{"title":"PLANT PHENOLICS AND THEIR SYNTHETIC DERIVATIVES AS INHIBITORS OF HELICOBACTER PYLORI: SUGGESTION FOR A NEW MECHANISM OF ACTION","authors":"Simone Carradori","doi":"10.29228/jrp.388","DOIUrl":"https://doi.org/10.29228/jrp.388","url":null,"abstract":"","PeriodicalId":17096,"journal":{"name":"Journal of Research in Pharmacy","volume":"1 1","pages":""},"PeriodicalIF":0.8,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"69838607","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}
: The main objective of this study was to model patient experience (PX) in community pharmacies as experimental marketing parameters via structural equation modeling (SEM). Our findings show that peace of mind, trust, pharmacy, customer engagement, interaction quality with the pharmacist and personnel, and atmosphere or periphery experience quality is the important component for a patient to re-visit the same pharmacy. The patient's journey to the pharmacy starts before entering the pharmacy, continues at the pharmacy, and then leaves the pharmacy. It is important to understand the touchpoint of the patient journey at a community pharmacy and the needs of the patients as well as other health services. Overall, whether it is patient experience or customer experience, both focus on people and understanding their needs as a service sector will add value to service quality. The research was conducted on 414 volunteer patients given informed consent and answered 73 items in Istanbul province. The data obtained from the questionnaire forms were analyzed using the IBM SPSS Statistics 23 package program. Confirmatory factor analysis (CFA) was applied using IBM SPSS AMOS 23 package program in the analysis of trust, pharmacy customer engagement (PCE), word of mouth (WoM), pharmacist interaction quality, personnel interaction quality, periphery experience quality, peace-of-mind (POM), and autobiographical memory parameters. Since the assumption of normality was not provided, the relationships among these items were calculated using Spearman's correlation coefficient. The results were evaluated at the significance level of p <0.05. Finally, a structural equation model was conducted to specify PX items.
{"title":"Patient experience in community pharmacies from an experiential marketing perspective: structural equation model","authors":"Demet AKALGAN AKLAR, G. Ozcelikay","doi":"10.29228/jrp.391","DOIUrl":"https://doi.org/10.29228/jrp.391","url":null,"abstract":": The main objective of this study was to model patient experience (PX) in community pharmacies as experimental marketing parameters via structural equation modeling (SEM). Our findings show that peace of mind, trust, pharmacy, customer engagement, interaction quality with the pharmacist and personnel, and atmosphere or periphery experience quality is the important component for a patient to re-visit the same pharmacy. The patient's journey to the pharmacy starts before entering the pharmacy, continues at the pharmacy, and then leaves the pharmacy. It is important to understand the touchpoint of the patient journey at a community pharmacy and the needs of the patients as well as other health services. Overall, whether it is patient experience or customer experience, both focus on people and understanding their needs as a service sector will add value to service quality. The research was conducted on 414 volunteer patients given informed consent and answered 73 items in Istanbul province. The data obtained from the questionnaire forms were analyzed using the IBM SPSS Statistics 23 package program. Confirmatory factor analysis (CFA) was applied using IBM SPSS AMOS 23 package program in the analysis of trust, pharmacy customer engagement (PCE), word of mouth (WoM), pharmacist interaction quality, personnel interaction quality, periphery experience quality, peace-of-mind (POM), and autobiographical memory parameters. Since the assumption of normality was not provided, the relationships among these items were calculated using Spearman's correlation coefficient. The results were evaluated at the significance level of p <0.05. Finally, a structural equation model was conducted to specify PX items.","PeriodicalId":17096,"journal":{"name":"Journal of Research in Pharmacy","volume":"1 1","pages":""},"PeriodicalIF":0.8,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"69838724","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}
: Magnesium oxide nanoparticles (MgO-NPs) were synthesis via green method using Opunita ficus indica extract as reducing and covering agent. The optimal formula for the preparation of MgO-NPs was determined by UV-Vis and DLS ( Opunita ficus -indica extracted by distilled water and ethanol solvent, magnesium nitrate salt (1mM), stirred at 70 °C for 24 h with pH= 9). UV-Vis analysis showed a peak at 300 nm, while DLS measured the hydrodynamic diameter of the nanoparticles. FTIR results suggested that the polysaccharides, phenols and amines present in the extract might have been involved in the formation of MgO-NPs from Mg (NO3)2 as the reducing agent. Image J was utilized to analyze the SEM results and determine the size, which was on average 99 nm, the shape of the nanoparticles was spherical, and EDX spectrum confirmed the presence of magnesium (Mg). It was found that MgO-NPs are highly toxic against Aspergillus niger . Which showed a gradual inhibitory effect when using the concentration of 0.5% and 1.25%, and the inhibitory ability was 66.6%, 100% respectively, when using the poisoned food technique.
{"title":"Biosynthesis of Magnesium Oxide Nanoparticles Using Opunita ficus-indica and Their Antifungal Effect Against Aspergillus Niger","authors":"Taif Alholy, Walid Khaddam","doi":"10.29228/jrp.408","DOIUrl":"https://doi.org/10.29228/jrp.408","url":null,"abstract":": Magnesium oxide nanoparticles (MgO-NPs) were synthesis via green method using Opunita ficus indica extract as reducing and covering agent. The optimal formula for the preparation of MgO-NPs was determined by UV-Vis and DLS ( Opunita ficus -indica extracted by distilled water and ethanol solvent, magnesium nitrate salt (1mM), stirred at 70 °C for 24 h with pH= 9). UV-Vis analysis showed a peak at 300 nm, while DLS measured the hydrodynamic diameter of the nanoparticles. FTIR results suggested that the polysaccharides, phenols and amines present in the extract might have been involved in the formation of MgO-NPs from Mg (NO3)2 as the reducing agent. Image J was utilized to analyze the SEM results and determine the size, which was on average 99 nm, the shape of the nanoparticles was spherical, and EDX spectrum confirmed the presence of magnesium (Mg). It was found that MgO-NPs are highly toxic against Aspergillus niger . Which showed a gradual inhibitory effect when using the concentration of 0.5% and 1.25%, and the inhibitory ability was 66.6%, 100% respectively, when using the poisoned food technique.","PeriodicalId":17096,"journal":{"name":"Journal of Research in Pharmacy","volume":"25 1","pages":""},"PeriodicalIF":0.8,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"69838789","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":"R&D STUDIES IN THE DEVELOPMENT OF TRADITIONAL HERBAL MEDICINAL PRODUCTS","authors":"Iffet Irem TATLI ÇANKAYA","doi":"10.29228/jrp.379","DOIUrl":"https://doi.org/10.29228/jrp.379","url":null,"abstract":"","PeriodicalId":17096,"journal":{"name":"Journal of Research in Pharmacy","volume":"1 1","pages":""},"PeriodicalIF":0.8,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"69838884","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}
R. Dubey, L. Sathiyanarayanan, Laxmi Rao, S. Sankaran
: Apis mellifera , a priceless bee species is known to produce various nutritional products. Royal Jelly (RJ) is one such bee product which has high nutritive value, functional and biological qualities. However factors such as bee species, environment, season, collection technique and larval age affect the composition of RJ at macro and micro levels thus there is a need to evaluate Indian Royal Jelly (IRJ) for its chemical properties. So in the present work IRJ samples collected from Southern, Central and Northern regions of India were evaluated for physicochemical parameters (nature, color, appearance, odor, and solubility,) residual content (moisture content, ash value and pesticide content), chemical attributes (total polyphenol content, total flavonoid content,), nutraceutical potential (total fat, protein, carbohydrate content, and energy), and antioxidant activity (DPPH assay, ABTS assay and reducing power,). The total flavonoid content and total phenolic content were in the range of 0.119-0.321 mg quercetin/g of IRJ and 25.2844-68.203 mg Gallic acid/g, respectively. High energy, protein and low fat value suggested IRJ as a suitable nutraceutical agent. Antioxidant activity (IC 50 ) of IRJ samples was found to be in the order of IRJ II > IRJ IV > IRJ I > IRJ III. Overall, it was observed that the IRJ-II showed better nutritional efficacy, polyphenolic content, and antioxidant properties.
蜜蜂是一种无价的蜜蜂，它能生产各种营养产品。蜂王浆(RJ)是一种具有较高营养价值、功能性和生物学品质的蜂产品。然而，蜜蜂种类、环境、季节、采集技术和幼虫年龄等因素对蜂王浆的组成有宏观和微观的影响，因此有必要对印度蜂王浆(IRJ)的化学性质进行评价。因此，在本工作中，从印度南部、中部和北部地区收集的IRJ样品进行了理化参数(性质、颜色、外观、气味和溶解度)、残留量(水分含量、灰分值和农药含量)、化学属性(总多酚含量、总黄酮含量)、营养潜力(总脂肪、蛋白质、碳水化合物含量和能量)和抗氧化活性(DPPH测定、ABTS测定和还原力)的评估。IRJ的总黄酮含量为0.119 ~ 0.321 mg槲皮素/g，总酚含量为25.2844 ~ 68.203 mg没食子酸/g。高能量、高蛋白质、低脂肪的营养价值表明IRJ是一种合适的营养保健剂。IRJ样品的抗氧化活性(IC 50)依次为IRJ II > IRJ IV > IRJ I > IRJ III。总体而言，IRJ-II具有更好的营养功效、多酚含量和抗氧化性能。
{"title":"Investigation of Nutraceutical Potential, in vitro Antioxidant and Free Radical Scavenging Activity of Indian Royal Jelly","authors":"R. Dubey, L. Sathiyanarayanan, Laxmi Rao, S. Sankaran","doi":"10.29228/jrp.417","DOIUrl":"https://doi.org/10.29228/jrp.417","url":null,"abstract":": Apis mellifera , a priceless bee species is known to produce various nutritional products. Royal Jelly (RJ) is one such bee product which has high nutritive value, functional and biological qualities. However factors such as bee species, environment, season, collection technique and larval age affect the composition of RJ at macro and micro levels thus there is a need to evaluate Indian Royal Jelly (IRJ) for its chemical properties. So in the present work IRJ samples collected from Southern, Central and Northern regions of India were evaluated for physicochemical parameters (nature, color, appearance, odor, and solubility,) residual content (moisture content, ash value and pesticide content), chemical attributes (total polyphenol content, total flavonoid content,), nutraceutical potential (total fat, protein, carbohydrate content, and energy), and antioxidant activity (DPPH assay, ABTS assay and reducing power,). The total flavonoid content and total phenolic content were in the range of 0.119-0.321 mg quercetin/g of IRJ and 25.2844-68.203 mg Gallic acid/g, respectively. High energy, protein and low fat value suggested IRJ as a suitable nutraceutical agent. Antioxidant activity (IC 50 ) of IRJ samples was found to be in the order of IRJ II > IRJ IV > IRJ I > IRJ III. Overall, it was observed that the IRJ-II showed better nutritional efficacy, polyphenolic content, and antioxidant properties.","PeriodicalId":17096,"journal":{"name":"Journal of Research in Pharmacy","volume":"1 1","pages":""},"PeriodicalIF":0.8,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"69839008","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}
: Shallot skin has potential as a medicinal raw material because it contains many quercetin compounds. It is necessary to conduct a study on the optimization of extraction methods and the extracts standardization. The purpose of this study is the standardization of simplicia, optimization of extraction methods and standardization of shallot skin purified extract as standardized on quercetin. This study is aimed to support quality control of simplicia and shallot skin extract as a source of quercetin. The methods of the study include the collection of raw materials, preparation of simplicia, standardization of simplicia, and optimization of extraction methods with Response Surface Methodology (RSM) using Box-Behnken Design (BBD), standardization of standardized quercetin purified extracts. Based on the results obtained, shallot skin simplicia has a moisture content of 7.98 and a total ash content of 9.91%. Based on the analysis, the optimum point of the solvent concentration factor, time, and the solvent ratio on the yield of the purified extract were respectively 60.42%, 1.29 hours, and 24.45 mL/g. The yield average obtained was 5.16 ± 0.1125 % with a content of 5.947 ppm (0.005497 mg/g).
{"title":"Response surface methodology-aided maceration method optimization of quercetin-standardized purified extract of shallot skin (Allium cepa L var. aggregatum)","authors":"Sapri Sapri, F. Riswanto, E. Wulandari","doi":"10.29228/jrp.428","DOIUrl":"https://doi.org/10.29228/jrp.428","url":null,"abstract":": Shallot skin has potential as a medicinal raw material because it contains many quercetin compounds. It is necessary to conduct a study on the optimization of extraction methods and the extracts standardization. The purpose of this study is the standardization of simplicia, optimization of extraction methods and standardization of shallot skin purified extract as standardized on quercetin. This study is aimed to support quality control of simplicia and shallot skin extract as a source of quercetin. The methods of the study include the collection of raw materials, preparation of simplicia, standardization of simplicia, and optimization of extraction methods with Response Surface Methodology (RSM) using Box-Behnken Design (BBD), standardization of standardized quercetin purified extracts. Based on the results obtained, shallot skin simplicia has a moisture content of 7.98 and a total ash content of 9.91%. Based on the analysis, the optimum point of the solvent concentration factor, time, and the solvent ratio on the yield of the purified extract were respectively 60.42%, 1.29 hours, and 24.45 mL/g. The yield average obtained was 5.16 ± 0.1125 % with a content of 5.947 ppm (0.005497 mg/g).","PeriodicalId":17096,"journal":{"name":"Journal of Research in Pharmacy","volume":"1 1","pages":""},"PeriodicalIF":0.8,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"69839357","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}
: Acute myeloid leukemia (AML) is a form of acute leukemia with the highest incidence and the lowest overall survival rates. Insufficiency of targeting leukemia stem cells (LSC) is the main obstacle that causes drug resistance and relapse in AML. Another important problem is chemotherapeutics’ toxicity. Developing a combination, including well-known chemotherapeutics in lower dose and new agent that have capacity to target LSC may be more reliable and practical way to overcome these limitations. Previously, we found that Casticin polyphenol induces apoptosis in AML stem-like (KG1a) and parental (KG1) cell lines without affecting healthy cell. Therefore, for the first time, we aimed to find synergistic combination of Daunorubicin (DNR) and Casticin to target apoptosis in both LSC and leukemic blasts with less toxicity. Synergism of DNR-Casticin combinations on KG1a, KG1, HL-60 cells were determined with MTT viability assay by Chou-Talalay method. The apoptotic/necrotic effects of combinations were evaluated with Annexin V- PI kit by flow cytometry. Synergistic combination of 0.25 µM DNR + 0.0625 µM Casticin (combination index, CI<1) decreased cell viability to 45.3% and 63.2% in KG1a, KG1 cell lines, respectively. However, the combination-induced apoptosis (KG1a: 5 %; KG1: 5.8%) were not higher than 0.25 µM DNR-induced (KG1a: 9.4%; KG1: 8.1%) or 0.0625 µM Casticin-induced (KG1a: 3.8%; KG1: 5.1%) apoptosis (p>0.05). Our study showed that synergistic combination of DNR-Casticin causes important decrease in cell viability. Although we did not detect increase in apoptosis with the combination, we presume that other cell death pathways may be included. The highest apoptosis was obtained by the treatment of 2 µM Casticin alone in KG1a (21.7%), KG1 (26.5%), HL-60 (14.6%). Therefore, we think that Casticin polyphenol might be the possible candidate for new targeted therapy studies for AML.
{"title":"Does Combination of DNR and Casticin show advantage in favor of apoptosis on AML leukemia stem-like cell lines? A preliminary study","authors":"Tuğba Erkmen, H. Ateş, A. S. Koçtürk","doi":"10.29228/jrp.416","DOIUrl":"https://doi.org/10.29228/jrp.416","url":null,"abstract":": Acute myeloid leukemia (AML) is a form of acute leukemia with the highest incidence and the lowest overall survival rates. Insufficiency of targeting leukemia stem cells (LSC) is the main obstacle that causes drug resistance and relapse in AML. Another important problem is chemotherapeutics’ toxicity. Developing a combination, including well-known chemotherapeutics in lower dose and new agent that have capacity to target LSC may be more reliable and practical way to overcome these limitations. Previously, we found that Casticin polyphenol induces apoptosis in AML stem-like (KG1a) and parental (KG1) cell lines without affecting healthy cell. Therefore, for the first time, we aimed to find synergistic combination of Daunorubicin (DNR) and Casticin to target apoptosis in both LSC and leukemic blasts with less toxicity. Synergism of DNR-Casticin combinations on KG1a, KG1, HL-60 cells were determined with MTT viability assay by Chou-Talalay method. The apoptotic/necrotic effects of combinations were evaluated with Annexin V- PI kit by flow cytometry. Synergistic combination of 0.25 µM DNR + 0.0625 µM Casticin (combination index, CI<1) decreased cell viability to 45.3% and 63.2% in KG1a, KG1 cell lines, respectively. However, the combination-induced apoptosis (KG1a: 5 %; KG1: 5.8%) were not higher than 0.25 µM DNR-induced (KG1a: 9.4%; KG1: 8.1%) or 0.0625 µM Casticin-induced (KG1a: 3.8%; KG1: 5.1%) apoptosis (p>0.05). Our study showed that synergistic combination of DNR-Casticin causes important decrease in cell viability. Although we did not detect increase in apoptosis with the combination, we presume that other cell death pathways may be included. The highest apoptosis was obtained by the treatment of 2 µM Casticin alone in KG1a (21.7%), KG1 (26.5%), HL-60 (14.6%). Therefore, we think that Casticin polyphenol might be the possible candidate for new targeted therapy studies for AML.","PeriodicalId":17096,"journal":{"name":"Journal of Research in Pharmacy","volume":"1 1","pages":""},"PeriodicalIF":0.8,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"69839467","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}
A. Moyeenul Huq, M. Roney, S. N. Tajuddin, M. Aluwi
: Aedes aegypti is the primary vector for the transmission of the dengue virus (DENV), which causes dengue fever (DF), dengue hemorrhagic fever (DHF), and dengue shock syndrome (DSS). There is now no antiviral medication available to treat DENV, which kills thousands of people year and infects millions of individuals. Due to the current situation, effective and useful treatments for this virus urgently need to be developed. Therefore, the goal of the current work was to determine, using molecular docking and drug-likeness analysis, the anti-viral potential of Nirmatrelvir inhibitor against DENV (1-4) NS2B-NS3 protease. Nirmatrelvir shown robust and stable bonding in the binding pocket of DENV (1-4) NS2B-NS3 protease, as demonstrated by molecular docking. According to the drug-likeness study, Nirmatrelvir shown druggability and may function as possible inhibitor to halt DENV proliferation. To establish their action and other qualities, it is also necessary to research how substances behave in both in-vitro and in-vivo settings.
{"title":"Molecular docking and drug-likeness study of nirmatrelvir as promising drug candidates of dengue virus NS2B-NS3 protease","authors":"A. Moyeenul Huq, M. Roney, S. N. Tajuddin, M. Aluwi","doi":"10.29228/jrp.460","DOIUrl":"https://doi.org/10.29228/jrp.460","url":null,"abstract":": Aedes aegypti is the primary vector for the transmission of the dengue virus (DENV), which causes dengue fever (DF), dengue hemorrhagic fever (DHF), and dengue shock syndrome (DSS). There is now no antiviral medication available to treat DENV, which kills thousands of people year and infects millions of individuals. Due to the current situation, effective and useful treatments for this virus urgently need to be developed. Therefore, the goal of the current work was to determine, using molecular docking and drug-likeness analysis, the anti-viral potential of Nirmatrelvir inhibitor against DENV (1-4) NS2B-NS3 protease. Nirmatrelvir shown robust and stable bonding in the binding pocket of DENV (1-4) NS2B-NS3 protease, as demonstrated by molecular docking. According to the drug-likeness study, Nirmatrelvir shown druggability and may function as possible inhibitor to halt DENV proliferation. To establish their action and other qualities, it is also necessary to research how substances behave in both in-vitro and in-vivo settings.","PeriodicalId":17096,"journal":{"name":"Journal of Research in Pharmacy","volume":"1 1","pages":""},"PeriodicalIF":0.8,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"69839524","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}
: In this study, orally disintegrating tablets (ODT) of pramipexole dihydrochloride monohydrate (PPX) was developed with direct compression method by using ready-to-use excipients Parteck ® ODT, Pharmaburst ® 500, Ludiflash ® , F-Melt ® , and Prosolv ® Easytab SP for pediatric restless leg syndrome (RLS). The formulated ODTs were circular in shape with a total weight of around 100 mg, which was appropriate for pediatric use. In spite of very low content of the drug, content uniformity could be obtained successfully in accordance to the pharmacopoeial specification with a satisfactory mechanical strength in terms of hardness and friability. However, formulations based on Parteck ® ODT and Ludiflash® could not achieve a disintegration time <30 s according to in vitro disintegration test, which was also supported by the simulated wetting test. The optimal ODTs based on Pharmaburst ® 500, F-Melt ® and Prosolv ® Easytab SP were further evaluated for in vitro dissolution study. A very fast release of the drug was observed with these formulations that reached a peak value in 10 min., which was superior than that of the reference conventional tablet formulation of PPX. As a result, pediatric orally disintegrating tablets of PPX were successfully formulated with Pharmaburst ® 500, F-Melt ® and Prosolv ® Easytab SP by using direct compression method with suitable characteristics, which can be further studied to use in pediatric RLS.
{"title":"Formulation and in vitro evaluation of pramipexole orally disintegrating tablets for pediatric restless leg syndrome","authors":"Ömer Türkmen, L. Pozharani, Moein Amel","doi":"10.29228/jrp.465","DOIUrl":"https://doi.org/10.29228/jrp.465","url":null,"abstract":": In this study, orally disintegrating tablets (ODT) of pramipexole dihydrochloride monohydrate (PPX) was developed with direct compression method by using ready-to-use excipients Parteck ® ODT, Pharmaburst ® 500, Ludiflash ® , F-Melt ® , and Prosolv ® Easytab SP for pediatric restless leg syndrome (RLS). The formulated ODTs were circular in shape with a total weight of around 100 mg, which was appropriate for pediatric use. In spite of very low content of the drug, content uniformity could be obtained successfully in accordance to the pharmacopoeial specification with a satisfactory mechanical strength in terms of hardness and friability. However, formulations based on Parteck ® ODT and Ludiflash® could not achieve a disintegration time <30 s according to in vitro disintegration test, which was also supported by the simulated wetting test. The optimal ODTs based on Pharmaburst ® 500, F-Melt ® and Prosolv ® Easytab SP were further evaluated for in vitro dissolution study. A very fast release of the drug was observed with these formulations that reached a peak value in 10 min., which was superior than that of the reference conventional tablet formulation of PPX. As a result, pediatric orally disintegrating tablets of PPX were successfully formulated with Pharmaburst ® 500, F-Melt ® and Prosolv ® Easytab SP by using direct compression method with suitable characteristics, which can be further studied to use in pediatric RLS.","PeriodicalId":17096,"journal":{"name":"Journal of Research in Pharmacy","volume":"1 1","pages":""},"PeriodicalIF":0.8,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"69839818","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}
Venkateswarlu Kudipudi, Ravishankar Kakarparthy, Prakash Nathaniel Kumar Sarella, V. R. Kolapalli
: Vancomycin Hydrochloride is a glycopeptide antibiotic used for the treatment of Pseudomembranous colitis. This drug is susceptible to proteolytic degradation in the gastric environment and it is associated with nephrotoxicity. As the therapeutic action of vancomycin hydrochloride is intended in the intestine, colon-targeted drug delivery could help the drug achieve sufficient concentration in the target site. A polyelectrolyte complex using chitosan and hupu gum is used to prepare the beads that control the drug release and minimize the adverse effects. Eudragit S100 is used as an enteric coating material to bypass the gastric environment. The beads thus formed by polyelectrolyte complex were filled into capsules and coated with Eudragit S100. The formulation (CHP3C8) containing chitosan and hupu gum with polyethylene glycol 400 and 8% Eudragit S100 coating has shown a controlled drug release of up to 24 hours with a predetermined lag time. The ex-vivo studies have shown higher drug release in rat cecal content which can be attributed to the degradation of polyelectrolyte complex by intestinal bacteria. The in-vivo studies are carried out using white New Zealand rabbits where the capsules (CHP3C8) and solution of pure drug of vancomycin hydrochloride are administered via the oral route. The peak plasma concentration (C max ) of Vancomycin Hydrochloride from CHP3C8 and the oral solution was found to be 809.53 µ g/ml and 402 µ g/ml respectively. All the results have shown the superiority of Vancomycin Hydrochloride polyelectrolyte beads (CHP3C8) over the pure drug indicating its suitability for colon drug delivery.
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