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Original Research

Simultaneous Determination of Loratadine and Its Metabolite Desloratadine in Beagle Plasma by LC-MS/MS and Application for Pharmacokinetics Study of Loratadine Tablets and Omeprazole‑Induced Drug–Drug Interaction

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Pages 5109-5122 | Published online: 22 Dec 2021

Figures & data

Figure 1 MS2 spectra of LTD (A), IS1 (B), DL (C) and IS2 (D).

Figure 1 MS2 spectra of LTD (A), IS1 (B), DL (C) and IS2 (D).

Figure 2 Dissolution profiles of LTD tablets (tablet R, tablet A and tablet B) in different pH media using stirring paddle method with media volume of 500 mL.

Figure 2 Dissolution profiles of LTD tablets (tablet R, tablet A and tablet B) in different pH media using stirring paddle method with media volume of 500 mL.

Table 1 Optimized Mass Spectrum Parameters of LTD, DL, IS1 and IS2 (Positive Ion Mode)

Figure 3 MRM chromatograms of LTD, DL, IS1 and IS2 in beagle dog plasma: (A) blank plasma sample, (B) blank plasma spiked with LTD and DL at LLOQ and the corresponding IS1 and IS2, (C) extracted plasma sample from a beagle after an oral administration of LTD tablet.

Figure 3 MRM chromatograms of LTD, DL, IS1 and IS2 in beagle dog plasma: (A) blank plasma sample, (B) blank plasma spiked with LTD and DL at LLOQ and the corresponding IS1 and IS2, (C) extracted plasma sample from a beagle after an oral administration of LTD tablet.

Table 2 Intra-Day and Inter-Day Precision and Accuracy for the Simultaneous Determination of LTD and DL in Spiked Beagle Plasma (Intra-Day: n = 6; Inter-Day: n = 6 Series per Day, 3 Days)

Table 3 Extraction Recovery and Matrix Effect of QC Samples for the Simultaneous Determination of LTD and DL in Spiked Beagle Plasma

Table 4 Stability Results of LTD and DL in Spiked Beagle Plasma Under Different Storage Conditions (n = 3)

Figure 4 Pharmacokinetic profiles of LTD (A), DL (B) and the sum of the two components (C) after oral administration of 10 mg LTD tablet formulation R, A and B in fasting state in male beagles.

Figure 4 Pharmacokinetic profiles of LTD (A), DL (B) and the sum of the two components (C) after oral administration of 10 mg LTD tablet formulation R, A and B in fasting state in male beagles.

Table 5 Key Pharmacokinetic Parameters of LTD and DL After Oral Administration of 10 Mg LTD Tablet R, A and B in Fasting State to Male Beagles

Table 6 Comparison of Mean LTD and DL Pharmacokinetic Parameters Between Beagles and Humans After Oral LTD or DL Tablets

Table 7 Pharmacokinetic Parameters of LTD and DL in Nine Male Beagle Dogs with the Combination of Three Tablets After Oral Administration of LTD Tablet Alone or LTD Tablet Under Pretreatment of Omeprazole

Figure 5 LTD (A) and DL (B) pharmacokinetic profiles with the combination of three tablets in nine male beagle dogs after oral administration of LTD tablet alone or LTD tablet under pretreatment of omeprazole.

Figure 5 LTD (A) and DL (B) pharmacokinetic profiles with the combination of three tablets in nine male beagle dogs after oral administration of LTD tablet alone or LTD tablet under pretreatment of omeprazole.