Orodispersible Mini-tablets based on galenIQ™ 721

Orodispersible mini-tablets (ODMTs) are becoming increasingly more important to pharmaceutical companies, as the clinical benefit for peadiatric patients has been proven. In literature mini-tablets are described as solid dosage forms with a diameter of 2-3 mm. In this study ODMTs should be produced by using a direct compression grade of isomalt galenIQ™ 721. Enalapril maleate (EM) was chosen as a model drug, as the therapeutic need of this drugs for children is well known. The study should evaluate the potential of galenIQ™ 721 for producing mini-tablets with respect to
content uniformity, disintegration time, drug release, tensile strength and stability.

See the explanation of the research results in the following video recorded at CPhI in Frankfurt
and have a look at the poster below.

Read the transcript of the poster presentation by Ard Lura from the university of Düsseldorf/Germany:

Hello. My name is Ard Lura, and I’m a PhD student in the Institute of Pharmaceutics and Biopharmaceutics in Düsseldorf.

My research topic is mini-tablets. Mini-tablets are solid dosage forms, with a diameter of two to three millimeters, that can be produced on conventional tablet presses but we have to use specific toolings, for example, multi-tips.

In this study, we had a collaboration with Beneo where we wanted to check the feasibility of Isomalt for producing orodispersible mini-tablets. Mini-tablets are gaining more importance to pharmaceutical companies, as clinical studies show the clinical benefit of those. In those clinical studies, it was proven that even neonates can swallow and accept mini-tablets. Furthermore, the European regulatory show and encourage (the) pharma industry to implement PIPs in order so they can develop suitable dosage forms for children.

So, based on those clinical studies, mini-tablets show the possibility to fulfill those requirements. In this study, Isomalt was investigated for producing orodispersible mini-tablets. We chose Enalapril maleate as a model API, as this drug is also listed on the essential list of medicines for children. We tried to produce orodispersible mini-tablets on a rotary tablet press by using 90 tips, multi-tips from Ritter. In this study, we wanted to gain orodispersible mini-tablets.

So when you have a look at the definition of mini-tablets, the European pharmacopeia defines orodispersible tablets as tablets that disintegrate within three minutes. On the other hand, the FDA defined orodispersible tablets which will disintegrate in the oral cavity within 30 seconds.

So based on this knowledge, we got the following results. If we just incorporate Isomalt as a filler with our API, we get orodispersible tablets which will disintegrate within three minutes. By incorporating a super disintegrant, like Kollidone CL or Kollidone CLSF, we could even meet the criteria, as you can see here, of the FDA.

Furthermore, we checked that the acceptance value of our tablets. We could reach, for all three formulations, acceptance values which were equal or lower than 15. Our dissolution studies also showed that we have an immediate release dosage form.

The tensile strength also showed good results, regarding the stability of the mechanical properties of our tablets. But nevertheless, with respect to the stability studies, we checked those under ambient conditions. We focused on the disintegration time, but also on the tensile strengths as two main properties for orodispersible tablets because we thought that those were two properties that would determine afterwards the compliance of the patients, especially of the pediatrics. If you got too hard ODMTs, which could lead to an unpleasant mouthfeel in the oral cavity of the pediatrics, or if the disintegration time is not any more orodispersible within the stability studies, we can’t talk about orodispersible mini-tablets anymore.

But nevertheless, we showed, in both studies, that orodispersible properties, as well as the tensile strengths, did not change that much that we doesn’t meet these quality attributes we set before.

So to conclude this project, we were able to produce mini-tablets with Isomalt which fulfills the criteria of the European pharmacopeia, but also of the FDA, when we incorporated the superdisintegrant.
In the dissolution profile, it showed immediate release, and the acceptance value of those tablets was met.

See the full research poster for Orodispersible Mini-tablets based on galenIQ here:
(click to enlarge or to download):

Ard Lura1, Oliver Luhn2, Jörg Breitkreutz1

1 Institute of Pharmaceutics and Biopharmaceutics, Heinrich Heine University, 40225 Düsseldorf, Germany
2 BENEO-Palatinit GmbH, Maximilianstraße 10, 68165 Mannheim, Germany

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