- Synthesis and characterization of poly(N-vinylcaprolactam)-based spray-dried microparticles exhibiting temperature and pH-sensitive properties for controlled release of ketoprofen. [Journal Article]
- DDDrug Dev Ind Pharm 2017 Apr 22; :1-31
- Poly(N-vinylcaprolactam) (PNVCL) and poly(N-vinylcaprolactam-co-acrylic acid) (poly(NVCL-co-AA)) were synthesized by solution free radical polymerization and displayed thermo-responsive behavior, wit...
Poly(N-vinylcaprolactam) (PNVCL) and poly(N-vinylcaprolactam-co-acrylic acid) (poly(NVCL-co-AA)) were synthesized by solution free radical polymerization and displayed thermo-responsive behavior, with lower critical solution temperatures (LCSTs) of 35°C and 39°C, respectively. The incorporation of AA unities made the poly(NVCL-co-AA) sensitive to both pH- and temperature. They were exploited in this work in preparing microparticles loaded with ketoprofen via spray-drying to modulate the drug release rate by changing pH or temperature. The interaction between polymer and drug was studied using x-ray diffractometry, Raman spectrometry and scanning electron microscopy (SEM). The biocompatibility of pure polymers, free ketoprofen as well as the spray-dried particles was demonstrated in vitro by low cytotoxicity and a lack of nitric oxide production in macrophages at concentrations as high as 100 µg mL(-1). The release profile of ketoprofen was evaluated by in vitro assays at different temperatures and pH values. Drug diffusion out of PNVCL's hydrated polymer network is increased at temperatures below the LCST. However, when poly(NVCL-co-AA) was used as the matrix, the release of Ketoprofen was primarily controlled by the pH of the medium. These results indicated that PNVCL and the novel poly(NVCL-co-AA) could be promising candidates for pH and temperature responsive drug delivery systems.
- Temporal dynamics of human-excreted pollutants in wastewater treatment plant influents: Toward a better knowledge of mass load fluctuations. [Journal Article]
- STSci Total Environ 2017 Apr 20; 596-597:246-255
- The occurrence of 25 drug target residues (illicit drugs or pharmaceutically active compounds) was investigated during 85 consecutive days in the influents of a wastewater treatment plant in the Regi...
The occurrence of 25 drug target residues (illicit drugs or pharmaceutically active compounds) was investigated during 85 consecutive days in the influents of a wastewater treatment plant in the Region Centre-Val de Loire, France. This long tracking period allowed a better understanding of the patterns affecting the occurrence of this type of contaminants. Among them, 2 were never detected (i.e. heroin and amphetamine). Concerning illicit drugs two patterns were found. Cocaine and ecstasy median loads varied considerably between weekdays and weekend days (i.e. 18.3 and 35.9% respectively) whereas cannabis and heroin (based on 6-mono-acetylmorphine loads) loads were within the same order of magnitude with a significant statistical correlation with pharmaceuticals such as acetaminophen or ketoprofen. The consumption of selected drugs was back-calculated from the loads. Among illicit drugs the highest consumption was found for cannabis with a median consumption of 51mg·day(-1)·inhabitant(-1) (inh) whereas the median consumption for cocaine (based on benzoylecgonine loads) and ecstasy was 32 and 6mg·day(-1)·10(3)·inh(-1) respectively. The highest consumption values of pharmaceutically active compounds (PACs) were found for acetaminophen and acetylsalicylic acid with 108.8 and 34.1mg·day(-1)·inh(-1) respectively, in good agreement with national sales data. A statistically significant weekly pattern was found for several PACs such as metoprolol and trimethoprim, but with the opposite pattern to that of illicit drugs. The variations in daily PAC loads could provide information about the mobility of people in the catchment, especially on the basis of daily taken PACs (i.e. to treat chronicle diseases).
- Pig castration: will the EU manage to ban pig castration by 2018? [Journal Article]
- PHPorcine Health Manag 2016; 2:29
- CONCLUSIONS: The deadlines of January 1, 2012, and of 2018 are far from being met. The opinions on the animal-welfare-conformity and the practicability of the alternatives to surgical castration without analgesia/anaesthesia and the alternatives to surgical castration are widely dispersed. Although countries using analgesia/anaesthesia routinely found this method practical and effective, only few countries seem to aim at meeting the deadline to phase out surgical castration completely.
- [Application of synthetic and semisynthetic polymers (Kollidon K30 and hydroxypropylmethylcellulose) as carriers of ketoprofen in solid oral prolonged-release dosage forms]. [Journal Article]
- PMPolim Med 2016 Jul-Dec; 46(2):145-153
- CONCLUSIONS: The model system of preformulation studies showed the usefulness of HPMC and Kollidon K30 in the technology of hydrophilic matrices with ketoprofen.
- Ketoprofen-loaded Eudragit electrospun nanofibers for the treatment of oral mucositis. [Journal Article]
- IJInt J Nanomedicine 2017; 12:2335-2351
- CONCLUSIONS: Eudragit L100 nanofibers (EL-NF) loaded with KET (F1) suppressed the inflammatory response associated with mucositis, which confirmed the efficacy of local buccal delivery of KET-loaded EL-NF in treating oral mucositis.
- Implementing ecopharmacovigilance (EPV) from a pharmacy perspective: A focus on non-steroidal anti-inflammatory drugs. [Review]
- STSci Total Environ 2017 Apr 05
- Environmental experts have made great efforts to control pharmaceutical pollution. However, the control of emerged environmental problems caused by medicines should draw more attention of pharmacy an...
Environmental experts have made great efforts to control pharmaceutical pollution. However, the control of emerged environmental problems caused by medicines should draw more attention of pharmacy and pharmacovigilance researchers. Ecopharmacovigilance (EPV) as a kind of pharmacovigilance for the environment is recognized worldwide as crucial to minimize the environmental risk of pharmaceutical pollutants. But continuing to treat the pollution of pharmaceuticals as a group of substances instead of targeting individual pharmaceuticals on a prioritized basis will lead to a significant waste of resources. Considering vulture population decline caused by non-steroidal anti-inflammatory drugs (NSAIDs) residues, we presented a global-scale analysis of 139 reports of NSAIDs occurrence across 29 countries, in order to provide a specific context for implementing EPV. We found a heavy regional bias toward research in Europe, Asia and America. The top 5 most frequently studied NSAIDs included ibuprofen, diclofenac, naproxen, acetaminophen and ketoprofen. The profile of NSAIDs was dominated by acetaminophen in wastewater influents and effluents. Ibuprofen was the most abundant NSAID in surface water. Only 9 NSAIDs were reported in groundwater samples. And majority of NSAIDs were detected in solid matrices at below 1μg/g except for ketoprofen, diclofenac and ibuprofen. From a pharmacy perspective, we get some implication and propose some management practice options for EPV implementation. These include: Further popularizing and applying the concept of EPV, together with developing relevant regulatory guidance, is necessary; More attention should be paid to how to implement EPV for the pollution control of older established drugs; Triggering "a dynamic watch-list mechanism" in conjunction with "source control"; Implementing targeted sewage treatment technologies and strengthening multidisciplinary collaboration; Pharmaceutical levels in aquatic organisms as biological indicators for monitoring pharmaceutical pollution within the water environment; Upgrading drinking water treatment plants with the aim of removing pharmaceutical residues; Paying more attention to EPV for pharmaceuticals in solid matrices.
- Removal characteristics of pharmaceuticals and personal care products: Comparison between membrane bioreactor and various biological treatment processes. [Journal Article]
- CChemosphere 2017; 179:347-358
- We investigated the concentrations of 57 target compounds in the different treatment units of various biological treatment processes in South Korea, including modified biological nutrient removal (BN...
We investigated the concentrations of 57 target compounds in the different treatment units of various biological treatment processes in South Korea, including modified biological nutrient removal (BNR), anaerobic-anoxic-aerobic (A2O), and membrane bioreactor (MBR) systems, to elucidate the occurrence and removal fates of PPCPs in WWTPs. Biological treatment processes appeared to be most effective in eliminating most PPCPs, whereas some PPCPs were additionally removed by post-treatment. With the exception of the MBR process, the A2O system was effective for PPCPs removal. As a result, removal mechanisms were evaluated by calculating the mass balances in A2O and a lab-scale MBR process. The comparative study demonstrated that biodegradation was largely responsible for the improved removal performance found in lab-scale MBR (e.g., in removing bezafibrate, ketoprofen, and atenolol). Triclocarban, ciprofloxacin, levofloxacin and tetracycline were adsorbed in large amounts to MBR sludge. Increased biodegradability was also observed in lab-scale MBR, despite the highly adsorbable characteristics. The enhanced biodegradation potential seen in the MBR process thus likely plays a key role in eliminating highly adsorbable compounds as well as non-degradable or persistent PPCPs in other biological treatment processes.
- Biochemical, Histopathologic, Physiologic, and Behavioral Effects of Nonsteroidal Antiinflammatory Drugs in Rainbow Trout (Oncorhynchus mykiss). [Journal Article]
- CMComp Med 2017 Mar 01; 67(2):106-111
- Because the number of fish being used in research is increasing rapidly, evaluating the analgesic and pathologic effects of NSAID in fish is essential. To determine the biochemical, histopathologic, ...
Because the number of fish being used in research is increasing rapidly, evaluating the analgesic and pathologic effects of NSAID in fish is essential. To determine the biochemical, histopathologic, physiologic and behavioral effects of 3 NSAID, 48 rainbow trout underwent anesthesia with tricaine methanesulfonate and exploratory celiotomy and were randomly assigned to receive flunixin (0.5 mg/kg IM), ketorolac (0.5 mg/kg IM), ketoprofen (2 mg/kg IM), or saline. Clinical pathologic variables were assessed 1 wk before surgery and 48 h after surgery. Histopathology was performed to evaluate the healing of the incision, tissue reaction at the injection site, and potential organ toxicity. Physiologic and behavioral parameters, including weight, feeding, opercular rate, and vertical position in the water, were measured to establish parameters for identifying pain in fish. The difference between the pre- and postoperative phosphorus concentrations was greater in the flunixin group than the saline group and was the only pathologic difference between treatment groups. Histopathology of incision site, injection site, and internal organs appeared normal, and healing did not appear to be inhibited by the drugs used. The physiologic parameters of opercular rate and weight were consistent and may be helpful in identifying pain in fish in future studies, whereas feeding and vertical position in the water were unhelpful as indicators of pain in this rainbow trout surgical model. Overall, according to clinical pathology and histopathology, the use of ketoprofen, ketorolac, and flunixin at the dosages used in this study lack negative effects in rainbow trout undergoing surgery.
- Ketoprofen Microemulsion for Improved Skin Delivery and In Vivo Anti-inflammatory Effect. [Journal Article]
- APAAPS PharmSciTech 2017 Apr 03
- We have designed a microemulsion (ME) containing Ketoprofen (KET) for anti-inflammatory effect evaluated using the rat paw edema model. The ME was prepared by adding propylene glycol (PG) loaded with...
We have designed a microemulsion (ME) containing Ketoprofen (KET) for anti-inflammatory effect evaluated using the rat paw edema model. The ME was prepared by adding propylene glycol (PG) loaded with 1% KET/water (3:1, w/w), to a mixture of sorbitan monooleate and polysorbate 80 (47.0%) at 3:1 (w/w) and canola oil (38.0%). The physicochemical characterization of KET-loaded ME involved particle size and zeta potential determination, entrapment efficiency, calorimetric analysis, and in vitro drug release. The in vivo anti-inflammatory study employed male Wistar rats. Measurement of the foot volume was performed using a caliper immediately before and 2, 4, and 6 h after injection of Aerosil. KET-loaded ME showed particle size around 20 nm, with zeta potential at -16 mV and entrapment efficiency at 70%. Moreover, KET was converted to the amorphous state when loaded in the formulation and it was shown that the drug was slowly released from the ME. Finally, the in vivo biological activity was similar to that of the commercial gel, but ME better controlled edema at 4 h. These results demonstrated that the ME formulation is an alternative strategy for improving KET skin permeation for anti-inflammatory effect. Furthermore, our findings are promising considering that the developed ME was loaded with only 1% KET, and the formulation was able to keep a similar release profile and in vivo effect compared to the commercial gel with 2.5% KET. Therefore, the KET-loaded developed herein ME is likely to have a decreased side effect compared with that of the commercial gel, but both presented the same efficacy.
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- PROPOFOL AS AN IMMERSION ANESTHETIC AND IN A MINIMUM ANESTHETIC CONCENTRATION (MAC) REDUCTION MODEL IN GOLDFISH (CARASSIUS AURATUS). [Journal Article]
- JZJ Zoo Wildl Med 2017; 48(1):48-54
- Propofol is a novel immersion anesthetic in goldfish ( Carassius auratus ). Objectives were to characterize propofol as an anesthetic and assess its suitability in a minimum anesthetic concentration ...
Propofol is a novel immersion anesthetic in goldfish ( Carassius auratus ). Objectives were to characterize propofol as an anesthetic and assess its suitability in a minimum anesthetic concentration (MAC) reduction model. Using a crossover design, eight goldfish were submerged in 1, 5, or 10 mg/L propofol. Data included induction time, recovery time, heart rate, opercular rate, and response to supramaximal stimulation. Baseline MAC (Dixon's up-and-down method) was determined, and 15 fish were anesthetized with propofol on 4 consecutive days with MAC determination on the fifth day, weekly, for 1 mo. Using a crossover design, MAC of propofol (n = 15) was determined 1 hr following administration of i.m. butorphanol 0.05, 0.5, and 1 mg/kg, dexmedetomidine 0.01, 0.02, and 0.04 mg/kg, ketoprofen 0.5, 1, and 2 mg/kg, morphine 5, 10, and 15 mg/kg, or saline 1 ml/kg. Comparisons were performed with Wilcoxon signed-rank tests (P < 0.05) and Tango's score confidence interval. Propofol at 1 mg/L did not produce anesthesia. Induction time with 10 mg/L (112, 84-166 s) was faster than 5 mg/L (233, 150-289 s; P = 0.0078). Heart and opercular rates for 5 and 10 mg/L were 36 (24-72) beats/min, 58 (44-68) operculations/min and 39 (20-48) beats/min, 57 (48-80) operculations/min, respectively. Recovery time was 249 (143-396) s and 299 (117-886) s with 5 and 10 mg/L, respectively. Response to supramaximal stimulation was not significantly different with 5 mg/L (1/8) compared with 10 mg/L (0/8). Baseline and weekly MAC following daily exposure was 8.4 and 9.0, 8.1, 8.1, and 8.7 mg/L, respectively. MAC reduction was no more than 8% following any drug or dosage. Propofol at 5 and 10 mg/L produced anesthesia, and anesthetic needs were similar following repeated exposure. Propofol was not suitable to test MAC reduction in goldfish in this study.