Evidence of Reliable Gastro-Resistance of Novel Enteric Ready-to-Fill Capsules Simplifying Pharmaceutical Manufacturing.

Developing delayed-release formulations for acid-sensitive actives can be a costly and time-consuming process. However, ready-to-fill functional capsules, such as EUDRACAP® can significantly mitigate these challenges. The in vitro performance of EUDRACAP® enteric was evaluated in two typical delayed-release scenarios: for diclofenac (a drug that can cause irritation to gastric mucosa), and for omeprazole (a drug susceptible to degradation due to the acidity of gastric fluid). The prototypes were tested in HCl 0.1N according to the USP <711> for at least 2 h and compared to commercial products. The results showed that the performance of EUDRACAP® was below LOD and in compliance with the requirements for drug release in acidic media (NMT 10%). Additionally, the impurities were evaluated after the acidic stress. The low total percentage of impurities of 0.44% for diclofenac (NMT 1.50%) and 0.22% for omeprazole (NMT 2.00%) indicates a very good protection by EUDRACAP®. A comprehensive comparative analysis of the in vitro performance clearly showed the acid protection capability of EUDRACAP® enteric capsules making them a serious alternative to existing enteric dosage forms alternatives. EUDRACAP® is an accessible solution both in large-scale industrial and smaller pharmacy settings. Offering increased accessibility, affordability, and convenience to manufacturers and consumers alike and leading to improved healthcare outcomes.

Kumada-Corriu coupling of Grignard reagents, probed with a chiral Grignard reagent.

The Grignard reagent 2, in which the magnesium-bearing carbon atom is the sole stereogenic centre has been coupled with vinyl bromide under Pd(0) or Ni(0)-catalysis to give compound 3 with full retention of configuration. Coupling using Fe(acac)3 or Co(acac)2 as catalyst was accompanied by considerable racemisation. These findings are discussed with respect to a dichotomy between concerted polar and stepwise SET transmetallation pathways.

Stereochemistry of the transmetalation of Grignard reagents to copper (I) and manganese (II).

Transmetalation of a chiral secondary Grignard reagent to Cu(I) or Mn(II) occurs with partial racemization in a manner that suggests the sequence of two transmetalation cycles, one with racemization (caused by ET ?) and the other one with (predominant) retention of configuration.