4-[4-[(2-Hydroxybenzoyl)amino]phenyl]butyric acid as a novel oral delivery agent for recombinant human growth hormone.

doi:10.1021/JM960038F

Paper

4-[4-[(2-Hydroxybenzoyl)amino]phenyl]butyric acid as a novel oral delivery agent for recombinant human growth hormone.

Published Jun 21, 1996 · A. Leone-Bay, K. K. Ho, R. Agarwal

Journal of medicinal chemistry

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61

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1

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Abstract

A series of N-acetylated, non-alpha, aromatic amino acids was prepared and shown to promote the absorption of recombinant human growth hormone (rhGH) from the gastrointestinal tract. Seventy compounds in this family were tested in vivo in rats. Of the compounds tested, 4-[4-[(2-hydroxybenzoyl)amino]phenyl]butyric acid was identified as a preclinical candidate and was used to demonstrate the oral delivery of rhGH in primates. A significant positive correlation was found between the relative log k' of the delivery agents, as determined by HPLC on an immobilized artificial membrane (IAM) column, and serum rhGH concentrations following oral or colonic dosing in rats. Structure-activity relationships have also been developed on the basis of electronic effects and hydrogen-bonding characteristics of the aromatic amide substituents.

Non-RCT

Animal Study

Study Snapshot

4-[4-[(2-hydroxybenzoyl)amino]phenyl]butyric acid] shows potential as an oral delivery agent for recombinant human growth hormone, with potential for clinical use in primates.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

4-[4-[(2-Hydroxybenzoyl)amino]phenyl]butyric acid as a novel oral delivery agent for recombinant human growth hormone.

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References

Citations

Oral Absorption of Middle-to-Large Molecules and Its Improvement, with a Focus on New Modality Drugs

Orally bioavailable middle-to-large molecules, such as peptides and oligonucleotides, show promise for new therapeutic modalities, but further improvements are needed for optimal absorption.

Gastrointestinal Permeation Enhancers for the Development of Oral Peptide Pharmaceuticals

Gastrointestinal permeation enhancers, such as SNAC and C8, can improve the permeability of oral peptide pharmaceuticals through the intestinal epithelium, potentially benefiting future oral peptide products.

FORMULATIONS AND TECHNOLOGIES IN GROWTH HORMONE DELIVERY

Alternative growth hormone delivery routes and technologies, such as intranasal, pulmonary, transdermal, and oral, have improved noncompliance and accessibility in treating growth hormone deficiency and related conditions.

A quality by design (QbD) study on enoxaparin sodium loaded polymeric microspheres for colon‐specific delivery

Quality by design (QbD) successfully designed enoxaparin sodium microspheres for colon-specific delivery, achieving a near-ideal in vitro release profile with optimal conditions.

Intestinal permeation enhancers for oral peptide delivery.

Intestinal permeation enhancers (PEs) can improve oral delivery of therapeutic peptides, but require high concentrations and formulations with poorly permeable molecules in solid dosage forms and lipoidal dispersions for clinical trials.

Lipid-based nanocarriers for oral peptide delivery.

Lipid-based nanocarriers for oral peptide delivery show promise, but their composition, physicochemical, and pharmaceutical properties must be optimized for successful drug delivery and commercial success.

Bioactive self-assembling lipid-like peptides as permeation enhancers for oral drug delivery.

Short, lipid-like peptides can enhance oral delivery of diagnostic and therapeutic molecules by increasing permeation through the intestinal barrier without affecting cell viability or integrity.

Development of enoxaparin sodium polymeric microparticles for colon-specific delivery

Eudragit® FS 30D microparticles are a suitable oral system for colonic delivery of enoxaparin, allowing targeted release in inflamed tissue.

Enhanced delivery of human growth hormone across cell membrane by Tat-PTD

Tat-PTD effectively enhances the intestinal absorption of human growth hormone, potentially paving the way for novel oral administration of growth hormone.