article · Journal of Chromatographic Science
A high-performance liquid chromatography method has been developed and validated to measure the diabetes drug linagliptin in rat blood plasma, using pindolol as an internal standard. The method separates the compounds on a C18 column at room temperature with ultraviolet detection. Validated in accordance with international regulatory guidelines, the assay demonstrated linearity across a concentration range of 5 to 1,000 nanograms per millilitre, with a quantification limit of 5 nanograms per millilitre using 100 microlitres of plasma. Both intra-day and inter-day precision showed variations under 10 percent, while accuracy ranged from 93.3 to 102.5 percent and extraction recovery exceeded 83 percent. The analytical procedure was subsequently deployed in an animal pharmacokinetic investigation following a single oral dose of 10 milligrams per kilogram, successfully capturing key parameters including peak concentration and overall drug exposure over 72 hours.
Developing reliable and accurate analytical methods to measure drug levels in biological fluids is essential for early-stage pharmaceutical testing. This method enables laboratories to track how the diabetes medication linagliptin is absorbed and cleared in animal models, supporting standard preclinical pharmacokinetic assessments that inform safe dosage and therapeutic evaluation.
This validated assay provides an applied testing tool for contract research organisations and pharmaceutical developers conducting preclinical drug studies. Having been validated to regulatory guidelines and tested in an in vivo rat study, the protocol is ready for direct adoption in laboratory-based animal trials, though it remains restricted to preclinical research rather than human clinical use.
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A sensitive and reproducible HPLC method for the determination of linagliptin (LNG) in rat plasma was developed and validated using pindolol (PIN) as the internal standard. Both LNG and PIN were separated on a Zorbax Eclipse XDB C18 column kept at ambient temperature using as mobile phase a combination of 75% methanol: 25% formic acid 0.1% pH 4.1 at a flow rate of 1.0 mL min-1. UV detection was performed at 254 nm. The method was validated in compliance with ICH guidelines and found to be linear in the range of 5-1,000 ng mL-1. The limit of quantification (LOQ) was found to be 5 ng mL-1 based on 100 µL of plasma. The variations for intra- and inter-assay precision were <10%, and the accuracy values were ranged between 93.3 and 102.5%. The extraction recovery (R%) was >83%. The assay was successfully applied to an in vivo pharmacokinetic study of LNG in rats that were administered a single oral dose of 10 mg kg-1 LNG. The maximum concentration (Cmax) and the area under the plasma concentration-time curve (AUC0-72) were 927.5 ± 23.9 and 18,285.02 ± 605.76 ng mL-1, respectively.
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DOI: 10.1093/chromsci/bmw106
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