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Acta Pharmaceutica Sinica. B Jul 2021Due to its safety, convenience, low cost and good compliance, oral administration attracts lots of attention. However, the efficacy of many oral drugs is limited to... (Review)
Review
Due to its safety, convenience, low cost and good compliance, oral administration attracts lots of attention. However, the efficacy of many oral drugs is limited to their unsatisfactory bioavailability in the gastrointestinal tract. One of the critical and most overlooked factors is the symbiotic gut microbiota that can modulate the bioavailability of oral drugs by participating in the biotransformation of oral drugs, influencing the drug transport process and altering some gastrointestinal properties. In this review, we summarized the existing research investigating the possible relationship between the gut microbiota and the bioavailability of oral drugs, which may provide great ideas and useful instructions for the design of novel drug delivery systems or the achievement of personalized medicine.
PubMed: 34386321
DOI: 10.1016/j.apsb.2020.09.013 -
Ecotoxicology and Environmental Safety Mar 2023Antibiotics have strong antibacterial activity, even trace antibiotics can greatly inhibit the pollutant degradation efficiency. In order to effectively improve the...
Antibiotics have strong antibacterial activity, even trace antibiotics can greatly inhibit the pollutant degradation efficiency. In order to effectively improve the pollutant degradation efficiency, it was hence of great significance to explore sulfapyridine (SPY) degradation and the mechanism of antibacterial activity. This study selected SPY as the research object, of which the trend of SPY concentration through hydrogen peroxide (HO), potassium peroxydisulfate (PDS) and sodium percarbonate (SPC) and resultant antibacterial activity at pre-oxidation was examined. The combined antibacterial activity (CAA) of SPY and its transformation products (TPs) was further analyzed. The SPY degradation efficiency reached more than 90 %. However, the degradation efficiency of antibacterial activity was between 40-60 %, and the mixture's antibacterial activity was difficult to be removed. The antibacterial activity of TP3, TP6 and TP7 was higher than that of SPY. TP1, and TP8 and TP10 were more prone to synergistic reaction with other TPs. The antibacterial activity of binary mixture gradually changed from synergism to antagonism as binary mixture concentration increased. The results provided a theoretical basis for the efficient degradation of antibacterial activity of the SPY mixture solution.
Topics: Sulfapyridine; Hydrogen Peroxide; Water Pollutants, Chemical; Anti-Bacterial Agents; Oxidation-Reduction; Environmental Pollutants
PubMed: 36796210
DOI: 10.1016/j.ecoenv.2023.114656 -
BMJ Case Reports Apr 2013The medical management of a patient with Crohn's disease should take into account the activity, site and behaviour of disease, and should be discussed with the patient,...
The medical management of a patient with Crohn's disease should take into account the activity, site and behaviour of disease, and should be discussed with the patient, and 5-aminosalicylates are a group of medications which have been commonly used. Sulfasalazine is a combination of 5-aminosalicylic acid and sulfapyridine which acts only as a carrier to the colonic site of action but can still cause systemic side-effects including lung disease. In mesalazine the specific sulfapyridine-related side-effects, especially pulmonary reactions, are avoided. However, we present a case of lung fibrosis which was associated with mesalazine in a Crohn's patient.
Topics: Aged, 80 and over; Anti-Inflammatory Agents, Non-Steroidal; Crohn Disease; Humans; Male; Mesalamine; Pulmonary Fibrosis; Tomography, X-Ray Computed
PubMed: 23576654
DOI: 10.1136/bcr-2013-008724 -
Journal of Pharmaceutical and... Oct 2023Sulfasalazine has been identified as a candidate molecule to be investigated as an intervention to treat preterm pre-eclampsia during pregnancy. However, placental...
Sulfasalazine has been identified as a candidate molecule to be investigated as an intervention to treat preterm pre-eclampsia during pregnancy. However, placental exposure of sulfasalazine and its systemically absorbed metabolite, sulfapyridine, is unknown. A robust liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated to simultaneously quantitate these analytes in human placenta with an application to a pilot clinical trial. The placental tissue was homogenised using a water:methanol (1:1, v/v) mixture, followed by sample extraction using both protein precipitation and solid phase extraction. Sulfasalazine-d4 and sulfapyridine-d4 were used as internal standards. An Agilent Poroshell EC-C18 (3.0 ×100 mm, 2.7 µm) column was used for chromatographic separation, with gradient elution employed at a flow rate of 0.450 mL/min over a total run time of seven minutes. The mobile phases consisted of water with 0.1% formic acid (mobile phase A) and acetonitrile:methanol (90:10, v/v) with 0.1% formic acid (mobile phase B). A Shimadzu-8040 mass spectrometer was operated in multiple reaction monitoring (MRM) mode using positive electrospray ionisation (ESI). For both analytes, the assay was validated over the range 30-30,000 ng/mL, or 150-150,000 ng/g. During inter-day validations (n = 18), the average accuracies of quality controls ranged from 101.6% to 112.7% with corresponding precisions of 4.4-6.7% for sulfasalazine, and from 97.4% to 108.4%, with corresponding precisions of 3.7-10.0% for sulfapyridine. No significant matrix effects were observed, and the method proved to be sensitive and specific for both analytes. This study presents the first validated analytical method for quantifying sulfasalazine and sulfapyridine in human placenta as part of a pilot clinical trial to generate preliminary data on its pharmacokinetics and efficacy as in intervention for preterm pre-eclampsia.
Topics: Pregnancy; Infant, Newborn; Humans; Female; Chromatography, Liquid; Sulfapyridine; Sulfasalazine; Methanol; Pre-Eclampsia; Tandem Mass Spectrometry; Placenta
PubMed: 37597383
DOI: 10.1016/j.jpba.2023.115633 -
American Journal of Kidney Diseases :... Dec 2017Sulfasalazine is an anti-inflammatory agent commonly used in the treatment of autoimmune conditions such as inflammatory bowel disease and rheumatoid arthritis....
Sulfasalazine is an anti-inflammatory agent commonly used in the treatment of autoimmune conditions such as inflammatory bowel disease and rheumatoid arthritis. Sulfasalazine is converted by gut bacteria into sulfapyridine and the clinically active metabolite 5-aminosalicylic acid (5-ASA), and its efficacy is proportional to the 5-ASA concentration within the intestinal lumen. Renal complications are commonly reported for the chemically similar 5-ASA derivative mesalamine, but are not well-known side effects of sulfasalazine therapy. We report a 72-year-old patient with Crohn's disease managed with sulfasalazine for more than 10 years who presented with severe acute kidney injury (serum creatinine, 9.7mg/dL). Renal ultrasound revealed calculi and he subsequently spontaneously voided innumerable stones, which were composed of sulfasalazine metabolites. His renal calculi cleared and serum creatinine concentration improved to 3.1mg/dL after discontinuing sulfasalazine therapy and intravenous fluid hydration. His kidney function eventually returned to baseline. This case demonstrates that renal complications, in particular nephrolithiasis, may be an under-reported but potentially serious phenomenon in patients with inflammatory bowel disease treated with sulfasalazine and that their hydration status may play an important role in this process.
Topics: Acute Kidney Injury; Aged; Anti-Inflammatory Agents, Non-Steroidal; Antiparkinson Agents; Carbidopa; Cholinesterase Inhibitors; Crohn Disease; Donepezil; Drug Combinations; Fluid Therapy; Humans; Indans; Kidney Calculi; Levodopa; Male; Parkinson Disease; Piperidines; Severity of Illness Index; Sulfasalazine; Ultrasonography
PubMed: 28669550
DOI: 10.1053/j.ajkd.2017.05.013 -
Water Research Jul 2023There has been a significant increase in antimicrobial agents (AAs) usage, globally - however the relative consumption is unevenly distributed between nations.... (Review)
Review
There has been a significant increase in antimicrobial agents (AAs) usage, globally - however the relative consumption is unevenly distributed between nations. Inappropriate use of antibiotics can harbour inherent antimicrobial resistance (AMR); therefore, it is important to understand and monitor community-wide prescribing and consumption behaviours throughout different communities around the world. Wastewater-Based Epidemiology (WBE) is a novel tool enabling low cost and large scale studies focussed on AA usage patterns. The back-calculation of community antimicrobial intake was performed from quantities measured in municipal wastewater and informal settlement discharge in the city of Stellenbosch, utilising WBE. Seventeen antimicrobials, and their human metabolites, were evaluated, in concordance with prescription records corresponding to the catchment region. The proportional excretion, biological/chemical stability, and method recovery of each analyte were all crucial factors in the efficacy of the calculation. Mass per day measurements were normalised to the catchment area via population estimates. Municipal wastewater treatment plant population estimates were used to normalise the wastewater samples and prescription data (mg/day/1000 inhabitants). Population estimates for the informal settlements were less accurate due to a lack of reliable sources that were relevant to the sampling time period. Both mass loads and normalised loads suggested higher than average usage throughout the settlements, relative to municipal wastewater. This was seen most prominently in emtricitabine and lamivudine; but also, sulfamethoxazole, trimethoprim, sulfadiazine, clindamycin, ciprofloxacin, ofloxacin, and doxycycline. Urban water fingerprinting (UWF) data triangulation with prescription datasets showed good correlations for several antimicrobial agents (AAs) (e.g., clindamycin, clarithromycin, ofloxacin, and doxycycline). It also revealed discrepancies in usage for some compounds (e.g., tetracycline and sulfapyridine). This might be linked with a lack of pharma compliance in prescription datasets; erroneous association of prescription boundaries with the sewerage catchment; and/or uncertainties within the sewerage catchment (e.g., population estimations). The UWF tool provided a comprehensive overview of multiclass AAs usage, both prescription and over-the counter. For example, tetracycline was not reported in available prescription statistics, but was detected at an average of 18.4 mg/day/1000inh; and no antiviral prescriptions were obtained, but emtricitabine and lamivudine were quantified at 2415.4 and 144.4 mg/day/1000inh, respectively. A lack of clarity regarding prescriptions and a lack of inclusion of several critical (often over-the-counter) medications in public health databases makes WBE a useful and comprehensive epidemiology tool for tracking pharma usage within a catchment.
Topics: Humans; Anti-Bacterial Agents; Wastewater; Clindamycin; Doxycycline; South Africa; Lamivudine; Ofloxacin; Water Pollutants, Chemical
PubMed: 37247434
DOI: 10.1016/j.watres.2023.120110