Influence of Dispersion Method on Dissolution Rate of Digoxin–Lactose and Hydrocortisone–Lactose Triturations I

Ampolsuk, Chareonsri; Mauro, James V.; Nyhuis, Alan A.; Shah, Navnit; Jarowski, Charles I.

doi:10.1002/jps.2600630131

Cited by 25 publications

(7 citation statements)

References 6 publications

(3 reference statements)

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“…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: 98%

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

Kim

Yoon

1995

Journal of Microencapsulation

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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.

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Section: Introductionmentioning

confidence: 98%

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

Kim

Yoon

1995

Journal of Microencapsulation

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“…Two pentapeptides, methionine-enkephalin and leucine-enkephalin, were identified (4) and postulated to be endogenous ligands for the opiate receptors in mammalian brain (5)(6)(7)(8). Both peptides mimic the ability of morphine to inhibit electrically induced contractions of the guinea pig ileum and mouse vas deferens.…”

mentioning

confidence: 99%

Solvent Deposition Method for Enhancement of Dissolution Rate: Importance of Drug-to-Excipient Ratio

Johansen¹,

Møller

1978

Journal of Pharmaceutical Sciences

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“…In an earlier report (9), it was shown that the application of frictional force to digoxin-lactose or hydrocortisone-lactose blends produced 1:20 triturations with markedly improved dissolution rates. Thus, for example, at the end of 60 min, 91.7 f 3.5% of digoxin had dissolved in simulated gastric fluid whereas a simple blend of 325-mesh digoxin and powdered lactose exhibited 65.4 f 5.2% dissolution at the end of 120 min.…”

mentioning

confidence: 99%

“…This procedure was described in an earlier publication (9). It was established that a saturated solution of digoxin in simulated gastric fluid contained 188.8 mg/200 ml (shaking for 13 days at 37").…”

mentioning

confidence: 99%

Influence of Dispersion Method on Dissolution Rate and Bioavailability of Digoxin from Triturations and Compressed Tablets II

Shah

Pytelewski

Eisen

et al. 1974

Journal of Pharmaceutical Sciences

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Influence of Dispersion Method on Dissolution Rate of Digoxin–Lactose and Hydrocortisone–Lactose Triturations I

Cited by 25 publications

References 6 publications

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

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

Solvent Deposition Method for Enhancement of Dissolution Rate: Importance of Drug-to-Excipient Ratio

Influence of Dispersion Method on Dissolution Rate and Bioavailability of Digoxin from Triturations and Compressed Tablets II

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