Reversible and pH-dependent weak drug-excipient binding does not affect oral bioavailability of high dose drugs

Narang, Ajit S.; Yamniuk, Aaron P.; Zhang, Limin; Çömezoglu, S. Nilgün; Bindra, Dilbir S.; Varia, Sailesh A.; Doyle, Michael L.; Badawy, Sherif

doi:10.1111/j.2042-7158.2011.01435.x

Cited by 20 publications

(10 citation statements)

References 31 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…At a simplistic level, these effects can be directly related to the functionality of excipients, such as the use of binder and disintegrant in tablets or direct drugexcipient interactions (5). However, recent research highlights the role of indirect mechanisms and possible interplay of more than one mechanism.…”

Section: Bioavailabilitymentioning

confidence: 98%

Physicochemical Interactions in Solid Dosage Forms

2012

Self Cite

View full text Add to dashboard Cite

Complete characterization and mechanistic understanding of physicochemical interactions in solid dosage forms are not only important for consistent manufacturability, stability, and bioavailability of the drug product, but are also expected under the quality-by-design paradigm of drug development. Lack of this understanding can impact successful and timely development, scale-up, and commercial manufacture of dosage forms. This article highlights the stability and bioavailability implications of physicochemical interactions in dosage forms citing a couple of examples where such interactions necessitated the recall of commercial drug products.

show abstract

Section: Bioavailabilitymentioning

confidence: 98%

Physicochemical Interactions in Solid Dosage Forms

2012

Self Cite

View full text Add to dashboard Cite

show abstract

“…Nevertheless, it is also worth noted that while these tableting excipients are usually considered inert excipients, cases of undesired drugexcipient interaction with them have been report. As an example, croscarmellose sodium, a superdisintegrant, has been reported to have significant interactions with several drugs [34][35][36], even though sometime an in vitro interaction may not translate into in vivo effect [34,37].…”

Section: Excipients Physicochemical Properties and Formulation Desigmentioning

confidence: 98%

Pre-absorption physicochemical compatibility assessment of 8-drug metabolic cocktail

Tye

Wang

Dockens

et al. 2016

International Journal of Pharmaceutics

View full text Add to dashboard Cite

“…Transfer 5 mL of medroxyprogesteron acetate injectable suspension into suitable dry clean glass beaker (10 mL) and dip the pH electrode in beaker (At room temperature, 25 o C). Allow it to stabilize and observed the pH of MPA suspension [20] .…”

Section: Phmentioning

confidence: 99%

Formulation Development and Evaluation of Injectable Depot Suspension

Bodhe¹,

Deshmukh²,

Shinde³

et al. 2021

IJMHR

View full text Add to dashboard Cite

narrow therapeutic index in gastro intestinal track [3]. Long acting hormonal contraceptives depot formulations are the method of birth control that provides effective contraceptive action for longer period of time. Hormonal contraceptives advance the practice of contraception where injectable and subdermal routes of administration are used. When oral contraceptive shows the difficulty of maintaining daily intake of medicines, then there is need of long acting hormonal contraceptives method. Long acting hormonal contraceptive formulations taken every two to three month and solve the problem of daily intake of medicine. The development of long-acting steroidal contraceptive systems this is believed to be an important solution to the problems of effectiveness, safety, and acceptability of steroidal contraceptives, especially in developing countries [4].

show abstract

Reversible and pH-dependent weak drug-excipient binding does not affect oral bioavailability of high dose drugs

Abstract: A pH-dependent and reversible weak drug-excipient binding interaction is unlikely to affect the oral bioavailability of high dose drugs.

Cited by 20 publications

References 31 publications

Physicochemical Interactions in Solid Dosage Forms

Physicochemical Interactions in Solid Dosage Forms

Pre-absorption physicochemical compatibility assessment of 8-drug metabolic cocktail

Formulation Development and Evaluation of Injectable Depot Suspension

Contact Info

Product

Resources

About