Oral dosage forms must pass the gastrointestinal tract before the active ingredient (API) can reach the blood circulation and its target. Depending on the API’s properties and the desired therapeutic effect, some can be immediately released in the stomach, while others should be released in a specific portion of the intestine and/or for a prolonged time. The following graph depicts some examples of controlled/modified release:
(concentration in the blood stream)
1: classical drug release profile
2: immediate release
3: delayed release
4: sustained release
Drug substances which are sensitive to the acidic environment of the stomach or which may harm the gastric mucosa are frequently transferred into gastro-resistant forms. By this means, drug release into the acidic stomach medium can be avoided whereas drug release into the intestine or colon can be achieved due to the pH dependent solubility of gastro-resistant polymers.
Pulsatile-release drug formulations can be used to avoid drug product applications during night time or to mimic the circadian rhythms of endocrine molecules. The drug is released either site-specific (drug release at the desired site within the intestinal tract) or time-controlled (drug release following a defined time period).
A pulsatile-release profile is characterized by a lag time followed by a more or less rapid and complete drug release.
Immediate release dosage forms release the active drug(s) within a short time (e.g. 80% of drug after 60 min.). Depending on the applied formulation and process technologies, even faster drug release can be achieved.
Modified release formulations show a sustained (= extended or delayed) release of the drug. The modified release concept is appropriate for drugs with short half-life to maintain therapeutic plasma concentrations over a longer period of time. The administration intervals can then be reduced. Moreover, high plasma peak levels which go along with side effects can be optimised. Modified release formulations are important for long-term treatment.
Thanks to our extended expertise with the different types of drug release kinetics, at Glatt Pharmaceutical Services, we can provide modular solutions for the development of your pharmaceutical products. Learn more about how we could help you by contacting us at pharmaceuticalservices@glatt.com
Here are some examples of controlled release formulations we can develop for you:
- Functional coating
- Matrix pellets à CPS, MicroPx (+details)
- Matrix tablets
- Mini-tablets
- Coating of mini-tablets à Wurster
- Coating of pellets à Wurster
- Dry suspension for reconstitution à spray granulation or pellets