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1.
Nephrology (Carlton) ; 28(12): 672-681, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37697492

RESUMO

AIM: This cross-sectional survey aimed to determine the prevalence of Interventional Nephrology (IN) practice amongst nephrologists in the Asia-Pacific Region (APR), specifically related to dialysis access (DA). METHODS: The Association of VA and intervenTionAl Renal physicians (AVATAR) Foundation from India conducted a multinational online survey amongst nephrologists from the Asia-Pacific to determine the practice of IN in the planning, creation, and management of dialysis access. The treatment modalities, manpower and equipment availability, monthly cost of treatment, specifics of dialysis access interventions, and challenges in the training and practice of IN by nephrologists were included in the survey. RESULTS: Twenty-one countries from the APR participated in the survey. Nephrologists from 18 (85.7%) countries reported performing at least one of the basic dialysis access-related IN procedures, primarily the placement of non-tunnelled central catheters (n-TCC; 71.5%). Only 10 countries (47.6%) reported having an average of <4% of nephrologists performing any of the advanced IN access procedures, the most common being the placement of a peritoneal dialysis (PD) catheter (20%). Lack of formal training (57.14%), time (42.8%), incentive (38%), institutional support (38%), medico-legal protection (28.6%), and prohibitive cost (23.8%) were the main challenges to practice IN. The primary obstacles to implementing the IN training were a lack of funding and skilled personnel. CONCLUSION: The practice of dialysis access-related IN in APR is inadequate, mostly due to a lack of training, backup support, and economic constraints, whereas training in access-related IN is constrained by a lack of a skilled workforce and finances.


Assuntos
Nefrologia , Humanos , Nefrologia/educação , Diálise Renal , Estudos Transversais , Cateterismo/métodos , Ásia/epidemiologia
2.
Molecules ; 28(6)2023 Mar 13.
Artigo em Inglês | MEDLINE | ID: mdl-36985575

RESUMO

The convenient and highly compliant route for the delivery of active pharmaceutical ingredients is the tablet. A versatile platform of tablets is available for the delivery of therapeutic agents to the gastrointestinal tract. This study aimed to prepare gastro retentive drug delivery floating tablets of silymarin to improve its oral bioavailability and solubility. Hydroxypropyl methylcellulose (HPMCK4M and HPMCK15), Carbopol 934p and sodium bicarbonate were used as a matrix, floating enhancer and gas generating agent, respectively. The prepared tablets were evaluated for physicochemical parameters such as hardness, weight variation, friability, floating properties (floating lag time, total floating time), drug content, stability study, in vitro drug release, in vivo floating behavior and in vivo pharmacokinetics. The drug-polymer interaction was studied by Differential Scanning Calorimetry (DSC) thermal analysis and Fourier transform infrared (FTIR). The floating lag time of the formulation was within the prescribed limit (<2 min). The formulation showed good matrix integrity and retarded the release of drug for >12 h. The dissolution can be described by zero-order kinetics (r2 = 0.979), with anomalous diffusion as the release mechanism (n = 0.65). An in vivo pharmacokinetic study showed that Cmax and AUC were increased by up to two times in comparison with the conventional dosage form. An in vivo imaging study showed that the tablet was present in the stomach for 12 h. It can be concluded from this study that the combined matrix system containing hydrophobic and hydrophilic polymers min imized the burst release of the drug from the tablet and achieved a drug release by zero-order kinetics, which is practically difficult with only a hydrophilic matrix. An in vivo pharmacokinetic study elaborated that the bioavailability and solubility of silymarin were improved with an increased mean residence time.


Assuntos
Silimarina , Preparações de Ação Retardada/química , Disponibilidade Biológica , Sistemas de Liberação de Medicamentos , Comprimidos/química , Solubilidade
3.
Pak J Pharm Sci ; 36(1): 81-87, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36967500

RESUMO

Population of pediatric intensive care units are at high risk of receiving off label and unlicensed drug use. Little is known about the characteristics and prevalence of unlicensed and off label prescriptions in pediatric intensive care units (PICUs) at tertiary care settings of Pakistan. Case notes of 420 children were reviewed for unlicensed and off label prescriptions during the one year. Medication profiles were assessed using Micromedex. Logistic regression was applied to calculate the odds-ratios for predictors of unlicensed and off label prescriptions. of the total prescriptions, 29.8% prescriptions were unlicensed from FDA and 42.27% prescriptions were off labelled. Dose (32.79%) was the most common reason for off label prescriptions followed by the indication (26.13%) and indication-dose (13.98%). Multivariate regression analysis revealed no significant association between the unlicensed prescriptions with their predictors. In reference to corresponding category, prescribed medications less than 5 (OR 0.280, 95%CL 0.137-0.570) were significantly less likely to receive off label prescriptions as compared to patients received 6 or more medications. Substantial numbers of children are exposed to unlicensed and off label prescriptions. Standards of drug quality, safety and efficacy should apply equally in adults and in pediatrics under ethical perspective. Suitable clinical interventions must be established by drug manufactures and government agencies for improved pediatric pharmacotherapy.


Assuntos
Unidades de Terapia Intensiva Pediátrica , Uso Off-Label , Humanos , Criança , Lactente , Centros de Atenção Terciária , Paquistão , Prescrições
4.
Molecules ; 27(13)2022 Jun 24.
Artigo em Inglês | MEDLINE | ID: mdl-35807316

RESUMO

In the current study, a series of new (2S,3S)-2-(4-isopropylbenzyl)-2-methyl-4-nitro-3-phenylbutanals (FM1-6) with their corresponding carboxylic acid analogues (FM7-12) has been synthesized. Initially, the aldehydic derivatives were isolated in the diastereomeric form, and the structures were confirmed with NMR, MS and elemental analysis. Based on the encouraging results in in vitro COX 1/2, 5-LOX and antioxidant assays, we oxidized the compounds and obtained the pure single (major) diastereomer for activities. Among all the compounds, FM4, FM10 and FM12 were the leading compounds based on their potent IC50 values. The IC50 values of compounds FM4, FM10 and FM12 were 0.74, 0.69 and 0.18 µM, respectively, in COX-2 assay. Similarly, the IC50 values of these three compounds were also dominant in COX-1 assay. In 5-LOX assay, the majority of our compounds were potent inhibitors of the enzyme. Based on the potency and safety profiles, FM10 and FM12 were subjected to the in vivo experiments. The compounds FM10 and FM12 were observed with encouraging results in in vivo analgesic and anti-inflammatory models. The molecular docking studies of the selected compounds show binding interactions in the minimized pocked of the target proteins. It is obvious from the overall results that FM10 and FM12 are potent analgesic and anti-inflammatory agents.


Assuntos
Antioxidantes , Ácidos Carboxílicos , Aldeídos , Analgésicos/química , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Anti-Inflamatórios não Esteroides/química , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Ácidos Carboxílicos/farmacologia , Ciclo-Oxigenase 2/metabolismo , Inibidores de Ciclo-Oxigenase 2/farmacologia , Edema/induzido quimicamente , Edema/tratamento farmacológico , Humanos , Simulação de Acoplamento Molecular , Estrutura Molecular , Relação Estrutura-Atividade
5.
BMC Pediatr ; 18(1): 242, 2018 07 25.
Artigo em Inglês | MEDLINE | ID: mdl-30045715

RESUMO

BACKGROUND: Unlicensed and off label drug use is an issue recognized worldwide in pediatric pharmacotherapy. The study was designed to assess the prevalence and predictors of unlicensed and off label drug use in neonatal population of Pakistan. METHOD: A prospective, observation study was conducted in nursery units at pediatric department of four tertiary care hospitals during the 1 year. Micromedex DRUGDEX was used to evaluate the case notes of 1300 patients. Logistic regression was employed to calculate the odds ratio for the predictors of unlicensed and off label drug use. RESULTS: A total of 1300 patients were included in this study who were treated with 52 different drugs. The prevalence of off label drug use was higher (52.14%) as compared to unlicensed drug use (33.35%). Dose (61.29%) and indication (13.68%) were the most frequent reasons for off label prescribing. In comparison to the corresponding reference categories, females and preterm infants were less likely to receive unlicensed prescriptions. While patients staying at hospital more than 5 days and infants receiving 3 or more medications were significantly more likely to receive unlicensed prescriptions. Moreover, in comparison to the corresponding reference categories, females were less likely to receive off label prescriptions while infants receiving 3 or more medications were 7 times more likely to receive off label prescriptions. CONCLUSION: The significant prevalence of unlicensed and off label drug prescriptions was found in neonatal population of Pakistan. The findings imply that more data on prevalence of unlicensed and off label prescriptions are required to provide a better picture of pediatric therapy in developing countries. Furthermore, advance formulations with new dosing in pediatrics is also necessary to minimize the risk of adverse drug events.


Assuntos
Berçários Hospitalares , Uso Off-Label/estatística & dados numéricos , Anti-Infecciosos/uso terapêutico , Fármacos do Sistema Nervoso Central/uso terapêutico , Revisão de Uso de Medicamentos , Humanos , Recém-Nascido , Recém-Nascido Prematuro , Paquistão , Estudos Prospectivos , Fatores Sexuais , Centros de Atenção Terciária
6.
Lipids Health Dis ; 15: 151, 2016 Sep 09.
Artigo em Inglês | MEDLINE | ID: mdl-27613388

RESUMO

BACKGROUND: Hyperlipidemia, a major pathological condition associated with disrupted lipid levels and physiological redox homeostasis. The excessive release of reactive oxygen species (ROS) leads to enhanced lipid peroxidation, aggravated atherosclerosis and oxidative stress. Integration of natural antioxidant blends in alone or with conventional treatments can alleviate these issues synergistically contributing least side effects. Published literature reported the efficacy of natural antioxidants as individual and in combinations in various conditions but less data is available on their evaluation in low dose ratio blends particularly in hypercholesterolemic diet. METHODS: Antihyperlipidemic effects of selected natural antioxidants; the phenolic oligomeric proanthocyanidins (OPC) and pterostilbene (PT) with niacin (NA) were investigated in current study. Their effects on lipid profile, lipid peroxidation and their aptitude to establish redox state between oxidants and antioxidants in body were evaluated in high cholesterol diet fed animal model. Male albino rabbits (n = 6) weighing 1.2-1.6 kg, supplemented with high cholesterol diet (400 mg/kg) for 12 weeks were used in the experiment. Antioxidants were administered individual high (100 mg/kg) and in low dose combinations (total dose = 100 mg/kg). Student's t test and one way analysis of variance (ANOVA) followed by Dunnet's test were used as statistical tools for evaluation. RESULTS: The results showed synergistic effects of low dose antioxidant blends. Therapies retarded elevation in blood lipid levels, lipid peroxidation and blood antioxidant depletion and consequently contributed in reestablishing redox homeostasis. The LDL/HDL ratio and atherogenic index were suppressed significantly in blend therapies with maximum effects of 59.3 and 25 % (p >0.001) observed in 50:30:20 ratios of OPC, NA and PT, compared to individual therapies 37 and 18 % max respectively. Moreover the results were also in close proximity with the statin therapy (52.66, 26.28 %). CONCLUSION: This study provides an evidence for natural antioxidants blends superiority over individual therapy in chronic diseases like hyperlipidemia. Such therapies in human equivalent doses can help in mitigating chronic illnesses in general populations.


Assuntos
Antioxidantes/metabolismo , Aterosclerose/dietoterapia , Produtos Biológicos/administração & dosagem , Sinergismo Farmacológico , Estresse Oxidativo/efeitos dos fármacos , Animais , Antioxidantes/administração & dosagem , Aterosclerose/tratamento farmacológico , Aterosclerose/patologia , Humanos , Hipolipemiantes/administração & dosagem , Metabolismo dos Lipídeos/efeitos dos fármacos , Peroxidação de Lipídeos/efeitos dos fármacos , Lipídeos/sangue , Masculino , Niacina/administração & dosagem , Proantocianidinas/administração & dosagem , Coelhos , Espécies Reativas de Oxigênio/metabolismo , Estilbenos/administração & dosagem
7.
BMC Complement Altern Med ; 16: 273, 2016 Aug 05.
Artigo em Inglês | MEDLINE | ID: mdl-27495801

RESUMO

BACKGROUND: Medicinal plants have proven their importance as a valuable source of molecules with therapeutic potential. Monotheca buxifolia (Falc.) A. DC. (family: Sapotaceae) is traditionally used as a hematinic, laxative, digestive, anthelmintic, antipyretic, and in the treatment of gastro-urinary disorders. To provide scientific evidence for its folkloric use, the present study investigated Monotheca buxifolia fruit hydro-ethanolic extract (MBHE) for its prospective antinociceptive, anti-inflammatory and antipyretic activities. MBHE was eluted through column chromatography to isolate the bioactive secondary metabolites which may probably involve in its beneficial properties. METHODS: The phytochemical constituents in MBHE was elucidated using UV, IR, (1)H-NMR, (13)C NMR, 2D-NMR spectra in combination with EIMS and FAB-MS spectrometric techniques and comparison with literature data of related compounds. The antinociceptive activity of MBHE was evaluated in the acetic acid induced abdominal constriction assay; the anti-inflammatory potential was assessed in the carrageenan induced paw edema, while the antipyretic effect was tested against brewer's yeast induced pyrexia in BALB/c mice at doses of 50, 100 and 150 mg/kg. RESULTS: Elution of MBHE along with various characterization techniques led to the isolation of oleanolic acid and isoquercetin. Significant attenuation of chemical induced nociception was observed with MBHE at tested doses of 50 mg/kg (P < 0.01, 68.87 %), 100 mg/kg (P < 0.01, 68.87 %) and 150 mg/kg (P < 0.001, 83.02 %). During a duration of 1-5 h in the carrageenan induced paw edema assay, significant ameliorative effect (P < 0.01, P < 0.001) was demonstrated by MBHE at 50 mg/kg (22.94-20 %), 100 mg/kg (33.23-21.13 %) and 150 mg/kg (38.23-25 %). MBHE also significantly alleviated the brewer's yeast induced pyrexic response when tested at doses of 50 mg/kg (P < 0.05 in 2nd h), 100 mg/kg (P < 0.05, P < 0.01 and P < 0.001 in 1-5 h) and 150 mg/kg (P < 0.01 and P < 0.001 in 1-5 h). CONCLUSION: These findings suggest that Monotheca buxifolia possess pain, inflammation and pyrexia ameliorating properties, probably mediated by the presence of oleanolic acid and isoquercetin contents, though the involvement of other important phytochemicals constituents cannot be ignored.


Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios/farmacologia , Antipiréticos/farmacologia , Extratos Vegetais/farmacologia , Sapotaceae/química , Analgésicos/química , Analgésicos/uso terapêutico , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/uso terapêutico , Antipiréticos/química , Antipiréticos/uso terapêutico , Comportamento Animal/efeitos dos fármacos , Edema/tratamento farmacológico , Inflamação/tratamento farmacológico , Camundongos , Camundongos Endogâmicos BALB C , Manejo da Dor , Extratos Vegetais/química
8.
Pak J Pharm Sci ; 28(5): 1637-46, 2015 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-26408871

RESUMO

Manifestation of microbial spoilage of any product by bacteria and to assess the effectiveness of the anti-microbial preservatives (parabens) used for the prevention and stability purpose. The aim of the present work is to study the effectiveness of preservatives used in the antacid suspensions and to analyze the effect of microbial growth on the quality of respective antacid suspensions. Samples of various antacid suspensions were randomly collected from local market and Government hospital pharmacies. Three different antacid formulations were prepared in the laboratory. All the formulations were preliminarily evaluated on the basis of organoleptic characteristics, pH, viscosity and assay. Efficacy of the preservative system in suspension formulation was determined by inoculating the samples in its final container, with specific strains of bacteria i.e. Escherichia coli ATCC 8739, Pseudomonas aeruginosa ATCC 9027 and Staphylococcus aureus ATCC 6538, taking samples from the inoculated preparation at specified intervals of time i.e. 0 time, 07 days, 14 days and 28 days, growing it on nutrient agar medium and colony forming units (CFUs) were scored by plate count. At the same time the samples were also subjected to qualitative and quantitative testing. The decrease in CFU and alteration in assay, pH and viscosity was observed in all the formulations except formulation M2 and F3 that showed stability throughout the study period.


Assuntos
Antiácidos/química , Contaminação de Medicamentos , Conservantes Farmacêuticos/farmacologia , Bactérias/isolamento & purificação , Química Farmacêutica , Estabilidade de Medicamentos , Suspensões , Viscosidade
9.
Drug Dev Ind Pharm ; 40(11): 1503-8, 2014 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-23984755

RESUMO

The objective of the current work was to develop and evaluate thermoreversible subcutaneous drug delivery system for Insulin. Thermoreversible in-situ gel system was developed and evaluated both in-vitro and in-vivo comprising of pluronic F-127 alone or in combination with methylcellulose in different ratios. The drug release kinetics and mechanism was predicted by applying various mathematical models to the in-vitro dissolution data. Rabbits were used as animal model following subcutaneous injection to predict various pharmacokinetic parameters by applying Pk-Summit® software. The in-vitro and in-vivo data revealed that the formulation IPM 15/3 consisting of the pluronic F-127 (15% w/v) and methylcellulose (3% w/v) was the most robust and capable formulation for extending the drug release and maintaining basal plasma insulin level between 10 and 40 µU/ml for 240 h (10 d).


Assuntos
Géis/química , Hipoglicemiantes/administração & dosagem , Insulina/administração & dosagem , Metilcelulose/química , Poloxâmero/química , Animais , Sistemas de Liberação de Medicamentos , Liberação Controlada de Fármacos , Hipoglicemiantes/farmacocinética , Injeções Subcutâneas , Insulina/farmacocinética , Coelhos , Tecnologia Farmacêutica , Viscosidade
10.
Curr Pharm Des ; 2024 Jun 11.
Artigo em Inglês | MEDLINE | ID: mdl-38867533

RESUMO

BACKGROUND: Cocrystals are an efficient way for the delivery of low soluble drugs but when dissolved they rapidly disproportionate. To formulate the cocrystals in tablets, cocrystals must be stabilized. In this study ibuprofen-nicotinamide (IBU-NIC) cocrystals were synthesized initially by slow solvent evaporation and for bulk production by fast solvent evaporation techniques. METHOD: The cocrystals were characterized by powder X-ray diffraction (PXRD), Fourier transform infrared spectrophotometer (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), and optical microscopy. The ibuprofen cocrystals showed greater solubility compared to the parent drug. RESULT: Intrinsic dissolution data was utilized for efficacious screening of tablet formulations. Using hydrophilic polymers at a ratio of 6:1 (polymer to IBU-NIC cocrystal ratio), hydroxypropyl methylcellulose (F1), polyvinylpyrrolidone (PVP) K-30 (F2) and PVP K-90 (F3), three tablet formulations were prepared that stabilized cocrystals during dissolution. The drug release profiles after 60 minutes from formulations F1 (92.30), F2 (98.54), F3 (99.88) were all higher compared to the marketed brand BRUFEN® F, (79.61%) in a simulated intestinal media (p<0.001). CONCLUSION: Significant increase in the dissolution rate of cocrystal was observed with no phase change in all formulations.

11.
Urol Case Rep ; 46: 102296, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36506796

RESUMO

Hydatid cyst of Echinococcus granulosus usually develops in liver and lungs of the affected individual and is considered a common health problem in endemic regions. Although, the cyst can be found in less common locations, such as brain, heart, and bones, the urinary bladder is extremely rare that may mimic malignancy radiologically and creates a diagnostic dilemma for clinicians and radiologists. Here we present a unique case of hydatid cyst in the urinary bladder with associated eosinophilic cystitis.

12.
Plants (Basel) ; 12(23)2023 Nov 27.
Artigo em Inglês | MEDLINE | ID: mdl-38068618

RESUMO

Plants, being sessile, have developed complex signaling and response mechanisms to cope with biotic and abiotic stressors. Recent investigations have revealed the significant contribution of phytohormones in enabling plants to endure unfavorable conditions. Among these phytohormones, jasmonic acid (JA) and its derivatives, collectively referred to as jasmonates (JAs), are of particular importance and are involved in diverse signal transduction pathways to regulate various physiological and molecular processes in plants, thus protecting plants from the lethal impacts of abiotic and biotic stressors. Jasmonic acid has emerged as a central player in plant defense against biotic stress and in alleviating multiple abiotic stressors in plants, such as drought, salinity, vernalization, and heavy metal exposure. Furthermore, as a growth regulator, JA operates in conjunction with other phytohormones through a complex signaling cascade to balance plant growth and development against stresses. Although studies have reported the intricate nature of JA as a biomolecular entity for the mitigation of abiotic stressors, their underlying mechanism and biosynthetic pathways remain poorly understood. Therefore, this review offers an overview of recent progress made in understanding the biosynthesis of JA, elucidates the complexities of its signal transduction pathways, and emphasizes its pivotal role in mitigating abiotic and biotic stressors. Moreover, we also discuss current issues and future research directions for JAs in plant stress responses.

13.
Pak J Pharm Sci ; 25(1): 51-8, 2012 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-22186309

RESUMO

In the present study four medicinal plants traditionally used in Pakistan for treatment of various ailments were evaluated for their heavy metals content, insecticidal, cytotoxic and phytotoxic actions. The metals like Cr, Cu, Zn, Mn, Ni, Pb, Fe and Co were determined in crude extract and various fractions. Soil samples were also tested for heavy metals to determine assimilation of any metal by the plant. Lead, Chromium, copper, nickel and cobalt exceeded the permissible limit in most of the tested samples while the concentration of zinc, manganese and iron was within the permissible limit. Chloroform fraction from Achyranthes aspera and ethyl acetate fraction from Duchesnea indica showed significant phytotoxic activities. Crude extract and chloroform fraction from Xanthium strumarium showed insecticidal activity comparable to that of permethrin and thus could be a significant source of natural insecticide. The butanol fraction from X. strumarium showed significant cytotoxicity with LC(50) 1.9306 µg/ml, having mortality rate 93% at highest dose, while the crude extract from Valeriana wallichii showed 90% mortality rate (LC(50) 4.9730 µg/ml) at highest dose. However, the extracts from other plants were not effective against the brine shrimps tested.


Assuntos
Citotoxinas/farmacologia , Herbicidas/farmacologia , Inseticidas/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Animais , Artemia , Bioensaio/métodos , Bioensaio/estatística & dados numéricos , Metais/análise , Metais Pesados/análise , Paquistão , Plantas Medicinais/química , Poluentes do Solo/análise
14.
Pak J Pharm Sci ; 24(4): 435-43, 2011 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-21959802

RESUMO

Conventional dosage form is nowadays mostly replaced by sustained release formulation in order to increase drug efficacy and patient compliance. The sustained release properties of the PVP K90 alone and in combination with guar gum, xanthan gum and gum tragacanth were evaluated using diclofenac sodium (100 mg/tablet) as a model drug. Tablets were processed using wet granulation method and evaluated for sustained drug release properties. The drug release from the formulations was studied in relationship with Commercially available Diclofenac Sodium SR, used as a reference tablets and results were expressed as similarity (f1) and differential factor (f2). The tablets prepared using PVP K90 160 mg/tablet sustained the release of diclofenac sodium for 12 hours. Formulations where the PVP K90 was partially replaced with different gums also sustained the release of drug for 12 hours. The release of the drug from these formulations mainly followed Higuchi model and super case-II and Non-Fickian diffusion. The in-vivo drug release was studied in healthy human volunteers using non-blinded cross over, two period design using Diclofenac Sodium SR Tablets as a reference drug. The relative bioavailability of the formulation containing PVP K90 and gum tragacanth was 0.91. The studies showed that the use of the PVP K90 in combination with gum tragacanth both in-vitro and in-vivo sustained the release of the drug.


Assuntos
Diclofenaco/administração & dosagem , Diclofenaco/farmacocinética , Gomas Vegetais/química , Povidona/química , Adulto , Área Sob a Curva , Disponibilidade Biológica , Estudos Cross-Over , Preparações de Ação Retardada/química , Diclofenaco/sangue , Galactanos/química , Dureza , Humanos , Masculino , Mananas/química , Polissacarídeos Bacterianos/química , Comprimidos , Tragacanto/química , Adulto Jovem
15.
J Pharm Sci ; 110(4): 1749-1760, 2021 04.
Artigo em Inglês | MEDLINE | ID: mdl-33460669

RESUMO

Cisplatin therapy faces low bioavailability and clastogenic potential limitations. Early payload leakage of nanocarriers may impair adequate therapeutic efficacy. We propose encapsulation of cisplatin in such nanocarrier that can be externally stimulated for high payload release and enhanced toxicity at site of action. Cisplatin conjugated gold nanorods (Pt-AuNRs) have been synthesized and characterized through UV visible spectroscopy, dynamic light scattering and transmission electron microscopy. Physico-chemical characterization through X-ray photon spectrometry confirms the covalent linkage between linker and aquated cisplatin with AuNRs. Laser exposure (850 nm, CW) enabled ~15-fold payload release from Pt-AuNRs nano-assembly, which is quite high (P < 0.0001) compared to non-stimulated conditions. The median growth inhibitory concentration (GI50) after laser exposure of Pt-AuNRs was ~11- and 13-fold low compared to corresponding Pt-AuNRs without laser exposure and cisplatin respectively, in sarcoma cells. Synergistic therapeutic difference is more significant (P < 0.01), at lower concentrations of Pt-AuNRs (0.5-10 µg/mL). Pt-AuNRs photothermal therapy indicates a convincible association of over-production of reactive oxygen species (P < 0.0001) and synergistic therapeutic efficacy. Clastogenic potential is found non-significant for Pt-AuNRs (10 µg/mL). Cisplatin nanoconjugate shows biocompatibility against blood cells. In conclusion, laser-stimulated Pt-AuNRs appear a promising drug delivery with synergistic toxic potential against cancer while attenuating cisplatin toxicity.


Assuntos
Nanotubos , Neoplasias , Cisplatino , Ouro , Humanos , Lasers
16.
Clin Drug Investig ; 29(4): 275-81, 2009.
Artigo em Inglês | MEDLINE | ID: mdl-19301941

RESUMO

BACKGROUND AND OBJECTIVE: Ciprofloxacin is a broad-spectrum, synthetic antibacterial used for the treatment of various bacterial infections. In multidrug therapy, ciprofloxacin is commonly prescribed with analgesics for the management of infection, pain and inflammation. The objective of this study was to evaluate the pharmacokinetic properties of ciprofloxacin tablets with concurrent administration of diclofenac tablets in healthy adult human volunteers. METHODS AND DESIGN: The disposition pharmacokinetics of a single oral dose of ciprofloxacin 500 mg alone and with co-administration of a diclofenac 50 mg tablet in 12 healthy male volunteers was investigated using a two-period, crossover design. The blood samples were collected at 0 (predose), 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16 and 24 hours after administration of the drugs and the concentration of ciprofloxacin in serum was determined using reversed phase high-performance liquid chromatography. The pharmacokinetic parameters were calculated using a noncompartmental model and a two-compartment model. RESULTS: The maximum plasma concentration (C(max)) of ciprofloxacin increased from 2.48 +/- 0.33 microg/mL when administered alone to 3.91 +/- 0.8 microg/mL with co-administration of diclofenac. Time to reach C(max) (t(max)) with ciprofloxacin reduced from 2.02 +/- 0.3 hours when administered alone to 1.49 +/- 0.2 h with co-administration of diclofenac. Significant increases in ciprofloxacin area under the serum concentration-time curve (AUC) and elimination half-life, together with a significant decrease in total body clearance of ciprofloxacin, were observed with concurrent administration of diclofenac. CONCLUSION: Oral co-administration of ciprofloxacin tablets with diclofenac tablets increased ciprofloxacin AUC and C(max), and reduced ciprofloxacin t(max) and total body clearance.


Assuntos
Anti-Infecciosos/farmacocinética , Anti-Inflamatórios não Esteroides/farmacocinética , Ciprofloxacina/farmacocinética , Diclofenaco/farmacocinética , Área Sob a Curva , Disponibilidade Biológica , Cromatografia Líquida de Alta Pressão , Estudos Cross-Over , Combinação de Medicamentos , Interações Medicamentosas , Meia-Vida , Humanos , Taxa de Depuração Metabólica , Comprimidos , Distribuição Tecidual , Adulto Jovem
17.
J Ayub Med Coll Abbottabad ; 21(3): 72-5, 2009.
Artigo em Inglês | MEDLINE | ID: mdl-20929018

RESUMO

BACKGROUND: Old World Cutaneous Leishmaniasis (OWCL) is a preventable skin infection that leads to morbidity and social isolation. It is spreading rapidly. The sore of OWCL may be a non-ulcerative red papule, nodule or a large mutilating ulcer. The ulcer is typically painless and can leave a disfiguring scar. METHODS: This was a descriptive study. The diagnosis of OWCL was established by finding LD bodies in skin smear preparation. RESULTS: This study identified 1680 cutaneous leishmaniasis in 1767 skin ulcers. Children (n = 924) were infected more than other age groups (n = 756). There were typical skin sore of OWCL in 1512 cases while 168 patients had atypical presentation. The ulcers were painless in 1603 patients. History of insect bite was present in 1366 cases, thorn prick in 156 patients, religious visit to endemic areas in 256 patients, and 4 patients had post surgical non healing wound. Lesions with 4 to 6 months of age had a maximum yield of LD bodies. There were 498 patients from different areas of Peshawar; 688 cases from leishmania endemic belt of FATA while 89 patients came from other urban and rural areas of NWFP. CONCLUSIONS: There is a tremendous increase in cases of OWCL and the disease became endemic in many regions of Pakistan. The bordering areas along Afghanistan have constituted an endemic belt that had invaded the neighboring urban and rural areas. Several chronic non healing ulcers had been diagnosed as OWCL. Many cases have been detected in Peshawar. People need education about the nature of the diseases and the efficacy of personal protective measures. Spray with suitable insecticides is required in all residential areas.


Assuntos
Leishmaniose Cutânea/epidemiologia , Úlcera Cutânea/parasitologia , Adolescente , Adulto , Criança , Diagnóstico Diferencial , Feminino , Humanos , Leishmaniose Cutânea/diagnóstico , Masculino , Pessoa de Meia-Idade , Paquistão/epidemiologia , Úlcera Cutânea/diagnóstico , Úlcera Cutânea/epidemiologia
18.
Pak J Pharm Sci ; 21(4): 379-89, 2008 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-18930859

RESUMO

Prevalence of microorganisms was studies in clinical samples of various body fluids (n=12,259), collected from patients at Post graduate Medical Institute Hayatabad Medical Complex (PGMI, HMC) Peshawar. Only 34.90% of samples exhibited growth, 36.25% of these isolates were Gram positive and 63.75% were Gram negative bacteria. E. coli was the most prevalent organism (39.45%) followed by S. aureus (32.23%), Proteus spp. (9.23%), Pseudomonas spp. (6.54%), Streptococuss spp. (3.51%), Acinetobacter spp. (2.66%), Citrobacter spp. (2.8%), Providencia spp. (2.2%) and miscellaneous bacteria (1.38%). The growth of bacteria was high in pus samples (44.03%) followed by urine (38.21%), high vaginal swab (HVS) (8.58%), cerebrospinal fluid (CSF) (1.96%), blood (3.39%) and miscellaneous samples (3.83%). E. coli and S. aureus were the most prevalent organism in urine (56.57%) and pus samples (44.02%), respectively. The frequency of E. coli (61.76%) was high in samples collected from female patients and percentage of the infections caused by the S. aureus in male and female patients was 47.9 and 52.1, respectively. During the study period, frequency of the E. coli was high during April to October and the prevalence of S. aureus was very common during March to October. Consistent but insignificant increase in the beta-lactamase producing S. aureus and E. coli was observed throughout the period of the study. However, increase in the beta-lactamase producing S. aureus and E. coli was above 80%. The prevalence of extended spectrum beta-lactamase (ESBL) in E. coli was increased from 13.85% in year 2000 to 22.66% in year 2003. The increasing in prevalence of microorganism, particularly of beta-lactamase producing E. coli and S. aureus and ESLB is alarming situation. Various measured like prescribing and patient compliance are required to control the increase in the prevalence of microorganism.


Assuntos
Bactérias/isolamento & purificação , Líquidos Corporais/microbiologia , Infecção Hospitalar/microbiologia , Hospitais de Ensino , beta-Lactamases/metabolismo , Antibacterianos/uso terapêutico , Bactérias/enzimologia , Bactérias/patogenicidade , Infecção Hospitalar/epidemiologia , Infecção Hospitalar/prevenção & controle , Infecção Hospitalar/transmissão , Farmacorresistência Bacteriana , Feminino , Hospitais de Ensino/estatística & dados numéricos , Humanos , Controle de Infecções , Transmissão de Doença Infecciosa do Paciente para o Profissional/prevenção & controle , Masculino , Paquistão/epidemiologia , Prevalência , Fatores Sexuais , Fatores de Tempo
19.
Pak J Pharm Sci ; 21(3): 290-4, 2008 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-18614427

RESUMO

One year prospective study was evaluated to ascertain the prevalence of nasal carriage of potentially pathogenic bacteria in health care workers and the antibiotic susceptibility profile. The bacterial strains were identified by conventional method and the antibiotic resistance was carried out by disc diffusion method. The prevalence of Staphylococcus aureus, coagulase negative staphylococci and methicillin resistant Staphylococcus aureus were 48%, 46% and 14% respectively. The antibiotic susceptibility pattern of these isolates revealed that Staphylococcus aureus were more resistant towards antibiotics than coagulase negative staphylococci. The most effective antibiotic for S. aureus was found to be vancomycin with 100% efficacy, then cephalothin 92%, ciprofloxacin 91%, amikacin 77% and erythromycin 55%, ampicillin 11% and penicillin 3%. Coagulase negative staphylococci were 100% sensitive to vancomycin and cephalothin. Oxacillin showed 78% effectiveness; while ampicillin and penicillin, demonstrated 64% and 59% respectively. Doxycycline (93%), amikacin (93%), fusidic acid (90%) and erythromycin (92%) were effective antimicrobials.


Assuntos
Anti-Infecciosos/uso terapêutico , Portador Sadio , Infecção Hospitalar/transmissão , Farmacorresistência Bacteriana , Nariz/microbiologia , Recursos Humanos em Hospital , Infecções Estafilocócicas/transmissão , Staphylococcus aureus/isolamento & purificação , Infecção Hospitalar/tratamento farmacológico , Infecção Hospitalar/microbiologia , Testes de Sensibilidade a Antimicrobianos por Disco-Difusão , Hospitais Pediátricos , Humanos , Higiene , Controle de Infecções , Resistência a Meticilina , Estudos Prospectivos , Infecções Estafilocócicas/tratamento farmacológico , Infecções Estafilocócicas/microbiologia , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/patogenicidade
20.
Pak J Pharm Sci ; 21(3): 311-5, 2008 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-18614431

RESUMO

A prospective study on various clinical isolates from patients admitted from various parts of NWFP and Afghanistan at Post Graduate Medical Institute (PGMI) Hayatabad Medical Complex, Peshawar was conducted from January 2000 to December 2004 to ascertain the prevalence and antimicrobial susceptibility of Pseudomonas aeruginosa infections. Among 4709 positive isolates, 314 (6.67%) were Pseudomonas aeruginosa. The highest rate of infection due to Pseudomonas aeruginosa was observed in orthopedic ward (24.61%) and OPD (20%), in other wards the infection was between 13% to 1.5%. Gender-wise prevalence showed 61.78% male and 38.22% females were infected by Pseudomonas aeruginosa. The highest percentage of Pseudomonas aeruginosa isolates were observed in pus (57.64%) and urine (24.2%) samples. Maximum Pseudomonas aeruginosa isolates were found between March to August and the highest percentage 13.846% was observed in June. Using the disc diffusion method, the resistance patterns of 314 isolates against 14 antimicrobial agents were determined. The highest resistance was observed against ampicillin (> or = 98.4%), ampicillin/sulbactam (85.3%), co-amoxiclave (83.8%) and ofloxacin (68.4%) and least resistance was observed against amikacin (24%). Similarly the MIC for ampicillin (4 to >2048 microg/ml), ampicillin/sulbactam (1 to 2048 microg/ml) and co-amoxiclave (1 to >2048 microg/ml) against clinical isolates of Pseudomonas aeruginosa was also high. High resistance of Pseudomonas aeruginosa against various commonly used antibiotics showed the alarming situation. The control of drug resistant Pseudomonas aeruginosa required rational prescribing and proper use of antibiotics.


Assuntos
Antibacterianos/farmacologia , Infecção Hospitalar/tratamento farmacológico , Farmacorresistência Bacteriana Múltipla , Infecções por Pseudomonas/tratamento farmacológico , Pseudomonas aeruginosa/efeitos dos fármacos , Infecção Hospitalar/epidemiologia , Infecção Hospitalar/microbiologia , Testes de Sensibilidade a Antimicrobianos por Disco-Difusão , Feminino , Hospitais , Humanos , Pacientes Internados , Masculino , Testes de Sensibilidade Microbiana , Prevalência , Estudos Prospectivos , Infecções por Pseudomonas/epidemiologia , Infecções por Pseudomonas/microbiologia , Pseudomonas aeruginosa/crescimento & desenvolvimento , Pseudomonas aeruginosa/isolamento & purificação , Estações do Ano , Supuração/microbiologia , Urina/microbiologia
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