Nelson Vergel
Founder, ExcelMale.com
PED5 Inhibitor Oral Dissolving Tablet (ODT)-
General Information
An orally disintegrating tablet or orally dissolving tablet (ODT) differ from traditional tablets in that they are designed to be dissolved on the tongue rather than swallowed whole.
An ODT is a solid dosage form that disintegrates and dissolves in the mouth (either on or beneath the tongue or in the buccal cavity) without water within 60 seconds or less.
Orally disintegrating tablets offer all the advantages of solid and liquid dosage forms together with special advantages, which include:
- ODT present no risk of obstruction of the gastrointestinal tract, which is beneficial for patients who do not have access to water such as patients who are traveling.
- The rapid disintegration of the resulting tablets results in a quick dissolution of the drug and fast absorption that provide a rapid onset of action (Behnke et al., 2003).
- The bioavailability of drugs that are absorbed in the mouth, pharynx, and esophagus is increased (Jaccard and Leyder, 1985; Dollo et al., 1999; Gafitanu et al., 1991).
- Absorption of drugs before reaching the stomach avoids hepatic metabolism, which reduces the dose and increases the bioavailability of the drug (Clarke et al., 2003). Faster onset of action and higher bioavailability occur via blood vessels under the tongue, rather than through the digestive tract.
- Fast-acting dissolution provides dispersion before being swallowed allowing faster metabolism.
- Allows some of the active ingredient to be absorbed directly into the bloodstream bypassing the patient's hepatic system and first-pass metabolism.
- Disintegration in the mouth within seconds.
- Pleasant taste and mouthfeel for improved compliance.
- No water required.
ABSORPTION DATA
A study done in healthy volunteers (18-50 years) comparing regular vardenafil tablets with an ODT version of the same drug showed improved absorption of the ODT formulation (www.accessdata.fda.gov)
Here are the results:
- The mean maximum blood concentration (Cmax) and total drug exposure (area under the curve or AUC) of vardenafil from the ODT formulation were higher by 15% and 44%, respectively compared to the regular 10 mg vardenafil tablets.
- Total exposure to the ODT formulation was not affected by food. When the ODT formulation was swallowed with water, the AUC of vardenafil was reduced by 29% and median Cmax was shortened by 60 minutes while Cmax was not affected. So, ODT PED5 inhibitor formulations are best taken without liquid.
- The ODT formulation when administered under fasted conditions without water results in an increased bioavailability (BA) of vardenafil (by 44 %) compared to the AUC of 10 mg regular formulation. The increased BA from the ODT is speculated to be due to the contribution of a local absorption component in the oral cavity that bypasses the first-pass metabolism.
- Although not apparent in all individuals, the peak concentrations of vardenafil resulting from the ODT formulation were sustained for a longer duration compared to the regular formulation.
References:
- Behnke, K et al. Journal of Clinical Psychopharmacology: August 2003 - Volume 23 - Issue 4 - p 358-364
- Clarke A, brewer F, Johnson ES, Mallard N, Hartig F, Taylor S. A new formulation of selegiline: improved bioavailability and selectivity for mao-b inhibition. J neural transm 2003; 110:124-5.
- Dollo G, Chevanne F, le Corre P, Chemtob C, le Verge R. Bioavailability of phloroglucinol in pha belg 1999; 54:75-82.
- Gafitanu E, Dumistracel I, Antochi S. Formulations and bioavailability of propyphenazone in lyophilized tablets. Rev med chir soc med nat iasi 1991; 95:127-8.
- Jaccard T, Leyder J. Une nouvelle forme galenique le lyoc. Ann pharm fr. 1985; 43:123-31.
