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Selection of Excipients Based on the Biopharmaceutics Classification System of Drugs

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Excipient Applications in Formulation Design and Drug Delivery

Abstract

Active agents have been considered the main ingredients of any therapeutic product since the early ages of formulation technology. However, the importance of the inactive ingredients has been realized during the last three decades. With the development and manufacturing of more intelligent and multifunction excipients, new ways became available for formulation technologists to increase the beneficial effects of drugs on human body. Many modern active agents have internal characteristics that significantly decrease their potential and theoretical bioavailability; however, today we have the widest variety of inactive ingredients that we can utilize in order to change these properties. The careful and educated selection of excipients might significantly influence the effect of the drugs, including hastening or delaying their onset of action, increasing their bioavailability by changing their physicochemical characteristics, and increasing their stability. In this chapter, we focus primarily on the factors determining and influencing bioavailability as well as the selection of excipients for formulating new dosage forms with enhanced therapeutic efficacy, based on the physicochemical properties of drugs. We will provide some examples from the scientific literature to demonstrate the achievements in this multidisciplinary area.

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Abbreviations

BA:

Bioavailability

BCS:

Biopharmaceutics classification system

BDDCS:

Biopharmaceutics drug disposition classification system

DSC:

Differential scanning calorimetry

DOSY:

Diffusion ordered NMR spectroscopy

EDTA:

Ethylenediaminetetraacetic acid

ESI-MS:

Electrospray ionization mass spectrometry

FDA:

Food and Drug Administration (US)

HPC:

Hydroxypropyl cellulose

HPMC:

Hydroxypropyl methylcellulose

MCG:

Medium chain triglycerides

NMR:

Nuclear magnetic resonance (spectroscopy)

PEG:

Polyethylene glycol

PEI:

Poly(ethyleneimine)

PVP:

Polyvinyl pyrrolidone

SNEDDS:

Self-nanoemulsifying drug delivery system

TPGS:

Tocopheryl polyethylene glycol succinate

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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

    Gabriella Baki & Sai HS. Boddu

  2. Circular Edge, 17 Clyde Rd #202, 08873, Somerset, NJ, USA

    Sachin Chaudhari

  3. Par Pharmaceutical Companies, Inc, One Ram Ridge Road, Spring Valley, 10977, NY, USA

    Ripal Gaudana

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  1. Gabriella Baki
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  2. Sachin Chaudhari
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  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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Baki, G., Chaudhari, S., Gaudana, R., Boddu, S. (2015). Selection of Excipients Based on the Biopharmaceutics Classification System of Drugs. 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_12

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