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Simultaneous determination of antihistamine anti-allergic drugs, cetirizine, domperidone, chlorphenamine maleate, loratadine, meclizine and buclizine in pharmaceutical formulations, human serum and pharmacokinetics application
Abstract and Figures
This article describes a new, accurate and highly specific high performance liquid chromatographic method with UV detection (HPLC-UV) for the simultaneous determination of cetirizine HCl (CZ), chlorpheniramine maleate (CPM), loratadine (LTD), domperidone (DP), buclizine (BZ) and meclizine (MZ) in pharmaceutical dosage form and human serum, involving pyridoxine (PYD) as the internal standard. The mobile phase consists of heptane sulphonic acid salt buffer and acetonitrile, drawn at a flow rate of 1.0 mL min�1 using
a symmetry C18 column with UV detection at 230 nm. The intraday and inter-day precision
measurements showed coefficients of variation always less than one. The calibration curve was tested in the range of 10–2150 ng mL�1 and the correlation coefficient of >0.9990 in all cases was obtained. The averages of the absolute and relative recoveries were found to be in the range of 98 to 102%. Up to six antihistamines were separated in the same chromatogram with good resolution. The proposed HPLC method has reasonable applications in pharmaceutical tablet dosage form and pharmacokinetics studies.
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... Similarly, the number of HPLC methods has been reported for the determination of cetirizine in the presence of several other drugs as pseudoephedrine [16], chloroquine and pyrimethamine [17], hydroxyzine [18], H 2 receptor antagonists [19], statins [20], with different antihistamine [21], calcium-channel blockers [22], and NSAIDs [23]. However, no method for the simultaneous determination of cetirizine in the presence of quinolones was reported. ...
... Due to the possible co-administration of these drugs, there is a need to develop an analytical method which is robust and less time consuming. Many methods already reported for estimations of cetirizine with many other drugs [16][17][18][19][20][21][22][23] and no method has been reported so far with any quinolones. The present work is validated according to ICH guidelines [24]. ...
Background
Present work describes a fast, simple, and sensitive procedure for the simultaneous determination of cetirizine in the presence of quinolones using diclofenac sodium as an internal standard. The present work was designed to analyze these compounds in pharmaceutical and clinical labs being economical for use.
Results
The mobile phase consisted of the simple composition of methanol, acetonitrile, and water in a ratio of 50:20:30 with a pH adjusted to 3.1 at a flow rate of 1 mL min ⁻¹ . The UV detection was performed at 225 nm. The linearity was assessed over the range of 2.5–50 μg mL ⁻¹ for all drugs. The parameters such as accuracy, precision, linearity (>0.999), and sensitivity were satisfactory.
Conclusion
The method was equally applicable for formulation and human serum with recovery values between 95 and 105%. The results of the method were validated statistically according to ICH guidelines.
... Next, plasma was frozen at − 20 °C until analysis. By employing the reported high-performance liquid chromatography (HPLC) with slight modifications, the plasma concentration of MCZ was assayed [28]. ...
... The flow rate of the isocratic elution was 1 mL/min. The samples were measured at 230 nm, and the injection volume was 50 μL [28]. ...
Meclizine hydrochloride (MCZ), a first-generation antihistamine of the piperazine class, is antiemetic and intended for the management of nausea and vomiting with few adverse effects. The introduction of orodispersible tablet (ODT) would solve the problems encountered in the administration of this drug to pediatric, geriatric, and psychiatric patients. It would be even more advantageous if the MCZ tablet could provoke rapid and prolonged efficacy. Achieving concomitant rapid and prolonged drug therapeutic effects in orodissolvable/dispersible dosage forms would be challenging. In this respect, the authors prepared tablets with coats and cores for immediate and prolonged drug absorption. To achieve this goal, nanoparticles of MCZ from chitosan (CS) and shellac (SH) were prepared by ionic crosslinking and then directly compressed with excipients to form the core in a coated tablet. The immediate release coat with MCZ with the same excipients as in the core was amenable by direct compression. MCZ in the coat dissolved in the presence of a superdisintegrant, leading to rapid absorption from the buccal cavity. Meanwhile, enteric-coated nanoparticles were swallowed and dissolved in the GIT. Intuitively, the absorption process was prolonged. The in vitro release characteristics of all the tablets were studied in comparison with a commercial tablet (CT). Additionally, evaluation of the in vivo pharmacokinetic profile of both the prepared and commercial tablets was performed in humans. The dual function tablet disintegrated in 58 s at pH 5.5. In vivo, noncompartmental pharmacokinetic analysis showed concomitant rapid absorption, possibly from the coat, followed by prolonged absorption from the core. Successfully, these good results confirm that combined rapid and prolonged MCZ therapy with the prepared dual function orodissolvable/dispersible tablet could be a promising oral drug delivery system to enhance convenience for patients. Hopefully, dual function tablets will confer a benefit through the accommodation of more than a single medication in the case of multiple therapies.
... Pyridoxine's anti-oxidative and anti-inflammatory capabilities may have a therapeutic effect in reducing the intensity of COVID-19 and its effects [8]. MZH has been determined with PYH using a variety of analytical methods, including spectrophotometry [9][10][11][12][13][14][15], HPLC [14,[16][17][18][19][20], and UV and/or chemometric approaches [9], according to inquiry of the literature. ...
Pharmaceutical quality control products (QC) demand quick, sensitive, and cost-effective methods to ensure high production at a low cost. Green analytical methods are also becoming more common in pharmaceutical research to cut down on the amount of waste that goes into the environment. Meclizine hydrochloride (MZH) and pyridoxine hydrochloride (PYH) are reported to be excellent for calming down COVID-19. As a result, the amount of MZH and PYH manufactured by multinational pharmaceutical organizations has increased considerably during the last several months. The present work proposes three environmentally friendly, straightforward, and sensitive spectrophotometric procedures for quantification of MZH in the presence of PYH in a pure and marketable formulations. The approaches under examination include ratio subtraction (RSM), induced dual wavelength (IDW), and Fourier self-deconvolution (FSD). PYH, on the other hand, was directly quantified at 290 nm. For both drugs, the procedures follow Beer’s law in the range of (5–50 µg/mL). The RSM, IDW, and FSD methods, as well as the zero-order approach for PYH, have all been verified in accordance with ICH standards. The ecological value of established methodologies was determined using four distinct ways: the national environmental methods index (NEMI), the analytical Eco-scale, the Analytical Greenness Metric (AGREE), and the green analytical process index (GAPI). Comparing the findings to those of the previously described spectrophotometric technique, no major changes were identified.
... To the best of our knowledge, PYR was determined with either MEC or CYC using different analytical methods, such as spectrophotometry (Arayne, Sultana, Siddiqui, Zuberi, & Mirza, 2007;El-Gindy, 2003;El-Gindy, Emara, & Mostafa, 2004;Habib, Abdelwhab, Abdelrahman, & Ali, 2016;Sharma, Sharma, Saxena, & Talwar, 1989;Shinde, Sayyed, Chaudhari, Chaware, & Biyani, 2016), HPLC (Al-Jallad, Al-Kurdi, Badwan, & Jaber, 1999; Arayne, Sultana, & Siddiqui, 2008;El-Gindy, Emara, & Mostafa, 2004;Li & Lu, 2005;Mao & Carr, 2001;Nawaz, 2013;Sher et al., 2014), and chemometric/UV methods (El-Gindy, 2003;El-Gindy, Emara, & Mostafa, 2004). Moreover, MEC was determined using LC stability-indicating assay method (LC-SIAM) in tablets (Peraman, Manikala, Kondreddy, & Yiragamreddy, 2015). ...
Cyclizine hydrochloride (CYC) and Meclozine hydrochloride (MEC) are antihistaminic drugs generally co‐formulated with Pyridoxine hydrochloride (PYR) to treat nausea and vomiting in pregnancy. Several analytical techniques were applied for determination of CYC or MEC with PYR but no one paid attention to determination of CYC impurity; Benzhydrol (BEH) or MEC impurity; 4‐Chlorobenzophenone (BEP). Therefore, micellar Ultra performance liquid chromatographic (UPLC) method is introduced for analysis of ternary mixtures containing PYR together with both CYC and BEH (mixture I) or MEC and BEP (mixture II). Chromatographic separation was achieved using Hypersil gold C8 column (50 mm x 2.1 mm, 1.9 μm) using 0.01M sodium dodecyl sulphate modified to pH 3.5 using phosphoric acid: acetonitrile (45:55 by volume) for mixture I and (0.1 % sodium dodecyl sulphate, 0.1% sodium bicarbonate adjusted to pH 2.6 by phosphoric acid): acetonitrile (47: 53 by volume) for mixture II as mobile phases. The separated peaks were detected at 230 nm and 245 nm for mixture I and II, respectively. The adopted methods were validated in consent to the International conference on harmonization (ICH) recommendations and were properly applied in commercial pharmaceutical formulations analysis. Comprehensive ecological comparison was achieved confirming higher ecological value of the presented methods compared to the reported methods.
... Literature survey reveals that buclizine can be assayed by UV spectrophotometric [3][4][5] , HPLC [6][7][8][9][10] methods individually or in combination with other drugs. In Spectrophotometric and chromatographic methods the procedure adopted for the estimation of buclizine hydrochloride was tedious, time consuming and quantity estimated in microgram level. ...
... Similarly, interaction with NSAIDs (18) and gliquidone (19) has also been reported using HPLC-UV methods. Many other RP HPLC methods have been reported in which cetirizine or levocetirizine dihydrochloride was determined in the presence of pioglitazone (20), with statins (21), calcium channel blockers (22) and with other antihistamine anti-allergic drugs (23). ...
A simple, accurate and precise RP-HPLC method was developed for the simultaneous determination of chloroquine, pyrimethamine and cetirizine hydrochloride concentrations in bulk drug and human serum. The assay was performed using a mobile phase of methanol: water (70:30) at pH of 2.8 ± 0.05 on the Purospher C-18 column with UV detection at 230 nm and rosuvastatin used as an internal standard. The retention times observed for chloroquine, pyrimethamine and cetirizine hydrochloride were 3.5, 2.5 and 5.5 minutes, respectively. The method was found to be specific for the assayed drugs showing a linear response in the concentration range of 1–100 μg mL−1 with coefficients of determination values of (r = 0.999). The method was developed and validated according to ICH guidelines. The method was used to monitor the serum samples and was found to be sensitive for therapeutic purposes, showing the potential to be a useful tool for routine analysis in laboratories.
... In this study, experiments have been made by changing the mobile phase composition, pH and flow rate, and the optimum separation condition has been found. As a further example, Sher and co-workers [37] were reported that simultaneous separation of MCZ and BCZ was carried out in C18 column at 25 o C. In the mobile phase, ACN was used as an organic modifier and heptane sulfonic acid was used as an ion pair former. No optimization study has been found in this study. ...
Herein, for the first time, the wasted cockle shells were modified with nitrogen and sulfur-doped carbon dots after carbonization and used as a suitable bio-based sorbent for the extraction of two important antiemetic drugs named ondansetron and domperidone. The extraction and separation were performed based on vortex-assisted dispersive solid-phase microextraction and high-performance liquid chromatography, respectively. Various techniques such as Fourier-transform infrared, fluorescence, field emission scanning electron microscopy, thermogravimetric analysis, nitrogen adsorption-desorption analysis, X-ray powder diffraction, and energy-dispersive spectroscopy were used to characterize the chemical composition of prepared sorbent. After examining the factors affecting the extraction efficiency and access to the optimal points using the response surface methodology, the linearity was in the range of 5-350 μg/L with acceptable coefficients of determination (R2 > 0.993). The limits of detection and quantification were in the range of 1.5-2.3 and 4.9-7.1 μg/L, respectively. In the end, the proposed method was applied for the quantitative determination of trace levels of target analytes from pharmaceutical tablets, serum, and urine samples. The recoveries were more than 95.2%, indicating the proposed method's excellent accuracy.
Background:
Noising is an undesirable phenomenon accompanying with development of the widely-used chemometric models such as partial least square regression (PLSR) and support vector regression (SVR).
Objective:
Optimizations of these chemometric models by applying Orthogonal projection to latent structures (OPLS) as a preprocessing step which characterized by cancelling noise is the purpose of the presented research study. Additionally a comprehensive comparative study between the developed methods was achieved highlighting pros and cons.
Methods:
OPLS conducted with PLSR and SVR for quantitative determination of Pyridoxine HCl (PYR), Cyclizine HCl (CYC), and Meclizine HCl (MEC) in presence of their related impurities. Training set was formed from twenty-five mixtures, as there are five mixtures for each compound at each concentration level. Additionally, to check the validity and predictive ability of the developed chemometric models, the independent test set mixtures were prepared by repeating the preparation of four mixtures of the training set plus preparation of another four independent mixtures.
Results:
Upon application of OPLS processing method, upswing of predictive abilities of PLSR and SVR was found. The root mean square error of prediction (RMSEP) of the test set was the basic benchmark for comparison.
Conclusion:
The major finding that was concluded from the conducted research is that processing with OPLS reinforces the ability of models to anticipate the future samples.
Highlights:
Novel optimizations of the widely-used chemometric models; application of comparative study between the suggested methods; application of OPLS pre-processing methods; quantitative determination of pyridoxine HCl, cyclizine HCl and meclizine HCl; checking the predictive power of developed chemometric models; analysis of the active ingredients in their pharmaceutical dosage forms.
A simple and sensitive flow injection‐chemiluminescence (FI‐CL) method has been developed for the determination of cetirizine dihydrochloride (CTZH) in pharmaceuticals. The method is primarily based at the enhancement effect of CTZH on tris(2,2′‐bipyridyl) ruthenium (II)‐diperiodatoargentate (III) ([Ru (bpy)3]2+‐Ag (III) complex) CL system in an acidic medium. The optimal investigated variables of the CL reaction were: [Ru (bpy)3]2+, 50×10–6 mol/L; sulfuric acid, 1.0×10–3 mol/L; Ag (III) complex, 100×10–6 mol/L; potassium hydroxide, 1.0×10–3 mol/L; flow rate, 3.0 mL/min and sample loop volume, 300 μL. The detection and quantification limits were of 2.0×10–4 and 5.0×10–4 mg/L (S/N of 3 and 10) respectively with a linear calibration range of 5.0×10–4 – 7.5 mg/L (R2 = 0.9999, n = 11), injection throughput of 110/h and the relative standard deviations (RSDs) of 1.5 – 3.5% over the range studied. The methodology was successfully applied to determine CTZH in different pharmaceutical samples and validated with a HPLC method and resulted in the recovery of 94.6 to 108.6%. The probable CL reaction mechanism is described in brief.
The experiment involves quality analysis of ten (10) samples of chlorpheniramine tablets using ultra violet spectrophotometer in the range of (200 - 400nm) in which the samples were dissolved in NaOH and their various absorbance and wavelength determined and compared with that of the standard, wavelength of the maximum absorbance at 223nm was determined so as to note if it was within the acceptable range of (90 - 110%) for those that passed the test or if it was below or above the range for samples that are substandard or highly concentrated. The amount of chlorpheniramine base in each sample was determined and compared with the actual content (4mg). It was observed that only seven (7) samples Banbiz, Bond, Dana, Emzor, Evans, Juhel and vitabiotics, met the british pharmaceutical codex range of 90 - 110% while the other three (3) samples Nasdmu, New devine and Sam, failed the test with values below the acceptable range.
Motion sickness is a self-limiting but uncomfortable phenomenon experienced by many people. It is common during civilian travel and also among professionals during travel or military manoeuvres. Meclizine is a piperzine antihistamine that is effective for the prevention and treatment of motion sickness, particularly during mild civilian travel. It is well tolerated with few adverse effects and its oral dosage form is convenient for patients to take prior to exposure to motion as a preventative measure. © the author(s), publisher and licensee Libertas Academica Ltd.
This is a summary report of the conference on “Analytical Methods Validation: Bioavailability, Bioequivalence and Pharmacokinetic Studies.” The conference was held from December 3 to 5, 1990, in the Washington, D.C., area and was sponsored by the American Association of Pharmaceutical Scientists, the U.S. Food and Drug Administration, Federation International Pharmaceutique, Health Protection Branch (Canada), and the Association of Official Analytical Chemists. The report presents our assessment of the major agreements and issues discussed at the conference. The report is also intended to provide guiding principles for validation of analytical methods used in bioavailability, bioequivaience, and pharmacokinetics studies in humans and animais. The objectives of the conference were as follows: (1) to reach a consensus on what should be required in analytical methods validation and the procedures to establish validation; (2) to determine processes of application of the validation procedures in bioavailability, bioequivalence, and pharmacokinetics studies; and (3) to develop a report on analytical methods validation that may be referred to in developing future formal guidelines. Acceptable standards for documenting and validating analytical methods with regard to processes, eters, or data treatments are discussed because of their importance in assessing pharmacokinetic, bioavailability, and bioequivalence studies. Other topics that were considered essential in the conduct of pharmacokinetic studies or in establishing bioequivalency criteria, including measurement of drug metabolites and stereoselective determinations, are also discussed.
The selectivity of the separation of five antihistamines has been investigated by TLC on silica gel 60 F254 and on aluminium oxide 60 F254 with a variety of mobile phases in horizontal chambers. The best separation selectivity and retention differences for the drugs on the two types of plate were obtained with the mobile phases chloroform-ethyl acetate, 1 + 1 (v/v), ethyl acetate, and butan-2-one-toluene, 7 + 3 (v/v). The plates were visualized by illumination at λ=254 nm and by reaction with different reagents. The greatest detection sensitivity -0.06 μg for cetirizine, 0.1 μg for chloropyramine, and 0.2 μg for antazoline, doxylamine, and ketotifene - was obtained by spraying with potassium iodoplatinate reagent.
A method for the quantitative determination of clemastine in human plasma has been developed and validated. The assay uses gas chromatography with nitrogen–phosphorus detection and a HP-1 capillary column (25 m×0.22 mm, film thickness 0.33 mm) coated with dimethylpolysiloxane. Clemastine (with orphenadrine as internal standard) was isolated from human plasma using liquid–liquid extraction. A linear relationship was observed between 0.1 and 12.8 ng/ml using the peak area ratio of clemastine to orphenadrine with a correlation coefficient greater than 0.99 (the detection limit for clemastine was 0.06 ng/ml). The intra- and inter-day coefficients of variation were less than 11%. The developed method was used for the analysis of plasma samples from healthy volunteers (n=19) to examine the pharmacokinetics of the antihistamine clemastine after single and multiple oral doses of clemastine fumarate.
Enantiomers of several different antihistamines were shown to undergo enantiomer enrichment (auto-resolution) under achiral conditions. Using an aminopropyl silica gel column with a hexane–isopropanol mobile phase, non-racemic mixtures yielded resolutions of very high optical purity. It has been demonstrated that auto-resolution of antihistamines is concentration-dependent, as very dilute samples are not resolved. The benzylic hydrogen on the chiral carbon appears to play a major role in the chiral recognition process.
Based on the oxidation reactions of u.v. radiation/hydrogen peroxide/oxygen with either phenol or salicylic acid a spectra library was established. The reaction products contain hydroxylated phenols, benzoquinone and aliphatic acids with up to six carbon atoms. Many of the substances have been identified by means of chromatography and spectra comparison. From the observed concentrations of the substances and the known reaction mechanisms the following course of reaction has been postulated. The first reaction step is the hydroxylation of the aromatic ring. Further oxidation occurs via abstraction of a hydrogen atom to form 1,2-benzoquinone which is cleaved to form muconic acid. The cleavage of the muconic acid by u.v. radiation/hydrogen peroxide/oxygen leads to maleic acid, fumaric acid and oxalic acid. The degradation of oxalic acid leads to formic acid and finally to carbon dioxide. The hydroxylation of the double bond of the maleic or fumaric acid and the abstraction of a hydrogen atom produces malic acid. The reactions can be seen as essential step in the photochemical transformation of refractory substances into biodegradable ones.