, L. Smieško, L. Fedorová, E. Gondáš","doi":"10.2478/afpuc-2023-0016","DOIUrl":"https://doi.org/10.2478/afpuc-2023-0016","url":null,"abstract":"Abstract Background The family of calcium-activated chloride channels, TMEM16, plays a significant role in contributing to the pathogenesis of airway inflammatory diseases. Targeting these ion channels and aiming to modulate them may provide an interesting new approach to the therapy of these potentially fatal diseases. Methods We tested this hypothesis in both healthy and ovalbumin (OVA)-sensitized male Dunkin-Hartley guinea pigs. The ion channel activity was modulated by TMEM16A-nonselective (benzbromarone) and TMEM16A-selective blockers (CaCCinh-A01). In vivo airway reactivity, induced by histamine and methacholine, was expressed as specific airway resistance (sRaw) values. The number of citric acid-induced coughs was counted using a double-chambered body plethysmograph, and the frequency of ciliary beating (CBF) was assessed in vitro by brushing method. For comparison, salbutamol and codeine were tested under the same conditions. Results The results showed significant differences in the responses of unsensitized and sensitized airways to both TMEM16 blockers administered. CaCCinh-A01 and benzbromarone significantly reduced the number of cough efforts in the group of OVA-sensitized guinea pigs. Significant improvement in sRaw values could be observed in OVA-sensitized TMEM16 blocker–treated animals compared to salbutamol when challenged with inhalational histamine, and the outcome was similar to salbutamol when challenged with methacholine. CBF was significantly inhibited in animals sensitized to OVA treated with selective inhibition of TMEM16A. Conclusions The results demonstrated that treatment with blockers of TMEM16 can reduce both cough effort and sRaw, and the difference between TMEM16A-selective and TMEM16A-nonselective blocking is only negligibly in favor of CaCCinh-A01. It is also worthwhile to note the impairment of CBF in OVA-sensitized animals treated with CaCCinh-A01.","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136280148","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A Multiple Unit Abuse-deterrent Dosage Form Based on Sodium Alginate","authors":"M. Papadakos, M. Špaglová, M. Čuchorová, M. Hanko","doi":"10.2478/afpuc-2023-0020","DOIUrl":"https://doi.org/10.2478/afpuc-2023-0020","url":null,"abstract":"Abstract There are several approaches for the formulation of abuse-deterrent, tamper-resistant, or alcohol-resistant dosage forms. This work is specifically focused on the formulation of microforms and multiple unit dosage forms with the mentioned resistant features. We prepared microcapsules based on sodium alginate by Ca 2+ -induced gelation, containing caffeine as a model drug. The prepared microcapsules were dried either by hot air or freeze-dried and the resistance in an alcoholic environment and the resistance against mechanical stress were observed. Subsequently, swelling studies were conducted to predict the behavior of prepared microcapsules during dissolution testing. Differences in the behavior of microcapsules during dissolution testing were strongly related to the different abilities of Ca 2+ -alginate microcapsules to swell in an acidic and alkaline environment. Alginate microcapsules exhibited gastro-resistant properties due to excellent swelling in an alkaline environment and poor swelling in a gastric environment. The addition of ethanol did not influence the swelling behavior of alginate microcapsules in the gastric fluid; rather, it showed the opposite effect, where swelling was slightly suppressed. Therefore, we conclude that alginate microcapsules are alcohol resistant. Also, they showed high mechanical strength, and therefore, grinding the microcapsules into a powder was impossible.","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-09-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135395525","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Book of Abstracts 39th Technology Days 7^th and 8^th September 2023","authors":"V. Mikušová","doi":"10.2478/afpuc-2023-0017","DOIUrl":"https://doi.org/10.2478/afpuc-2023-0017","url":null,"abstract":"","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-09-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135734150","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Synthesis, antioxidant activity, and HPLC enantioseparation of aryloxyaminopropanols derived from naphthalen-2-ol","authors":"R. Čižmáriková, L. Habala, J. Valentová, A. Némethy, K Bruchatá, K. Hroboňová","doi":"10.2478/afpuc-2023-0015","DOIUrl":"https://doi.org/10.2478/afpuc-2023-0015","url":null,"abstract":"Abstract The present work describes the synthesis, physico-chemical characteristics, antioxidative properties, and high-performance liquid chromatography (HPLC) enantioseparation of novel, potentially bioactive aryloxyaminopropanols – derivatives of naphthalen-2-ol modified in the basic part of their molecules. Reaction of naphthalene-2-ol with chloromethyloxirane leads to 2-[(naphthalen-2-yloxy)methyl]oxirane, which reacts in the next step with branched aliphatic amines (isopropylamine, tert -butylamine, and dimethylamine), aromatic amines (aniline, 3,4-dimethoxyphenylethylamine), and heterocyclic amines (pyrrolidine, imidazole, 2-methylimidazole, piperidine, morpholine, 4-methylpiperidine, or 2-methoxyphenylpiperidine). The target compounds were isolated in the form of free bases, as well as their salts with fumaric or hydrochloric acid. Their purity was established by thin-layer chromatography and their IR, UV, 1 H-NMR, and 13 C-NMR spectra were recorded. The antioxidant activities of prepared compounds were measured by the 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) method and they were compared with the values for the corresponding salts. Enantioseparation was accomplished by means of enantioselective HPLC using amylose tris(3,5-dimethylphenyl)carbamate (Chiralpak AD), as well as Chirobiotic T (native teicoplanin) in some cases.","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-09-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135734149","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Formulation Options for Mucoadhesive Dosage Forms for Use in the Oral Cavity","authors":"V. Šimunková, E. Tichý, M. Špaglová, M. Potúčková","doi":"10.2478/afpuc-2023-0012","DOIUrl":"https://doi.org/10.2478/afpuc-2023-0012","url":null,"abstract":"Abstract Mucoadhesive dosage forms, which are used for topical application in the oral cavity, are currently a very intensively developing field in pharmaceutical technology. Considering the physiological conditions of the oral cavity, the formulation of these mucoadhesive forms is still a challenge. Various types and forms of polymers are used in the experiments, in combination with a large number of drugs, while the achieved effect can be local or systemic and the release rate can be controlled. For many drugs, buccal application is one of the ways to increase their bioavailability.","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-09-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135734682","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Technological Processing of Dried Powdered Rosehips to Tablets Through Wet Granulation","authors":"M. Špaglová, M. Matušková, M.K. Lawson, M. Čuchorová, M. Čierna, D. Krchňák, V. Mikušová, J. Piešťanský, P. Mikuš","doi":"10.2478/afpuc-2023-0061","DOIUrl":"https://doi.org/10.2478/afpuc-2023-0061","url":null,"abstract":"Abstract The pseudo-fruits of Dog Rose are a rich source of L-ascorbic acid and several other active substances, which means their high supportive therapeutic potential. The study aimed to examine the impact of the chosen technological procedure for the preparation of tablets containing rosehip powder on the amount of L-ascorbic acid in the final pharmaceutical form. Drying of the plant drug was performed at room temperature to avoid possible thermal degradation of this heat-sensitive compound. Similarly, drying of the granules after wet granulation in the oven was replaced by natural drying at room temperature. The composition of two types of prepared granule formulations differed in the filler – lactose (LAC) or microcrystalline cellulose (MCC). Apart from the disintegration test, they meet the technological requirements for granules or tablets. Lactose was confirmed as a more suitable filler, which despite the unsuccessful disintegration of the granules, ensures the disintegration of tablets within 15 minutes even without the addition of a special excipient acting as a disintegrant. The content of L-ascorbic acid detected using isotachophoresis – capillary zone electrophoresis was 87.16 ± 5.06 µg in LAC tablets and 63.33 ± 2.83 µg in MCC tablets.","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-09-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47482798","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}