A. Nowicka, E. Szałek, L. Gil, M. Šíma, A. Karbownik
The prognosis for patients with acute myeloid leukaemia (AML) varies depending on genetic factors. The presence of mutations in the fms-like tyrosine kinase 3 (FLT3) gene is found in approximately 30% of AML patients. Midostaurin, a first-generation multi-targeted tyrosine kinase inhibitor, is the first FLT3 inhibitor approved for the treatment of newly diagnosed AML patients with the FLT3 mutation in combination with standard induction and consolidation chemotherapy. However, as numerous clinical trials have shown, the list of indications for this drug is likely to be extended. Midostaurin can be administered orally, which improves the patient’s comfort during treatment. In general, it has a favourable safety profile, but interactions with other drugs, such as strong CYP3A4 inhibitors or inducers, which are often used in the concomitant therapy of AML patients, may lead to changes in midostaurin plasma concentrations. In consequence, such interactions may increase the toxicity of the treatment or reduce its therapeutic effect. The aim of this review is to summarise the current knowledge on midostaurin, i.e. its mechanisms of actions, dosage, adverse effects, mechanisms of resistance and limitations to its use. Due to the growing importance of the management of drug-drug interactions mediated via cytochrome CYP3A4, the main focus of this study is the pharmacokinetics of midostaurin and the variability of its plasma concentrations. The Authors emphasise therapeutic drug monitoring with midostaurin as a potential method of managing AML patients with FLT3 mutation.
{"title":"Midostaurin – the First Targeted Therapy Drug for Patients with Acute Myeloid Leukaemia with FLT3 Mutation","authors":"A. Nowicka, E. Szałek, L. Gil, M. Šíma, A. Karbownik","doi":"10.32383/appdr/159470","DOIUrl":"https://doi.org/10.32383/appdr/159470","url":null,"abstract":"The prognosis for patients with acute myeloid leukaemia (AML) varies depending on genetic factors. The presence of mutations in the fms-like tyrosine kinase 3 (FLT3) gene is found in approximately 30% of AML patients. Midostaurin, a first-generation multi-targeted tyrosine kinase inhibitor, is the first FLT3 inhibitor approved for the treatment of newly diagnosed AML patients with the FLT3 mutation in combination with standard induction and consolidation chemotherapy. However, as numerous clinical trials have shown, the list of indications for this drug is likely to be extended. Midostaurin can be administered orally, which improves the patient’s comfort during treatment. In general, it has a favourable safety profile, but interactions with other drugs, such as strong CYP3A4 inhibitors or inducers, which are often used in the concomitant therapy of AML patients, may lead to changes in midostaurin plasma concentrations. In consequence, such interactions may increase the toxicity of the treatment or reduce its therapeutic effect. The aim of this review is to summarise the current knowledge on midostaurin, i.e. its mechanisms of actions, dosage, adverse effects, mechanisms of resistance and limitations to its use. Due to the growing importance of the management of drug-drug interactions mediated via cytochrome CYP3A4, the main focus of this study is the pharmacokinetics of midostaurin and the variability of its plasma concentrations. The Authors emphasise therapeutic drug monitoring with midostaurin as a potential method of managing AML patients with FLT3 mutation.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2023-03-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41946910","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
K. Karłowicz-Bodalska, T. Han, N. Sauer, W. Szlasa, Olga Szczepańska, N. Janicka, K. Wacławczyk, E. Kuchar, A. Wiela-Hojeńska
Ketoprofen belongs to a group of widely used non-steroidal anti-inflammatory drugs (NSAIDs). It is found in several doses and various forms of medications. Therapeutic efficacy is related to the rate of release of the active substances, which depends on the formulation, the quality of the constituent substances and solubility. In order to determine the efficacy of drug products containing ketoprofen available on the pharmaceutical market in Poland, studies comparing the release profiles of the active substance contained in specific formulation and doses, Ketokaps MAX, 50 mg, soft capsules, Ketonal Active, 50 mg, hard capsules, Ketokaps MED, 100 mg, soft capsules, Refastin, 100 mg, film-coated tablets and Ketonal Forte, 100 mg, film-coated tablets have been conducted. Drug release has been tested using FaSSGF and FaSSIF bioequivalent media in a type IV flow apparatus. The results indicate that the product Ketokaps MAX, 50 mg has a shorter release time of ketoprofen and a faster reached maximum concentration of the released active substance than the market product Ketonal Active, 50 mg. The same outcomes will be achieved by the product Ketokaps MED, 100 mg compared to the market products Refastin, 100 mg and Ketonal Forte, 100 mg. In vitro studies confirm that the tested products differ noticeably in the kinetics of release of the active substance. Ketokaps MAX, 50 mg and Ketokaps MED, 100 mg achieve c max in a shorter time.
{"title":"In vitro dissolution test of ketoprofene: development and evaluation of release from soft and hard gelatine capsules","authors":"K. Karłowicz-Bodalska, T. Han, N. Sauer, W. Szlasa, Olga Szczepańska, N. Janicka, K. Wacławczyk, E. Kuchar, A. Wiela-Hojeńska","doi":"10.32383/appdr/158885","DOIUrl":"https://doi.org/10.32383/appdr/158885","url":null,"abstract":"Ketoprofen belongs to a group of widely used non-steroidal anti-inflammatory drugs (NSAIDs). It is found in several doses and various forms of medications. Therapeutic efficacy is related to the rate of release of the active substances, which depends on the formulation, the quality of the constituent substances and solubility. In order to determine the efficacy of drug products containing ketoprofen available on the pharmaceutical market in Poland, studies comparing the release profiles of the active substance contained in specific formulation and doses, Ketokaps MAX, 50 mg, soft capsules, Ketonal Active, 50 mg, hard capsules, Ketokaps MED, 100 mg, soft capsules, Refastin, 100 mg, film-coated tablets and Ketonal Forte, 100 mg, film-coated tablets have been conducted. Drug release has been tested using FaSSGF and FaSSIF bioequivalent media in a type IV flow apparatus. The results indicate that the product Ketokaps MAX, 50 mg has a shorter release time of ketoprofen and a faster reached maximum concentration of the released active substance than the market product Ketonal Active, 50 mg. The same outcomes will be achieved by the product Ketokaps MED, 100 mg compared to the market products Refastin, 100 mg and Ketonal Forte, 100 mg. In vitro studies confirm that the tested products differ noticeably in the kinetics of release of the active substance. Ketokaps MAX, 50 mg and Ketokaps MED, 100 mg achieve c max in a shorter time.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2023-03-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45501286","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
K. Sosnowska, M. Tomczykowa, K. Winnicka, D. Kalemba, M. Tomczyk
In our study, lavandin oil was hydrodistillated from Lavandula × intermedia (Lamiaceae), and new alginate-based hydrogel formulations containing lavandin oil, linalool, and linalyl acetate were prepared for the first time. Using the gas chromatography (GC) and gas chromatography - mass spectrometry (GC-MS) methods fifty eight components of obtained essential oil were identified. Subsequently, the antipsoriatic activity of the created formulations was investigated by applying an imiquimod-induced mouse model. Alginate-based hydrogels were used as carriers for lavandin oil, linalool, and linalyl acetate. The histopathological examination of imiquimod-induced psoriasis-like mice ear skin stained with H&E (haematoxylin and eosin) was conducted after applying the examined formulations. Additionally, the impact of lavandin oil, linalool, and linalyl acetate on the expression of CD3 (cluster of differentiation 3), CD68 (monoclonal mouse anti-human), and Ki67 (marker of proliferation Ki-67) were studied. Histopathological studies showed that analysed formulations decreased the mice ears’ thickness and the analysed psoriasis symptoms (parakeratosis epidermal thickening, hypertrophy of the spinous layer, inflammatory infiltrates, Munro's microabscesses, Kogoj's micro-pustules, and dermal papillae oedema). The prepared formulations inhibited proliferation of the cells (Ki67 staining method) and expression of CD3 and CD68. The most potent activity against the inflammation in psoriasis was the preparation containing 5% lavandin oil.
{"title":"In vivo evaluation of the antipsoriatic effect of hydrogel with lavandin essential oil and its main components after topical application","authors":"K. Sosnowska, M. Tomczykowa, K. Winnicka, D. Kalemba, M. Tomczyk","doi":"10.32383/appdr/160162","DOIUrl":"https://doi.org/10.32383/appdr/160162","url":null,"abstract":"In our study, lavandin oil was hydrodistillated from Lavandula × intermedia (Lamiaceae), and new alginate-based hydrogel formulations containing lavandin oil, linalool, and linalyl acetate were prepared for the first time. Using the gas chromatography (GC) and gas chromatography - mass spectrometry (GC-MS) methods fifty eight components of obtained essential oil were identified. Subsequently, the antipsoriatic activity of the created formulations was investigated by applying an imiquimod-induced mouse model. Alginate-based hydrogels were used as carriers for lavandin oil, linalool, and linalyl acetate. The histopathological examination of imiquimod-induced psoriasis-like mice ear skin stained with H&E (haematoxylin and eosin) was conducted after applying the examined formulations. Additionally, the impact of lavandin oil, linalool, and linalyl acetate on the expression of CD3 (cluster of differentiation 3), CD68 (monoclonal mouse anti-human), and Ki67 (marker of proliferation Ki-67) were studied. Histopathological studies showed that analysed formulations decreased the mice ears’ thickness and the analysed psoriasis symptoms (parakeratosis epidermal thickening, hypertrophy of the spinous layer, inflammatory infiltrates, Munro's microabscesses, Kogoj's micro-pustules, and dermal papillae oedema). The prepared formulations inhibited proliferation of the cells (Ki67 staining method) and expression of CD3 and CD68. The most potent activity against the inflammation in psoriasis was the preparation containing 5% lavandin oil.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2023-03-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44649544","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Nimesulide is a poorly water-soluble, non-steroidal anti-inflammatory drug for both systemic and topical application. The aim of the study was to assess the influence of the type of base and surfactants (Tween80, Span80, soy lecithin, sodium lauryl sulphate) on drug release from rectal suppositories. Suppositories were prepared in the Unquator® using Cacao butter, Witepsol H15 and PEG1500:PEG400 as a base. The physicochemical properties of the prepared suppositories were in accordance to the Pharmacopoeia’s requirements. In vitro dissolution profile of the formulations was evaluated using USP apparatus 1. It has been shown that most of the nimesulide was released from suppositories prepared on PEG base. Addition of 2% surfactant to lipophilic base suppositories, significantly increased the amount of nimesulide released from all the investigated formulae. Among the formulations containing surfactants, only Witepsol H15 with Span 80 released a nearly complete drug during 210 minutes. The results indicate that the First-Order model is the best fit with the nimesulide in-vitro release from lipophilic suppositories, while the Higuchi model - to the PEG suppositories. The drug release kinetics from suppositories showed that the Cacao butter bases adequately fit data for zero-order kinetics model, while the Higuchi model - for the PEG suppositories.
{"title":"Formulation, characterization, and in vitro evaluation release nimesulide from different rectal suppository bases","authors":"B. Szulc-Musioł, L. Bułaś, B. Dolińska","doi":"10.32383/appdr/159289","DOIUrl":"https://doi.org/10.32383/appdr/159289","url":null,"abstract":"Nimesulide is a poorly water-soluble, non-steroidal anti-inflammatory drug for both systemic and topical application. The aim of the study was to assess the influence of the type of base and surfactants (Tween80, Span80, soy lecithin, sodium lauryl sulphate) on drug release from rectal suppositories. Suppositories were prepared in the Unquator® using Cacao butter, Witepsol H15 and PEG1500:PEG400 as a base. The physicochemical properties of the prepared suppositories were in accordance to the Pharmacopoeia’s requirements. In vitro dissolution profile of the formulations was evaluated using USP apparatus 1. It has been shown that most of the nimesulide was released from suppositories prepared on PEG base. Addition of 2% surfactant to lipophilic base suppositories, significantly increased the amount of nimesulide released from all the investigated formulae. Among the formulations containing surfactants, only Witepsol H15 with Span 80 released a nearly complete drug during 210 minutes. The results indicate that the First-Order model is the best fit with the nimesulide in-vitro release from lipophilic suppositories, while the Higuchi model - to the PEG suppositories. The drug release kinetics from suppositories showed that the Cacao butter bases adequately fit data for zero-order kinetics model, while the Higuchi model - for the PEG suppositories.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2023-03-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44812326","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
M. Nikolić, V. Jakovljevic, Jovana V Bradic, M. Tomovic, B. Petrović, A. Petrovic
Background: Pinus sibirica and Pinus koraiensis are belonging to the same subsection Strobus, within the Pinaceae family. The most abundant classes of bioactive compounds isolated from them are terpenes, phenols and fatty acids. Different forms of the abovementioned plants have been used in folk medicine for the prevention and treatment of many diseases. Pinus sibirica has been used to cure rheumatism, arthritis as well as to treat infections, fungal diseases and wounds. It is also considered to exhibit a hypolipidemic, anti-allergic and antiseptic properties. Similarly, Pinus koraiensis is used tradidionaly to treat cough, infections, wounds and rheumatism. Furthermore, essential oil from Korean pine has antitumor, anti-ageing, and sedative effects. Objective: Our aim was to compile literature data regarding chemical composition and pharmacological effects of different preparations from Pinus sibirica and Pinus koraiensis plants, covering from pre-clinical data to upcoming clinical studies. Method: Articles were collected by searching databases: Medline/PubMed, SCOPUS, Embase, and Web of Science. There was no limitation for year of publication and search was not limited only on articles in English language. Results: Given the literature reports, both Siberian and Korean pines, rich in terpenes and phenols, are mainly used in investigations where they expressed antitumor, hepatoprotective or appetite suppressant properties. Conclusion: This review provided compilation of available data about chemical composition, biological profile and therapeutic usage of Pinus sibirica and Pinus koraiensis. Numerous ingredients found in those plants have great potential for examination of numerous pharmacological effects which can lead to production of innovative therapeutic agent.
背景:西伯利亚松(Pinus sibirica)和红松(Pinus koraiensis)同属松科松分节。从它们中分离出的最丰富的一类生物活性化合物是萜烯、酚类和脂肪酸。上述植物的不同形式已在民间医学中用于预防和治疗许多疾病。西伯利亚松被用来治疗风湿病、关节炎以及治疗感染、真菌疾病和伤口。它还被认为具有降血脂、抗过敏和防腐的特性。同样，红松传统上用于治疗咳嗽、感染、伤口和风湿病。此外，红松精油具有抗肿瘤、抗衰老和镇静作用。目的:收集西伯利亚松和红松植物不同制剂的化学成分和药理作用的文献资料，涵盖从临床前数据到即将进行的临床研究。方法:通过检索Medline/PubMed、SCOPUS、Embase、Web of Science等数据库收集文献。没有出版年份的限制，搜索不仅限于英文文章。结果:根据文献报道，西伯利亚松和红松富含萜烯和酚类物质，主要用于抗肿瘤、保肝或抑制食欲的研究。结论:本文综述了西伯利亚松和红松的化学成分、生物学特性和治疗用途等方面的资料。在这些植物中发现的许多成分具有巨大的潜力，可以用于研究许多药理作用，从而生产出创新的治疗剂。
{"title":"Korean and Siberian pine: Review of chemical composition and pharmacological profile","authors":"M. Nikolić, V. Jakovljevic, Jovana V Bradic, M. Tomovic, B. Petrović, A. Petrovic","doi":"10.32383/appdr/161040","DOIUrl":"https://doi.org/10.32383/appdr/161040","url":null,"abstract":"Background: Pinus sibirica and Pinus koraiensis are belonging to the same subsection Strobus, within the Pinaceae family. The most abundant classes of bioactive compounds isolated from them are terpenes, phenols and fatty acids. Different forms of the abovementioned plants have been used in folk medicine for the prevention and treatment of many diseases. Pinus sibirica has been used to cure rheumatism, arthritis as well as to treat infections, fungal diseases and wounds. It is also considered to exhibit a hypolipidemic, anti-allergic and antiseptic properties. Similarly, Pinus koraiensis is used tradidionaly to treat cough, infections, wounds and rheumatism. Furthermore, essential oil from Korean pine has antitumor, anti-ageing, and sedative effects. Objective: Our aim was to compile literature data regarding chemical composition and pharmacological effects of different preparations from Pinus sibirica and Pinus koraiensis plants, covering from pre-clinical data to upcoming clinical studies. Method: Articles were collected by searching databases: Medline/PubMed, SCOPUS, Embase, and Web of Science. There was no limitation for year of publication and search was not limited only on articles in English language. Results: Given the literature reports, both Siberian and Korean pines, rich in terpenes and phenols, are mainly used in investigations where they expressed antitumor, hepatoprotective or appetite suppressant properties. Conclusion: This review provided compilation of available data about chemical composition, biological profile and therapeutic usage of Pinus sibirica and Pinus koraiensis. Numerous ingredients found in those plants have great potential for examination of numerous pharmacological effects which can lead to production of innovative therapeutic agent.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2023-03-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43890091","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Piotr Bramora, M. Zych, Weronka Borymska, Ilona Kaczmarczyk-Żebrowska
Chronic hyperglycemia is one of the most important causes of the formation of oxygen free radicals in diabetes, which damage various organs. Damage to proteins and lipids in the heart can lead to the development of diabetic cardiomyopathy, which in turn may cause cardiovascular failure. In order to counteract oxidative stress, the innate antioxidant mechanisms of the system should be supported by supplementation with exogenous antioxidants, for instance of plant origin. In this experiment, the role of silymarin, a plant-derived flavonolignan on the oxidative stress parameters and oxidative damage markers in the hearts was determined in an experimental model of diabetes. Male Wistar rats were injected with streptozotocin at a dose of 60 mg/kg (ip). Then, silymarin was administered at doses of 50 and 100 mg/kg for four weeks via a gastric tube. In diabetic animals an increase in malondialdehyde, advanced oxidation protein products, as well as increased activity of antioxidant enzymes in heart tissues was noted. Administration of silymarin inhibited oxidative stress by increasing the total antioxidant response, decreasing the concentration of malondialdehyde and advanced oxidation protein products and a slight increase in the level of glutathione. It can be concluded that the redox state in the examined tissue improved. Based on the results in can be concluded that silymarin demonstrates a potential in preventing the development of oxidative damage in the heart tissue in the course of experimental diabetes.
{"title":"Effect of silymarin on the parameters of oxidative stress in hearts in the course of diabetes mellitus in Wistar rats","authors":"Piotr Bramora, M. Zych, Weronka Borymska, Ilona Kaczmarczyk-Żebrowska","doi":"10.32383/appdr/159412","DOIUrl":"https://doi.org/10.32383/appdr/159412","url":null,"abstract":"Chronic hyperglycemia is one of the most important causes of the formation of oxygen free radicals in diabetes, which damage various organs. Damage to proteins and lipids in the heart can lead to the development of diabetic cardiomyopathy, which in turn may cause cardiovascular failure. In order to counteract oxidative stress, the innate antioxidant mechanisms of the system should be supported by supplementation with exogenous antioxidants, for instance of plant origin. In this experiment, the role of silymarin, a plant-derived flavonolignan on the oxidative stress parameters and oxidative damage markers in the hearts was determined in an experimental model of diabetes. Male Wistar rats were injected with streptozotocin at a dose of 60 mg/kg (ip). Then, silymarin was administered at doses of 50 and 100 mg/kg for four weeks via a gastric tube. In diabetic animals an increase in malondialdehyde, advanced oxidation protein products, as well as increased activity of antioxidant enzymes in heart tissues was noted. Administration of silymarin inhibited oxidative stress by increasing the total antioxidant response, decreasing the concentration of malondialdehyde and advanced oxidation protein products and a slight increase in the level of glutathione. It can be concluded that the redox state in the examined tissue improved. Based on the results in can be concluded that silymarin demonstrates a potential in preventing the development of oxidative damage in the heart tissue in the course of experimental diabetes.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2023-03-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45802551","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Ketamine, a phencyclidine derivative, is most usually used to induce dissociative general anesthesia, but it is also beneficial for bronchospasm, a congenital cardiac disease with the right to left shunting, and, more recently, treatment of resistant depression. Several studies have revealed that ketamine may help damaged neurons recover. Ketamine has been proven to offer neuroprotection in a variety of neuro injury models. Following that, many routes and targets were identified to demonstrate how ketamine may protect the brain. Ketamine has been shown to modulate neuronal excitotoxicity, apoptosis, and inflammation, among other things. The present work examined the relative interaction of ketamine with potential targets of brain excitotoxicity, apoptosis, and inflammation using an in-silico approach. Furthermore, ketamine has been shown to protect against isoflurane-induced cognitive impairment in rats.
{"title":"In silico and in vivo investigation of the neuroprotective benefits of Ketamine against isoflurane-induced cognitive impairment","authors":"P. Krishnamurthy, Shenghui Luan","doi":"10.32383/appdr/157502","DOIUrl":"https://doi.org/10.32383/appdr/157502","url":null,"abstract":"Ketamine, a phencyclidine derivative, is most usually used to induce dissociative general anesthesia, but it is also beneficial for bronchospasm, a congenital cardiac disease with the right to left shunting, and, more recently, treatment of resistant depression. Several studies have revealed that ketamine may help damaged neurons recover. Ketamine has been proven to offer neuroprotection in a variety of neuro injury models. Following that, many routes and targets were identified to demonstrate how ketamine may protect the brain. Ketamine has been shown to modulate neuronal excitotoxicity, apoptosis, and inflammation, among other things. The present work examined the relative interaction of ketamine with potential targets of brain excitotoxicity, apoptosis, and inflammation using an in-silico approach. Furthermore, ketamine has been shown to protect against isoflurane-induced cognitive impairment in rats.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2023-01-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41595709","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The frequent occurrence of bacterial skin infections makes it necessary to search new solutions. Due to the limited effectiveness of traditional antibacterial agents, novel treatment alternatives are investigated. The use of plant origin compounds seems to be beneficial, because they are usually well tolerated and do not cause as many side effects as synthetic substances. Tea tree oil (TTO) is noted for well-established antimicrobial activity, so it can be used in the treatment of various skin diseases. It is effective against Gram-negative as well as Gram-positive bacteria. The aim of this work was to develop the composition and preparation technology of emulsion with TTO using natural emulsifier Olivem 1000 - combination of cetearyl olivate and sorbitan olivate. The designed formulations were evaluated by testing pH, stability and droplets size of the dispersed phase in the prepared emulsions. The type of emulsions was determined by selective phase staining method. In addition, rheological, mechanical, ex vivo bioadhesive properties of the prepared emulsions were studied and their antibacterial activity against selected strains was estimated. Obtained formulations were non-Newtonian systems, showing a shear-thinning behaviour and thixotropic properties, with proper textural features and beneficial bioadhesive properties. It was also demonstrated that formulations with lower viscosity showed higher antimicrobial efficacy against tested microorganisms and larger zones of inhibition were observed in case of Escherichia coli strains. The results of the study showed that the prepared emulsions appear to be a suitable form of topical administration of TTO.
{"title":"Composition development and in vitro evaluation of O/W emulsions based on natural emulsifier Olivem 1000 as tea tree oil carriers","authors":"M. Wróblewska, K. Winnicka","doi":"10.32383/appdr/158784","DOIUrl":"https://doi.org/10.32383/appdr/158784","url":null,"abstract":"The frequent occurrence of bacterial skin infections makes it necessary to search new solutions. Due to the limited effectiveness of traditional antibacterial agents, novel treatment alternatives are investigated. The use of plant origin compounds seems to be beneficial, because they are usually well tolerated and do not cause as many side effects as synthetic substances. Tea tree oil (TTO) is noted for well-established antimicrobial activity, so it can be used in the treatment of various skin diseases. It is effective against Gram-negative as well as Gram-positive bacteria. The aim of this work was to develop the composition and preparation technology of emulsion with TTO using natural emulsifier Olivem 1000 - combination of cetearyl olivate and sorbitan olivate. The designed formulations were evaluated by testing pH, stability and droplets size of the dispersed phase in the prepared emulsions. The type of emulsions was determined by selective phase staining method. In addition, rheological, mechanical, ex vivo bioadhesive properties of the prepared emulsions were studied and their antibacterial activity against selected strains was estimated. Obtained formulations were non-Newtonian systems, showing a shear-thinning behaviour and thixotropic properties, with proper textural features and beneficial bioadhesive properties. It was also demonstrated that formulations with lower viscosity showed higher antimicrobial efficacy against tested microorganisms and larger zones of inhibition were observed in case of Escherichia coli strains. The results of the study showed that the prepared emulsions appear to be a suitable form of topical administration of TTO.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2023-01-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43970051","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Dan Liang, Zelian Chen, Jian Zhang, Lan Su, Zhifeng Chen
Objective：To establish a method for the dissolutions profile determination of Eldecalcitol softgels, evaluate the in vitro dissolutions behavior between domestic Eldecalcitol soft capsules and the original preparation。Methods：The effects of different stirring apparatus, different dissolutions medium, different agitation speeds on the dissolutions behavior of Eldecalcitol soft capsules were investigated, cumulative dissolutions were calculated by measuring the dissolutions samples with HPLC-MS/MS method. Results：The dissolutions test of Eldecalcitol soft capsules was carried out by rotating basket method, agitation speed of 75 rpm, temperature of 37℃ in four mediums。Conclusion：This dissolutions method can be effectively applied to the dissolutions test of soft Eldecalcitol capsules. and the selected generics have good dissolution consistency with the original drugs. Keywords：Eldecalcitol soft capsules；dissolutions method；dissolutions behavior；consistency evaluation
{"title":"Study on dissolution behavior in vitro of an osteoporosis treatment drug: eldecalcitol soft capsule","authors":"Dan Liang, Zelian Chen, Jian Zhang, Lan Su, Zhifeng Chen","doi":"10.32383/appdr/154948","DOIUrl":"https://doi.org/10.32383/appdr/154948","url":null,"abstract":"Objective：To establish a method for the dissolutions profile determination of Eldecalcitol softgels, evaluate the in vitro dissolutions behavior between domestic Eldecalcitol soft capsules and the original preparation。Methods：The effects of different stirring apparatus, different dissolutions medium, different agitation speeds on the dissolutions behavior of Eldecalcitol soft capsules were investigated, cumulative dissolutions were calculated by measuring the dissolutions samples with HPLC-MS/MS method. Results：The dissolutions test of Eldecalcitol soft capsules was carried out by rotating basket method, agitation speed of 75 rpm, temperature of 37℃ in four mediums。Conclusion：This dissolutions method can be effectively applied to the dissolutions test of soft Eldecalcitol capsules. and the selected generics have good dissolution consistency with the original drugs.\u0000Keywords：Eldecalcitol soft capsules；dissolutions method；dissolutions behavior；consistency evaluation","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2023-01-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44798502","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
M. Ćulafić, Milena Kovačević, Marija Jovanović, M. Roganović, S. Vezmar Kovačević, K. Vučićević, B. Miljković
Background: COPD is a chronic condition requiring care from a multidisciplinary team in which pharmacists play an important role. Aim: We aimed to evaluate the impact of structured pharmacist-patient counseling on patient’s knowledge, attitudes about medicines and the impact of COPD on patients’ health status. Methods: A prospective study was conducted in ten community pharmacies. Patients were counseled using detailed approach after completing validated questionnaires. The patients returned to a pharmacy for a follow-up after three months. Four validated questionnaires have been used to assess different aspects of patient’s knowledge about the disease, their attitudes about medicines and the impact of disease on patients’ health status: COPD Assessment Test (CAT), Modified Medical Research Council Dyspnea Scale (mMRC), Bristol COPD Knowledge Questionnaire (BCKQ), and The Beliefs about Medicines Questionnaire (BMQ). Results: Pharmacists recruited 83 COPD patients, from which 73 patients attended a follow-up visit. Before pharmacist intervention, the CAT median score was 20. After counseling, the CAT score decreased to 18 (p<0.05). The highest improvement in patient’s knowledge was observed for inhaled bronchodilators (28.2%), vaccination (25.8%), oral steroids (24.4%), and smoking (24.2%). The median score for necessity increased, whereas the harm and concern median scores considerably decreased (p<0.05). Conclusion: The results showed significant improvements in all aspects covered throughout pharmacist-patient counseling. Based on our results, proactive role of the pharmacist in the care of COPD patients may be beneficial to patients, to physicians and to healthcare: improving care, alleviating the strain on overloaded doctors with containing the costs.
{"title":"Community pharmacist-driven interventions in COPD: improving knowledge, attitude and health status","authors":"M. Ćulafić, Milena Kovačević, Marija Jovanović, M. Roganović, S. Vezmar Kovačević, K. Vučićević, B. Miljković","doi":"10.32383/appdr/155353","DOIUrl":"https://doi.org/10.32383/appdr/155353","url":null,"abstract":"Background: COPD is a chronic condition requiring care from a multidisciplinary team in which pharmacists play an important role. \u0000Aim: We aimed to evaluate the impact of structured pharmacist-patient counseling on patient’s knowledge, attitudes about medicines and the impact of COPD on patients’ health status. \u0000Methods: A prospective study was conducted in ten community pharmacies. Patients were counseled using detailed approach after completing validated questionnaires. The patients returned to a pharmacy for a follow-up after three months. Four validated questionnaires have been used to assess different aspects of patient’s knowledge about the disease, their attitudes about medicines and the impact of disease on patients’ health status: COPD Assessment Test (CAT), Modified Medical Research Council Dyspnea Scale (mMRC), Bristol COPD Knowledge Questionnaire (BCKQ), and The Beliefs about Medicines Questionnaire (BMQ).\u0000Results: Pharmacists recruited 83 COPD patients, from which 73 patients attended a follow-up visit. Before pharmacist intervention, the CAT median score was 20. After counseling, the CAT score decreased to 18 (p<0.05). The highest improvement in patient’s knowledge was observed for inhaled bronchodilators (28.2%), vaccination (25.8%), oral steroids (24.4%), and smoking (24.2%). The median score for necessity increased, whereas the harm and concern median scores considerably decreased (p<0.05).\u0000Conclusion: The results showed significant improvements in all aspects covered throughout pharmacist-patient counseling. Based on our results, proactive role of the pharmacist in the care of COPD patients may be beneficial to patients, to physicians and to healthcare: improving care, alleviating the strain on overloaded doctors with containing the costs.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2023-01-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42636365","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
京公网安备 11010802042870号
京ICP备2023020795号-1
扫码关注我们
求助内容：
应助结果提醒方式：