Design of a dissolution system for the evaluation of the release rate characteristics of artemether and dihydroartemisinin from tablets

Preliminary pharmaceutical development of antimalarial–antibiotic cotherapy as a pre-referral paediatric treatment of fever in malaria endemic areas

“…AZ aqueous solubility (39 g L −1 at pH 7.4 and 37 °C (Pfizer, 2013)) was not limiting regarding the dose considered (421 mg AZ dihydrate). In contrast, artemisinin derivatives are characterized by their low aqueous solubility: 0.296 g L −1 (Kauss et al, 2010) and 0.161 g L −1 (Gabriëls & Plaizier-Vercammen, 2004) for AS and AM respectively at 37 °C. For dosage forms containing 300 mg of an artemisinin derivative, this solubility was insufficient to meet solubility (ideally sink, i.e.…”

“…The addition of 1% w/v of SLS to the buffer at pH 7 was necessary to obtain requested AM solubility, but this changed the dissolution rate (drug release was slower for both AM and AZ) as a consequence of the increased viscosity of the medium. The Gabriëls and Plaizier-Vercammen (2004) octanol–buffer biphasic system was adopted as the best compromise between physiological conditions and pharmacopoeia specifications. Of note, as this method required that each sample was treated individually, the variance of results was inherently higher than in a conventional monophasic dissolution assay.…”

“…result Section 3.3). Finally, a bi-phasic dissolution method, initially developed for AM tablets (Gabriëls and Plaizier-Vercammen, 2004), was adapted for AMAZ cotherapy. Briefly, 150 mL of 50 mM phosphate buffer pH 6.0 and 100 mL of isooctane were placed into teach dissolution bowel.…”

Nanopharmaceutics: Phytochemical-Based Controlled or Sustained Drug-Delivery Systems for Cancer Treatment

“…96 Similarly, dihydroartemisin (DHA) is susceptible to light, heat and oxygen due to its peroxy bond and has low bioavailability for oral administration. 97 DHA-loaded MPEG5000-PLLA3200 amphiphilic block copolymeric micelles were devised using modified solvent evaporation method. Nanomicelles had mean sizes below 130 nm.…”

In vitro evaluation of efficacy of dihydroartemisinin‐loaded methoxy poly(ethylene glycol)/poly(l‐lactic acid) amphiphilic block copolymeric micelles

“…2 The mechanisms of action for their antitumor activities are not fully understood, but it might be due to transferrin conjugates. Also, DHA has low bioavailability for oral administration, 6 due to its poor water solubility (0.168 mg mL À1 at 30 C). 4,5 However, DHA is susceptible to light, heat, and oxygen for its special peroxy bond.…”