OBJECTIVE To study the sustained release hydrophilic matrix tablets containing hydroxypropylmethylcellulose (HPMC) and carbopol with phenylpropanolamine hydrochloride (PPA) as the model drug.METHODS The tablets were prepared by direct compression method and the concentrations of PPA in the release media were determined by HPLC. The composition of polymers was selected employing orthogonal design and the values of "similarity factor, f2" were calculated as the criterion. Also the influencing factors on drug release were studied.RESULTS In all cases the plot of cumulative drug release percent against time1/2 produced a straight line (r＞0.98，P＜0.01). The release profiles of the selected preparation and reference preparation were similar in 0.1 mol·L-1 HCl，distilled water, phosphate buffer pH 5.0 ，6.8, 7.4 and in 0.1 mol·L-1 HCl for 2 h followed by release in phosphate buffer pH 6.8 for 10 h.The values of "similarity factor, f2" varied among 63～74 in these cases. In the ranges examined，the rate of PPA released in distilled water decreased with the content of HPMC K100M or carbopol 971P increased (P＜0.05).The variations of the polymers ratio（using the same total content of polymers）, the content of magnesium stearate or hardness of matrices appeared to insignificantly affect the release (P＞0.05).CONCLUSION The PPA hydrophilic matrix tablets containing HPMC K100M and carbopol 971P had sustained release effects in vitro.The main influencing factors on drug release were the contents of HPMC K100M and carbopol 971P.
Key words
hydroxypropylmethylcellulose /
carbopol 971P /
hydrophilic sustained release matrix tablets /
similarity factor
{{custom_keyword}} /
{{custom_sec.title}}
{{custom_sec.title}}
{{custom_sec.content}}
References
[1］Marcos B，Ford J，Armstrong D， et al. Influence of pH on the release of propranolol hydrochloride from matrices containing hydroxypropylmethylcellulose K4M and carbopol 974［J］. J Pharm Sci ,1996，85（3）：330.
[2］Parfitt K. Martindale the complete drug reference . 32nd［M］. London：Pharmaceutical Press,1999:1067.
[3］Zimmerman CL.The effect of urinary pH modification on the disposition of phenylpropanolamine［J］. Pharm Res ,1988，5：120.
[4］Dowse R，Haigh J，Kanfer I.Pharmacokinetics of phenylpropanolamine in humans after a single-dose study［J］. Int J Pharm ，1987，39:141.
[5］Moore J，Flanner H.Mathematical comparison of dissolution profiles［J］. Pharm Technology ,1996，20（6）219.
[6］Pillay V，Fassihi R.Evaluation and comparison of dissolution data derived from different modified release dosage forms：an alternative method［J］. J Controlled Release ,1998，55：45.
[7］Higuchi W.Analysis of data on the medicament release from ointments［J］. J Pharm Sci ，1962，51：802.
[8］Higuchi T.Mechanism of sustained-action medication：Theoretical analysis of rate of release of solid drugs dispersed in solid matrices［J］. J Pharm Sci ,1963，52（12）：1145.
[9］Velasco M,Ford J,Rowe R， et al .Influence of drug:hydroxypropylmethylcellulose ratio, drug and polymer particle size and compression force on the release of diclofenac sodium from HPMC tablets［J］. J Controlled Release ,1999, 57:75.
[10］Sarisuta N,Mahahpunt P.Effects of compression force and type of fillers on release of diclofenac sodium from matrix tablets［J］. Drug Dev Ind Pharm ,1994,20:1049.
{{custom_fnGroup.title_en}}
Footnotes
{{custom_fn.content}}
