Assessment of antacid characteristics of drugs containing a combination of aluminium and magnesium salts using the "artificial stomach" model.
Antacid characteristics of three drugs containing aluminium and magnesium salts (combination of clay with aluminium and magnesium hydroxides, aluminium and magnesium hydroxide mixture and hydrotalcite) have been studied in a dynamic situation simulated by the "artificial stomach" model, simultaneously taking into account both gastric fluxes, a constant secretory flux and variable emptying fluxes. Therapeutic doses of the drugs were added 1. to 100 ml of 0.1 N HCl, without or with 1% or 5% meat extract, and 2. 100 ml of pooled human gastric juice (96 mmol/l, pH 1.1). In addition, antacid activity of 0.5 g aluminium and magnesium hydroxides, taken alone or in combination, were evaluated when added to 100 ml of 0.1 N HCl. In aqueous HCl solution or in human gastric juice, the three antacid drugs exhibited 1. a neutralising activity characterised by pH-rise and 2. a buffering capacity close to pH 3.8. In addition, hydrotalcite exhibited also buffering capacity at pH 1.2. The antacid-induced capacity, expressed as H+ mmol, to recover initial pH were very similar, indicating that antacid physiochemical properties are similar in HCl solution or in gastric juice. H+ consumption depended upon emptying fluxes. The same antacid characteristics were observed when antacids were mixed with 1% meat extract while 5% meat extract resulted in a modification of antacid characteristics. Therefore the antacid capacities of respective mixtures were of smaller magnitude (50-60%) than the sum of the activities of antacids plus meat extracts.(ABSTRACT TRUNCATED AT 250 WORDS)
Vatier
J
J
INSERM U 10, Hôpital Bichat, Paris, France.
Vitre
M T
MT
Lionnet
F
F
Poitevin
C
C
Mignon
M
M
D000536:Aluminum Hydroxide / Q000494:pharmacology*; D000818:Animals; D000863:Antacids / Q000494:pharmacology*; D004338:Drug Combinations / Q000494:pharmacology; D005746:Gastric Emptying / Q000187:drug effects; D005750:Gastric Juice / Q000187:drug effects / Q000378:metabolism; D006851:Hydrochloric Acid; D006863:Hydrogen-Ion Concentration; D008274:Magnesium / Q000494:pharmacology*; D008276:Magnesium Hydroxide / Q000494:pharmacology*; D008460:Meat / Q000032:analysis; D008954:Models, Biological; D013270:Stomach / Q000187:drug effects / Q000502:physiology*
D000863:Antacids; D004338:Drug Combinations; C010467:hydrotalcite; C013591:aluminum hydroxide, magnesium hydroxide, drug combination; D000536:Aluminum Hydroxide; D008274:Magnesium; D008276:Magnesium Hydroxide; D006851:Hydrochloric Acid