In vitro and in vivo evaluation of a sulfobutyl ether β‐cyclodextrin enabled etomidate formulation

McIntosh, Michelle Paula; Schwarting, Nancy; Rajewski, Roger A.

doi:10.1002/jps.20160

Cited by 37 publications

(21 citation statements)

References 28 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…For example, oral absorption of [ 3 H]benzo[a]pyrene was reduced upon simultaneous administration of the compound and relatively large doses of β CD [93] and large oral dosages of α CD are used to reduce oral absorption of dietary fat (FBC X tablets; ArtJen, Canada). Several studies in both animals and humans have indicated that drug–HP β CD and drug–SBE β CD complexation has negligible effects on the drug pharmacokinetics after parenteral administration [94–101] . It has been shown that the binding constant of drug–CD complexes must be greater than about 10 5 m −1 to have any effect on the drug pharmacokinetics after parenteral administration [21] .…”

Section: Introductionmentioning

confidence: 99%

Pharmaceutical applications of cyclodextrins: basic science and product development

Loftsson

Brewster

2010

Journal of Pharmacy and Pharmacology

836

496

View full text Add to dashboard Cite

Objectives Drug pipelines are becoming increasingly difficult to formulate. This is punctuated by both retrospective and prospective analyses that show that while 40% of currently marketed drugs are poorly soluble based on the definition of the biopharmaceutical classification system (BCS), about 90% of drugs in development can be characterized as poorly soluble. Although a number of techniques have been suggested for increasing oral bioavailability and for enabling parenteral formulations, cyclodextrins have emerged as a productive approach. This short review is intended to provide both some basic science information as well as data on the ability to develop drugs in cyclodextrin-containing formulations. Key findings There are currently a number of marketed products that make use of these functional solubilizing excipients and new product introduction continues to demonstrate their high added value. The ability to predict whether cyclodextrins will be of benefit in creating a dosage form for a particular drug candidate requires a good working knowledge of the properties of cyclodextrins, their mechanism of solubilization and factors that contribute to, or detract from, the biopharmaceutical characteristics of the formed complexes. Summary We provide basic science information as well as data on the development of drugs in cyclodextrin-containing formulations. Cyclodextrins have emerged as an important tool in the formulator's armamentarium to improve apparent solubility and dissolution rate for poorly water-soluble drug candidates. The continued interest and productivity of these materials bode well for future application and their currency as excipients in research, development and drug product marketing.

show abstract

Section: Introductionmentioning

confidence: 99%

Pharmaceutical applications of cyclodextrins: basic science and product development

Loftsson

Brewster

2010

Journal of Pharmacy and Pharmacology

836

496

View full text Add to dashboard Cite

show abstract

“…11,12 Cyclodextrins are cyclic oligosaccharides with a hydrophilic exterior surface and a hydrophobic interior cavity. As such, they can interact with molecules of small size to form total inclusion complexes, or with macromolecular drugs to form partial inclusion complexes via their hydrophobic side chains.…”

mentioning

confidence: 99%

Development of a chitosan‐based nanoparticle formulation for delivery of a hydrophilic hexapeptide, dalargin

et al. 2008

View full text Add to dashboard Cite

Nanoparticle based delivery systems can offer opportunities for targeting, controlled release, and enhanced stability of their drug, protein, or gene therapy payload. This study investigated the use of chitosan in combination with the ionic additives sulfobutyl-ether-7-beta-cyclodextrin (SB-CD) or SB-CD/dextran sulfate (SB-CD/DS) mixture in comparison with chitosan: DS in the formulation of nanoparticles incorporating the hexapeptide dalargin. The physical characteristics (particle size, zeta potential), entrapment and loading efficiency, and release of dalargin were quantified. It was demonstrated that anionic cyclodextrin, SB-CD, can be used in complex coacervation with chitosan, with and without the presence of DS, to form nanoparticles. The presence of SB-CD or DS in the nanoparticle formulation and the weight ratio of chitosan to anionic additive(s) influenced the physical properties of the nanoparticles and their ability to carry dalargin. In addition, the particle size of nanoparticles was also affected by the molecular weight of chitosan and DS. The use of either DS or SB-CD/DS mixture produced chitosan nanoparticles with small particle size, high dalargin entrapment efficiency, enhanced peptide stability, and sustained release characteristics.

show abstract

“…This difference occurred even though the same depth and duration of cortical depression was present in both treatment groups evidenced by the same BIS values shown in Figure 3. The maximum decreases in systolic blood pressure, median (IQR), were 12 (11)(12)(13)(14)(15)(16)(17)(18)(19)(20)(21)(22) mm Hg for PHAX and 25 (17)(18)(19)(20)(21)(22)(23)(24)(25)(26)(27)(28) mm Hg for propofol and diastolic blood pressure were 14 (9-16) mm Hg for PHAX and 26 (22)(23)(24)(25)(26)(27)(28)(29)(30) mm Hg for propofol. Further, these differences in pressure occurred when the heart rate increases after administration of anesthetic injection, median (IQR) were: 21 (16-24) beats/minute for PHAX and 15 (11)(12)(13)(14)(15)(16)(17)(18)(19)(20)(21)(22)…”

Section: Resultsmentioning

confidence: 99%

“…[23][24][25][26][27] It has not been previously investigated as an excipient for alphaxalone. Such a preparation, alphaxalone in aqueous solution with SBECD, Phaxan™ (PHAX), has been made and tested in preclinical studies.…”

mentioning

confidence: 99%

A Phase 1c Trial Comparing the Efficacy and Safety of a New Aqueous Formulation of Alphaxalone With Propofol

Monagle

Siu

Worrell

et al. 2016

Survey of Anesthesiology

View full text Add to dashboard Cite

In vitro and in vivo evaluation of a sulfobutyl ether β‐cyclodextrin enabled etomidate formulation

Cited by 37 publications

References 28 publications

Pharmaceutical applications of cyclodextrins: basic science and product development

Pharmaceutical applications of cyclodextrins: basic science and product development

Development of a chitosan‐based nanoparticle formulation for delivery of a hydrophilic hexapeptide, dalargin

A Phase 1c Trial Comparing the Efficacy and Safety of a New Aqueous Formulation of Alphaxalone With Propofol

Contact Info

Product

Resources

About