Insulin suppository: enhanced rectal absorption of insulin using an enamine derivative as a new promoter

Yagi, Toshihito; Hakui, Nobuyoshi; Yamasaki, Yoshimitsu; Kawamori, Ryuzo; Shichiri, Motoaki; Abe, Hiroshi; Kim, Soonih; Miyake, Mari; Kamikawa, Kunihisa; Nishihata, Toshiaki; Kamada, Aiko

doi:10.1111/j.2042-7158.1983.tb04301.x

Cited by 25 publications

(2 citation statements)

References 5 publications

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“…This enamine is formed by reacting phenylalanine and the food additive ethyl acetoacetate, but which is hydrolysed to phenylalanine and ethyl acetoacetate in the body; suggesting that safety might not be a significant consideration. A variety of enamines have been shown to improve intestinal permeability in pre-clinical models, but phenylalanine ethyl acetoacetate exhibited stronger enhancement than several other enamines [400], and improved rectal absorption of insulin from a suppository in diabetic dogs [408].…”

Section: Case 15: Salicylates and Enaminesmentioning

confidence: 97%

Intestinal permeation enhancers for oral peptide delivery

Maher

Mrsny

Brayden

2016

Advanced Drug Delivery Reviews

282

201

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Publication informationAdvanced Drug Delivery Reviews, (Part B): 277-319 Publisher ElsevierItem record/more information http://hdl.handle.net/10197/7800Publisher's statement þÿ T h i s i s t h e a u t h o r s v e r s i o n o f a w o r k t h a t w a s a c c e p t e d f o r p u b l i c a t i o n i n A d v a n c e d D r u g Delivery Reviews. Changes resulting from the publishing process, such as peer review,

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Section: Case 15: Salicylates and Enaminesmentioning

confidence: 97%

Intestinal permeation enhancers for oral peptide delivery

Maher

Mrsny

Brayden

2016

Advanced Drug Delivery Reviews

282

201

View full text Add to dashboard Cite

show abstract

“…Because insulin absorption from the rectum in simple formulations is poor and erratic (Yagi et al, 1983;Ritschel and Ritschel, 1984;Hoogdalem et al, 1990;Yamamoto et al, 1992), the use of promoters is imperative. An extensive array of enhancers, including nonionic, cationic, anionic, and amphoteric surfactants, bile salts, phospholipids, alkylglycosides, salicylates, enamines, chelating agents, and enzyme inhibitors have been experimentally tested in numerous animal studies during the last 15 years.…”

Section: Rectal Deliverymentioning

confidence: 99%

Protein Delivery

2002

Pharmaceutical Biotechnology

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A major challenge confronting pharmaceutical scientists in the future will be to design successful dosage forms for the next generation of drugs. Many of these drugs will be complex polymers of amino acids (e.g., peptides, proteins), nucleosides (e.g., antisense molecules), carbohydrates (e.g., polysaccharides), or complex lipids.Through rational drug design, synthetic medicinal chemists are preparing very potent and very specific peptides and antisense drug candidates. These molecules are being developed with molecular characteristics that permit optimal interaction with the specific macromolecules (e.g., receptors, enzymes, RNA, DNA) that mediate their therapeutic effects. Rational drug design does not necessarily mean rational drug delivery, however, which strives to incorporate into a molecule the molecular properties necessary for optimal transfer between the point of administration and the pharmacological target site in the body.Like rational drug design, molecular biology is having a significant impact on the pharmaceutical industry. For the first time, it is possible to produce large quantities of highly pure proteins, polysaccharides, and lipids for possible pharmaceutical applications. Like peptides and antisense molecules, the design of successful dosage forms for these complex biotechnology products represents a major challenge to pharmaceutical scientists.Development of an acceptable drug dosage form is a complex process requiring strong interactions between scientists from many different divisions in a pharmaceutical company, including discovery, development, and manufacturing. The series editor, the editors of the individual volumes, and the publisher hope that this new series will be particularly helpful to scientists in the development areas of a pharmaceutical company (e.g., drug metabolism, toxicology, pharmacokinetics and pharmacodynamics, drug ix x Preface to the Series delivery, preformulation, formulation, and physical and analytical chemistry). In addition, we hope this series will help to build bridges between the development scientists and scientists in discovery (e.g., medicinal chemistry, pharmacology, immunology, cell biology, molecular biology) and in manufacturing (e.g., process chemistry, engineering). The design of successful dosage forms for the next generation of drugs will require not only a high level of expertise by individual scientists, but also a high degree of interaction between scientists in these different divisions of a pharmaceutical company.Finally, everyone involved with this series hopes that these volumes will also be useful to the educators who are training the next generation of pharmaceutical scientists. In addition to having a high level of expertise in their respective disciplines, these young scientists will need to have the scientific skills necessary to communicate with their peers in other scientific disciplines. RONALD T. BORCHARLDT Series Editorxi xii Preface sometimes unanticipated formulation challenges. Such problems have plagued efforts to develop ...

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Enhanced Rectal Absorption of Sodium Ampicillin by N-Acyl Derivatives of Collagen Peptide in Rabbits and Rats

Yata

Yamajo

et al. 1985

Journal of Pharmaceutical Sciences

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Insulin suppository: enhanced rectal absorption of insulin using an enamine derivative as a new promoter

Cited by 25 publications

References 5 publications

Intestinal permeation enhancers for oral peptide delivery

Intestinal permeation enhancers for oral peptide delivery

Protein Delivery

Enhanced Rectal Absorption of Sodium Ampicillin by N-Acyl Derivatives of Collagen Peptide in Rabbits and Rats

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