title: Oral insulin: a comparison with subcutaneous regular human insulin in patients with type 2 diabetes.
abstract: OBJECTIVE
  To determine the pharmacokinetic and pharmacodynamic properties of an oral insulin (OI) formulation compared with subcutaneously injected regular human insulin (RHI).
  
  
  METHODS
  Ten male patients with type 2 diabetes (means +/- SD; A1C 7.0 +/- 1.1%; BMI 28.3 +/- 2.7 kg/m(2)) received either 300 units of insulin combined with 400 mg of delivery agent orally or 15 units RHI subcutaneously under isoglycemic clamp conditions.
  
  
  RESULTS
  Maximum insulin concentration was greater and onset of action was faster with OI (C(max) 93 +/- 71 vs. 33 +/- 11 microU/ml; AUC(GIR)((0-1h)) 173 +/- 86 vs. 27 +/- 32 mg/kg; P < 0.05). Mean insulin concentration and glucose infusion rate returned to baseline within 3 h after OI administration. Relative bioavailability of OI was 7 +/- 4% (1st 2 h).
  
  
  CONCLUSIONS
  This proof-of-concept study demonstrated that absorption of OI is feasible under fasting conditions. OI has a fast onset and a short duration of action but also shows a rather high between-subject variability in absorption.
authors.affiliation: Profil Institut für Stoffwechselforschung GmbH, Neuss, Germany. christoph.kapitza@profil-research.de
authors.forename: Christoph
authors.initials: C
authors.lastname: Kapitza
authors.forename: Eric
authors.initials: E
authors.lastname: Zijlstra
authors.forename: Lutz
authors.initials: L
authors.lastname: Heinemann
authors.forename: M Cristina
authors.initials: MC
authors.lastname: Castelli
authors.forename: Gary
authors.initials: G
authors.lastname: Riley
authors.forename: Tim
authors.initials: T
authors.lastname: Heise
mesh_terms: D000284:Administration, Oral; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy*; D006801:Humans; D007004:Hypoglycemic Agents / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D007279:Injections, Subcutaneous; D007328:Insulin / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D008297:Male; D008875:Middle Aged
chemical_list: D007004:Hypoglycemic Agents; D007328:Insulin