Tablet dissolution of Ibuprofen: conventional versus granulated drug

Speaking about tablet dissolution of Ibuprofen for most of the marketed products, you might think about Ibuprofen in the conventional physical form. Since a while, a granulated form of Ibuprofen is available on the market, serving certain advances, which as listed elsewhere. So, it is on this application note to address the first comparison in dissolution kinetics of both drug forms.

Granulated Ibuprofen consisting of 100% pure active without additional excipients – a novum in the pharmaceutical industry. Until now, this drug was pelletized with the help of excipients. In turn, it was tricky to substitute the drug in an existing formulation. With Ibuprofen DC100, things become easy: no further excipient is employed for granulation and the drug is nothing more than another physical form of itself. The high concentration of API provides maximum freedom in formulation design and allows creating diverse dosage forms such as tablets, sachets and others. A better patients’ compliance is achieved by improved taste-masking or optimized tablet sizes. Process experts know about the difficulties in compression steps for tableting Ibuprofen: Conventional formulations result in critical compression behavior of the drug. This might induce a loss in yield and increasing product costs.

Expert’s opinion

The granulated Ibuprofen (Ibuprofen DC100) is just another physical form of the conventional drug. Dissolution kinetics are well comparable. Through designed formulations, extended and modified drug releases can be achieved. Try in lab-scale and later do easily the upscaling.

Test the product

Tablet dissolution of Ibuprofen

Figure 1 presents the time-dependent dissolution kinetics of Ibuprofen tablets in two different physical forms of the drug. The green curve represents a formulation on 800 mg Ibuprofen originally processed from powder, while the blue curve shows the kinetics of a 800 mg Ibuprofen DC100 formulation, wherein the drug has a granular form.

Ibuprofen DC 100 – tablet dissolution

Figure 1: Time-dependent dissolution kinetics of Ibuprofen tablets in two different physical forms of the drug. Green: 800 mg Ibuprofen originally from powder; blue: 800 mg Ibuprofen DC100 as granulated drug.

The dissolution profiles of Ibuprofen and Ibuprofen compare well. In case of Ibuprofen DC100 formulation, this might induce certain exemplary drug formulations as given in Table 1. Therein, an API load of 80% is assumed. Targeting a dosage of 400 mg results in a tablet mass of 500 mg. Future application notes will present data on specific oral formulations, inform about tablet sizes and dissolution profiles.

Dosage [mg] Product Tablet mass [mg] API load [%]
200 Ibuprofen DC 100 tablet acute 250 80
400 Ibuprofen DC 100 tablet acute 500 80
400 Ibuprofen DC 100 tablet 500 80
600 Ibuprofen DC 100 tablet 750 80
800 Ibuprofen DC 100 tablet 1000 80

Table 1: exemplary dosages of Ibuprofen in oral drug formulation with an API load of 80%. Dosage and tablet mass in [mg], API load in [%].

Conclusion

Important things first: Tablet dissolution of Ibuprofen is on highest levels for both drug forms, the conventional and the granulated one. Both drug forms exhibit excellent dissolution kinetics. The cumulative release is somewhat faster for Ibuprofen DC100 than for the conventional Ibuprofen. If this is a measured effect or artefact needs to be pointed out in further investigations. This might also count for the saturation level which seems to be slightly higher for the conventional drug form.