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Adkin, D.A.; Kenyon, Christopher J.; Lerner, E I; Landau, I.; Strauss, E; Caron, Dania; Penhasi, Adel; Rubinstein, Abraham; Wilding, Ian R.

doi:10.1023/a:1012019820603

Cited by 57 publications

(3 citation statements)

References 9 publications

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“…Gamma scintigraphic studies, in humans, of pectin-based tablets (13) as well as pectin-based press-coated tablets (14), have shown that the tablets arrived essentially intact in colon and then are degraded locally by enzymes. Pectin tablets have been produced either by direct compression on manual (11) or slow hydraulic presses (6,10,15) or by compaction of granular pectin on a single-punch machine (16).…”

Section: Introductionmentioning

confidence: 99%

Direct Compression Behavior of Low- and High-Methoxylated Pectins

2009

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The objective of this study was to evaluate possible usefulness of pectins for direct compression of tablets. The deformation behavior of pectin grades of different degree of methoxylation (DM), namely, 5%, 10%, 25%, 35%, 40%, 50%, and 60% were, examined in terms of yield pressures (YP) derived from Heckel profiles for both compression and decompression and measurements of elastic recovery after ejection. All pectin grades showed a high degree of elastic recovery. DM 60% exhibited most plastic deformation (YP 70.4 MPa) whereas DM 5% (104.6 MPa) and DM 10% (114.7 MPa) least. However, DM 60% gave no coherent tablets, whereas tablet tensile strengths for DM 5% and DM 10% were comparable to Starch 1500®. Also, Heckel profiles were similar to Starch 1500®. For sieved fractions (180–250 and 90–125 μm) of DM 25% and DM 40% originating from the very same batch, YPs were alike, indicating minor effects of particle size. These facts indicate that DM is important for the compaction behavior, and batch-to-batch variability should also be considered. Therefore, pectins of low degree of methoxylation may have a potential as direct compression excipients.

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Section: Introductionmentioning

confidence: 99%

Direct Compression Behavior of Low- and High-Methoxylated Pectins

2009

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“…Calcium pectinate has been formulated into matrix tablets or compression-coated tablets and evaluated both in vitro and in vivo for potential colon-specific delivery. 3,4,[14][15][16][17][18] The calcium level influences the pectin gel strength, which increases with calcium ions added to a critical concentration, and, thereby, influences the drug release. 4,18 Calcium and pectin association can also be achieved through in situ crosslinking systems.…”

Section: Introductionmentioning

confidence: 99%

“…The calcium‐induced associations of pectin chains are stable at low solution pH and are able to resist extensive hydration in vivo in the gastrointestinal tract. Calcium pectinate has been formulated into matrix tablets or compression‐coated tablets and evaluated both in vitro and in vivo for potential colon‐specific delivery 3, 4, 14–18. The calcium level influences the pectin gel strength, which increases with calcium ions added to a critical concentration, and, thereby, influences the drug release 4, 18.…”

Section: Introductionmentioning

confidence: 99%

Physicochemical characterization of a pectin/calcium matrix containing a large fraction of calcium chloride: Implications for sigmoidal release characteristics

Wei

Chen

Lü

et al. 2009

J of Applied Polymer Sci

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The physicochemical properties of pectin/ calcium matrix tablets were studied with an emphasis on the effect of over 50% of calcium chloride to better understand the fundamentals of the drug-release mechanisms. The absence of the adsorption of methylene blue onto the calciumcontaining pectin matrix served as evidence of the calciumion-induced in situ crosslinking of pectin chains. Visual and scanning electron microscopy observation showed the reinforced robustness of the pectin/calcium matrix, whereas cryo-SEM revealed the formation of a pectin aggregate network as a result of calcium-induced crosslinking. The aggregate network underwent gradual erosion to a lower density, which indicated the erosion of the matrix. However, little change in the texture of the pectin/calcium matrix was observed at earlier times, which was interpreted as the initial stages of drug-release retardation. The apparent viscosity of the pectin aqueous dispersion increased biphasically as the calcium amount increased. The initial sharp increase was interpreted as calcium-induced crosslinking, whereas the following gradual increase was ascribed to a possible salt effect. We concluded that the salt effect and calcium-induced crosslinking contributed to a series of physical changes of the pectin matrix, which correlated to the sigmoidal release of indomethacin from the pectin/calcium matrix tablet.

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Natural polysaccharides as targeting tools of drugs to the human colon

Rubinstein¹

2000

Drug Dev. Res.

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Abstract: These results provide "proof of concept" data for the use of calcium pectinate preparations for drug delivery to the colon and highlight the value of scintigraphy in focusing the development strategy for colonic targeting preparations.

Cited by 57 publications

References 9 publications

Direct Compression Behavior of Low- and High-Methoxylated Pectins

Direct Compression Behavior of Low- and High-Methoxylated Pectins

Physicochemical characterization of a pectin/calcium matrix containing a large fraction of calcium chloride: Implications for sigmoidal release characteristics

Natural polysaccharides as targeting tools of drugs to the human colon

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