Design of spray dried ternary solid dispersions comprising itraconazole, soluplus and HPMCP: Effect of constituent compositions

Mark T. Davis; Catherine B. Potter; Maryam Mohammadpour; Ahmad B. Albadarin; Gavin M. Walker

doi:10.1016/j.ijpharm.2017.01.043

Design of spray dried ternary solid dispersions comprising itraconazole, soluplus and HPMCP: Effect of constituent compositions

Mark T. Davis, Catherine B. Potter, Maryam Mohammadpour, Ahmad B. Albadarin, Gavin M. Walker

Department of Chemical Sciences

Research output: Contribution to journal › Article › peer-review

Abstract

A range of 17 ternary formulations of itraconazole (ITZ), HPMCP and Soluplus have been manufactured using spray drying. These amorphous solid dispersions (ASDs) were very stable against crystallisation and ITZ was found to be amorphous in all formulations after one year at 40 °C/75% RH. A number of solid state analytical techniques including PXRD, DSC, small angle X-ray scattering, FTIR and solid state NMR were used to characterise the physicochemical properties of the ASDs following processing and storage and to assess any interactions between components. Microtrac laser scattering analysis revealed a relationship between polymer levels and particle size distribution (PSD). Dissolution studies indicated that higher Soluplus content in the formulation resulted in higher concentrations of ITZ in acidic media.

Original language	English
Pages (from-to)	365-372
Number of pages	8
Journal	International Journal of Pharmaceutics
Volume	519
Issue number	1-2
DOIs	https://doi.org/10.1016/j.ijpharm.2017.01.043
Publication status	Published - 15 Mar 2017

Keywords

Amorphous
HPMCP
Itraconazole
Soluplus
Spray drying
Ternary

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10.1016/j.ijpharm.2017.01.043

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title = "Design of spray dried ternary solid dispersions comprising itraconazole, soluplus and HPMCP: Effect of constituent compositions",

abstract = "A range of 17 ternary formulations of itraconazole (ITZ), HPMCP and Soluplus have been manufactured using spray drying. These amorphous solid dispersions (ASDs) were very stable against crystallisation and ITZ was found to be amorphous in all formulations after one year at 40 °C/75% RH. A number of solid state analytical techniques including PXRD, DSC, small angle X-ray scattering, FTIR and solid state NMR were used to characterise the physicochemical properties of the ASDs following processing and storage and to assess any interactions between components. Microtrac laser scattering analysis revealed a relationship between polymer levels and particle size distribution (PSD). Dissolution studies indicated that higher Soluplus content in the formulation resulted in higher concentrations of ITZ in acidic media.",

keywords = "Amorphous, HPMCP, Itraconazole, Soluplus, Spray drying, Ternary",

author = "Davis, {Mark T.} and Potter, {Catherine B.} and Maryam Mohammadpour and Albadarin, {Ahmad B.} and Walker, {Gavin M.}",

note = "Publisher Copyright: {\textcopyright} 2017 Elsevier B.V.",

year = "2017",

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day = "15",

doi = "10.1016/j.ijpharm.2017.01.043",

language = "English",

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T2 - Effect of constituent compositions

AU - Davis, Mark T.

AU - Potter, Catherine B.

AU - Mohammadpour, Maryam

AU - Albadarin, Ahmad B.

AU - Walker, Gavin M.

PY - 2017/3/15

Y1 - 2017/3/15

N2 - A range of 17 ternary formulations of itraconazole (ITZ), HPMCP and Soluplus have been manufactured using spray drying. These amorphous solid dispersions (ASDs) were very stable against crystallisation and ITZ was found to be amorphous in all formulations after one year at 40 °C/75% RH. A number of solid state analytical techniques including PXRD, DSC, small angle X-ray scattering, FTIR and solid state NMR were used to characterise the physicochemical properties of the ASDs following processing and storage and to assess any interactions between components. Microtrac laser scattering analysis revealed a relationship between polymer levels and particle size distribution (PSD). Dissolution studies indicated that higher Soluplus content in the formulation resulted in higher concentrations of ITZ in acidic media.

AB - A range of 17 ternary formulations of itraconazole (ITZ), HPMCP and Soluplus have been manufactured using spray drying. These amorphous solid dispersions (ASDs) were very stable against crystallisation and ITZ was found to be amorphous in all formulations after one year at 40 °C/75% RH. A number of solid state analytical techniques including PXRD, DSC, small angle X-ray scattering, FTIR and solid state NMR were used to characterise the physicochemical properties of the ASDs following processing and storage and to assess any interactions between components. Microtrac laser scattering analysis revealed a relationship between polymer levels and particle size distribution (PSD). Dissolution studies indicated that higher Soluplus content in the formulation resulted in higher concentrations of ITZ in acidic media.

KW - Amorphous

KW - HPMCP

KW - Itraconazole

KW - Soluplus

KW - Spray drying

KW - Ternary

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SN - 0378-5173

VL - 519

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JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

IS - 1-2

ER -

Design of spray dried ternary solid dispersions comprising itraconazole, soluplus and HPMCP: Effect of constituent compositions

Abstract

Keywords

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