Many active substances are poorly soluble in water. However, the active substance release and bioavailability may be optimized by specific optimized formulation and process methods depending on the physico-chemical property of the active substance, allowing for the desired pharmaceutical effect to be achieved.
One way to improve the release of poorly soluble substances is the embedding of the active substance in a polymer-active ingredient matrix. Poorly soluble, crystalline substances are converted to amorphous co-precipitates – a kind of mixed crystal – depending on their degree of solubility. The supersaturated solutions obtained in this process provide optimized bioavailability.
Another possibility is the adsorption of an active ingredient – micronized to fine dust or nano-ground – on substances with a large geometric surface. The combination of very fine drug particles and a high surface area allows for improved drug release and bioavailability.
A further possibility is the dissolution of the active ingredients in emulsions, micelles, or mixed micelles. They are then converted to solids by adsorption of these solubilizates to a powder or a mixture of powder with a large geometric surface.
Take advantage of our intelligent solutions for optimized bioavailability!
Controlled drug release
The controlled release of active substances and targeted transport to the site of action can significantly improve the therapeutic profile of a drug. With our expertise and our innovative technologies, we are able to achieve targeted release profiles, which are decisive for the application of the respective drug. Tailor-made for optimal therapy success.
Depending on the requirements, we assist you in the formulation and process development to achieve an individual adaptation of the dissolution profile based on the specific drug:
Fast drug release
With specific formulation approaches and process technologies, we are able to develop a drug formulation with a fast release. Even with poorly soluble drugs, a rapid release in accordance with your objectives can be achieved.
Modified, delayed drug release
We have specific know-how and effective methods to achieve modified or delayed release profiles. These aim to maintain the therapeutic plasma level over a period of time in order to extend the intake intervals of the drug. This provides, for example, reduced side effects and a distinctly higher patient compliance and drug loyalty. A delayed release of the active ingredient is suitable particularly for long-term therapies.
Targeted drug delivery in the gastrointestinal tract
Acid-sensitive drugs that are to be delivered to the intestinal tract must be formulated to be resistant to gastric juice. With pH-dependent, enteric polymer coatings, we can achieve a targeted release in the intestine. In addition, we are able to control the release at the desired site with even more differentiation, if needed.
Pulsatile drug release
A pulsatile release formulation allows a targeted drug release at certain times in coordination with the day-night rhythm of endocrine molecules. This can prevent a release at night, for example. Depending on the desired therapeutic effect, the active ingredient is released either time-controlled, i.e., within a certain period of time, or limited to a specific site of action – in a certain part of the gastrointestinal tract, for example. A pulsatile release profile thus requires an initial time delay in the drug release, followed by a more or less rapid complete release of the drug at the desired site of action.
Thanks to our years of experience with different release types, we are able to offer modular solutions for the development of corresponding pharmaceutical products.
Benefit from customized release options. Individually tailored to your specific requirements.
If a drug has an unpleasant taste, taking it can be torturous. A bitter or sour taste is perceived by many people as repulsive. With unpleasant tasting APIs, it is therefore necessary to mask the taste to achieve optimal patient compliance. These days, taste masking is a must for pediatric, geriatric, and veterinary drugs.
We have many years of experience and proven expertise in the taste masking of APIs. With our technologies and formulation approaches, we are able to achieve effective taste masking of drugs.
A proven approach is the micro-pelletizing of APIs with the subsequent application of functional coatings. Micropellets with a very high active ingredients content can be manufactured with our innovative MicroPX™ and CPS ™ technologies, for example. The active ingredients are hereby incorporated directly into the pellet matrix, without the use of starter pellets.
The taste-masked APIs can then be processed in different forms, including dispersible tablets, ODTs, chewable tablets, sachets, stick packs, straws, or oral fluids. For best possible patient compliance.
Take advantage of our know-how and our technical solutions for taste masking your APIs! For increased drug loyalty and optimized therapy success.