Research Article
Extemporaneous Compounding and Physiological Modeling of Amlodipine/Valsartan Suspension
| Parameter | Value | Amlodipine (as besylate) | Valsartan |
| Molecular weight (g/mole) | 567.051 | 435.53 | Partition/distribution coefficient | 2.66 (pH = 7.4)a | −0.34 (pH = 7)b | Pka1 | 8.7c | 3.9d | Pka2 | — | 4.73d | Solubility (mg/ml) | 0.774 (pH 7.4)e | 16.8 (pH = 8)f | Peff (human jejunal permeability) (cm/sec) | 0.0743 ∗ 10−4g (caco-2) | 0.262 ∗ 10−4h (rat) | Dose (mg) | 5 | 80 | Dose volume (ml) | 250 | 250 | Mean precipitation time (sec) | 900i | 900i | Diffusion coefficient (cm2/s) | 4.2 ∗ 10−8j | 1.1 ∗ 10−8k | Drug particle density (g/ml) | 1.2i | 1.2i | Blood plasma concentration ratio | 1i | 1i | Body weight (kg) | 70 | 70 | Unbound percent in plasma (%) | 2l | 5m | Clearance (l/hr) | 28n | fn | Volume of distribution, Vc (L/Kg) | 17n | 0.23n | Elimination half-life (h) | 27.03o | 5.58o | Simulation time (hr) | 144 | 72 |
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aFrom [ 17, 18], bfrom [ 19], cfrom [ 20, 21], d,ffrom[ 22], efrom [ 23], g from[ 18], hfrom [ 24], ifrom GastroPlus default values, j, kfrom[ 25], lfrom [ 26], mfrom [ 27], nGastroPlus calculated using PBPKPlus™ module, and oGastroPlus calculated (built-in calculation from PK parameters). |