Programmed delivery of verapamil hydrochloride from tablet in a capsule device

Abstract

The aim of the present work was to develop a programmed drug delivery system which would be able to release the drug after 6 h of lag time by use of hydrophilic polymers. The capsule body was made impermeable by use of formaldehyde vapor treatment, while the cap was untreated. The capsule was filled with two layered tablets (tablet-in-capsule), followed by a sodium bicarbonate:citric acid mixture (SBCM) and lactose as bulking agent. Sodium alginate, chitosan, HPMC K15 and chitosan:sodium alginate complex (CSAC) were used as the rate modulating layer. Through combined use of HPMC K15 and adjusting the ratio of CSAC, the desired lag time of 6 h was obtained. The effect of the bulking agents on the lag time were also studied and it was found that the lag time was decreased with higher amounts of lactose, and delayed dissolution and decreased lag time was observed at higher amount of effervescent mixture.Uniterms: Circadian rhythm. Chitosan/sodium alginate complex. HPMC K15. Lactose. Effervescent mixture.O objetivo do presente trabalho foi desenvolver sistema de liberação programada de cloridrato de verapamil capaz de liberação imediata do fármaco após 6 h de intervalo de tempo usando polímeros hidrofílicos. O corpo da cápsula foi impermeabilizado por tratamento de vapor de formaldeído, enquanto a tampa não foi submetida ao tratamento. Dois comprimidos foram inseridos na cápsula (comprimidos em cápsula) seguido de mistura de bicarbonato de sódio: ácido cítrico e lactose, utilizados como excipientes. O alginato de sódio, a quitosana, o HPMC K15 e o complexo quitosana:alginato de sódio foram utilizados para modular a razão de liberação do fármaco. A combinação entre o HPMC K15 e o ajuste da proporção do complexo quitosana:alginato de sódio permitiu a liberação do fármaco após 6 h. O efeito dos excipientes na liberação do fármaco foi também avaliado. Verificou-se que o tempo de latência foi reduzido na presença de maior quantidade de lactose, enquanto o menor tempo foi observado empregando maior concentração da mistura efervescente.Unitermos: Ritmo circadiano. Quitosana/complexo de alginato de sódio. HPMC-K15. Lactose. Mistura efervescente.

Tablet Formulation Containing Chitosan-Alginate Microparticles: Characterization and Release Profile of Xanthones

“…The observed burst releases could be explained by the fact that mannitol and lactose rapidly dissolve in water, leading to the swelling and disintegration of the tablets. Furthermore, previous studies have reported increased release rates of atenolol from HPMC matrices (Lotfipour et al, 2004), chlorhexidine digluconate from vaginal inserts (Abruzzo et al, 2013) and verapamil hydrochloride from chitosan-alginate tablets (Sah and Juyal, 2012) in the presence of NaCMC, mannitol and lactose as excipients, respectively. Despite the observed burst releases, the tablet formulation of chitosan-alginate microparticles demonstrates the potential for the delivery of xanthones to the gastrointestinal tract.…”