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Related Concept Videos

What is Monogastric Digestion?01:50

What is Monogastric Digestion?

The human body contains a monogastric digestive system. In a monogastric digestive system, the stomach only contains one chamber in which it digests food. Several other animal species also have monogastric digestive systems, including pigs, horses, dogs, and birds. This chapter, however, focuses on the human digestive system.
Stomach pH Regulation01:21

Stomach pH Regulation

The human body carefully regulates the internal pH of different organs to maintain homeostasis. For example, while the blood plasma maintains a neutral pH of 7, the stomach lumen has an acidic pH of 1.5 - 3.5. The low pH of stomach lumen helps kill pathogens in the food and break down complex food molecules.
The acid-secreting gastric mucosal epithelial cells (parietal cells) lining the stomach lumen maintain the low pH in the lumen. Numerous ion transporters and channels on these parietal...
Acid Suppressive Drugs for Peptic Ulcer Disease: Antacids01:31

Acid Suppressive Drugs for Peptic Ulcer Disease: Antacids

In the complex environment of the gastric lumen, excessive acid secretion can lead to the formation or worsening of ulcers within the delicate mucosal layer. Antacids, such as sodium bicarbonate and calcium carbonate, provide relief by neutralizing this acid, transforming it into harmless salt and water. This neutralization process raises the gastric pH from a highly acidic level of 1 to a more basic 3-4, reducing the acidity within the stomach.
However, this neutralization reaction between...
Gastric Phase of Digestion01:26

Gastric Phase of Digestion

The gastric phase of digestion begins as soon as food enters the stomach. The incoming food bolus triggers neural and hormonal mechanisms, which last approximately 3 to 4 hours. During this phase, the stomach undergoes significant changes to prepare the food for further digestion and absorption.
When food enters the stomach, it stretches the stomach walls and activates stretch receptors. This triggers local reflexes of the enteric nervous system, mediated through the myenteric plexus. These...
Mucosal Barrier of the Stomach01:25

Mucosal Barrier of the Stomach

The gastric glands contain parietal cells that secrete hydrochloric acid (HCl) for digestion. The cells secrete HCl because it is highly corrosive and essential for breaking down food. To achieve this, they secrete hydrogen and chloride ions into the lumen of the gastric glands, which combine to form HCl.
Within parietal cells, carbonic acid is first formed through the reaction of water and carbon dioxide. The dissociation of carbonic acid releases bicarbonate and hydrogen ions. The bicarbonate...
pH Homeostasis01:31

pH Homeostasis

Acid-base homeostasis is essential for maintaining normal physiological activities in humans. The pH of various body fluids is strictly regulated because it is critical for the optimal activity of enzymes involved in metabolic reactions. Enzymes are basically proteins, so, any significant change in pH can affect their structure and activity. In humans, pH is regulated using three primary mechanisms— chemical buffer systems, respiratory regulation, and renal regulation.
Respiratory Regulation of...

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Supersaturation in human gastric fluids.

Jan Bevernage1, Bart Hens, Joachim Brouwers

  • 1Laboratory for Pharmacotechnology and Biopharmacy, KU Leuven, Herestraat 49, Leuven, Belgium.

European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V
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Drug supersaturation in human gastric fluids is unstable, with limited inhibition by common excipients. These findings suggest targeting drug supersaturation to the intestine for improved stability and efficacy.

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Physical Chemistry

Background:

  • Poorly soluble drugs often exhibit limited oral bioavailability.
  • Supersaturation is a strategy to enhance drug dissolution and absorption.
  • Gastric fluid conditions can impact drug solubility and stability.

Purpose of the Study:

  • To investigate supersaturation and precipitation of five poorly soluble drugs in gastric fluids.
  • To assess the precipitation inhibition by common pharmaceutical excipients.
  • To compare drug behavior in human gastric fluids (HGFs) versus simulated gastric fluids (SGF and FaSSGF).

Main Methods:

  • Induction of supersaturation via solvent shift in HGFs, SGF, and FaSSGF.
  • Time-dependent assessment of supersaturation and precipitation.
  • Evaluation of precipitation inhibition by Eudragit® E PO, HPMC-E5, and PVP K25.

Main Results:

  • All model drugs achieved supersaturation in HGFs, but were largely unstable, precipitating rapidly (except itraconazole).
  • HPMC-E5 and Eudragit® E PO showed modest stabilization effects; PVP K25 had no effect.
  • Precipitation behavior in FaSSGF mirrored that in HGFs, differing from SGF.

Conclusions:

  • Supersaturation stability in gastric fluids is generally inferior to intestinal fluids.
  • Limited efficacy of excipients in inhibiting precipitation in gastric fluids.
  • Targeting supersaturation to the intestine is recommended for enhanced drug performance.