Sustained and Controlled Drug Release Technology
Introduction
Sustained Release Technology enables a controlled and consistent release of an active ingredient from a lozenge held within the mouth over a prolonged period of time. Delivery of active ingredients under the tongue (i.e. sublingual delivery) is an ideal mode of delivery as blood flow under the tongue is high. Sustained Release Technology presents an attractive alternative to more traditional oral delivery methods, as it not only avoids the first-pass effect, but its direct absorption into the blood stream enables the desired effects to be seen much faster. This technology will revolutionize drug administration, making drugs easier to take (e.g. for those who can’t swallow or have fear of needles), and avoiding the need for frequent dosing.

The Technology
Sustained Release Technology allows the creation of long lasting, flavoured lozenges for sustained release of beneficial agents within the mouth over a desired period of time. This release period can be varied from minutes to up to 2 hours.

Existing oral sustained release systems cannot provide optimal delivery of beneficial agents in the mouth as lozenges based on such systems can last for only a matter of minutes. For instance, halitosis - commonly known as bad breath - is often treated with flavored lozenges and gums that deliver pharmacologically active agents. Another example is nicotine gum taken to assist in smoking cessation. However, most flavored lozenges dissolve in several minutes, and therefore provide only a very short-term effect. Similarly, most gums tend to release substantially all of a beneficial agent (e.g., a flavoring agent or a pharmacologically active agent such as nicotine) in well under half an hour.

Dosage forms for sustained release of beneficial agents in the mouth can be problematic in other ways as well. For example, commercially available zinc lozenges for treating the common cold tend to dissolve or degrade in well under 15 minutes. To the best of our knowledge, no zinc lozenge has been able to provide sustained release of zinc for over 40 minutes, but this was achieved through Sustained Release Technology. Please refer to Graph 1 below which shows that zinc is consistently released over 2 hours through the use of Sustained Release Technology. The release of active ingredients over a sustained and prolonged period of time is desirous to treat medical ailments.

Vivo Release Kinetics for Zinc Lozenge Graph
Graph 1: In Vivo Release Kinetics for Zinc Lozenge

In summary, Sustained Release Technology has the following advantages:

  • Long-lasting and controlled release of drugs, flavours or other desired active ingredients
  • Linear first order drug release kinetics
  • Release period can be varied from minutes to up to 2 hours
  • Matrix consists of natural ingredients
  • Removes the need for frequent dosing
  • Active ingredients reach the blood stream faster than if delivered orally
  • Bypasses the gastro-intestinal system, hence reducing side effects

SUSTAYN™ Caffeine Lozenges
Lynk Biotechnologies is taking the Sustained Release Technology to new heights through the development and manufacture of the first sustained release peppermint-flavoured caffeine lozenge. These lozenges will release caffeine at a controlled and consistent rate, enabling coffee drinkers and mint poppers alike to maintain their caffeine buzz throughout the duration of the lozenge dissolution. This will not only keep their breath fresh, but keep them alert as well. A major additional advantage of such a controlled release mechanism is the absence of any sudden highs and lows in caffeine absorption usually experienced through taking caffeinated beverages. Please note that this product is currently not available for sale commercially. If you are interested in evaluating the prototypes or are keen to market the product, please contact us at business@lynkbiotech.com.
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