Production of Carbopol 974P and Carbopol 971P pellets by extrusion-spheronization: optimization of the processing parameters and water content.
Pellets obtained by extrusion-spheronization represent multiparticulate dosage forms whose interest in intestinal drug delivery can be potentiated and targeted through bioadhesive properties. However, adhesion itself makes the process difficult or even impossible. The problem of tackiness encountered with bioadhesive wet masses was previously eliminated by the use of electrolytes such as CaCl2. This approach is known to reduce the viscosity of polyacrylic acids by disturbing the interactions between carboxylate groups on adjacent polymer molecules, thereby decreasing their bioadhesive properties. The present study aimed at producing pellets containing carbomers without addition of electrolytes in order to maintain their bioadhesive potentiality at its maximum. Carbopol 974P (10%, 15% and 20%) and Carbopol 971P (10%) were used in combination with Avicel PH101. The extrusion speed (30, 45, 60, 90, and 150 rpm), spheronizer speed (350, 700, 960, 1000, and 1300 rpm), spheronization time (5, 10, 15, and 20 minutes) and amount of water (45%, 50%, 54%, and 58%) were optimized in order to obtain the highest yield of spherical pellets ranging 710-1000 microm in diameter. For pellets containing 10%, 15% Carbopol 974P or 10% Carbopol 971P and 45% water content, 30 rpm extrusion speed, 960 rpm, and 10 minutes spheronization speed and time led to the highest yields and sphericities, respectively, 72% and 0.91, 67% and 0.78, and 76% and 0.80. Production of pellets with 20% Carbopol 974P could be achieved through the increase of the water content up to 58% and implementation of 30 rpm extrusion speed, 1300 rpm, and 10 minutes spheronization speed and time. The yield and sphericity were 42% and 0.78 respectively.
Mezreb
N
N
Laboratoire de Pharmacie Galénique, Faculté des Sciences Pharmaceutiques et Biologiques de L'Université René Descartes, Paris, France.
Charrueau
Christine
C
Boy
P
P
Allain
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P
Chaumeil
J C
JC
D000179:Acrylates; D004343:Drug Implants; D010316:Particle Size; D013678:Technology, Pharmaceutical
D000179:Acrylates; D004343:Drug Implants; C117167:carbopol 974P NF