FAST DISSOLVING PELETS

Introduction into Fast Dissolving Drug Products

Conventional solid dosage forms such as tablets or hard gelatine capsules are mostly taken intact with water or any other suitable liquid. In contrast to these preparations, fast dissolving oral drug products are administered without any liquid at all. The API is delivered upon instantaneous disintegration and/or dissolution of the dosage form without co-administered liquid; absorption of the API occurs locally and/or in the deeper segments of the gastro-intestinal tract. Fast dissolving preparations are ideal dosage forms for patients who have distinct difficulties in swallowing conventional dosage forms.

Fast Dissolving Pellets

Our fast dissolving products are designed as multiple-unit systems, which consist of several thousand spherical particles. These Fast Dissolving Pellets are manufactured using proprietary pelletisation techniques. Fast Dissolving Pellets consist entirely of very water soluble and/or swellable excipients and can be compressed into orally dispersible tablets (ODTs). The typical features of our Fast Dissolving Pellets can be summarised as follows:

Ø Narrow particle size distribution, e.g. 100 - 400 µm

Ø Smooth mouthfeel

Ø Highly water soluble & swellable pharmacopoeial constituents with low hygroscopic behaviour

Ø Addition of flavouring agents possible

Ø Spherical pellets with porous structure; porosity facilitates disintegration and dissolution

Ø Mechanically very stable; easy product handling

Ø Packaging into conventional stick packs feasible

Ø Pellets can be compressed into oral dispersible tablets (ODTs)

The dissolution behaviour of typical Fast Dissolving Pellets, e.g. with Loperamide and Zopiclone as APIs, is depicted below. The SEMs reveal the porous structure of Fast Dissolving Pellets, which facilitates and ensures instant disintegration and dissolution.

TIMED RELEASE PRODUCTS

Significant research and efforts are directed towards drug delivery systems, which are suited to:

Ø Control the onset time of drug release and/or

Ø Deliver the active ingredient to distal sites within the gastro-intestinal tract (GIT)

These delivery devices are in particular advantageous for drugs/dosage forms with the following features and/or needs:

Ø Circadian variations in pharmacokinetics and/or pharmacologic responses

Ø Requirement of night-time dosing or multiple dosing intervals

Ø Need to deliver the active ingredient to distal parts of the GIT

ADD Technologies Ltd has established a platform technology, which is suited to control the onset of drug release (Figure 1) and release rate of oral delivery devices with superior reproducibility and low system variability. Also multiple pulse systems can be realised with this technology (Figure 2). Drug release is pH-independent.

The final dosage form is presented as hard-gelatine capsule, tablet or sachet.

Figure I: In vitro dissolution profiles of products with differing onset times

Figure 2: In vitro dissolution behaviour of multiple pulse systems

The profiles below (Figures 3 - 6) illustrate the in vitro and in vivo performance of clinical test preparations with differing delayed release characteristics developed with the proprietary technology. Prototype I exhibits a shorter onset time, Prototype II a prolonged lag-phase in vitro and in vivo as well.

Figure 3: In vitro dissolution of Prototype I

Figure 4: In vivo performance of Prototype I

Figure 5: In vitro dissolution of Prototype II

Figure 6: In vivo performance of Prototype II