Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
7
pubmed:dateCreated
1997-9-2
pubmed:abstractText
Nasal drug delivery is an interesting route of administration for dihydroergotamine in migraine therapy. The currently available formulation contains dihydroergotamine at 4 mg/mL. For a nasal dose of 2 mg, a volume of 0.5 mL has to be administered, which sometimes leads to spillage of the formulation. The aim of the present study was to develop a nasal spray with a dihydroergotamine concentration of 10 mg/mL. To increase the solubility and stability of dihydroergotamine, randomly methylated beta-cyclodextrin was used. Liquid formulations and lyophilized powders of dihydroergotamine and randomly methylated beta-cyclodextrin were prepared. The liquid and powder formulations were compared by determining their pharmacokinetics and absolute bioavailability after nasal administration in rabbits. Nasal sprays were significantly more effective than drops in increasing the nasal bioavailability of dihydroergotamine, but the amount of randomly methylated beta-cyclodextrin in liquid sprays did not significantly alter the nasal absorption. For powder formulations, the dihydroergotamine absorption was dependent on the amount of methylated beta-cyclodextrin and powder volume, and the nasal bioavailability from the optimal powder was slightly, but not significantly, higher than that for liquids. In conclusion, the formulations investigated are a substantial improvement of the current commercial formulation, not only because the spray volume of the liquid spray can be reduced 2.5 times, but also because of the increased stability of liquid and powder sprays with randomly methylated-beta-cyclodextrin.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jul
pubmed:issn
0022-3549
pubmed:author
pubmed:issnType
Print
pubmed:volume
86
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
802-7
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1997
pubmed:articleTitle
Nasal absorption of dihydroergotamine from liquid and powder formulations in rabbits.
pubmed:affiliation
Leiden/Amsterdam Center for Drug Research, Division of Pharmaceutical Technology and Biopharmaceutics, The Netherlands.
pubmed:publicationType
Journal Article, Comparative Study