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Excipients That Facilitate Amorphous Drug Stabilization

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Excipient Applications in Formulation Design and Drug Delivery

Abstract

The importance of the amorphous state in studying bioavailability of poorly water-soluble drugs cannot be over-emphasized. The higher free energy and therefore the apparent high solubility of the amorphous phase are some of the advantages for promoting the amorphous phase, as compared to its crystalline counterpart. It is well known that the amorphous phase is thermodynamically unstable. This might result in the conversion of the metastable form to its stable crystalline form during storage. This conversion might also lead to product failure during storage owing to the poor dissolution properties of the crystalline form. Excipients can play a key role in preventing such a transformation during storage as well as maximizing the therapeutic efficacy of the amorphous material. This book chapter intends to highlight the delivery issues pertaining to amorphous drugs with a special emphasis on the most commonly used excipients in stabilizing amorphous drug substances in formulations.

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Abbreviations

AI:

Amorphicity index

API:

Active pharmaceutical ingredient

ASD:

Amorphous solid dispersion

BCS:

Biopharmaceutics classification system

HPMC:

Hydroxyl propyl methyl cellulose

HPMCAS:

Hydroxyl propyl methyl cellulose acetate succinate

IMC:

Indomethacin

PAA:

Poly(acrylic acid)

PEG:

Polyethylene glycol

PSSA:

Poly(styrene sulfonic acid)

PVP:

Poly (vinyl pyrrolidone)

PVPVA:

Poly(vinylpyrrolidone-vinyl acetate)

pSi:

Porous silica particles

pSi-ox:

Oxidized porous silicon particles

SLS:

Sodium lauryl sulfate

Tg:

Glass transition temperature

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Authors and Affiliations

  1. Department of Pharmacy Practice, The University of Toledo, Health Science Campus, 3000 Arlington Ave., 43614, Toledo, OH, USA

    Yangjie Wei, Bhaswati Dattachowdhury, Niraja Patel, Kenneth Alexander & Sai HS. Boddu

  2. Insys Therapeutics, Inc. Phoenix, Arizona Area, Chandler, USA

    Kiran K. Vangara

Authors
  1. Yangjie Wei
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  2. Bhaswati Dattachowdhury
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  3. Kiran K. Vangara
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  4. Niraja Patel
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  5. Kenneth Alexander
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  6. Sai HS. Boddu
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Corresponding author

Correspondence to Sai HS. Boddu .

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Editors and Affiliations

  1. Bristol-Myers Squibb, Co., New Brunswick, New Jersey, USA

    Ajit S Narang

  2. Division of Industrial Pharmacy, Department of Pharmacy Practice, The University of Toledo, TOLEDO, Ohio, USA

    Sai H S. Boddu

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Wei, Y., Dattachowdhury, B., Vangara, K., Patel, N., Alexander, K., Boddu, S. (2015). Excipients That Facilitate Amorphous Drug Stabilization. In: Narang, A., Boddu, S. (eds) Excipient Applications in Formulation Design and Drug Delivery. Springer, Cham. https://doi.org/10.1007/978-3-319-20206-8_15

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