Metabolism and pharmacokinetics of sucrose acetate isobutyrate (SAIB) and sucrose octaisobutyrate (SOIB) in rats, dogs, monkeys or humans: a review

Reynolds, R.C.

doi:10.1016/s0278-6915(97)00123-3

Cited by 16 publications

(10 citation statements)

References 5 publications

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“…Altogether, there was no indication that SAIB compromises the integrity of the epithelium. This finding is in agreement with reported long-term in vivo studies in rats, dogs, monkeys, and humans, showing no signs of toxic effect post oral administration of SAIB (Reynolds, 1998; Reynolds & Chappel, 1998; Food Additive Status List, 2002). In addition, it was revealed that the ethanol concentration used in the SAIB DDS did not have any effect on epithelial integrity and cell viability.…”

Section: Resultssupporting

confidence: 91%

Exploring the mucoadhesive behavior of sucrose acetate isobutyrate: a novel excipient for oral delivery of biopharmaceuticals

et al. 2019

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Oral drug delivery is an attractive noninvasive alternative to injectables. However, oral delivery of biopharmaceuticals is highly challenging due to low stability during transit in the gastrointestinal tract (GIT), resulting in low systemic bioavailability. Thus, novel formulation strategies are essential to overcome this challenge. An interesting approach is increasing retention in the GIT by utilizing mucoadhesive biomaterials as excipients. Here, we explored the potential of the GRAS excipient sucrose acetate isobutyrate (SAIB) to obtain mucoadhesion in vivo. Mucoadhesive properties of a 90% SAIB/10% EtOH (w/w) drug delivery system (DDS) were assessed using a biosimilar mucus model and evaluation of rheological behavior after immersion in biosimilar intestinal fluid. To ease readability of this manuscript, we will refer to this as SAIB DDS. The effect of SAIB DDS on cell viability and epithelial membrane integrity was tested in vitro prior to in vivo studies that were conducted using SPECT/CT imaging in rats. When combining SAIB DDS with biosimilar mucus, increased viscosity was observed due to secondary interactions between biosimilar mucus and sucrose ester predicting considerable mucoadhesion. Mucoadhesion was confirmed in vivo , as radiolabeled insulin entrapped in SAIB DDS, remained in the small intestine for up to 22 h after administration. Moreover, the integrity of the system was investigated using the dynamic gastric model under conditions simulating the chemical composition of stomach fluid and physical shear stress in the antrum under fasted conditions. In conclusion, SAIB is an interesting and safe biomaterial to promote high mucoadhesion in the GIT after oral administration.

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Section: Resultssupporting

confidence: 91%

Exploring the mucoadhesive behavior of sucrose acetate isobutyrate: a novel excipient for oral delivery of biopharmaceuticals

et al. 2019

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“…Isobutyric acid and acetaldehyde are both listed as generally recognized as safe materials in the Food and Drug Administration food additive database (Center for Food Safety and Applied Nutrition, U.S. Food and Drug Administration, U.S. Department of Health and Human Services). Isobutyric acid is also a metabolite of the widely used food additive sucrose acetate isobutyrate (Reynolds, 1998). Acetaldehyde is a metabolite of ethanol and several approved prodrugs including candesartan cilexetil (Gleiter and Morike, 2002) and cefuroxime axetil (Campbell and Langley, 1985).…”

Section: Discussionmentioning

confidence: 99%

XP13512 [(±)-1-([(α-Isobutanoyloxyethoxy)carbonyl] aminomethyl)-1-cyclohexane Acetic Acid], A Novel Gabapentin Prodrug: I. Design, Synthesis, Enzymatic Conversion to Gabapentin, and Transport by Intestinal Solute Transporters

Cundy¹,

Branch²,

Chernov-Rogan³

et al. 2004

J Pharmacol Exp Ther

150

125

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“…No human studies have been conducted as it is considered that the clinical experience of lecithin is sufficient proof of safety. The weighting agent, sucrose acetate isobutyrate, has been studied in detail and no known toxicity, although, in dogs, has reversible hepatic effects …”

Section: Knowledge Of Stabilisers In the Food Supplymentioning

confidence: 99%

Review article: emulsifiers in the food supply and implications for gastrointestinal disease

Halmos

Mack

Gibson

2018

Aliment Pharmacol Ther

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Summary Background Dietary emulsifiers are the latest food additives to be associated with intestinal, cardiovascular and metabolic health. Most recently, there are postulations around certain emulsifiers playing a role in the development of Crohn's disease. Aim To review the use of food‐based emulsifiers, their content in the food supply and mechanisms by which they might exert potentially detrimental biological effects. Methods Information on emulsifiers and thickeners relevant to human health was critically examined. Results The term, “emulsifier,” has been used loosely and has included thickeners as well as agents that truly promote emulsions. These comprise proteins, phospholipids and carbohydrates, alone or in combination, and play roles in optimising food appearance, texture and mouthfeel, delivering or disguising flavours and achieving palatable low‐fat foods. Their presence in the food supply is common, but not “ubiquitous” as frequently stated. Strict regulations limit the amount added to foods, but the lack of established methodologies to measure the actual food content of these diverse compounds limits our knowledge of consumption. Emulsifiers and thickeners have effects on the gut microbiota, mucosal barrier and inflammatory pathways, and can induce disease in experimental models. However, differentiating pharmacological from physiological effects and translating findings in experimental animals to humans raise uncertainties about the relevance of such effects. Conclusions There is limited evidence to directly link emulsifiers and thickeners to human disease, but multiple potential pathogenic mechanisms. Knowledge of actual dietary intake and high‐quality interventional studies is needed to enable the risks associated with their intake to be understood.

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Metabolism and pharmacokinetics of sucrose acetate isobutyrate (SAIB) and sucrose octaisobutyrate (SOIB) in rats, dogs, monkeys or humans: a review

Cited by 16 publications

References 5 publications

Exploring the mucoadhesive behavior of sucrose acetate isobutyrate: a novel excipient for oral delivery of biopharmaceuticals

Exploring the mucoadhesive behavior of sucrose acetate isobutyrate: a novel excipient for oral delivery of biopharmaceuticals

XP13512 [(±)-1-([(α-Isobutanoyloxyethoxy)carbonyl] aminomethyl)-1-cyclohexane Acetic Acid], A Novel Gabapentin Prodrug: I. Design, Synthesis, Enzymatic Conversion to Gabapentin, and Transport by Intestinal Solute Transporters

Review article: emulsifiers in the food supply and implications for gastrointestinal disease

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