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AuthorPaprskarova, Alice
AuthorMozna, Petra
AuthorOga, Enoche F.
AuthorElhissi, Abdelbary
AuthorAlhnan, Mohamed A.
Available date2021-06-07T09:59:14Z
Publication Date2016
Publication NameAAPS PharmSciTech
ResourceScopus
URIhttp://dx.doi.org/10.1208/s12249-015-0444-4
URIhttp://hdl.handle.net/10576/20542
AbstractSupersaturation and precipitation are common limitations encountered especially with poorly soluble basic drugs. The aims of this work were to explore the pattern of dissolution and precipitation of poorly soluble basic drugs using a United States Pharmacopoeia (USP) IV dissolution apparatus and to compare it to the widely used USP II dissolution apparatus. In order to investigate the influence of gastric emptying time on bioavailability, tables of two model drugs (dipyridamole 100 mg and cinnarizine 15 mg) were investigated and pH change from 1.2 to 6.8 were achieved after 10, 20 or 30 min using USP II or USP IV dissolution apparatuses. Using USP II, dipyridamole and cinnarizine concentrations dropped instantly as a result of drug precipitation with drug crystals evident in the dissolution vessel. At pH change times of 10, 20 and 30 min, the total amount of dissolved drug was dependent on pH change time. Using USP IV, at a flow rate of 8 ml/min, it was possible to have comparable release to agitation at 50 rpm using USP II suggesting that comparable hydrodynamic forces are possible. No drop in drug percentage occurs as the dissolved fraction was readily emptied from the flow cell, preventing drug accumulation in the dissolution medium. However, a negligible percentage of drug release took place following pH change. In conclusion, the use of the flow-through cell dissolution provided laminar flow, use of realistic fluid volumes and avoided precipitation of dissolved drug fraction in the gastric phase as it is discharged before pH change
Languageen
PublisherSpringer New York LLC
Subjectcinnarizine
Subjectdipyridamole
Subjecthydrochloric acid
Subjectcinnarizine
Subjectdipyridamole
SubjectArticle
Subjectdrug accumulation
Subjectdrug solubility
Subjectflow rate
Subjecthigh performance liquid chromatography
Subjecthydrodynamics
Subjectlaminar flow
Subjectlimit of detection
Subjectmedical device
SubjectpH
Subjectpriority journal
Subjectspectrophotometry
Subjectstomach emptying
Subjecttablet disintegration
SubjectUnited States Pharmacopoeia IV dissolution apparatus
Subjectbioavailability
Subjectchemistry
Subjectmetabolism
Subjectphysiology
Subjectsolubility
Subjectstomach
SubjectBiological Availability
SubjectCinnarizine
SubjectDipyridamole
SubjectGastric Emptying
SubjectHydrogen-Ion Concentration
SubjectSolubility
SubjectStomach
TitleInstrumentation of Flow-Through USP IV Dissolution Apparatus to Assess Poorly Soluble Basic Drug Products: a Technical Note
TypeArticle
Pagination1261-1266
Issue Number5
Volume Number17


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