Comparative Fasting Bioavailability and Pharmacokinetic Properties of 2 Formulations of Glucosamine Hydrochloride in Healthy Chinese Adult Male Volunteers

Abstract

Glucosamine (CAS 66-84-2) hydrochloride is an amino monosaccharide indicated for the treatment of arthrosis, especially osteoarthritis of the knee joint. This study was conducted to assess and compare the pharmacokinetic (PK) properties, bioavailability of a newly developed dispersible tablet formulation (test) of glucosamine hydrochloride with those of an established branded capsule formulation (reference) in healthy Chinese adult male volunteers.

This single-dose, randomized, open-label, 2-period crossover study was conducted in 18 healthy Chinese adult male volunteers under fasting condition. Plasma samples were collected at pre-specified times over a 12-h period following administration in each period and analyzed the plasma glucosamine concentrations by Liquid Chromatography coupled with Tandem Mass Spectrometry (LC/MS/MS) method. The mean (SD) PK parameters of C_max, T_max, AUC_0–12, and AUC_0–∞ after administration of the test and reference formulations were, respectively, as follows: C_max, 907.01 (444.22) vs. 944.40 (429.89) ng/mL, T_max, 3.03 (0.95) vs. 3.30 (0.99) hours, AUC_0–12, 2891.41 (1352.30) vs. 2889.69 (925.48) ng/mL/h, and AUC_0–∞, 3029.90 (1321.36) vs. 3091.87 (870.36) ng/mL/h. The mean (SD) t_1/2 was 1.10 (0.52) hours for the test formulation and 1.50 (1.17) hours for the reference formulation. On ANOVA, neither period nor sequence effects were observed for any PK properties. The relative bioavailability of the test formulation was 98.3% assessed by AUC_0-12. The 90% CIs of glucosamine for the log-transformed ratios of C_max, AUC_0–12, and AUC_0–∞ were 78.4–113.9%, 80.8–108.5% and 80.8–105.8%, respectively, meeting the predetermined criteria for bioequivalence of SFDA.

Key words

glucosamine hydrochloride - bioequivalence - pharmacokinetics - LC/MS/MS

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