Abstract：
:Rizatriptan produces antimigraine activity by acting as selective agonist of 5-HT1B and 5-HT1D receptors present on intracranial and extracerebral blood vessels. Absorption from oral tablet is slow with Tmax of approximately 1-1.5 h. A few attempts have been made to promote rapid absorption such as oral or sublingual films with limited success. The aim of our study was to develop intranasal spray formulation of rizatriptan with quick onset of action. Solubility was enhanced by a co-solvent system where we studied solubility of rizatriptan benzoate in pure solvents, binary and ternary mixtures. Binary and ternary co-solvents using ethanol, water, propylene glycol and polyethylene glycol resulted rizatriptan equivalent base solubility more than 60 mg/mL. Same co-solvents were used at different level to make nasal spray formulations and evaluated pharmacokinetics using beagle dog animal model. Nasal spray formulation containing 20% w/w ethanol exhibited highest exposure, where Cmax (312 ng/mL) reached in 5 min and maintained higher concentration than oral dose for more than 30 min.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Chokshi A,Vaishya R,Inavolu R,Potta Tdoi
10.1016/j.ijpharm.2019.118702subject
Has Abstractpub_date
2019-11-25 00:00:00pages
118702eissn
0378-5173issn
1873-3476pii
S0378-5173(19)30747-1journal_volume
571pub_type
杂志文章abstract：:The aim of this research was to study the gastrointestinal transit and gastric emptying of non-disintegrating solid dosage forms in rats using X-ray imaging. Commercial gelatin minicapsules were filled with barium sulfate and enterically coated using Eudragit S100. The capsules were administered orally to rats followe...
journal_title：International journal of pharmaceutics
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