Development of tablets for controlled joint release of nifedipine and atenolol.
Oral combinations of nifedipine and atenolol are widely used in the treatment of hypertension, proving particularly effective when the atenolol is released immediately and the nifedipine is released in a sustained manner. This work examined the potential of combining nifedipine and atenolol in a tablet, which would be easier to manufacture than currently available combined formulations. The results indicated that a 40:60 (w/w) nifedipine-atenolol mixture forms a eutectic melting at 140 degrees C. Nevertheless, both drugs were stable when incorporated in tablets elaborated using cellulose ethers as base excipients. Tablets prepared from atenolol-lactose granules and solid dispersions of nifedipine-hydroxypropylmethylcellulose (100 cP) had more adequate dissolution profiles than a more complex reference formulation in hard capsules.
Iglesias
R
R
Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad de Santiago de Compostela, Spain.
Taboada
C
C
Souto
C
C
Martínez-Pacheco
R
R
Gómez-Amoza
J L
JL
Concheiro
A
A
D001262:Atenolol / Q000493:pharmacokinetics*; D002121:Calcium Channel Blockers / Q000493:pharmacokinetics*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D003692:Delayed-Action Preparations; D004355:Drug Stability; D004987:Ethers; D006973:Hypertension / Q000188:drug therapy*; D008055:Lipids / Q000737:chemistry; D009543:Nifedipine / Q000493:pharmacokinetics*; D012995:Solubility; D013607:Tablets; D014867:Water / Q000737:chemistry
D002121:Calcium Channel Blockers; D003692:Delayed-Action Preparations; D004987:Ethers; D008055:Lipids; D013607:Tablets; D014867:Water; D001262:Atenolol; D009543:Nifedipine