Econazole Nitrate-Loaded MCM-41 for an Antifungal Topical Powder Formulation

被引：37

作者：

Ambrogi, Valeria ^{[1
]}

Perioli, Luana ^{[1
]}

Pagano, Cinzia ^{[1
]}

Marmottini, Fabio ^{[2
]}

Moretti, Massimo ^{[3
]}

Mizzi, Fabiola ^{[1
]}

Rossi, Carlo ^{[1
]}

机构：

[1] Dipartimento Chim & Tecnol Farmaco, I-06123 Perugia, Italy

[2] Dipartimento Ingn Civile & Ambientale, Perugia, Italy

[3] Dipartimento Specialita Med Chirurg & Sanita Pubb, Perugia, Italy

来源：

JOURNAL OF PHARMACEUTICAL SCIENCES | 2010年 / 99卷 / 11期

关键词：

mesoporous materials; skin mycotic infections; inclusion compound; X-ray diffractometry; drug dissolution; adsorption; crystals; formulation; moisture sorption; excipients; physical stability; DISSOLUTION RATE; DRUG; IMPROVEMENT; SOLUBILITY; ADSORPTION; INCLUSION; COMPLEXES; STATE;

D O I：

10.1002/jps.22183

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

The aim of this article was to prepare a topical powder for the treatment of fungal infections, such as Candida intertrigo and tinea pedis. Thus, an econazole nitrate (ECO) formulation with improved drug dissolution and proper moisture adsorption was designed. ECO was melt with the mesoporous silicate MCM-41 (drug/MCM-41 1/3) and the resulting inclusion compound was characterized by X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC). The drug loading was confirmed by the decrease of specific surface area and pore volume between MCM-41 and the inclusion compound. Formulations containing the inclusion compound were prepared and submitted to in vitro dissolution test and in vitro antifungal activity. A remarkable dissolution rate improvement as well as a higher antifungal activity was observed for the inclusion compound if compared to a commercial product. Moisture sorption properties for MCM-41 and formulations were evaluated as well. (C) 2010 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 99:4738-4745, 2010

引用

页码：4738 / 4745

页数：8

共 24 条

[1]

Airaksinen S, 2005, AAPS PHARMSCITECH, V6

[2]

Influence of the preparation method on the physicochemical properties of econazole-β-cyclodextrin complexes [J].

Al-Marzouqi, Ali H. ;

Solieman, Ayser ;

Shehadi, Ihsan ;

Adem, Abdu .

JOURNAL OF INCLUSION PHENOMENA AND MACROCYCLIC CHEMISTRY, 2008, 60 (1-2) :85-93

[3]

Improvement of dissolution rate of piroxicam by inclusion into MCM-41 mesoporous silicate [J].

Ambrogi, V. ;

Perioli, L. ;

Marmottini, F. ;

Giovagnoli, S. ;

Esposito, M. ;

Rossi, C. .

EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2007, 32 (03) :216-222

[4]

Effect of MCM-41 on the dissolution rate of the poorly soluble plant growth regulator, the indole-3-butyric acid [J].

Ambrogi, V. ;

Famiani, F. ;

Perioli, L. ;

Marmottini, F. ;

Di Cunzolo, I. ;

Rossi, C. .

MICROPOROUS AND MESOPOROUS MATERIALS, 2006, 96 (1-3) :177-183

[5]

Role of mesoporous silicates on carbamazepine dissolution rate enhancement [J].

Ambrogi, Valeria ;

Perioli, Luana ;

Marmottini, Fabio ;

Accorsi, Oriana ;

Pagano, Cinzia ;

Ricci, Maurizio ;

Rossi, Carlo .

MICROPOROUS AND MESOPOROUS MATERIALS, 2008, 113 (1-3) :445-452

[6]

A NEW FAMILY OF MESOPOROUS MOLECULAR-SIEVES PREPARED WITH LIQUID-CRYSTAL TEMPLATES [J].

BECK, JS ;

VARTULI, JC ;

ROTH, WJ ;

LEONOWICZ, ME ;

KRESGE, CT ;

SCHMITT, KD ;

CHU, CTW ;

OLSON, DH ;

SHEPPARD, EW ;

MCCULLEN, SB ;

HIGGINS, JB ;

SCHLENKER, JL .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1992, 114 (27) :10834-10843

[7]

BONONI LJ, 1988, Patent No. 288019

[8]

Adsorption of gases in multimolecular layers [J].

Brunauer, S ;

Emmett, PH ;

Teller, E .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1938, 60 :309-319

[9]

Critical appraisal of classical methods for determination of mesopore size distributions of MCM-41 materials [J].

Choma, J ;

Jaroniec, M ;

Burakiewicz-Mortka, W ;

Kloske, M .

APPLIED SURFACE SCIENCE, 2002, 196 (1-4) :216-223

[10]

Davis J. D., 1995, Primary Care Update for Ob/Gyns, V2, P157, DOI 10.1016/1068-607X(95)00033-3

← 1 2 3 →