StarLac® for Orally Disintegrating Tablets

Oral application of drugs is not only the most common way for systemic drug application, it is also patient’s route of choice. Oral formulations are – compared to injections or infusions – convenient and painless. As they do not require sterility they are cost effective and reveal good patient compliance. But apparently even amongst oral formulations, there are favorites: Eli Lilly sponsored a study with the objective of comparing patients’ preference for olanzapine orodispersible tablets (ODT) with conventional oral tablets (OCT). After a 12-week randomized, crossover, multinational, open-lable evaluation, the result showed that 61 % of stable schizophrenia patients preferred ODT and the conclusion was that ODT should be routinely considered as treatment option.1

Moreover, there are some specific patient subgroups which naturally have more problems in swallowing conventional tablets then others: small children and geriatric patients. Not to mention those patients suffering from dysphagia for any other reasons. Taking this and the increasing world population of elderly people (16 %) into account, the increasing interest in ODT is explained easily.2

Besides the fast disintegration without swallowing, it is also important that those medicines are affordable and convenient to produce. Transportation and storage requirements should also be taken into consideration. All these topics are important to guarantee a good adherence to the treatment.3

Manufacturing of ODT

It is true that freeze-drying, molding and sublimation, spray drying and direct compression followed by vacuum drying have been used for the manufacturing of ODT, but still simple direct compression is the most common process.

When formulating an ODT, many factors must be taken into consideration. Talking only about the physical properties of the tablet, scientists have been working with high levels of superdisintegrants, effervescent agents, highly compressible diluents and binders, combinations of ion exchange resins and cyclodextrins.

Despite of the variety of techniques and formulations, there are always the same concerns when developing an ODT:

• Fast disintegration
• Taste
• Mechanical resistance
• Stability
• Mouth feel

What can lactose and starch do for an ODT formulation?

Target of the study
In order to better understand and determine the characteristics of StarLac® as a robust excipient for ODT application the study described in this article has been carried out. First, placebo tablets of StarLac® were prepared and submitted to an accelerated stability study. The aim of this evaluation was to avoid the interference of other components in the formulation so that a clear picture of StarLac®’s performance in ODT could be gained.

As a second step, a similar study comparing a StarLac® based formulation with the nonsteroidal anti-inflammatory drug Ketorolac tromethamine (Ketorolac) as model API and a Ketorolac formulation based on the polyols sorbitol and mannitol which are together with a disintegrant commonly used excipients in ODT formulations.

Download the publication for more details: StarLac® for Orally Disintegrating Tablets

Conclusion
StarLac® alone proved to be a robust excipient for ODT application, presenting stable results for weight, hardness, disintegration and friability when submitted to stability study at 40 °C / 75 % R.H., independent of the packaging material.

When formulated with API and other excipients like sweetener and aroma, StarLac® ODT proved to be less sensible to the accelerated stability conditions compared to polyol containing formulations, offering the possibility to have a final formulation packed with the most economic packaging material the PVC-Aluminium blister.

StarLac® can provide important benefits to the pharmaceutical companies if the API does not show any degradation due to moisture. With StarLac® it is possible to achieve a faster development process, a robust formulation for a trouble free production process with less components, resulting in an overall more economic formulation and allowing for the use of the most economic packaging material.

Benefits for the patients are given by resistant tablets which do not break when pushed out of the blisters, by fast disintegration in the mouth, providing a good mouth-feel without a “sandy” sensation and by a high adherence rate.

Lactose and maize starch, two of the oldest and safest excipients on the pharmaceutical market, can generate impressive benefits when co-processed in StarLac®.

MORE INFORMATION ON MEGGLE EXCIPIENTS

StarLac® for Orally Disintegrating Tablets: What can lactose and starch do for an ODT formulation?
Carolina Paz de Almeida, Dr. Franz Penz, Fábio Luis Ikuno, Guilherme Brandão, Sabine Hauptstein