Colon-targeted delivery of solubilized bisacodyl by doubly enteric-coated multiple-unit tablet

Park, Hee J.; Jung, Hyuck Jun; Ho, Myoung Jin; Lee, Dae R.; Cho, Ha R.; Choi, Yong Seok; Jun, Joon-Ho; Son, Miwon; Kang, Myung Joo

doi:10.1016/j.ejps.2017.03.006

Cited by 25 publications

(13 citation statements)

References 17 publications

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“…In addition, variability in the GI fluid composition, feeding status, and GI transit time affect the site-specific drug release from the pH-dependent system [45]. Therefore, there have been continuous efforts to improve the targeting effectiveness via the multi-unit formulations based on the integration of the different mechanism-based systems with pH-dependent coating [46]. For example, Park et al [46] prepared a bisacodyl-loaded multi-unit tablet by coating with different combinations of pH-dependent polymers (Eudragit S and Eudragit L) and time-dependent polymer (Eudragit RS).…”

Section: Tablets and Capsulesmentioning

confidence: 99%

“…Therefore, there have been continuous efforts to improve the targeting effectiveness via the multi-unit formulations based on the integration of the different mechanism-based systems with pH-dependent coating [46]. For example, Park et al [46] prepared a bisacodyl-loaded multi-unit tablet by coating with different combinations of pH-dependent polymers (Eudragit S and Eudragit L) and time-dependent polymer (Eudragit RS). Drug release from the optimized tablet was minimal in the simulated gastric and intestinal fluids while extensive drug release was observed in the colonic fluid [46].…”

Section: Tablets and Capsulesmentioning

confidence: 99%

“…For example, Park et al [46] prepared a bisacodyl-loaded multi-unit tablet by coating with different combinations of pH-dependent polymers (Eudragit S and Eudragit L) and time-dependent polymer (Eudragit RS). Drug release from the optimized tablet was minimal in the simulated gastric and intestinal fluids while extensive drug release was observed in the colonic fluid [46]. Recently, Foppoli et al [47] also reported the effective colonic delivery system of 5-aminosalicylic acid based on the combination of time-dependent and pH-dependent approaches, which was prepared by successive coating of a tablet core with low-viscosity HPMC and Eudragit ® L. Furthermore, based on a γ-scintigraphy study in human, they confirmed that there was no premature drug release before reaching the colon in both fed and fasted states [47].…”

Section: Tablets and Capsulesmentioning

confidence: 99%

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Strategic Approaches for Colon Targeted Drug Delivery: An Overview of Recent Advancements

et al. 2020

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Colon targeted drug delivery systems have gained a great deal of attention as potential carriers for the local treatment of colonic diseases with reduced systemic side effects and also for the enhanced oral delivery of various therapeutics vulnerable to acidic and enzymatic degradation in the upper gastrointestinal tract. In recent years, the global pharmaceutical market for biologics has grown, and increasing demand for a more patient-friendly drug administration system highlights the importance of colonic drug delivery as a noninvasive delivery approach for macromolecules. Colon-targeted drug delivery systems for macromolecules can provide therapeutic benefits including better patient compliance (because they are pain-free and can be self-administered) and lower costs. Therefore, to achieve more efficient colonic drug delivery for local or systemic drug effects, various strategies have been explored including pH-dependent systems, enzyme-triggered systems, receptor-mediated systems, and magnetically-driven systems. In this review, recent advancements in various approaches for designing colon targeted drug delivery systems and their pharmaceutical applications are covered with a particular emphasis on formulation technologies.

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Section: Tablets and Capsulesmentioning

confidence: 99%

Section: Tablets and Capsulesmentioning

confidence: 99%

Section: Tablets and Capsulesmentioning

confidence: 99%

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Strategic Approaches for Colon Targeted Drug Delivery: An Overview of Recent Advancements

et al. 2020

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“…This design could be realized involving either film coating or by preparing two different film-coated granules as was reported by Howden et.al. 37 , 38 The designed formulation was composed of two proton pump inhibitor granules with the first ingredient released within two hours after dose administration providing day-time therapy for gastroesophageal reflux disease (GORD); while the second ingredient released within 6 hours after dose administration and addressed overnight GORD. Based on the variability of GIT pH recognized within the general population (especially with colonic-pH), the efficiency of colon-specific drug delivery systems involving pH alone has been extensively discussed.…”

Section: Classification Of Film Coatingmentioning

confidence: 99%

<p>A Comprehensive Review on Pharmaceutical Film Coating: Past, Present, and Future</p>

Zaid¹

2020

DDDT

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Pharmaceutical film coating is considered a key part in the production of solid pharmaceutical dosage forms since it gives superior organoleptic properties products. In addition, it can improve the physical and chemical stability of dosage forms, and modify the release characteristics of the drug. Several troubleshooting problems such as twinning mottling, chipping, etc., may arise during or after or even during the shelf life of the film coated dosage forms. These troubleshooting problems may be due to tablet core faults, coating formulation faults and/or coating process faults. These problems must be overcome to avoid unnecessary product problems. Film coating as well as other parts of the pharmaceutical technology is subjecting to continuous innovation. The innovation may be at different levels including pharmaceutical excipients, processes, software, guidelines and equipment. In fact, of particular note is the growing interest in process analytical technology, quality by design, continuous coating processing and the inclusion of new ready for use coating formulations. In this review, we tried to explore and discuss the status of pharmaceutical film coating, the challenges that face this manufacturing process and the latest technological advances in this important manufacturing process.

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“…For example, Park et al, reported that an enteric coated multiple-unit tablet system of bisacodyl consisting of Eudragit S/L-based pHdependent and time-dependent controlled release polymer of Eudragit RS provided selective drug release in colon. The pharmacokinetic evaluation in rabbits suggested that drug absorption from the time-and pH-dependent tablet was effectively retarded in stomach and small intestinal with lowered systemic exposure compared to marked product of Dulcolax ® , but profound drug liberation was achieved in colon part (Park et al, 2017). C o n s i d e r i n g t h e d i s a d v a n t a g e s o f t a b l e t manufacturing, including capping, laminations, variations in weight and the processing cost, an attempt was made to develop tacrolimus SD-based controlledrelease pellets.…”

Section: Introductionmentioning

confidence: 99%

Solid dispersion-based pellet for colon delivery of tacrolimus through time- and pH-dependent layer coating: preparation, in vitro and in vivo studies

Guo

Fang

Gui

et al. 2019

Braz. J. Pharm. Sci.

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The intent of the present investigation is to develop and evaluate colon-specific coated tacrolimus solid dispersion pellet (SDP) that retards drug release in the stomach and small intestine but progressively releases in the colon. Tacrolimus-SDP was prepared by extrusion-spheronization technology and optimized by the micromeritic properties including flowability, friability, yields and dissolution rate. Subsequently, the pH-dependent layer (Eudragit L30D55) and time-dependent layer (Eudragit NE30D and L30D55) were coated on the SDP to form tacrolimus colon-specific pellets (CSP) using a fluidized bed coater. Under in vitro gradient pH environment, tacrolimus only released from CSP after changing pH to 6.8 and then quickly released in the phosphate buffer solution of pH 7.2. The Cmax of CSP was 195.68 ± 3.14 ng/mL at Tmax 4.5 ± 0.24 h where as in case of SDP, the Cmax was 646.16 ± 8.15 ng/mL at Tmax 0.5 ± 0.03 h, indicating the ability of CSP targeted to colon. The highest area under the curve was achieved 2479.58 ± 183.33 ng•h/mL for SDP, which was 2.27-fold higher than tacrolimus suspension. However, the best biodistribution performance was achieved from CSP. In conclusion, SDP combining of pH-and time-dependent approaches was suitable for targeted delivery of tacrolimus to colon.

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Colon-targeted delivery of solubilized bisacodyl by doubly enteric-coated multiple-unit tablet

Cited by 25 publications

References 17 publications

Strategic Approaches for Colon Targeted Drug Delivery: An Overview of Recent Advancements

Strategic Approaches for Colon Targeted Drug Delivery: An Overview of Recent Advancements

<p>A Comprehensive Review on Pharmaceutical Film Coating: Past, Present, and Future</p>

Solid dispersion-based pellet for colon delivery of tacrolimus through time- and pH-dependent layer coating: preparation, in vitro and in vivo studies

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