Estimation of crystallinity of trehalose dihydrate microspheres by usage of terahertz time-domain spectroscopy.

Crystalline state of pharmaceutical materials is of great importance in the preparation of pharmaceutics because their physicochemical properties affect bioavailability, quality of products, therapeutic level, and manufacturing process. In this study, we have estimated the crystallinity of trehalose dihydrate microspheres by measuring terahertz (THz) spectroscopy. The commercially available trehalose dihydrate takes in general a crystalline state, but trehalose dihydrate microspheres prepared by using spray-drying method are in an amorphous state. We have prepared amorphous anhydrous trehalose by using melt-quenched method from crystalline trehalose dihydrate. We have measured the absorbance of trehalose dihydrate containing amorphous anhydrous trehalose (0%, 25%, 50%, 75%, and 100%) using THz time-domain spectroscopy (THz-TDS) to prepare calibration curves. Using the calibration curves, we have estimated the crystallinity of trehalose dihydrate microspheres prepared by using spray-drying method. Our results suggest that THz-TDS is well suited to distinguish crystallinity differences in pharmaceutical compounds.

[1]  Chung C. Hsu,et al.  Effect of mannitol crystallization on the stability and aerosol performance of a spray-dried pharmaceutical protein, recombinant humanized anti-IgE monoclonal antibody. , 1998, Journal of pharmaceutical sciences.

[2]  J. Freyhof,et al.  Physiochemical factors influencing the absorption of the anhydrous and trihydrate forms of ampicillin. , 1968, Current therapeutic research, clinical and experimental.

[3]  Keishiro Tomoda,et al.  Effects of pulmonary surfactant system on rifampicin release from rifampicin-loaded PLGA microspheres. , 2005, Colloids and surfaces. B, Biointerfaces.

[4]  R R Alfano,et al.  Torsional vibrational modes of tryptophan studied by terahertz time-domain spectroscopy. , 2004, Biophysical journal.

[5]  B. Fischer,et al.  Collective vibrational modes in biological molecules investigated by terahertz time-domain spectroscopy. , 2002, Biopolymers.

[6]  E. Yonemochi,et al.  Solubility Parameter and Dissolution Behavior of Cefalexin Powders with Different Crystallinity , 1992 .

[7]  G. A. Jeffrey,et al.  The crystal structure of anhydrous a,a-trehalose at -150 , 1985 .

[8]  Thomas Rades,et al.  Using terahertz pulsed spectroscopy to study crystallinity of pharmaceutical materials , 2004 .

[9]  J. Crowe,et al.  Human platelets loaded with trehalose survive freeze-drying. , 2001, Cryobiology.

[10]  G. Zografi,et al.  The Quantitative Analysis of Crystallinity Using FT-Raman Spectroscopy , 1998, Pharmaceutical Research.

[11]  Bruno C. Hancock,et al.  Characteristics and significance of the amorphous state in pharmaceutical systems. , 1997, Journal of pharmaceutical sciences.

[12]  A J Aguiar,et al.  Effect of polymorphism on the absorption of chloramphenicol from chloramphenicol palmitate. , 1967, Journal of pharmaceutical sciences.

[13]  D. Grischkowsky,et al.  Terahertz time-domain spectroscopy of water vapor. , 1989, Optics letters.

[14]  Yunqing Chen,et al.  Characterization of anhydrous and hydrated pharmaceutical materials with THz time-domain spectroscopy. , 2007, Journal of pharmaceutical sciences.

[15]  R. Suryanarayanan,et al.  Effect of Preparation Method on Physical Properties of Amorphous Trehalose , 2004, Pharmaceutical Research.

[16]  P. Taday,et al.  Nondestructive analysis of tablet coating thicknesses using terahertz pulsed imaging. , 2005, Journal of pharmaceutical sciences.

[17]  T. Nagai,et al.  Stability and several physical properties of amorphous and crystalline form of indomethacin. , 1980, Chemical & pharmaceutical bulletin.

[18]  T. Arita,et al.  Effect of polymorphism on the dissolution behavior and gastrointestinal absorption of chlortetracycline hydrochloride. , 1974, Chemical & pharmaceutical bulletin.

[19]  M. Descamps,et al.  Direct crystal to glass transformation of trehalose induced by ball milling , 2001 .

[20]  Martin Koch,et al.  Analyzing Morphology and Thermal History of Polybutylene Terephthalate by THz Time-domain Spectroscopy , 2011 .

[21]  Isao Tomita,et al.  Quantitative measurements of amino acids by terahertz time-domain transmission spectroscopy. , 2006, Analytical chemistry.

[22]  Minoru Sakurai,et al.  De- and rehydration behavior of α,α-trehalose dihydrate under humidity-controlled atmospheres , 2005 .