BSC Class I APIs in oral formulations
APIs of BSC Class I in oral formulations represent one of four groups following the Biopharmaceutical Classification System (BCS). The BCS predicts potential effects of oral formulations on the human drug oral bioavailability. Thereby, it is a scientific tool differentiating the drug substances on the basis of solubility and intestinal permeability under prescribed condition. While the solubility classification is based on a United States Pharmacopoeia (USP) aperture, the classification of permeability is based on a comparison to the intravenous injection.
Permeability | Class I
High solubility High permeability |
Class II
Low solubility High permeability |
Class III
High solubility Low permeability |
Class IV
Low solubility Low permeability |
|
Solubility |
Table 1: Biopharmaceutics Classification System (BCS).
BSC Class I
BSC Class I drugs are characterized by a high solubility and a high permeability (Table 1). Typical drugs are Amantadine, Diazepam, Itopride HCl, Paracetamol, or Zidovudine [1]. High solubility is given in cases that the highest strength is soluble in pH ranges from pH 1 to pH 6 at body temperature, and a high permeability means an extent of absorption in humans of at least 85%.
Due to high water solubility of BSC class I drugs, a potential substrate in pharmaceutical formulations for oral drugs needs to be water insoluble. In case of MUPS (Multiple Unit Pellet Systems) or capsule dosage forms, pellets of Microcrystalline Cellulose – MCC pellets – are the first choice. Depending on the pellet size, they serve as starter beads in MUPS formulations (smaller than about 800 µm) or in capsules (larger than approx. 800 µm).
![Figure 1: Pellet sizes for potential BSC Class I MUPS and capsule formulations.](https://cellets.com/wp-content/uploads/2022/02/Cellets_BCS_class_I-300x142.png)
Figure 1: Pellet sizes for potential BSC Class I MUPS and capsule formulations.
MCC spheres or pellets for BSC Class I capsule formulations:
CELLETS® 1000 (1000-1400 µm)
CELLETS® 700 (700-1000 µm)
MCC spheres or pellets for MUPS formulations:
CELLETS® 500 (500-710 µm)
CELLETS® 350 (350-500 µm)
CELLETS® 200 (200-355 µm)
CELLETS® 100 (100-200 µm)
Further information
Are you working with BSC Class IV actives? Read more here.
References
[1] https://www.pharmaspecialists.com/, time: Feb 16th, 2022.