In vitro evaluation of pectin–HPMC compression coated 5-aminosalicylic acid tablets for colonic delivery

Türkoğlu, Murat; Uğurlu, Timuçin

doi:10.1016/s0939-6411(01)00225-9

Cited by 99 publications

(37 citation statements)

References 10 publications

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“…Among these, pectin and guar gum have been studied extensively. However, pectin coat alone has been found insufficient to protect the core from premature release due to its higher aqueous solubility and poor mechanical strength, and a larger amount of pectin is required to prevent precolonic release (13,30,31). Similar findings have been reported with guar gum used as compressioncoating material (8,32,33).…”

Section: Discussionmentioning

confidence: 99%

Compression-Coated Tablet for Colon Targeting: Impact of Coating and Core Materials on Drug Release

Maity

2015

AAPS PharmSciTech

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Abstract. This work was envisaged to develop compression-coated tablets using a blend of Ca +2 ion crosslinked carboxymethyl xanthan gum (CMXG) and sodium alginate (SAL) for delayed release of immediate pulse release tablets of prednisolone (PDL) in the colon without the need of colonic bacterial intervention for degradation of the polysaccharide coat. The core tablets containing PDL and other compatible excipients were prepared by direct compression method and subsequently compression coated with different ratios of CMXG and SAL. Long T lag , the time required to restrict the drug release below 10%, and short T rap , the time required for immediate release following the T lag , were considered as suitable release parameters for evaluation of colon targeting of PDL tablets. Among the various compression coats, a blend of CMXG and SAL in a ratio of 1.5:3.5 provided T lag of 5.12±0.09 h and T rap of 6.50±0.05 h. The increase in microcrystalline cellulose (MCC) and crospovidone (CP) in the core tablets did not change T lag significantly although decreased the T rap marginally. Inclusion of an osmogen in the core tablets decreased the T lag to 4.05±0.08 h and T rap to 3.56±0.06 h. The increase in coat weight to 225 mg provided a reasonably long T lag (6.06±0.09 h) and short T rap (4.36±0.20 h). Drug release from most of the formulations followed the Hixson-Crowell equation and sigmoidal pattern as confirmed by the Weibull equation. In conclusion, tablets, compression coated with CMXG and SAL in a ratio of 1.5:3.5 and having 225-mg coat weight, were apparently found suitable for colon targeting.

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Section: Discussionmentioning

confidence: 99%

Compression-Coated Tablet for Colon Targeting: Impact of Coating and Core Materials on Drug Release

Maity

2015

AAPS PharmSciTech

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“…In addition, pectin-based, colon-specific drug delivery vehicles have been developed using a chemically modified pectin polymer. [9][10][11][12][13][14] Oral controlled drug delivery systems based on blend polysaccharidic matrix are gaining widespread acceptance in the pharmaceutical industries because of their flexibility to obtain a desirable drug-release profile, costeffectiveness, and broad regulatory acceptance. The composites take the advantages of their parent polymers and/or create useful new properties.…”

Section: Introductionmentioning

confidence: 99%

Preparation and characteristics of high-amylose corn starch/pectin blend microparticles: A technical note

Desai

2005

AAPS PharmSciTech

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“…Ethyl cellulose is one of the most widely used water-insoluble polymers in film-coating to achieve extended drug release. In order to evaluate enzyme-triggered drug release of pectin compression-coated tablets, 7.4 to simulate the degradation of the polymers by the microflora (Turkoglu & Ugurlu, 2002).…”

Section: In Vitro Release Of Bdz From Compression Coated Tabletsmentioning

confidence: 99%

Bumadizone calcium dihydrate microspheres compressed tablets for colon targeting: formulation, optimization andin vivoevaluation in rabbits

2014

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The objective of this study was the development of a colon-targeted microspheres which were compressed into tablets containing the non-steroidal anti-inflammatory bumadizone calcium dihydrate. A 3 2 full factorial design was adopted for the evaluation of the prepared microspheres. The effect of two independent variables namely polymer type (Eudragit RS100, ethyl cellulose and cellulose acetate butyrate), and drug: polymer ratio (1:1, 9:1 and 18:1) was studied on the entrapment efficiency and in vitro drug release for 12 h. Colon targeting aims to minimize the release of the drug off target area (pH 1.2 and 6.8) and to maximize the release of the drug in target area (pH 7.4). Candidate formulae were compressed into core tablets and colon targeting was achieved using the enzyme-dependent polymer (pectin) as coat in three different concentrations 50, 75 and 90%. Candidate formula F15 (microspheres prepared using BDZ:CAB in a ratio of 18:1 and compressed into tablets using 50% pectin and 50% Avicel in the coat) was able to adequately modulate drug release avoiding drug release in the gastric ambient, and reaching the colonic targeting where 99.7% release was achieved within 12 h following zero-order model. In vivo studies showed that F15 achieved significant decrease in myeloperoxidase activity and inflammation with delayed T max (4 h) and lower C max (2700 ng/ml) when compared to marketed product.

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In vitro evaluation of pectin–HPMC compression coated 5-aminosalicylic acid tablets for colonic delivery

Cited by 99 publications

References 10 publications

Compression-Coated Tablet for Colon Targeting: Impact of Coating and Core Materials on Drug Release

Compression-Coated Tablet for Colon Targeting: Impact of Coating and Core Materials on Drug Release

Preparation and characteristics of high-amylose corn starch/pectin blend microparticles: A technical note

Bumadizone calcium dihydrate microspheres compressed tablets for colon targeting: formulation, optimization andin vivoevaluation in rabbits

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