Controlled release of drug via methylcellulose-carboxyvinylpolymer interpolymer complex solid dispersion

Abstract

The purpose of this research was to examine the controlled release of phenacetin (PHE) from solid dispersion by the formation of an interpolymer complex between methylcellulose (MC) and carboxyvinylpolymer (CP). The PHE/ polymer composition ratio was fixed at 20:80 (w/w) in the solid dispersion. The effect of the MC/CP ratio and molecular weight of MC on the PHE release was studied. The release of PHE from the solid-dispersion granules depended on the MC/CP ratio, with a ratio of 50:50 giving the lowest rate of release. In aqueous solution, this MC/CP ratio resulted in the lowest transmittance, suggesting a maximal extent of interpolymer complex formation between MC and CP. Furthermore, at a MC/CP ratio of 50:50, the release of PHE from the solid dispersion granules decreased as the molecular weight of the MC increased, reaching a plateau at molecular weights 180,000. The contributions of diffusion and polymer relaxation to PHE release increased as the molecular weight of the MC increased. This study shows that it is feasible to control the release of PHE from MC-CP solid dispersion granules by modulating complex formation between MC and CP, which can be accomplished by altering the MC/CP ratio and the molecular weight of MC.

Potential application of thermo-sensitive hydrogels for controlled release of phenacetin

“…Phenacetin was chosen as one part of the wider investigation of the selected nonsteroidal anti-inflammatory drugs: paracetamol, which is a precursor of phenacetin, then ibuprofen, naproxen, and piroxicam. Recent studies show the results of a series of formulations of phenacetin with interpolymer carboxyvinylpolymer complexes with poly(ethylene oxide) [23][24][25], carbopol [26] or methylcellulose [27], as well as the comparative determination of a particle size of phenacetin bulk powder [28].…”

Interpolymer complexes of carbopol® 971 and poly(2-ethyl-2-oxazoline): Physicochemical studies of complexation and formulations for oral drug delivery

“…POZ was predominantly present in the non-hydrated core at 4 h of swelling, evidenced by a strong band at 1627 cm -1 . In particular, the peak at 1704 cm -1 assigned to the selfassociated carboxylic groups of C971 exhibited a gradual increase in the intensity with time and shifted to 1715 cm -1 corresponding to the carbonyl C=O stretching vibrations bands (Takayama and Nagai, 1987;Satoh et al, 1989;Ozeki et al, 1998aOzeki et al, , 1998bOzeki et al, , 1999Ozeki et al, , 2000Ozeki et al, , 2005.…”

“…The formulations consisting of proton-accepting non-ionic polymers (PVP, PEO, HPMC, HPC, MC, etc.) and proton-donating polycarboxylic acids -(polyacrylic / polymethacrylic acids, Carbopol ® grades) could form IPCs under acidic pH and their swelling and drug release properties are controlled by threedimensional network structure, which was formed as a result of complex formation between the polymers following water penetration into the matrix (Takayama and Nagai, 1987;Satoh et al, 1989;Ozeki et al, 1998aOzeki et al, , 1998bOzeki et al, , 1999Ozeki et al, , 2000Ozeki et al, , 2005Tan et all., 2001).…”

Pharmaceutical significance of cellulose: A review

“…The T 50 of the MC-CP solid dispersion increased as the molecular weight of the MC increased, and it essentially leveled off when the molecular weight of MC was 180 000 (Figure 4). So, from this study it is feasible to control the release of PHE from MC-CP polymer solid dispersion granules by modulating complex formation between MC and CP, which can be accomplished by altering the MC/CP ratio and the molecular weight of MC [112].…”