Pub Date : 2018-06-12DOI: 10.21608/APRH.2018.2362.1047
K. Attia, O. Abdel-Aziz, N. Nasef, G. Mohamed
Objectives: The aim of this study was to develop four simple and accurate spectrophotometric methods for determination of flucloxacillin-sodium in binary mixture with ampicillin-trihydrate without separation. Methods: One of them was a univariate constant center method and the other three methods were multivariate chemometric methods named; Savitsky-Golay filters, continuous wavelet transform of ratio spectra and wavelet transform of first derivative of the ratio spectra. Results: The proposed methods adopted for selective determination of flucloxacillin-sodium and obey Beer’s law in the range (2-20 µg mL-1). Conclusion: The proposed methods were simple, rapid, economic, accurate and precise; they were successfully applied for the determination of flucloxacillin-sodium in pure form and in pharmaceutical preparations.
{"title":"Determination of Flucloxacillin-sodium in Binary Mixture with Ampicillin-trihydrate Using Univariate and Multivariate Spectrophotometric Methods: A Comparative Study","authors":"K. Attia, O. Abdel-Aziz, N. Nasef, G. Mohamed","doi":"10.21608/APRH.2018.2362.1047","DOIUrl":"https://doi.org/10.21608/APRH.2018.2362.1047","url":null,"abstract":"Objectives: The aim of this study was to develop four simple and accurate spectrophotometric methods for determination of flucloxacillin-sodium in binary mixture with ampicillin-trihydrate without separation. Methods: One of them was a univariate constant center method and the other three methods were multivariate chemometric methods named; Savitsky-Golay filters, continuous wavelet transform of ratio spectra and wavelet transform of first derivative of the ratio spectra. Results: The proposed methods adopted for selective determination of flucloxacillin-sodium and obey Beer’s law in the range (2-20 µg mL-1). Conclusion: The proposed methods were simple, rapid, economic, accurate and precise; they were successfully applied for the determination of flucloxacillin-sodium in pure form and in pharmaceutical preparations.","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-06-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77164470","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}
Pub Date : 2018-06-12DOI: 10.21608/APRH.2018.2848.1050
A. Shatla, M. Osman
Objective: The aim of this work was to enhance the dissolution rate of telmisartan with the goal of developing fast disintegrating tablets (FDTs) with subsequent rapid dissolution for sublingual administration. Methods: Binary solid dispersion systems (SDS) were prepared by solvent evaporation technique for the drug with Gelucire 44/14 (formula A), polyethylene glycol 4000 (PEG4000) (formula B), Pluronic F68 (formula C), hydroxypropyl methylcellulose E5 (HPMC E5) (formula D), and finally by using sodium bicarbonate with the drug in (0.5: 1) ratio (formula E), and (1:1) ratio (formula F). These systems were evaluated for drug dissolution in addition to the physicochemical changes of the drug utilizing FTIR spectroscopy, thermal analysis, and X-ray diffraction. Results: The prepared formulations using sodium bicarbonate significantly enhanced the dissolution rate of the drug compared with those prepared using different types of polymers. The order of enhanced dissolution of the drug in the first 5 min Q5 (%) was: formula E > F > D5, where the % drug dissolved was 88.94 ± 1.31, 84.77 ± 1.1 and72.6 ± 0.81 (mean + SD) for each formula, respectively. Formula E was selected for the formulation of the rapidly dissolving tablet of telmisartan since it showed enhanced dissolution of the drug, more palatable taste in the buccal cavity, relatively inexpensive material and ease of processing compared with a solid dispersion prepared using polymer. Conclusion: Sodium bicarbonate can be utilized in the preparation of telmisartan FDT with fast dissolution rate. Conclusion: sodium bicarbonate can be utilized in the preparation of telmisartan FDT with fast dissolution rate.
{"title":"PREPARATION AND EVALUATION OF RAPIDLY DISSOLVING TABLET OF TELMISARTAN","authors":"A. Shatla, M. Osman","doi":"10.21608/APRH.2018.2848.1050","DOIUrl":"https://doi.org/10.21608/APRH.2018.2848.1050","url":null,"abstract":"Objective: The aim of this work was to enhance the dissolution rate of telmisartan with the goal of developing fast disintegrating tablets (FDTs) with subsequent rapid dissolution for sublingual administration. Methods: Binary solid dispersion systems (SDS) were prepared by solvent evaporation technique for the drug with Gelucire 44/14 (formula A), polyethylene glycol 4000 (PEG4000) (formula B), Pluronic F68 (formula C), hydroxypropyl methylcellulose E5 (HPMC E5) (formula D), and finally by using sodium bicarbonate with the drug in (0.5: 1) ratio (formula E), and (1:1) ratio (formula F). These systems were evaluated for drug dissolution in addition to the physicochemical changes of the drug utilizing FTIR spectroscopy, thermal analysis, and X-ray diffraction. Results: The prepared formulations using sodium bicarbonate significantly enhanced the dissolution rate of the drug compared with those prepared using different types of polymers. The order of enhanced dissolution of the drug in the first 5 min Q5 (%) was: formula E > F > D5, where the % drug dissolved was 88.94 ± 1.31, 84.77 ± 1.1 and72.6 ± 0.81 (mean + SD) for each formula, respectively. Formula E was selected for the formulation of the rapidly dissolving tablet of telmisartan since it showed enhanced dissolution of the drug, more palatable taste in the buccal cavity, relatively inexpensive material and ease of processing compared with a solid dispersion prepared using polymer. Conclusion: Sodium bicarbonate can be utilized in the preparation of telmisartan FDT with fast dissolution rate. Conclusion: sodium bicarbonate can be utilized in the preparation of telmisartan FDT with fast dissolution rate.","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"86 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-06-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80712816","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}
Parkinson disease (PD) is the second most common age-related neurodegenerative disease after Alzheimer disease, characterized by loss of dopaminergic neurons in substantia nigra pars compacta, accompanied by motor and non-motor symptoms. Idiopathic PD is the most common cause of Parkinsonism (primary Parkinsonism) while, certain medication and different groups of neurological disorder may be causes of secondary Parkinsonism. The presence of intraneuronal proteinaceous cytoplasmic inclusions “Lewy Bodies” and the loss of the nigrostriatal dopaminergic neurons are the main neuropathological hallmarks of PD. However, the etiology of the disease is still undefined; several studies assume that oxidative stress, mitochondrial defects, neuroinflammation, apoptosis and excitotoxicity play vital roles in the pathogenesis and progress of the disease. Experimental models of PD can be induced by several neurotoxins such as 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine, 6-hydroxydopamine, rotenone and paraquat which produce neuropathological and neurochemical changes that are identical to those seen in PD. The primary drug for PD treatment is L-dopa; however, drug-induced dyskinesia and motor complications restricted its use as long term treatment. Dopamine agonists are alternative options for initial treatment of PD and have been reported to retard the onset of motor complications. Combination of L-dopa with other medications, such ascatechol-O-methyltransferase inhibitors and monoamine oxidase B inhibitors has the ability to alleviate L-dopa-induced motor complications. Anticholinergic drugs can be used to control the symptoms of PD but their cognitive and autonomic side effects make them unsuitable for the elderly.
帕金森病(PD)是仅次于阿尔茨海默病的第二常见的与年龄相关的神经退行性疾病，其特征是黑质致密部多巴胺能神经元的丧失，伴有运动和非运动症状。特发性帕金森病是帕金森病(原发性帕金森病)最常见的病因，而某些药物和不同类型的神经系统疾病可能是继发性帕金森病的病因。神经元内蛋白胞质包涵体“路易体”的存在和黑质纹状体多巴胺能神经元的丧失是PD的主要神经病理学标志。然而，该病的病因尚不明确;一些研究认为氧化应激、线粒体缺陷、神经炎症、细胞凋亡和兴奋毒性在疾病的发病和进展中起重要作用。PD的实验模型可由几种神经毒素诱导，如1-甲基-4-苯基-1,2,3,6-四氢吡啶，6-羟多巴胺，鱼藤酮和百草枯，它们产生与PD相同的神经病理和神经化学变化。治疗帕金森病的主要药物是左旋多巴;然而，药物引起的运动障碍和运动并发症限制了其作为长期治疗的使用。多巴胺激动剂是帕金森病初始治疗的替代选择，据报道可以延缓运动并发症的发生。左旋多巴与其他药物联合使用，如儿茶酚- o -甲基转移酶抑制剂和单胺氧化酶B抑制剂，可以减轻左旋多巴引起的运动并发症。抗胆碱能药物可用于控制帕金森病的症状，但其对认知和自主神经的副作用使其不适合老年人。
{"title":"Parkinson's disease: A Review about Pathogenesis, Pharmaceutical Treatment and Experimental Models","authors":"El Sayed, A. Eissa, S. Nofal, Engy Elmorsy","doi":"10.21608/APRH.2018.8013","DOIUrl":"https://doi.org/10.21608/APRH.2018.8013","url":null,"abstract":"Parkinson disease (PD) is the second most common age-related neurodegenerative disease after Alzheimer disease, characterized by loss of dopaminergic neurons in substantia nigra pars compacta, accompanied by motor and non-motor symptoms. Idiopathic PD is the most common cause of Parkinsonism (primary Parkinsonism) while, certain medication and different groups of neurological disorder may be causes of secondary Parkinsonism. The presence of intraneuronal proteinaceous cytoplasmic inclusions “Lewy Bodies” and the loss of the nigrostriatal dopaminergic neurons are the main neuropathological hallmarks of PD. However, the etiology of the disease is still undefined; several studies assume that oxidative stress, mitochondrial defects, neuroinflammation, apoptosis and excitotoxicity play vital roles in the pathogenesis and progress of the disease. Experimental models of PD can be induced by several neurotoxins such as 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine, 6-hydroxydopamine, rotenone and paraquat which produce neuropathological and neurochemical changes that are identical to those seen in PD. The primary drug for PD treatment is L-dopa; however, drug-induced dyskinesia and motor complications restricted its use as long term treatment. Dopamine agonists are alternative options for initial treatment of PD and have been reported to retard the onset of motor complications. Combination of L-dopa with other medications, such ascatechol-O-methyltransferase inhibitors and monoamine oxidase B inhibitors has the ability to alleviate L-dopa-induced motor complications. Anticholinergic drugs can be used to control the symptoms of PD but their cognitive and autonomic side effects make them unsuitable for the elderly.","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"59 1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-06-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90115163","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}
Pub Date : 2018-06-12DOI: 10.21608/APRH.2018.3450.1055
S. El-Gizawy, M. Osman, S. Ibrahim
Objective: Investigate the effect of ethanol, polyethylene glycol 400, propylene glycol, glycerol and sorbitol on the absorptive clearance of ketotifen fumarate in the rabbit. Methods: In-situ intestinal perfusion technique, through and through was used for estimation of membrane transport parameters of ketotifen fumarate from duodenum, jejunum, ileum and ascending colon in the rabbit. These parameters include absorptive clearance per unit length PeA/L (ml/min.cm), percentage fraction absorbed per unit length (% Fa/cm) and anatomical length that required for complete absorption in specific segment (L95%). Results: The absorption was in the order ascending colon> duodenum > jejunum> ileum; where the absorptive clearance normalized to intestinal segment length PeA/L (ml/min.cm) was 0.0071 ± 0.0003, 0.0058 ± 0.0001, 0.0051 ± 0.0001, and 0.0047 ± 0.0001 in each segment respectively. The effect of cosolvents in jejunum was in the order; ethanol 15% >glycerol 30% > propylene glycol (PG40%) > polyethylene glycol400 (PEG-400 40%) >sorbitol 40%, Where the absorptive clearance normalized to intestinal segment length PeA/L (ml/min.cm), mean ± SE was: 0.0142 ±0.0011, 0.0086 ± 0.0002, 0.0075 ± 0.0003, 0.0022 ± 0.0001, and 0.0014 ± 0.0001 for each cosolvents respectively. The same order was obtained in the ascending colon. Conclusion: The enhancing action of the ethanol, propylene glycol and glycerol may be due fluidization of the cell membrane with a subsequent increase in transcellular absorption, while the inhibitory effect of polyethylene glycol and sorbitol could attributed to water secretion, H-bonding formation and reduced thermodynamic activity of drug molecules.
{"title":"INFLUENCE OF COSOLVENTS ON THE ABSORPTIVE CLEARANCE OF KETOTIFEN FUMARATE FROM RABBIT INTESTINE, IN-SITU","authors":"S. El-Gizawy, M. Osman, S. Ibrahim","doi":"10.21608/APRH.2018.3450.1055","DOIUrl":"https://doi.org/10.21608/APRH.2018.3450.1055","url":null,"abstract":"Objective: Investigate the effect of ethanol, polyethylene glycol 400, propylene glycol, glycerol and sorbitol on the absorptive clearance of ketotifen fumarate in the rabbit. Methods: In-situ intestinal perfusion technique, through and through was used for estimation of membrane transport parameters of ketotifen fumarate from duodenum, jejunum, ileum and ascending colon in the rabbit. These parameters include absorptive clearance per unit length PeA/L (ml/min.cm), percentage fraction absorbed per unit length (% Fa/cm) and anatomical length that required for complete absorption in specific segment (L95%). Results: The absorption was in the order ascending colon> duodenum > jejunum> ileum; where the absorptive clearance normalized to intestinal segment length PeA/L (ml/min.cm) was 0.0071 ± 0.0003, 0.0058 ± 0.0001, 0.0051 ± 0.0001, and 0.0047 ± 0.0001 in each segment respectively. The effect of cosolvents in jejunum was in the order; ethanol 15% >glycerol 30% > propylene glycol (PG40%) > polyethylene glycol400 (PEG-400 40%) >sorbitol 40%, Where the absorptive clearance normalized to intestinal segment length PeA/L (ml/min.cm), mean ± SE was: 0.0142 ±0.0011, 0.0086 ± 0.0002, 0.0075 ± 0.0003, 0.0022 ± 0.0001, and 0.0014 ± 0.0001 for each cosolvents respectively. The same order was obtained in the ascending colon. Conclusion: The enhancing action of the ethanol, propylene glycol and glycerol may be due fluidization of the cell membrane with a subsequent increase in transcellular absorption, while the inhibitory effect of polyethylene glycol and sorbitol could attributed to water secretion, H-bonding formation and reduced thermodynamic activity of drug molecules.","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"72 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-06-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80040463","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}
Pub Date : 2018-06-12DOI: 10.21608/APRH.2018.3134.1052
B. Yılmaz, Nurullah Yilmaz
Objectives: In this work, a new, rapid, simple, precise and specific method has been developed for the simultaneous determination of amlodipine (AML) and rosuvastatin (ROS) in pharmaceutical preparations by square wave voltammetry (SWV). Methods: Electrochemical behavior and simultaneous voltammetric determination of AML and ROS were investigated using platinum disk electrode. Validation parameters such as specificity, linearity, accuracy, precision, ruggedness, stability, limit of quantification and limit of detection were studied according to the ICH Guidelines. Results: The linearity of this developed method was established in the concentration range of 5-40 μg/mL for AML and ROS, respectively. The precision was less than 1.88 and 1.93%, determined from quality control samples for AML and ROS, and accuracy was within 1.69 and 1.97% in terms of relative error, respectively. The percentage recovery obtained for AML and ROS in pharmaceutical preparations were 99.5 and 100.2%, respectively. Limit of detection and quantification for AML were 0.70 and 2.10 µg/mL, for ROS 0.80 and 2.40 µg/mL, respectively. Conclusion: The developed SWV method can be used for routine analysis of AML and ROS in pharmaceutical preparations.
{"title":"Simultaneous Determination of Amlodipine and Rosuvastatin in Pharmaceutical Preparations by Square Wave Voltammetry","authors":"B. Yılmaz, Nurullah Yilmaz","doi":"10.21608/APRH.2018.3134.1052","DOIUrl":"https://doi.org/10.21608/APRH.2018.3134.1052","url":null,"abstract":"Objectives: In this work, a new, rapid, simple, precise and specific method has been developed for the simultaneous determination of amlodipine (AML) and rosuvastatin (ROS) in pharmaceutical preparations by square wave voltammetry (SWV). Methods: Electrochemical behavior and simultaneous voltammetric determination of AML and ROS were investigated using platinum disk electrode. Validation parameters such as specificity, linearity, accuracy, precision, ruggedness, stability, limit of quantification and limit of detection were studied according to the ICH Guidelines. Results: The linearity of this developed method was established in the concentration range of 5-40 μg/mL for AML and ROS, respectively. The precision was less than 1.88 and 1.93%, determined from quality control samples for AML and ROS, and accuracy was within 1.69 and 1.97% in terms of relative error, respectively. The percentage recovery obtained for AML and ROS in pharmaceutical preparations were 99.5 and 100.2%, respectively. Limit of detection and quantification for AML were 0.70 and 2.10 µg/mL, for ROS 0.80 and 2.40 µg/mL, respectively. Conclusion: The developed SWV method can be used for routine analysis of AML and ROS in pharmaceutical preparations.","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"16 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-06-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81793111","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}
Pub Date : 2018-06-12DOI: 10.21608/APRH.2018.3242.1053
A. Abdel-Fattah, Nasr M. El-Abasawi, Khalid A M Attia, A. A. Abo-serie, S. Morshedy
Objectives: A simple, accurate, selective and sensitive densitometric method was developed for the determination of ezetimibe in the presence of its alkaline degradation product. Methods: TLC-densitometric separation of ezetimibe from its degradation products was carried out on silica gel plates using ethyl acetate: n-hexane (2:1 v/v) as a developing system. This method depends on quantitative densitometric evaluation of ezetimibe at 230 nm over a concentration range of 1–8 µg/spot. Ezetimibe and its alkaline degradation product were resolved with Rf values of 0.49 and 0.68 respectively. Results: The proposed method has been successfully applied to the analysis of ezetimibe in pharmaceutical dosage form without interference from additives and the results were statistically compared with the reported method. Conclusion: TLC- densitometric technique has provided a simple, straightforward method for separating ezetimibe and its alkaline degradation product simultaneously.
{"title":"Densitometric Determination of Ezetimibe in the Presence of its Alkaline Degradation Product","authors":"A. Abdel-Fattah, Nasr M. El-Abasawi, Khalid A M Attia, A. A. Abo-serie, S. Morshedy","doi":"10.21608/APRH.2018.3242.1053","DOIUrl":"https://doi.org/10.21608/APRH.2018.3242.1053","url":null,"abstract":"Objectives: A simple, accurate, selective and sensitive densitometric method was developed for the determination of ezetimibe in the presence of its alkaline degradation product. Methods: TLC-densitometric separation of ezetimibe from its degradation products was carried out on silica gel plates using ethyl acetate: n-hexane (2:1 v/v) as a developing system. This method depends on quantitative densitometric evaluation of ezetimibe at 230 nm over a concentration range of 1–8 µg/spot. Ezetimibe and its alkaline degradation product were resolved with Rf values of 0.49 and 0.68 respectively. Results: The proposed method has been successfully applied to the analysis of ezetimibe in pharmaceutical dosage form without interference from additives and the results were statistically compared with the reported method. Conclusion: TLC- densitometric technique has provided a simple, straightforward method for separating ezetimibe and its alkaline degradation product simultaneously.","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"105 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-06-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89938771","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}
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