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Table 2 Pharmacokinetics parameters for MTX plasma profiles of antigen-induced arthritis after treatment with oral MTX or DK226

From: Novel hyaluronic acid–methotrexate conjugate suppresses joint inflammation in the rat knee: efficacy and safety evaluation in two rat arthritis models

Compound Dose Tmax (h) Cmax (pg/mL) AUCinf (ng · h/mL) t1/2 (h)
MTX 1.25 mg/kg, orala 0.9 ± .0.3 72,600 ± 10,000 365 ± 37 2.78 ± 0.18
DK226 50 μL/body, intra-articularb 20.0 ± 8.0 1900 ± 180 68.4 ± 6.1 11.2 ± 0.4
  1. AIA rats were dosed with oral MTX (five times a week, day −7 to day 14) or intra-articular DK226 (weekly, day −7 to day 14) to produce a comparable suppression of knee joint swelling. Serial blood samples were collected from AIA rats on day 14 at 0 h (immediately before treatment) and at 0.25, 0.5, 1, 2, 4, 8, and 24 h after treatment with oral MTX, and at 4, 8, 24, 48, and 72 h after treatment with DK226. Plasma concentrations of MTX were then determined by LC-MS/MS. PK parameters were calculated by a non-compartmental model
  2. MTX methotrexate, T max time to reach maximum plasma concentration, C max maximum plasma concentration, AUC inf area under the plasma concentration-time curve calculated from time zero to infinity, t 1/2 terminal phase elimination half-life
  3. aThe dose of MTX administered; 375 μg
  4. bThe dose of MTX injected; 13.6 μg