PMID- 12527186
OWN - NLM
STAT- MEDLINE
DCOM- 20030716
LR  - 20190910
IS  - 0378-5173 (Print)
IS  - 0378-5173 (Linking)
VI  - 251
IP  - 1-2
DP  - 2003 Jan 30
TI  - Characterization of solid dispersions of itraconazole and 
      hydroxypropylmethylcellulose prepared by melt extrusion--Part I.
PG  - 165-74
AB  - Solid dispersions containing different ratios of itraconazole and 
      hydroxypropylmethylcellulose (HPMC) were prepared by solvent casting. Based on 
      dose, differential scanning calorimetry and dissolution results, a drug/polymer 
      ratio of 40/60 w/w was selected in order to prepare dispersions by melt 
      extrusion. The melt extrusion process was characterized using a design of 
      experiments (DOE) approach. All parameter settings resulted in the formation of 
      an amorphous solid dispersion whereby HPMC 2910 5 mPas prevents 
      re-crystallization of the drug during cooling. Dissolution measurements 
      demonstrated that a significantly increased dissolution rate was obtained with 
      the amorphous solid dispersion compared to the physical mixture. The outcome of 
      DOE further indicated that melt extrusion is very robust with regard to the 
      itraconazole/HPMC melt extrudate characteristics. Stability studies demonstrated 
      that the itraconazole/HPMC 40/60 w/w milled melt extrudate formulation is 
      chemically and physically stable for periods in excess of 6 months as indicated 
      by the absence of degradation products or re-crystallization of the drug.
FAU - Verreck, Geert
AU  - Verreck G
AD  - Pharmaceutical Sciences, Johnson & Johnson Pharmaceutical Research & Development, 
      Janssen Pharmaceutica, Turnhoutseweg 30, 2340, Beerse, Belgium. 
      gverreck@prdbe.jnj.com
FAU - Six, Karel
AU  - Six K
FAU - Van den Mooter, Guy
AU  - Van den Mooter G
FAU - Baert, Lieven
AU  - Baert L
FAU - Peeters, Jef
AU  - Peeters J
FAU - Brewster, Marcus E
AU  - Brewster ME
LA  - eng
PT  - Journal Article
PL  - Netherlands
TA  - Int J Pharm
JT  - International journal of pharmaceutics
JID - 7804127
RN  - 304NUG5GF4 (Itraconazole)
RN  - 3NXW29V3WO (Hypromellose Derivatives)
RN  - 9004-67-5 (Methylcellulose)
SB  - IM
MH  - Hypromellose Derivatives
MH  - Itraconazole/analysis/*chemistry/pharmacokinetics
MH  - Methylcellulose/*analogs & derivatives/analysis/*chemistry/pharmacokinetics
MH  - Technology, Pharmaceutical/*methods
EDAT- 2003/01/16 04:00
MHDA- 2003/07/17 05:00
CRDT- 2003/01/16 04:00
PHST- 2003/01/16 04:00 [pubmed]
PHST- 2003/07/17 05:00 [medline]
PHST- 2003/01/16 04:00 [entrez]
AID - S0378517302005914 [pii]
AID - 10.1016/s0378-5173(02)00591-4 [doi]
PST - ppublish
SO  - Int J Pharm. 2003 Jan 30;251(1-2):165-74. doi: 10.1016/s0378-5173(02)00591-4.