Dielectric relaxation studies and dissolution behavior of amorphous verapamil hydrochloride.
Verapamil hydrochloride (VH) is a very popular calcium channel blocker. Solubility of its crystalline form in the blood reaches only 10-20%. Thus, it seems to be very important to improve its bioavailability. In this article, we show that the preparation of the amorphous form of VH enhance its dissolution rate. In addition we performed dielectric measurements to describe molecular dynamics of this active pharmaceutical ingredient (API). Since examined sample is typical ionically conducting material, to gain information about structural relaxation we employed the dielectric modulus formalism. The temperature dependence of the structural relaxation time can be described over the entire measured range by a single Vogel-Fulcher-Tamman (VFT) equation. From the VFT fits the glass transition temperature was estimated as T(g) = 320.1 K. Below glass transition temperature one clearly visible secondary relaxation, with activation energy E(a) = 37.8 kJ/mol, was reported. Deviations of experimental data from KWW fits on high-frequency flank of alpha-peak indicate the presence of an excess wing in tested sample. Based on Kia Ngai's coupling model we identified the excess wing as true Johari-Goldstein process.
Adrjanowicz
K
K
Institute of Physics, Silesian University, Katowice, Poland. kadrjano@us.edu.pl
Kaminski
K
K
Paluch
M
M
Wlodarczyk
P
P
Grzybowska
K
K
Wojnarowska
Z
Z
Hawelek
L
L
Sawicki
W
W
Lepek
P
P
Lunio
R
R
D000465:Algorithms; D000701:Analgesics, Opioid / Q000737:chemistry; D001682:Biological Availability; D002121:Calcium Channel Blockers / Q000008:administration & dosage / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D003460:Crystallization; D004304:Dosage Forms; D004563:Electrochemistry; D008968:Molecular Conformation; D012995:Solubility; D013056:Spectrophotometry, Ultraviolet; D013057:Spectrum Analysis; D013696:Temperature; D014147:Tramadol / Q000737:chemistry; D014700:Verapamil / Q000008:administration & dosage / Q000737:chemistry*; D014961:X-Ray Diffraction
D000701:Analgesics, Opioid; D002121:Calcium Channel Blockers; D004304:Dosage Forms; D014147:Tramadol; D014700:Verapamil