Raytor facilitates efficient and compliant R&D of orally soluble film formulations

Twin Engines of Oral Formulation Development

Hello, everyone! Let's go to talk to you about a super interesting pharmacy "metamorphosis" - the conversion of oral drugs into oral absorption formulations!

Oral membrane agents hold good promise for research, but there are a lot of doors, especially for dissolution and absorption at the mouth that need extra attention.

Why do we need to change our "medication posture"?

Conventional oral medications are "blocked" by the liver as they pass through the stomach and intestines (first-pass effect), resulting in a decrease in the amount of medication that is actually absorbed. Oral mucosal absorption bypasses this barrier and allows the drug to "shortcut" into the bloodstream! This results in lower doses and fewer side effects. However, due to the differences between the oral environment and the regular gastrointestinal environment, drug release needs to be re-examined.

Dissolution Pass:

Oral environment must be simulated to test the rate of drug release

RT6 Automated Dissolution System (Small Cup Method) can meet the needs of dissolution studies of oral preparations.

As a representative tool for oral solid dosage formulations, RT6 Automated Dissolution System can meet the needs of oral dosage form dissolution research. However, since the volume required for oral dissolution is relatively small compared with that of gastrointestinal dissolution, it is necessary to choose a dissolution cup that simulates the dissolution environment of the oral cavity to carry out oral dissolution experiments, and we generally recommend the use of a dissolution cup with a volume of 250 mL.

Raytor Instruments Small Cup Method Kit

Absorption pass: validation of mucosal osmotic efficiency

Raytor Instruments NCE Micro Dissolution and Permeation Analyzer

We recommend Raytor Instruments NCE Micro Dissolution and Permeation Analyzer to test the mucosal osmotic efficiency, and we also conducted experiments on oral and conventional drug delivery formulations and made comparisons, and the results are as follows:

	API Comparison	Original formulation (oral)	Original formulation (oral)
Ingredient	API	API + Accessories 1	API + Accessories 2
Physiological condition	Human intestine	Human intestine	Human intestine
Peff	-3.5961	-3.5306	-3.5474
Penetration enhancement rate	—	+18.4%	+12.1%

Oral medication: large intestinal area (200 m²!) , stays for 4-6 hours, influenced by gastric emptying and intestinal fluids → "large volume and fullness"

Oral soluble drugs: small oral area (only 100 cm²), stay 0.5-1 hour, direct exposure to high concentrations → "delicate fast food"

Although the penetration rates are close, different sites of administration can lead to inconsistent final therapeutic effects.

Conclusion:

Absorption ≠ bioequivalence, innovative formulations need to consider both drug dissolution site and penetration capacity, one or the other.

Want to let the oral soluble drugs "combat power" upgrade?

Raytor gives two directions:

For the above analysis of drug design, we found that based on the framework of permeability and dissolution, we can at least enhance the prescribing ability of innovative drugs to improve their bioefficacy in the clinic through the dual escort of Raytor Instruments RT6 Automated Dissolution System + NCE Micro Dissolution and Permeation Analyzer.

-One second simulation of the "battle environment" at different absorption sites.

-Accurately predict the dissolution + penetration effect of the modified prescription

-Save money and time, less waste of time!

Modification of dosage forms is not a simple "change of place to eat", it has to use data to speak! Want to play with innovative formulations? Raytor Instruments RT6 Automated Dissolution System + NCE Micro Dissolution and Permeation Analyzer are your "pharmacy calculators"!