Bioavailability and Dissolution Properties of two Commercial Digoxin Tablets

Klink, Paul R.; Poust, Rolland I.; Colaizzi, John L.; McDonald, Robert H.

doi:10.1002/jps.2600630813

Cited by 24 publications

(8 citation statements)

References 13 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…It is well known that the bioavailability of digoxin preparations was reported to vary significantly (Ampoulsuk et al 1974, Klink et al 1974. The main cause of this variability appears to be related to such factors as low water solubility and chemical instability in acidic media (Khalil andEl-Masry 1978, Chiou andKyle 1979).…”

Section: Introductionmentioning

confidence: 97%

Development of digoxin dry elixir as a novel dosage form using a spray-drying technique

Kim

Yoon

1995

Journal of Microencapsulation

View full text Add to dashboard Cite

A rapidly absorbed new novel oral dosage form for digoxin termed 'digoxin dry elixir' was developed by the spray-drying technique. Digoxin, dextrin and sodium lauryl sulphate were dissolved in a ethanol-water mixture (20:25 w/w) and therefore spray-dried to form the digoxin dry elixir. According to scanning electron micrographs, digoxin dry elixir is spherical in shape with a smooth surface. The geometric mean diameter of dry elixir determined by laser particle size analysis was about 13 microns. The appearance and flow properties were almost unchanged and about 10% of ethanol contents in the dry elixir decreased during 180 days in a sealed bottle at room temperature. Comparative studies on the in vitro dissolution and in vivo absorption of digoxin in the form of digoxin dry elixir, digoxin elixir and digoxin powder were carried out. Digoxin in the dry elixirs was completely dissolved within 2 min. On the other hand, only about 87% of digoxin powder dissolved in 60 min. The initial dissolution rates of digoxin in the dry elixirs markedly increased in distilled water at 37 degrees C, which were over 100 fold higher than that of digoxin powder alone. The maximal plasma concentration of digoxin (Cmax) and area under the digoxin concentration-time curve from zero to 6 h (AUC0-6h) after the oral administration of digoxin dry elixir were almost 3.8 and 5.5 fold increased compared to digoxin powder alone. No significant difference of AUC0-6 h between dry elixir and elixir was observed, but the Cmax of digoxin in the form of dry elixir was significantly reduced compared to the digoxin elixir (0.57 versus 0.83). Digoxin dry elixir might be a useful solid dosage form to improve the dissolution rate and bioavailability of poorly water-soluble digoxin compared to digoxin powder alone. It also indicates that dry elixir might reduce the side effects in oral digitalis glycoside therapy compared to the digoxin elixir due to the reduction of Cmax.

show abstract

Section: Introductionmentioning

confidence: 97%

Development of digoxin dry elixir as a novel dosage form using a spray-drying technique

Kim

Yoon

1995

Journal of Microencapsulation

View full text Add to dashboard Cite

show abstract

“…Of the various methods studied, the urinary excretion of digoxin was the most valid measure of bioavailability of oral digoxin preparations. The bioavailability and dissolution properties of two commercial digoxin tablets and an elixir were evaluated (1239). The elixir form gave much higher blood levels than either tablet during the first two sampling times, but the two tablets showed nearly identical blood levels and relative bioavailabilities.…”

Section: Bioph Armaceuticsmentioning

confidence: 99%

Pharmaceutical Sciences—1974: Literature Review of Pharmaceutics

Haleblian¹,

Goodhart²

1975

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

“…Several comprehensive listings of chemical ionization and electron-impact mass spectra are available for comparison with spectra of unknown drugs (1)(2)(3). Successful identification of drug metabolites and multicomponent drug mixtures, such as those received by forensic laboratories, is an excellent example of the utility of chemical ionization mass spectrometry.…”

Section: To the Editormentioning

confidence: 99%

“…A recent report by Klink et al (1) indicated that the "paddle-water" method for determining dissolution rates for digoxin tablets failed to reflect the comparative bioavailability properties of two commer-The dissolution properties of six tablets each from Treatment I1 and Treatment 112 tablets were determined using the USP rotating-basket apparatus and employing the conditions specified in the USP (9). Samples were withdrawn and assayed by a fluorometric method (10) at 15, 30, 60, and 120 min after commencement of the studies.…”

Section: To the Editormentioning

confidence: 99%