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2-Phenitidine derivatives as suitable inhibitors of butyrylcholinesterase BJPS
Abbasi,Muhammad Athar; Aziz-ur-Rehman,; Qureshi,Muhammad Zahid; Khan,Farhan Mehmood; Khan,Khalid Mohmmed; Ashraf,Muhammad; Afzal,Iftikhar.
This manuscript reports the synthesis of a series of N-substituted derivatives of 2-phenitidine. First, the reaction of 2-phenitidine (1) with benzene sulfonyl chloride (2) yielded N-(2-ethoxyphenyl) benzenesulfonamide (3), which further on treatment with sodium hydride and alkyl halides (4a-g) furnished into new sulfonamides (5a-g). Second, the phenitidine reacted with benzoyl chloride (6) and acetyl chloride (8) to yield the reported N-benzoyl phenitidine (7) and N-acetyl phenitidine (9), respectively. These derivatives were characterized by infrared spectroscopy, ¹H-NMR, and EI-MS, and then screened against acetylcholinesterase, butylcholinesterase, and lipoxygenase enzyme, and were found to be potent inhibitors of butyrylcholinesterase alone.
Tipo: Info:eu-repo/semantics/article Palavras-chave: 2-Phenitidine/inhibitor activity; Sulfonamides; Acetamide; Benzamide; Butyrylcholinesterase.
Ano: 2013 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502013000100014
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Synthesis of new 2-{2,3-dihydro-1,4-benzodioxin-6-yl[(4-methylphenyl) sulfonyl]amino}-N-(un/substituted-phenyl)acetamides as α-glucosidase and acetylcholinesterase inhibitors and their in silico study BJPS
Abbasi,Muhammad Athar; Riaz,Sajid; Rehman,Aziz-ur-; Siddiqui,Sabahat Zahra; Shah,Syed Adnan Ali; Ashraf,Muhammad; Lodhi,Muhammad Arif; Khan,Farman Ali.
The aim of the present research work was to investigate the enzyme inhibitory potential of some new sulfonamides having benzodioxane and acetamide moieties. The synthesis was started by the reaction of N-2,3-dihydrobenzo[1,4]-dioxin-6-amine (1) with 4-methylbenzenesulfonyl chloride (2) in the presence of 10% aqueous Na2CO3 to yield N-(2,3-dihydrobenzo[1,4]-dioxin-6-yl)-4-methylbenzenesulfonamide (3), which was then reacted with 2-bromo-N-(un/substituted-phenyl)acetamides (6a-l) in DMF and lithium hydride as a base to afford various 2-{2,3-dihydro-1,4-benzodioxin-6-yl[(4-methylphenyl)sulfonyl]amino}-N-(un/substituted-phenyl)acetamides (7a-l). All the synthesized compounds were characterized by their IR and 1H-NMR spectral data along with CHN analysis data....
Tipo: Info:eu-repo/semantics/article Palavras-chave: Benzodioxane; Acetamide; Spectral analysis; A-Glucosidase; Acetylcholinesterase; Molecular docking.
Ano: 2019 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502019000100518
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Acetylcholinesterase inhibition, antioxidant and identification of some chemical constituents of Phyllanthus atropurpureus cultivated in Egypt BJPS
Abdallah,Walid Elsayed; Elsayed,Wael Mohamady; Hassan,Rasmia Ali; Nazif,Naglaa Mohammed; Ali,Mohammed Ibrahim; Abdelshafeek,Khaled Abdelhady.
Investigation of the lipid constituents of the aerial parts of Phyllanthus atropurpureus resulted in isolation and identification of the fatty acid mixture which consists of eight acids with linolenic acid as major and the unsaponifiable fraction that contain a series of hydrocabons, sterols, in addition to one triterpene (α-amyrin). The acetone insoluble fraction was found to contain two fatty alcohols and three n-hydrocabons in which the n-eicosane is the most abundant (44.16%). The flavonoidal constituents were isolated from ethyl acetate and butanol fractions which were identified as: luteolin-7-O-glucoside, kaempferol 3-O-(p-coumaroylglucoside), kaempferitrin, luteolin and kaempferol. Evaluation of different extracts as acetylcholinesterase inhibitors...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Phyllanthus atropurpureus; Euphorbiaceae; Flavonoids; Acetylcholineesterase inhibitors; Antioxidant.
Ano: 2019 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502019000100575
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Stability of antioxidant vitamins in commercial vitamin supplements BJPS
Abe-Matsumoto,Lucile Tiemi; Sampaio,Geni Rodrigues; Bastos,Deborah Helena Markowicz.
The stability of vitamins A, E, and C was determined in 12 brands of vitamin supplements over a 12-month storage period. The variations in concentrations of these vitamins across three different batches of five brands were measured. Vitamins A and E was determined by HPLC method, and vitamin C was measured by using potentiometric titration. All samples for stability studies were maintained at room temperature and protected from light. Measurements were carried out in the first semester of the expiration date and then every six months up to 12 months of storage. After this period, only one sample showed no significant decrease in vitamin A and E concentrations in relation to the concentrations measured at the beginning of the study. The concentration of...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Supplements/stability Vitamins A; E C/concentration.
Ano: 2018 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502018000400623
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Synaptic vesicle cycling is not impaired in a glutamatergic and a cholinergic synapse that exhibit deficits in acidification and filling BJPS
Abreu,Bento João; Leite,Luciana Ferreira; Oliveira,Débora Lopes; Amaral,Ernani.
The purpose of the present work was to investigate synaptic vesicle trafficking when vesicles exhibit alterations in filling and acidification in two different synapses: a cholinergic frog neuromuscular junction and a glutamatergic ribbon-type nerve terminal in the retina. These synapses display remarkable structural and functional differences, and the mechanisms regulating synaptic vesicle cycling might also differ between them. The lipophilic styryl dye FM1-43 was used to monitor vesicle trafficking. Both preparations were exposed to pharmacological agents that collapse ΔpH (NH4Cl and methylamine) or the whole ΔµH+ (bafilomycin), a necessary situation to provide the driving force for neurotransmitter accumulation into synaptic vesicles. The results...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Synaptic vesicle; Acidification; Lipophilic styryl dye/use; Neuromuscular junction; Bipolar cell; Retina.
Ano: 2012 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502012000100017
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Prevalence and costs of hospitalizations for poisoning and accidental intoxication in Brazilian elderly BJPS
Abreu,Marcelle Silva de; Ferreira,Silvandro Diego de Albuquerque; Ferreira,Larissa Pelágia de Lima; Toneo Júnior,José Ferreira; Maciel,Wamberto Vieira; Maciel,Shirley Suely Soares Veras.
A cross-sectional study of secondary data/information obtained from the Hospital Information System (HIS) spanning the years 2008 - 2009 was performed. The distribution of the main hospital admissions by gender, age, color/race, region and federal unit of residence, average expenditure and average length of hospital stay, year of hospitalization and mortality rates (MR) were studied. The data collected were tabulated by TabNet and keyed into Microsoft Excel 2007. It was verified that elderly males (54.3%), from 60 to 69 years old (50.6%), nonwhites (36.3%) and residents of Southeast and North regions of the country had the highest rates of hospitalization. Seniors were hospitalized for an average of 4.8 days, and the major...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Hospital Information System; Elderly patients/hospitalization; Medicines/inappropriated use; Hospitalization/rates; Poisoning; Alcohol/use.
Ano: 2013 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502013000400007
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Chemical composition and bioactivity of methanolic extract obtained from Lepista sordida BJPS
Acharya,Krishnendu; Ghosh,Sandipta; Biswas,Rhituparna.
The present study aimed at the evaluation of chemical composition and bioactive potential of methanolic extract obtained from Lepista sordida in terms of antioxidative and antimicrobial efficacy. The macrofungus is recognized for its high nutritional value and medicinal properties. However, to the best of our knowledge bioactivity of its methanolic extract is yet to be explored. In this investigation, quantitative analysis of mycochemicals revealed the extract contained significant amount of phenolic compounds such as phenols and flavonoids. Ascorbic acid was found in higher amount than β carotene and lycopene which were present in vestigial amounts. A phenolic profile was also determined using high performance liquid chromatography that further confirmed...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Antimicrobial; Free radical scavenger; High performance liquid chromatography; Mycotaxon; Mycochemicals.
Ano: 2019 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502019000100600
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Sucrose hydrolysis by invertase using a membrane reactor: effect of membrane cut-off on enzyme performance BJPS
Addezio,Francesco Di; Yoriyaz,Ester Junko; Cantarella,Maria; Vitolo,Michele.
Sucrose hydrolysis by invertase [EC.3.2.1.26] produces inverted sugar syrup, an ingredient mainly used in the food industry. To properly catalyze hydrolysis, the enzyme should be reused after this reaction. It is advisable to maintain constant activity over a considerable period. Thus, sucrose hydrolysis was performed in a membrane bioreactor - a continuously stirred tank reactor coupled with an ultrafiltration membrane (UFM) which provides good diffusion and high activity per unit volume. Molecular weight cut-off for soluble invertase UFMs was up to 100kDa. This study focused on the role of UFM invertase cut-off as it is the main element in the process. We demonstrated that both the cut-off and chemical nature of the UFM affected specific invertase...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Invertase; Membrane Reactor; Sucrose/hydrolysis.
Ano: 2014 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502014000200257
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Preparation and evaluation of azithromycin binary solid dispersions using various polyethylene glycols for the improvement of the drug solubility and dissolution rate BJPS
Adeli,Ehsan.
ABSTRACT Azithromycin is a water-insoluble drug, with a very low bioavailability. In order to increase the solubility and dissolution rate, and consequently increase the bioavailability of poorly-soluble drugs (such as azithromycin), various techniques can be applied. One of such techniques is "solid dispersion". This technique is frequently used to improve the dissolution rate of poorly water-soluble compounds. Owing to its low solubility and dissolution rate, azithromycin does not have a suitable bioavailability. Therefore, the main purpose of this investigation was to increase the solubility and dissolution rate of azithromycin by preparing its solid dispersion, using different Polyethylene glycols (PEG). Preparations of solid dispersions and physical...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Azithromycin/solubility; Azithromycin/dissolution; Solid dispersion; Polyethylene glycols..
Ano: 2016 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502016000100002
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In vitro antimicrobial efficacy of a fixed-dose combination of RHZE against M. tuberculosis BJPS
Agertt,Vanessa Albertina; Bonez,Pauline Cordenonsi; Mizdal,Caren Rigon; Rossi,Grazielle Guidolin; Flores,Vanessa da Costa; Campos,Marli Matiko Anraku de.
ABSTRACT The use of drugs in fixed-dose combination (FDC) is now recommended by the World Health Organization (WHO) due to the emergence of multidrug-resistant strains of Mycobacterium tuberculosis. FDC uses different drugs against tuberculosis (TB) in a single tablet for phase-intensive therapeutic intervention. This therapy aims to optimize treatment, to prevent inappropriate use of drugs, and to prevent the emergence of new resistant strains. This study aims to evaluate the susceptibility of clinical isolates of M. tuberculosis against rifampicin, isoniazid, ethambutol, and pyrazinamide. The antimicrobials were tested separately and in associations according to FDC. This was used for broth microdilution method, which was compared to the proportions...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Mycobacterium tuberculosis/treatment/drug combination; Mycobacterium tuberculosis/drug resistance; Mycobacterium tuberculosis/susceptibility/fixed dose combination..
Ano: 2016 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502016000300575
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Development of a new analytical method for determination of acetylsalicylic and salicylic acids in tablets by reversed phase liquid chromatography BJPS
Aguiar,José Luiz Neves de; Leandro,Katia Christina; Abrantes,Shirley de Mello Pereira; Albert,André Luis Mazzei.
Acetylsalicylic acid (AAS) is a drug utilized as analgesic, anti-inflammatory, and antipyretic medication, available worldwide and commonly used in Brazil. Salicylic acid (AS) is a precursor in AAS synthesis and is also produced during its degradation. The official United States Pharmacopoeia (USP) suggests the determination of these drugs by high performance liquid chromatography (HPLC), with ultraviolet detection, but this method has neither a high sensitivity (S AAS=0.12 mAbs/(μg/mL) and S AS=0.48 mAbs/(μg/mL)) nor resolution (Rs=1.61). The purpose of this study was to develop a new more adequate, accurate method by liquid phase chromatography than the current official methodology, and to use this new method in the determination of the tenors of...
Tipo: Info:eu-repo/semantics/article Palavras-chave: High performance liquid chromatography; Acetylsalicylic acid/determination in tablets; Salicylic acid/determination in tablets; Tablets/quantitative analysis.
Ano: 2009 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502009000400016
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Effects of Arctium lappa aqueous extract on lipid profile and hepatic enzyme levels of sucrose-induced metabolic syndrome in female rats BJPS
Ahangarpour,Akram; Ali-Akbari,Fatemeh Ramazani; Mohaghegh,Seyyedeh Marjan; Asadinia,Ebtesam.
ABSTRACT Arctium lappa is known to have antioxidant and antidiabetic effects in traditional medicine. Objectives: The aim of this paper was to study the effects of A. lappa root extract (AE) on lipid profile and hepatic enzyme levels in sucrose-induced metabolic syndrome (MS) in female rats. The study used 40 adult female Wistar rats weighing 150 g-250 g randomly divided into five groups: control, metabolic syndrome (MS), metabolic syndrome+AE at 50,100, 200 mg/kg. MS was induced by administering 50% sucrose in drinking water for 6 weeks. AE was intra-peritoneally administered daily at doses of 50,100, and 200 mg/kg for two sequential weeks at the end of the fourth week in metabolic syndrome rats. Twenty-four hours after the last administration of AE,...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Lappa arctium/effects; Metabolic syndrome; Sucrose/lipid profile/hepatic enzymes..
Ano: 2016 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502016000300425
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Microbial biotransformation of beclomethasone dipropionate by Aspergillus niger BJPS
Ahmad,Saeed; Khaliq,Farhan Hameed; Madni,Asadullah; Shahid,Muhammad Nabeel; Pervaiz,Irfan.
In the present research, the steroidal anti-asthmatic drug beclomethasone dipropionate was subjected to microbial biotransformation by Aspergillus niger. Beclomethasone dipropionate was transformed into various metabolites first time from microbial transformation. New drug metabolites produced can act as new potential drug molecules and can replace the old drugs in terms of safety, efficacy, and least resistance. They were purified by preparative thin layer chromatography technique, and their structures were elucidated using modern spectroscopic techniques, such as 13C NMR, 1H NMR, HMQC, HMQC, COSY, and NOESY, and mass spectrometry, such as EI-MS. Four metabolites were purified: (i) beclomethasone 17-monopropionate, (ii) beclomethasone 21-monopropionate,...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Anti-asthmatics; Aspergillus niger/use in biotransformation; Beclomethasone dipropionate/microbial biotransformation; Steroids/microbial transformation; Biotransformation.
Ano: 2014 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502014000400903
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Retrospective cost-utility and budget impact assessments of Hypericum perforatum in contrast with Fluoxetine treatment for depression in Karachi, Pakistan BJPS
Ahmad,Syed Muzzammil; Masroor,Darakhshan; Azhar,Iqbal; Ahmed,Nadia.
In this study we have compared two different types of therapies i.e. herbal and allopathic system of therapies for Depression and studied them from the social perspectives. The Hypericum perforatum is compared with Fluoxetine [HCL] in terms of cost-utility and financial savings thereby evaluating its influence on annual expenditure of depressive patients that were randomly selected from 178 union councils of the city of Karachi, Pakistan. For both system of therapies a total of 356 patients were selected by stratified random sampling. Taking frequency of depression as ‘1’ annually with discount rate at 3% for calculating the burden-of-illness in terms of disability-adjusted-life-years. The cost-utility and the budget-impact assessments were carried out to...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Hypericum perforatum; Fluoxetine; Burden of illness; Disability-Adjusted-Life-Years; Incremental-Cost-Effectiveness-Ratio.
Ano: 2019 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502019000100581
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Atorvastatin calcium loaded chitosan nanoparticles: in vitro evaluation and in vivo pharmacokinetic studies in rabbits BJPS
Ahmed,Abdul Baquee; Konwar,Ranjit; Sengupta,Rupa.
Tipo: Info:eu-repo/semantics/article Palavras-chave: Atorvastatin calcium/oral bioavailability/experimental study; Atorvastatin calcium/in vitro release; Atorvastatin calcium/pharmacokinetics; Nanoparticles/drugs bioavailability.
Ano: 2015 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502015000200467
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Acute hypotensive and diuretic activities of Berberis vulgaris root bark aqueous extract in normal rats BJPS
Ahmed,Muhammad; Azmat,Aisha; Khan,Salahuddin.
ABSTRACT The aim of this study is to investigate the effectiveness of intravenous administration of Berberis vulgaris root bark aqueous extract (BRBD) on the cardiovascular and renal functions of healthy normotensive rats. The different doses of BRBD 1, 10 and 20 mg/kg were administered intravenously (i.v) in normal rats. Blood pressure, diuretic activity and serum renal profile were analyzed. Intravenous injection of BRBD at the different doses of 1, 10 and 20 mg/kg showed a dose-dependent reduction in mean arterial blood pressure (P<0.001). At different doses of 1, 10 and 20 mg/kg, the hypotensive effect remained for more than one hour. Single dose administration of BRBD at doses of 10 and 20 mg/kg caused a significant increase in urine output...
Tipo: Info:eu-repo/semantics/other Palavras-chave: Berberis vulgaris root bark/ aqueous extract (BRBD); Mean arterial blood pressure (MABP); Diuresis; Serum renal profile test.
Ano: 2017 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502017000400301
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A conglomeration of preclinical models related to myocardial infarction BJPS
Ahsan,Farogh; Mahmood,Tarique; Usmani,Shazia; Bagga,Paramdeep; Shamim,Arshiya; Tiwari,Reshu; Verma,Neeraj; Siddiqui,Mohammed Haris.
Cardiovascular diseases are the main source of death and morbidity in developed and developing nations. Animal models are required to propel our understanding of the pathogenesis, increase our knowledge, disease progress, and mechanism behind cardiovascular disorder, providing new approaches focused to improve the diagnostic and the treatment of these pathological conditions and additionally to test various therapeutic ways to deal with tissue regeneration and re-establish heart working following damage. A perfect model framework ought to be reasonable, effectively controlled, reproducible, and physiologically illustrative of human disease, show cardinal signs and pathology that resembles after the human ailment and ethically stable. The decision of...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Myocardial infarction; Animal model; Isoproterenol; Chemical induced; Ischeamia.
Ano: 2020 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502020000100557
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Formulation and evaluation of topical herbal gel for the treatment of arthritis in animal model BJPS
Aiyalu,Rajasekaran; Govindarjan,Arulkumaran; Ramasamy,Arivukkarasu.
ABSTRACT The objective of the study is to formulate and evaluate a topical herbal gel containing Cardiospermum halicacabum and Vitex negundo leaf extracts for their anti-arthritic activity in rats. Twelve herbal gel formulations were prepared using 1.5% of gelling agents carbopol 934 (F1-F6) and carbopol 940 (F6-F12) and they were evaluated for physical appearance, net content, viscosity, extrudability, pH, spreadability, in vitro diffusion profile and primary skin irritation tests. The stability study for the topical herbal gel formulation was done as per ICH guidelines and anti-arthritic activity was evaluated by Freund's Complete Adjuvant (FCA) induced arthritis method. Assessment of body weight, paw volume, hematological and biochemical parameters,...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Arthritis/treatment/herbal gel; Cardiospermum halicacabum/topical herbal gel; Vitex negundo/topical herbal gel; Medicinal plants/arthritis..
Ano: 2016 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502016000300493
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Barriers to the provision of asthma services and perceived practice towards asthma management among urban community pharmacists in Selangor, Malaysia BJPS
Akram,Waqas; Ijaz,Naeem; Ahmad,Hassan; Jamshaid,Muhammad; Ismail,Nahlah Elkudssiah.
This study aims to assess the perceived practice and barriers towards the provision of asthma management services among urban community pharmacists in Selangor, Malaysia. The study also highlights both pharmacist and patient-related barriers in asthma counseling. One hundred fifty urban community pharmacists in Selangor, Malaysia, were randomly selected and recruited for the present cross sectional baseline study. Previous studies have explored pharmacists’ perception on their roles in asthma management in different parts of the world. The data was collected through self-explanatory questionnaires (containing 47 items). The extracted data from the completed questionnaires were analyzed descriptively and inferentially using Statistical Package for Social...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Asthma; Perceived practive; Treatment barriers; Community pharmacists; Disease management.
Ano: 2018 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502018000400614
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Effect of pH on weakly acidic and basic model drugs and determination of their ex vivo transdermal permeation routes BJPS
Akula,Pranitha; P.K.,Lakshmi.
ABSTRACT The aim of the present study was to investigate the effect of donor pH on the transdermal permeability of the model drugs across rat skin and also to determine the major route of transport of the drugs. Weakly acidic drugs (partition coefficient) ibuprofen (3.6), aceclofenac (3.9), glipizide (1.9) and weakly basic drugs olanzapine (3.6), telmisartan (6.0), and sildenafil citrate (1.9) were selected for the study. The ex vivo permeation studies of these drugs at different donor pH (pH - 1.2, 4, 5, 6.8, 7.4, and 8) using Franz diffusion cell (area, 7.54 cm2) has shown a pH-dependent permeability. Among these drugs the weakly acidic drugs has shown higher permeation rates compared to the weakly basic drugs. The...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Donor pH/effects; Weakly acidic drugs; Weakly basic drugs; PH solubility; Distribution coefficient; Ionization.
Ano: 2018 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502018000200628
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