PMID- 22530305
OWN - NLM
STAT- MEDLINE
DCOM- 20120517
LR  - 20181201
IS  - 0031-7144 (Print)
IS  - 0031-7144 (Linking)
VI  - 67
IP  - 3
DP  - 2012 Mar
TI  - Phase I clinical study to select a novel oral formulation for ibandronate 
      containing the excipient sodium N-[8-(2-hydroxybenzoyl) amino] caprylate (SNAC).
PG  - 233-41
AB  - The aim of this study was to select a novel oral formulation for ibandronate 
      (IBN, CAS number: 13892619). In four cohorts of 28, 21, 19 and 29 healthy 
      volunteers, the impact of the carrier molecule sodium N-[8-(2-hydroxybenzoyl) 
      amino] caprylate (SNAC, CAS number: 203787-91-1) on the bioavailability of IBN 
      was investigated. Within each cohort different oral formulations with one dose of 
      ibandronate (30 mg) and three different ratios of IBN:SNAC (1:5, 1:10 and 1:20) 
      were compared to the approved oral IBN tablet formulations (150 and 50 mg IBN) in 
      a 4-way cross-over design and a one week washout between the administrations. The 
      highest mean IBN exposure was achieved with a capsule formulation containing 
      drug-coated beadlets and an IBN:SNAC ratio of 1:5. AUC(last) and C(max) of IBN 
      were approximately 1.3- and 2.2-fold higher compared to the reference treatment 
      (150 mg IBN without SNAC). Increasing the post-dose fasting duration from 15 to 
      30 min resulted in a more than 2-fold increase in AUC(last), while superimposable 
      IBN serum concentration-time profiles were achieved after a 30 and 60 min fast. 
      The tolerability of the IBN/SNAC treatments in all cohorts was similar to that in 
      the IBN reference groups and most adverse events (AEs) were of mild to moderate 
      intensity.
FAU - Bittner, B
AU  - Bittner B
AD  - F Hoffmann-La Roche Ltd., Clinical Pharmacology, Grenzacher Strasse 124, CH-4070 
      Basel, Switzerland. beate.bittner@email.de
FAU - McIntyre, C
AU  - McIntyre C
FAU - Tian, H
AU  - Tian H
FAU - Tang, K
AU  - Tang K
FAU - Shah, N
AU  - Shah N
FAU - Phuapradit, W
AU  - Phuapradit W
FAU - Ahmed, H
AU  - Ahmed H
FAU - Chokshi, H
AU  - Chokshi H
FAU - Infeld, M
AU  - Infeld M
FAU - Fotaki, N
AU  - Fotaki N
FAU - Ma, H
AU  - Ma H
FAU - Portron, A
AU  - Portron A
FAU - Jordan, P
AU  - Jordan P
FAU - Schmidt, J
AU  - Schmidt J
LA  - eng
PT  - Clinical Trial, Phase I
PT  - Journal Article
PT  - Randomized Controlled Trial
PL  - Germany
TA  - Pharmazie
JT  - Die Pharmazie
JID - 9800766
RN  - 0 (Bone Density Conservation Agents)
RN  - 0 (Caprylates)
RN  - 0 (Diphosphonates)
RN  - 0 (Excipients)
RN  - 0 (N-(8-(2-hydroxybenzoyl)amino)caprylate)
RN  - UMD7G2653W (Ibandronic Acid)
SB  - IM
MH  - Administration, Oral
MH  - Adolescent
MH  - Adult
MH  - Algorithms
MH  - Analysis of Variance
MH  - Area Under Curve
MH  - Bone Density Conservation Agents/*administration & dosage/pharmacokinetics
MH  - Caprylates/*chemistry
MH  - Chemistry, Pharmaceutical
MH  - Cohort Studies
MH  - Cross-Over Studies
MH  - Diphosphonates/*administration & dosage/pharmacokinetics
MH  - Drug Delivery Systems
MH  - Excipients/*chemistry
MH  - Female
MH  - Half-Life
MH  - Humans
MH  - Ibandronic Acid
MH  - Male
MH  - Middle Aged
MH  - Solubility
MH  - Young Adult
EDAT- 2012/04/26 06:00
MHDA- 2012/05/18 06:00
CRDT- 2012/04/26 06:00
PHST- 2012/04/26 06:00 [entrez]
PHST- 2012/04/26 06:00 [pubmed]
PHST- 2012/05/18 06:00 [medline]
PST - ppublish
SO  - Pharmazie. 2012 Mar;67(3):233-41.