Development of a gastric retentive system as a sustained-release formulation of pranlukast hydrate and its subsequent in vivo verification in human studies.
Eur J Pharm Sci
; 53: 62-8, 2014 Mar 12.
Article
in En
| MEDLINE
| ID: mdl-24316098
ABSTRACT
Pranlukast hydrate was demonstrated in a human site-of-absorption study to have extremely poor absorption properties in the lower gastrointestinal tract. The ratios of AUC0-24 in the distal small bowel and colon compared to stomach delivery were approximately 1/7 and 1/70, respectively. As a consequence, a gastroretentive double-layered tablet formulation (gastric swelling system; GSS), consisting of a swelling layer and a drug release layer, was developed for once-daily dosing. To study the gastric retention of the optimized GSS, an in vivo gamma scintigraphic study was carried out in nine healthy volunteers. The transit profiles demonstrated that the GSS was retained in the stomach for more than 10h. The plasma profile was prolonged, especially following administration after an evening meal. The human data validated the design concept and suggest that GSS could be a promising approach for the development of sustained-release formulation for drugs with a limited absorption window in the upper small bowel.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Chromones
/
Drug Delivery Systems
/
Anti-Asthmatic Agents
/
Gastric Mucosa
Type of study:
Clinical_trials
Limits:
Adolescent
/
Adult
/
Humans
/
Male
/
Middle aged
Language:
En
Journal:
Eur J Pharm Sci
Journal subject:
FARMACIA
/
FARMACOLOGIA
/
QUIMICA
Year:
2014
Document type:
Article