Light degradation of ketorolac tromethamine

Gu, Liangcai; Hi-Shi, Chiang; Johnson, David M.

doi:10.1016/0378-5173(88)90142-1

Cited by 29 publications

(4 citation statements)

References 11 publications

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“…Results suggest that no significant level of phototoxicity is achieved by ketorolac. In the presence of light, triplet excited state of ketorolac is observed, which is followed by oxidation (24). This single mechanism could be accounted for the observed very slight level of toxicity by ketorolac in our investigation.…”

Section: Al Phototoxicity Of Drugs For Ocular Usesupporting

confidence: 53%

Photochemical toxicity of drugs intended for ocular use

Sahu

Singh

Saraf

et al. 2014

Archives of Industrial Hygiene and Toxicology

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The present investigation was undertaken to evaluate the possible ocular phototoxicity of drugs used in ophthalmic formulations. Sulphacetamide, ketoconazole, voriconazole, diclofenac, and ketorolac were assessed in the concentrations available in the market for their ocular use. The suitable models viz Hen's Egg Test Chorioallantoic Membrane (HET-CAM) test, Isolated Chicken Eye (ICE) test, and Red Blood Cell (RBC) haemolysis test as recommended by ECVAM, ICCVAM, and OECD guidelines were performed. Results of HET-CAM and ICE tests suggest that sulphacetamide is moderately toxic in the presence of light/UV-A and very slightly irritant without irradiation. Ketoconazole and voriconazole were found slightly irritant in presence of light/UV-A and non-irritant in dark. Diclofenac and ketorolac demonstrated slight irritancy in the light and were found to be non-irritant in dark. The results suggest that some of the drugs have potential toxic effect in the presence of light. The extent of phototoxicity might get extended when used for longer time. The recommendation is that these drugs should be stored and used in the dark for a specified time and be labelled with specific instructions for patients, especially for those working longer in the sunlight.

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Section: Al Phototoxicity Of Drugs For Ocular Usesupporting

confidence: 53%

Photochemical toxicity of drugs intended for ocular use

Sahu

Singh

Saraf

et al. 2014

Archives of Industrial Hygiene and Toxicology

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“…In the case of ketorolac, studies have reported decomposition by decarboxylation, followed by autoxidation and pH-dependent kinetics [ 18 ]. It has also been determined that ketorolac rapidly decomposes in aqueous solutions and ethanol under UV light owing to the production of four types of products and CO 2 [ 19 ]. Given the characteristics of ketorolac, the decomposition of this ligand could reduce the antibacterial effect of silver compounds in the context of a pH from 4 to 5 and an extended period of exposure to sunlight.…”

Section: Resultsmentioning

confidence: 99%

Stability of Antibacterial Silver Carboxylate Complexes against Staphylococcus epidermidis and Their Cytotoxic Effects

et al. 2018

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The antibacterial effects against Staphylococcus epidermidis of five silver carboxylate complexes with anti-inflammatory ligands were studied in order to analyze and compare them in terms of stability (in solution and after exposure to UV light), and their antibacterial and morphological differences. Four effects of the Ag-complexes were evidenced by transmission electronic microscopy (TEM) and scanning electronic microscopy (SEM): DNA condensation, membrane disruption, shedding of cytoplasmic material and silver compound microcrystal penetration of bacteria. 5-Chlorosalicylic acid (5Cl) and sodium 4-aminosalicylate (4A) were the most effective ligands for synthesizing silver complexes with high levels of antibacterial activity. However, Ag-5Cl was the most stable against exposure UV light (365 nm). Cytotoxic effects were tested against two kinds of eukaryotic cells: murine fibroblast cells (T10 1/2) and human epithelial ovarian cancer cells (A2780). The main objective was to identify changes in their antibacterial properties associated with potential decomposition and the implications for clinical applications.

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“…In pharmaceutical industry, force degradation study has its importance before starting a new formulation, which provides an insight into degradation pathways and impurity of the drug substance also helps in elucidation of the structure of the degraded products. The degradation products of KTR have been identified from the stress degradation study under hydrolysis (acid, base, and neutral), oxidation, photolysis, thermal conditions [13][14][15]. Few computational studies of KTR and its modified derivatives also were reported previously [16,17].…”

Section: Introductionmentioning

confidence: 99%

Optimization of structures, biochemical properties of ketorolac and its degradation products based on computational studies

Uzzaman

Uddin

2019

DARU J Pharm Sci

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Background Ketorolac (KTR) is used as an analgesic drug with an efficacy close to that of the opioid family. It is mainly used for the short term treatment of post-operative pain. It can inhibit the prostaglandin synthesis by blocking cyclooxygenase (COX). Methods In this investigation, the inherent stability and biochemical interaction of Ketorolac (KTR) and its degradation products have been studiedon the basis of quantum mechanical approaches. Density functional theory (DFT) with B3LYP/ 6-31G (d) has been employed to optimize the structures. Thermodynamic properties, frontier molecular orbital features, dipole moment, electrostatic potential, equilibrium geometry, vibrational frequencies and atomic partial charges of these optimized structureswere investigated. Molecular docking has been performed against prostaglandin H2 (PGH2) synthase protein 5F19 to search the binding affinity and mode(s). ADMET prediction has performed to evaluate the absorption, metabolism and carcinogenic properties.Results The equilibrium geometry calculations support the optimized structures. Thermodynamic results disclosed the thermal stability of all structures. From molecular orbital data, all the degradents are chemically more reactive than parent drug (except K3). However, the substitution of carboxymethyl radicalin K4 improved the physicochemical properties and binding affinity. ADMET calculations predict the improved pharmacokinetic and non-carcinogenic properties of all degradents. Conclusion Based on physicochemical, molecular docking, and ADMET calculation, this study can be helpful to understand the biochemical activities of Ketorolac and its degradents and to design a potent analgesic drug.

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Light degradation of ketorolac tromethamine

Cited by 29 publications

References 11 publications

Photochemical toxicity of drugs intended for ocular use

Photochemical toxicity of drugs intended for ocular use

Stability of Antibacterial Silver Carboxylate Complexes against Staphylococcus epidermidis and Their Cytotoxic Effects

Optimization of structures, biochemical properties of ketorolac and its degradation products based on computational studies

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