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Microanalysis of Selected Nsaids Using the Spectrophotometric Method

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Microanalysis of Selected Nsaids Using the Spectrophotometric Method Article Microanalysis of Selected NSAIDs Using the Spectrophotometric Method Paweł Gumułka, Monika D ˛abrowska* and Małgorzata Starek * Department of Inorganic and Analytical Chemistry, Faculty of Pharmacy, Jagiellonian University Medical College, 9 Medyczna St, 30-688 Kraków, Poland; [email protected] * Correspondence: [email protected] (M.D.); [email protected] (M.S.) Received: 9 October 2020; Accepted: 31 October 2020; Published: 2 November 2020 Abstract: Non-steroidal anti-inflammatory drugs (NSAIDs) are the group of drugs most commonly used in medicine. They are available over the counter to treat fevers and pains of various origins. The clinical and pharmaceutical analysis of these drugs requires effective analytical procedures for drug quality control, pharmacodynamic and pharmacokinetic studies. This article presents the spectrophotometric method that was used to analyze selected drugs from the NSAID group. The conditions for the determination of selected coxibs and oxicams in the UV range with the use of microplates have been developed. The presented procedure has been validated in accordance with the requirements, guaranteeing reliable results. The obtained results give the basis for the conclusion that the method can be successfully used in the quality control of pharmaceutical preparations with a small amount of available sample. Keywords: spectrophotometry; coxibs; oxicams; validation of the method 1. Introduction Non-steroidal anti-inflammatory drugs (NSAIDs) are a group of drugs most commonly used in human and veterinary medicine. Many of them are available over the counter, most often to treat fever and moderate pain. NSAIDs include chemical compounds of various structures and therapeutic applications. However, they share certain characteristics, i.e., identical basic pharmacological properties, similar basic mechanisms of action as well as similar side effects. In addition, all drugs in this group are acidic in nature (pK values in the range 3.0–5.0). NSAID molecules can contain both hydrophilic (carboxyl or enol groups) and lipophilic (e.g., aromatic ring) groups. Due to their acidic nature, they are present in gastric juice in a protonated form. Also in the small intestine, there are favorable conditions for the absorption of weak acids due to the environment prevailing there. NSAIDs may exist in an ionized form in plasma. They are characterized by a very high level of plasma protein binding (>97%) and values of the volume of distribution ranging from 0.1 to 1.0. Most NSAIDs are metabolized in the liver through oxidation and conjugation of inactive metabolites which are excreted in the urine or bile. The metabolism of NSAIDs may be disturbed in some disease states, then accumulation of the drug may occur even at normal doses [1–3]. Disease entities in which NSAIDs are used include pain accompanying infection, metabolic and neoplastic diseases, systemic diseases of connective tissue, degenerative joint diseases, neurovascular disorders and other diseases accompanied by inflammatory and pain symptoms from the skeletal system [4,5]. The mechanism of action of this group of drugs is associated with the inhibition of the transformation of eicosanoids (prostanoids, leukotrienes), which are products of transformation of polyunsaturated fatty acids. The substrate for this synthesis is arachidonic acid, which is released from cell membranes by phospholipase A2. The activity of this enzyme is stimulated by calmodulin, bradykinin, thrombin and calcium, while inhibition is caused by glucocorticosteroids. Eng 2020, 1, 211–221; doi:10.3390/eng1020014 www.mdpi.com/journal/eng Eng 2020, 1, FOR PEER REVIEW 2 phospholipase A2. The activity of this enzyme is stimulated by calmodulin, bradykinin, thrombin and calcium, while inhibition is caused by glucocorticosteroids. The NSAID group also includes oxicams and coxibs (Figure 1), substances whose mechanism of action is to inhibit COX prostaglandin cyclooxygenase. There are two isoenzymes: COX-1 (a cellular enzyme responsible for the synthesis of prostaglandins necessary for physiological processes) and EngCOX-22020, 1(appears in cells where the inflammatory process takes place and determines the formation212 of prostaglandins during this process) [6,7]. Taking the chemical structure into account, oxicams are classified as derivatives of enolic acids. DrugsThe belonging NSAID group to this also family includes include oxicams piroxica andm, coxibs tenoxicam (Figure and1), substances meloxicam—drugs whose mechanism with strong, of actionlong-lasting is to inhibit anti-inflammatory COX prostaglandin and analgesic cyclooxygenase. effects that There are arerelatively two isoenzymes: well tolerated COX-1 [2,3]. (a Oxicams cellular enzymeare quickly responsible absorbed for from the the synthesis gastrointestinal of prostaglandins tract and are necessary over 90% for bound physiological to plasma processes) proteins. They and COX-2are metabolized (appears in mainly cells where to glucuronides the inflammatory and excreted process in takes feces place and and urine. determines The half-life the formation of oxicams, of prostaglandinsranging from 30–40 during h, thisallows process) for once-a-day [6,7]. dosing of the drug. O O S CH3 O O N H3C S O N H N S OH HN N S N O OH CH 3 Tenoxicam (4-hydroxy-2-methyl-1,1-dioxo-N- Meloxicam (4-hydroxy-2-methyl-N-(5-methyl- (pyridin-2-yl)-2H-1λ⁶-thieno [2–e][1,2]thiazine- 1,3-thiazol-2-yl)-1,1-dioxo-2H-1λ⁶,2- 3-carboxamide) benzothiazine-3-carboxamide) Cl F O F N O S CH F 3 N S NH3 N O O N CH3 CH3 Etoricoxib (5-chloro-3-(4- Celecoxib (4-[5-(4-methylphenyl)-3- methanesulfonylphenyl)-2-(6-methylpyridin-3- (trifluoromethyl)-1H-pyrazol-1-yl]benzene-1- yl)pyridine) sulfonamide) FigureFigure 1.1. ChemicalChemical structuresstructures ofof analyzedanalyzed compounds.compounds. TakingDrugs thebelonging chemical to structurethe coxib intogroup account, are selective oxicams for are the classified COX-2 asisoform. derivatives The development of enolic acids. of Drugsdrugs that belonging selectively to this inhibit family the includeinducible piroxicam, cyclooxygenase tenoxicam isoform and allowed meloxicam—drugs for a significant with reduction strong, long-lastingin side effects anti-inflammatory while maintaining and full analgesic anti-inflammat effects thatory areand relatively analgesic well activity. tolerated It has [2 ,been3]. Oxicams shown that are quicklythese drugs absorbed have froman anti-inflammatory the gastrointestinal effect tract comparable and are over to 90%non-selective bound to cyclooxygenase plasma proteins. inhibitors, They are metabolizedand at the same mainly time to they glucuronides are almost and completely excreted devo in fecesid of and adverse urine. effects The half-life on the gastrointestinal of oxicams, ranging tract from[4,8]. 30–40 Studies h, that allows assessed for once-a-day the condition dosing of ofthe the gastric drug. mucosa by using gastroscopy have shown that the useDrugs of coxib belonging is associated to the coxibwith a group much arelower selective incidence for of the ulcer COX-2 complications isoform. The than development other NSAIDs. of drugsAt the that same selectively time, selective inhibit theCOX-2 inducible inhibitors cyclooxygenase are not without isoform side allowed effects. for They a significant are known reduction to slow inulcer side healing effects whileand can maintaining under certain full conditions anti-inflammatory impair kidney and analgesic function. activity. Two generations It has been of shown drugs that can thesebe distinguished drugs have anwithin anti-inflammatory the group of ecoxibs:ffect comparable the 1st generation to non-selective includes cyclooxygenase rofecoxib, celecoxib inhibitors, and andvaldecoxib, at the same while time the 2nd they generation are almost includes completely etoric devoidoxib and of lumiracoxib. adverse effects The on 1st the generation gastrointestinal inhibits tractCOX-2 [4,8 2]. to Studies 35 times that more assessed than the COX-1. condition In turn, of the the gastric second mucosa generation by using inhibits gastroscopy COX-2 that have is shown 106 to that the use of coxib is associated with a much lower incidence of ulcer complications than other NSAIDs. At the same time, selective COX-2 inhibitors are not without side effects. They are known to slow ulcer healing and can under certain conditions impair kidney function. Two generations of drugs can be distinguished within the group of coxibs: the 1st generation includes rofecoxib, celecoxib and valdecoxib, while the 2nd generation includes etoricoxib and lumiracoxib. The 1st generation inhibits COX-2 2 to 35 times more than COX-1. In turn, the second generation inhibits COX-2 that Eng 2020, 1 213 is 106 to 515 times stronger than COX-1. Celecoxib is a drug of the diarylpyrazole group, which is used to relieve symptoms of rheumatoid arthritis and osteoporosis as an analgesic. Administration of celecoxib has also been shown to inhibit the development of colorectal adenomas. Contraindication to use is caused by an allergy to sulfonamides or acetylsalicylic acid, and caution should be exercised in patients with asthma, liver and kidney damage and allergy sufferers. Etoricoxib, belonging to the NSAIDs from the dipyridine derivative group, is used in the symptomatic treatment of osteoarthritis, rheumatoid arthritis, symptoms of joint inflammation, pain treatment and in the acute phase of gout. The widespread use of NSAIDs causes the creation of new, more effective combinations, and at the same time
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