Novel polymeric film coatings for colon targeting: Drug release from coated pellets

Karrout, Youness; Neut, Christel; Wils, Daniel; Siepmann, Florence; Deremaux, Laetitia; Flament, Marie‐Pierre; Dubreuil, L.; Desreumaux, Pierre; Siepmann, Juergen

doi:10.1016/j.ejps.2009.03.014

Cited by 61 publications

(32 citation statements)

References 34 publications

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“…6 To achieve the successful delivery of drugs to the target site, that is, colon drug needs to be protected from the GIT environment or absorption in the upper GIT and then releases in the colon. 7 A variety of approaches are available for the delivery of drugs to the colon such as pH dependent, time dependent or enzyme dependent system and prodrug. [8][9][10] The prodrug is one of the most important approach for the targeting of drugs to the colon in which drug is covalently bound to the carrier that is susceptible to cleave in the colon.…”

mentioning

confidence: 99%

Design, synthesis and ex vivo evaluation of colon-specific azo based prodrugs of anticancer agents

Sharma

Rawal

Gaba

et al. 2013

Bioorganic & Medicinal Chemistry Letters

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mentioning

confidence: 99%

Design, synthesis and ex vivo evaluation of colon-specific azo based prodrugs of anticancer agents

Sharma

Rawal

Gaba

et al. 2013

Bioorganic & Medicinal Chemistry Letters

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“…This allows the administration of two or more types of drugs that may or not be chemically compatible, at the same or different sites within the gastro-intestinal tract. Furthermore, pellets with different release rates from the same drug can be combined in a single unit dosage form in order to achieve the desired drug release profile (Karrout et al, 2009). Due to low surface area to volume ratio, ideal shape for film coating, good flowability, low friability, narrow particle size distribution, uniform and reproducible batches are obtained.…”

Section: Multiparticulate As Oral Er Drug Delivery Systemmentioning

confidence: 99%

Oral multiunit pellet extended release dosage form: A review

Sachdeva¹,

Alam²,

Kumar³

et al. 2013

Int Curr Pharm J

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Oral drug delivery is the most preferred route for the various drug molecules among all other routes of drug delivery, because ease of administration which lead to better patient compliance. So, oral extended release drug delivery system becomes a very promising approach for those drugs that are given orally but having the shorter half-life and high dosing frequency. Recent trends indicate that multiparticulate drug delivery systems are especially suitable for achieving extended release oral formulations with low risk of dose dumping, flexibility of blending to attain different release patterns as well as reproducible and short gastric residence time. The release of drug from pellets depends on a variety of factors including the carrier used to form pellets and the amount of drug contained in them. Consequently, pellets provide tremendous opportunities for designing new controlled and extended release oral formulations, thus extending the frontier of future pharmaceutical development.DOI: http://dx.doi.org/10.3329/icpj.v2i10.16413 International Current Pharmaceutical Journal, September 2013, 2(10): 177-184

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“…Various polymers such as HPMCAS (Krogars et al, 2000), methacrylic acid-methyl methacrylate copolymer (Bendas et al, 2010;Brachkova et al, 2009;Chuong et al, 2009), branched dextrin (Karrout et al, 2009), ethylcellulose (Freire et al, 2010;Karrout et al, 2009), and amylose maize starch (Freire et al, 2010) were applied to the colon-specific drug delivery, and in many cases, mesalamine (5-aminosalicylic acid) was used as the model drug for the local treatment of inflammatory bowel diseases (Bendas et al, 2010;Chuong et al, 2009;Freire et al, 2010;Karrout et al, 2009). …”

Section: Coated Pellets For Colon Deliverymentioning

confidence: 99%

Controlled-Release Pelletized Dosage Forms Using the Extrusion-Spheronization Process

Rhee¹,

Lee²,

Lee³

et al. 2010

Journal of Pharmaceutical Investigation

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− Pellets, which are multiple-unit dosage systems, have the several therapeutic advantages over single-unit dosage systems in oral drug delivery. This review focuses on the current status and explores extrusion-spheronization technique with special attention to controlled-release application of pellets including coated pellets for delayed release formulations, coated pellets for colon delivery, coated pellets for sustained drug delivery, sustained-release matrix pellets, pellets compressed into tablets, bioadhesive pellets, floating pellets, and pelletization with solubilization techniques.Key words − Pellets, Multiparticulates, Modified-release, Pelletization, Solubilization Pelletization process is an agglomeration process that results in agglomerates of a narrow size distribution in the range of 0.5-1.5 mm with a low intra-agglomerate porosity (about 10%) and the higher density compared to the granules. Pellets are produced by pelletization process and these agglomerates have the relatively spherical shape, low friability and free flowing properties, which facilitate the handling of pellets in the manufacturing process. Pelletization process can prevent the segregation of co-agglomerated components, resulting in an improvement of the content uniformity. Pelletization process can also avoid the dust formation resulting in an improvement of the process safety, as fine powders can cause dust explosions and respiratory health problems. Pellets are widely used in multiparticulate systems and multiparticulate systems have the several therapeutic advantages over single-unit dosage systems in oral drug delivery. The low inter-and intra-subject variability can be achieved by multiparticulate systems because multiparticulates can pass through the pylorus immediately after administration. Moreover, less effect of food on drug absorption and rather uniform gastric emptying time than single-unit dosage systems can be attainable in multiparticulate systems. Safety concerns due to dose dumping of drugs, which have narrow therapeutic index, is minimized in multiparticulate systems, and more foreseeable drug delivery in sustained release formulation is possible because the total drug dose is divided over many units, not in a single-unit system. The small size of multiparticulates also enables them to be well dispersed along the gastrointestinal (GI) tract, enhancing drug absorption and reducing the irritant effect that single-unit systems may cause to the mucosal lining, especially if remained for an extended time at a specific site. The spherical pellets can be coated with rate-controlling polymers or compressed into tablets to achieve delayed-release, extended-release, and targeted-release profiles. Multiparticulate systems with different dose strengths can be obtained from the same batch of drug-loaded pellets without additional formulation or process modification. Pellets with different drugs or with different release profiles can be blended and formulated in a single-unit dosage form such as capsule, which promo...

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Novel polymeric film coatings for colon targeting: Drug release from coated pellets

Cited by 61 publications

References 34 publications

Design, synthesis and ex vivo evaluation of colon-specific azo based prodrugs of anticancer agents

Design, synthesis and ex vivo evaluation of colon-specific azo based prodrugs of anticancer agents

Oral multiunit pellet extended release dosage form: A review

Controlled-Release Pelletized Dosage Forms Using the Extrusion-Spheronization Process

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