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

The influence of digoxin particle size on absorption of digoxin and the effect of propantheline and metoclopramide.

“…Florence, Salole & Stenlake (1974) reported increased dissolution rate of digoxin after milling to reduce particle size. Shah, Pytelewski, Eisen & Jarowski (1974) confirmed that milling of digoxin enhanced its dissolution rate and also demonstrated significantly increased peak blood levels of digoxin in rats following oral administration of digoxin milled with lactose as compared to unmilled digoxin and lactose. Jounela, Pentikainen & Sothman (1975) have also demonstrated significantly lower bioavailability from digoxin tablets of large particle size material given to healthy volunteers.…”

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

“…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.…”

Pharmaceutical Sciences—1974: Literature Review of Pharmaceutics

“…Evaluation of pharmacological response intensities showed evidence for variable digoxin absorption (1118). Ball milling or Muller milling digoxin with a 20-fold excess of lactose, sucrose, dibasic calcium phosphate, or microcrystalline cellulose significantly enhanced its dissolution rate (1119). Tablets prepared with such triturations also exhibited superior rates of dissolution.…”