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Pharmacokinetics and retrograde spread of budesonide enemas in patients with distal ulcerative colitis

Nyman-Pantelidis, Margareta ; Nilsson, Åke LU ; Wagner, Zoltan and Borgå, Olof (1994) In Alimentary Pharmacology and Therapeutics 8(6). p.617-622
Abstract
METHODS:

The retrograde spread of two budesonide enema formulations with different viscosities was investigated. The study design was open, randomized and two-period crossover. Three female and two male patients (age range: 35-45 years) with distal ulcerative colitis or proctitis participated. Both enema formulations contained a dose of 2 mg budesonide/100 mL. An unabsorbable radioactive marker (99mTc-labelled human serum albumin microcolloid) was added to the enema just before administration. All doses were given in the evening with the patients lying in a supine position during the whole investigation. The intestinal spread was followed for 8 h using scintigraphic imaging. Plasma samples for budesonide assay were taken during... (More)
METHODS:

The retrograde spread of two budesonide enema formulations with different viscosities was investigated. The study design was open, randomized and two-period crossover. Three female and two male patients (age range: 35-45 years) with distal ulcerative colitis or proctitis participated. Both enema formulations contained a dose of 2 mg budesonide/100 mL. An unabsorbable radioactive marker (99mTc-labelled human serum albumin microcolloid) was added to the enema just before administration. All doses were given in the evening with the patients lying in a supine position during the whole investigation. The intestinal spread was followed for 8 h using scintigraphic imaging. Plasma samples for budesonide assay were taken during the 12 h after administration of the low viscosity enema.

RESULTS:

Budesonide plasma levels were measurable for up to 4-6 h. Cmax was 2.5 nmol/L (range: 0.9-4.5 nmol/L) and was attained in 1.5 h (range 1-3 h). The patients had no difficulty in retaining the enemas. There was a statistically significant difference in spread between the low and high viscosity enema. The low viscosity enema spread over an area situated between the rectum and the splenic flexure. The spread occurred mainly in the first 15 min after administration. In contrast, the high viscosity enema, in most cases, spread only over a minor part of this area and the rate and extent of spreading was also more variable with this formulation.

CONCLUSION:

The spread of a low viscosity enema appears to be well suited for the treatment of proctitis and distal colitis.
(Less)
Abstract (Swedish)
METHODS:

The retrograde spread of two budesonide enema formulations with different viscosities was investigated. The study design was open, randomized and two-period crossover. Three female and two male patients (age range: 35-45 years) with distal ulcerative colitis or proctitis participated. Both enema formulations contained a dose of 2 mg budesonide/100 mL. An unabsorbable radioactive marker (99mTc-labelled human serum albumin microcolloid) was added to the enema just before administration. All doses were given in the evening with the patients lying in a supine position during the whole investigation. The intestinal spread was followed for 8 h using scintigraphic imaging. Plasma samples for budesonide assay were taken during... (More)
METHODS:

The retrograde spread of two budesonide enema formulations with different viscosities was investigated. The study design was open, randomized and two-period crossover. Three female and two male patients (age range: 35-45 years) with distal ulcerative colitis or proctitis participated. Both enema formulations contained a dose of 2 mg budesonide/100 mL. An unabsorbable radioactive marker (99mTc-labelled human serum albumin microcolloid) was added to the enema just before administration. All doses were given in the evening with the patients lying in a supine position during the whole investigation. The intestinal spread was followed for 8 h using scintigraphic imaging. Plasma samples for budesonide assay were taken during the 12 h after administration of the low viscosity enema.

RESULTS:

Budesonide plasma levels were measurable for up to 4-6 h. Cmax was 2.5 nmol/L (range: 0.9-4.5 nmol/L) and was attained in 1.5 h (range 1-3 h). The patients had no difficulty in retaining the enemas. There was a statistically significant difference in spread between the low and high viscosity enema. The low viscosity enema spread over an area situated between the rectum and the splenic flexure. The spread occurred mainly in the first 15 min after administration. In contrast, the high viscosity enema, in most cases, spread only over a minor part of this area and the rate and extent of spreading was also more variable with this formulation.

CONCLUSION:

The spread of a low viscosity enema appears to be well suited for the treatment of proctitis and distal colitis.
(Less)
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author
; ; and
publishing date
type
Contribution to journal
publication status
published
in
Alimentary Pharmacology and Therapeutics
volume
8
issue
6
pages
617 - 622
publisher
Wiley-Blackwell
external identifiers
  • scopus:0027962564
  • pmid:7696451
ISSN
0269-2813
DOI
10.1111/j.1365-2036.1994.tb00339.x
language
English
LU publication?
no
id
3aebeb3a-c0ec-4a88-9346-05bc56b65651
date added to LUP
2019-05-25 08:59:14
date last changed
2021-09-12 03:03:01
@article{3aebeb3a-c0ec-4a88-9346-05bc56b65651,
  abstract     = {{METHODS: <br/><br/>The retrograde spread of two budesonide enema formulations with different viscosities was investigated. The study design was open, randomized and two-period crossover. Three female and two male patients (age range: 35-45 years) with distal ulcerative colitis or proctitis participated. Both enema formulations contained a dose of 2 mg budesonide/100 mL. An unabsorbable radioactive marker (99mTc-labelled human serum albumin microcolloid) was added to the enema just before administration. All doses were given in the evening with the patients lying in a supine position during the whole investigation. The intestinal spread was followed for 8 h using scintigraphic imaging. Plasma samples for budesonide assay were taken during the 12 h after administration of the low viscosity enema.<br/><br/>RESULTS: <br/><br/>Budesonide plasma levels were measurable for up to 4-6 h. Cmax was 2.5 nmol/L (range: 0.9-4.5 nmol/L) and was attained in 1.5 h (range 1-3 h). The patients had no difficulty in retaining the enemas. There was a statistically significant difference in spread between the low and high viscosity enema. The low viscosity enema spread over an area situated between the rectum and the splenic flexure. The spread occurred mainly in the first 15 min after administration. In contrast, the high viscosity enema, in most cases, spread only over a minor part of this area and the rate and extent of spreading was also more variable with this formulation.<br/><br/>CONCLUSION: <br/><br/>The spread of a low viscosity enema appears to be well suited for the treatment of proctitis and distal colitis.<br/>}},
  author       = {{Nyman-Pantelidis, Margareta and Nilsson, Åke and Wagner, Zoltan and Borgå, Olof}},
  issn         = {{0269-2813}},
  language     = {{eng}},
  month        = {{12}},
  number       = {{6}},
  pages        = {{617--622}},
  publisher    = {{Wiley-Blackwell}},
  series       = {{Alimentary Pharmacology and Therapeutics}},
  title        = {{Pharmacokinetics and retrograde spread of budesonide enemas in patients with distal ulcerative colitis}},
  url          = {{http://dx.doi.org/10.1111/j.1365-2036.1994.tb00339.x}},
  doi          = {{10.1111/j.1365-2036.1994.tb00339.x}},
  volume       = {{8}},
  year         = {{1994}},
}