Preparation of enteric coated timed-release press-coated tablets and evaluation of their function by in vitro and in vivo tests for colon targeting

Fukui, Eiji; Miyamura, Nobuteru; Uemura, Katsuji; Kobayashi, Masao

doi:10.1016/s0378-5173(00)00454-3

Cited by 96 publications

(50 citation statements)

References 11 publications

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“…Shun et al,ethylcellulose membrane is the most important factor for disintegration of the formulation [25]. The system also appeared to depend on capsule size and density.…”

Section: Rubin Et Al 1992mentioning

confidence: 98%

“…Parallel dissolution studies in different buffers may be undertaken to characterize the behavior of formulations at different pH levels. Dissolution tests of a colonspecific formulation in various media simulating pH conditions and times likely to be encountered at various locations in the gastrointestinal tract [25]. ii) Drug release study is done in buffer medium containing enzymes (enzyme pectinase, dextranase), or rat or guinea pig or rabbit cecal contents.…”

Section: In Vitro Evaluationmentioning

confidence: 99%

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Primary and novel approaches for colon targeted drug delivery – A review

Tiwari¹,

Tiwari²,

Wal³

et al. 2010

Int. J. Drug Delivery

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The colon is a site where both local and systemic delivery of drugs can take place. Local delivery could, for example, allow topical treatment of inflammatory bowel disease. Treatment could be made more effective if it were possible for drugs to be targeted directly on the colon. Systemic side effects could also be reduced. Colon specific systems might also allow oral administration of peptide and protein drugs, which are normally inactivated in the upper parts of the gastrointestinal tract. Primary approaches for CDDS (Colon Specific Drug Delivery), which includes prodrugs, pH and time dependent systems and microbially triggered drug delivery system achieved limited success and having limitations. Newly developed CDDS, which includes pressure controlled colonic delivery capsules (PCDCS), CODES TM and osmotic controlled drug delivery are unique in terms of achieving in vivo site specificity and feasibility of manufacturing process. This review also focuses on evaluations of CDDS in general.

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“…Shun et al,ethylcellulose membrane is the most important factor for disintegration of the formulation [25]. The system also appeared to depend on capsule size and density.…”

Section: Rubin Et Al 1992mentioning

confidence: 98%

Section: In Vitro Evaluationmentioning

confidence: 99%

Primary and novel approaches for colon targeted drug delivery – A review

Tiwari¹,

Tiwari²,

Wal³

et al. 2010

Int. J. Drug Delivery

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“…In addition, it is possible to control lag time by changing the coating thickness and composition. 17 Aceclofenac, a nonsteroidal anti-inflammatory drug, is used for the symptomatic relief of pain and joint s tiffness in patients suffering from rheumatoid arthritis, which is c haracterized by diurnal variation in circulating levels of proinflammatory cytokines, interleukin-6 and/or tumor necrosis factor-α. Due to this diurnal variation, many symptoms and signs of active rheumatoid arthritis are manifested in the morning.…”

Section: Introductionmentioning

confidence: 99%

Chronomodulated press-coated pulsatile therapeutic system for aceclofenac: optimization of factors influencing drug release and lag time

Patil¹,

Pund²,

Joshi³

et al. 2011

CPT

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Background:The objective of this study was to develop and evaluate a press-coated pulsatile drug delivery system intended for treatment of early morning stiffness and symptomatic relief from pain in patients with rheumatoid arthritis. Methods: The formulation involved press coating of a rupturable coat around a rapidly d isintegrating core tablet of aceclofenac. A three-factor, two-level, full factorial design was used to i nvestigate the influence of amount of glyceryl behenate, amount of sodium chloride in the coating c omposition, and the coating level on the responses, ie, lag time to release and amount of aceclofenac released in 450 minutes. Results: Glyceryl behenate and the coating level had a significant influence on lag time, while sodium chloride helped in the rupture of the coat by acting as a channeling agent. After the coat was ruptured, the core tablet showed a rapid release of aceclofenac due to the presence of Ac-Di-Sol ® . Graphical analysis of effects by Lenth's method and Bayesian analysis of coefficients enabled identification of variables active on the selected responses. The optimized formulation comprised 20% w/w glyceryl behenate and 2.2% w/w sodium chloride with a 650 mg coating level, and showed a desired lag time of 358.23 minutes, which mimics the fluctuating symptoms of rheumatoid arthritis, followed by rapid release of aceclofenac.

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“…The use of pH-dependant and time-dependant polymers as coating materials for colonic drug delivery has been reported previously. In those studies sustained release and pH-dependant polymers have been applied as separate coating layers on top of each other (Gupta et al, 1993;Fukui et al, 2000;Qi et al, 2003). The combination of time-and pH-dependant polymer as a single coating has been used to provide the pulsatile drug release in the unit formulation .…”

Section: Introductionmentioning

confidence: 99%