Plasma concentrations of remoxipride and the gastrointestinal transit of 111In-marked extended-release coated spheres

Journal Article · Mon Jan 01 00:00:00 EST 1990 · Pharmaceutical Research; (USA)

DOI:https://doi.org/10.1023/A:1015835609333· OSTI ID:6994204

Graffner, C; Wagner, Z; Nilsson, M I; Widerloev, E ^[1]

---

1. Research and Development Laboratories, Soedertaelje (Sweden)

To explore the oral absorption of remoxipride, spheres of remoxipride were labeled with indium-111 colloid before coating with a release-controlling ethylcellulose membrane. Since the labeling remained inside the coating, it was suitable as a marker. Eight healthy volunteers were given a single dose of 100 mg remoxipride in 111In-marked spheres as a multiple-unit capsule. The radioactivity and the position of the spheres (microcapsules) were followed externally for 30 hr by gamma scintigraphy. Parallel to this, plasma concentrations were drawn for 48 hr to confirm the extended dissolution and absorption of remoxipride. The hard gelatin, multiple-unit capsule released the microcapsules within the stomach. These were then rapidly emptied into the small intestine, within 0.5-1 hr. There was then an immediate distribution in the upper small intestine before collection in the lower portion, within 2-5 hr. After passing into the large intestine, there was again extended distribution of the microcapsules. A mean Cmax of 2.7 microM remoxipride was achieved 4 hr after drug administration and a mean AUC of 26.1 mumol.L-1.hr was achieved. Judging from the absorption versus time profile, calculated according to the Wagner-Nelson method, and the scintigraphic images, it is concluded that the main absorption occurs from the small intestine. Data from four volunteers, however, indicated a comparatively good absorption also from the large intestine. Due to the good absorption properties, it is reasonable to expect a low variation in the extent of bioavailability of remoxipride after administration in an extended-release, multiple-unit capsule formulation.

• OSTI ID: 6994204
• Journal Information: Pharmaceutical Research; (USA), Vol. 7:1; ISSN 0724-8741
• Country of Publication: United States
• Language: English

Related Subjects

62 RADIOLOGY AND NUCLEAR MEDICINE
DRUGS
INTESTINAL ABSORPTION
GASTROINTESTINAL TRACT
DYNAMIC FUNCTION STUDIES
INDIUM 111
MAN
METABOLISM
MICROSPHERES
ORAL ADMINISTRATION
SCINTISCANNING
ABSORPTION
ANIMALS
BETA DECAY RADIOISOTOPES
COUNTING TECHNIQUES
DAYS LIVING RADIOISOTOPES
DIAGNOSTIC TECHNIQUES
DIGESTIVE SYSTEM
ELECTRON CAPTURE RADIOISOTOPES
INDIUM ISOTOPES
INTERMEDIATE MASS NUCLEI
ISOMERIC TRANSITION ISOTOPES
ISOTOPES
MAMMALS
MINUTES LIVING RADIOISOTOPES
NUCLEI
ODD-EVEN NUCLEI
PRIMATES
RADIOISOTOPE SCANNING
RADIOISOTOPES
UPTAKE
VERTEBRATES
550601* - Medicine- Unsealed Radionuclides in Diagnostics