The Use of Capsule Endoscopy to Determine Tablet Disintegration In Vivo

Abstract

The preferred delivery route for drugs targeted for systemic effect is by oral administration. Following oral administration, a solid dosage form must disintegrate and the drug dissolve, thereafter permeating the intestinal mucosa. Several different in vitro methods are used to investigate these processes, i.e., disintegration tests, dissolution tests, and permeability models. However, the actual behavior of oral dosage forms in the environment of the gastro-intestinal tract is not very well elucidated using these conventional methods. In this study, the use of capsule endoscopy to determine tablet disintegration in vivo was assessed. Panadol and Panadol Rapid (acetaminophen/paracetamol) were used as the test material. The in vivo tablet disintegration behavior in beagle dogs was assessed by the use of capsule endoscopy. The in vitro tablet disintegration behavior was assessed using the European Pharmacopeia (Ph. Eur.) disintegration test. The study showed that the in vivo disintegration times of Panadol and Panadol Rapid were 24.7 and 16.5 min, respectively, when determined by capsule endoscopy, which corresponded to the pharmacokinetic data. By contrast, the in vitro disintegration times of the same formulations were 5.5 and 4.0 min, respectively, when determined by the Ph. Eur. disintegration test. In conclusion, capsule endoscopy can be used to determine the in vivo tablet disintegration behavior. By contrast, the in vitro methods appear to not be predictive of the disintegration behavior in vivo but may be used to rank the order the formulations with respect to disintegration time.

Effects of housing environment on oral absorption of acetaminophen in healthy Beagles

“…One of our objectives was to correlate stomach emptying of acetaminophen with gastric emptying time measured with a telemetric motility capsule. However, we judged our results to be excessively long, compared with results of previous studies, 1,14,15 and not representative of the true gastric emptying time in these dogs. Delayed gastric emptying of the capsule may have been a result of the large size of the telemetric motility capsule (13 X 27 mm) we used.…”

“…A cetaminophen has historically been used as a marker drug for evaluation of gastrointestinal absorption. [1][2][3][4][5][6] Because the rate of drug absorption is dependent on the rate at which the stomach delivers the drug to the small intestine, the rate of absorption reflects the gastric emptying time. The motility of the gastrointestinal tract is directly influenced by the autonomic nervous system.…”

A review of emerging technologies enabling improved solid oral dosage form manufacturing and processing

“…Capsule endoscopy involves oral administration of a non-invasive capsule supplied with two cameras at both ends which can provide video recording. Blaabjerg et al employed this technique for visualizing the disintegration / dissolution behaviour of acetaminophen tablets in beagle dogs [262]. Despite of its ease of administration and integrity of sensor in the body, this technique encounters limited wireless communication and lacks an efficient control of the sensor [263].…”

Video Capsule Endoscopy and Ingestible Electronics: Emerging Trends in Sensors, Circuits, Materials, Telemetry, Optics, and Rapid Reading Software

“…When the copper coils were electrically activated, the magnetic force detached the drug chamber from capsule's body to release the drug in its vicinity. In a separate study to determine the timeline of tablet disintegration within the gastrointestinal tract, paracetamol tablets were retrofitted to an ingestible capsule and administered to beagle dogs [135]. The time taken for tablet's in vivo dissolution was obtained from its plasma concentration profile and visual confirmation from the camera capsule.…”