Calcium pectinate gel beads for controlled release drug delivery:

Sriamornsak, Pornsak; Nunthanid, Jurairat

doi:10.1016/s0378-5173(97)00310-4

Cited by 147 publications

(78 citation statements)

References 9 publications

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“…Similar results have previously been reported. 13,16 Increasing the amount of calcium leads to a greater degree of cross-linking and aggregation of the initial dimers giving higher gel strength and results in the slower drug release pattern. 16 However, a large amount of added calcium (24 mg/tablet) produced a greater drug release ( Figure 6) and shorter T 50 ( Figure 5).…”

Section: Effect Of Calcium Amount On Drug Releasementioning

confidence: 99%

Effect of degree of esterification of pectin and calcium amount on drug release from pectin-based matrix tablets

Sungthongjeen¹,

Sriamornsak²,

Pitaksuteepong³

et al. 2004

AAPS PharmSciTech

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INTRODUCTIONThe aim of this work was to assess the effect of 2 formulation variables, the pectin type (with different degrees of esterification [DEs]) and the amount of calcium, on drug release from pectin-based matrix tablets. Pectin matrix tablets were prepared by blending indomethacin (a model drug), pectin powder, and various amounts of calcium acetate and then tableting by automatic hydraulic press machine. Differential scanning calorimetry, powder x-ray diffraction, and Fourier transformed-infrared spectroscopy studies of the compressed tablets revealed no drug-polymer interaction and the existence of drug with low crystallinity. The in-vitro release studies in phosphate buffer (United States Pharmacopeia) and tris buffer indicated that the lower the DE, the greater the time for 50% of drug release (T 50 ). This finding is probably because of the increased binding capacity of pectin to calcium. However, when the calcium was excluded, the pectins with different DEs showed similar release pattern with insignificant difference of T 50 . When the amount of calcium acetate was increased from 0 to 12 mg/tablet, the drug release was significantly slower. However, a large amount of added calcium (ie, 24 mg/tablet) produced greater drug release because of the partial disintegration of tablets. The results were more pronounced in phosphate buffer, where the phosphate ions induced the precipitation of calcium phosphate. In conclusion, both pectin type and added calcium affect the drug release from the pectin-based matrix tablets.Hydrophilic polymer matrix systems are widely used in oral controlled drug delivery because of their flexibility to obtain a desirable drug release profile, cost-effectiveness, and broad regulatory acceptance. [1][2][3] The ability of the hydrophilic polymer matrices to release an entrapped drug in aqueous medium and to regulate the release of such drug by control of swelling and cross-linking makes them particularly suitable for controlled-release applications.2 These matrices can be applied for the release of both hydrophilic and hydrophobic drugs and charged solutes. Recently, many controlled-release formulations based on hydrophilic polymer matrices have been developed. [3][4][5][6] Pectins are hydrophilic polysaccharides derived from plant cell walls. They contain linear chains of (1→4) linked α-Dgalacturonic acid residues.7 These uronic acids have carboxyl groups, some of which are naturally presented as methyl esters. The degree of esterification (DE), which is expressed as a percentage of the esterified carboxyl groups, is an important means to classify pectins. High methoxy (HM) pectins (with DE >50%) require a relatively high concentration of soluble solids and a low pH for gel formation. [7][8] Low methoxy (LM) pectins (with DE <50%) form rigid gels by the action of calcium or multivalent cations, which cross-link the galacturonic acid chains. 7 The nontoxicity and the low production costs of pectins make them of great interest for the formulation of controlled-release do...

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Section: Effect Of Calcium Amount On Drug Releasementioning

confidence: 99%

Effect of degree of esterification of pectin and calcium amount on drug release from pectin-based matrix tablets

Sungthongjeen¹,

Sriamornsak²,

Pitaksuteepong³

et al. 2004

AAPS PharmSciTech

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“…Calcium pectinate gel (CaPG) beads has been used as a vehicle for controlled release of drugs (9,10) and for targeting drugs to the colon (11)(12)(13). The benefits include cheap and abundant sources, excellent biocompatibility, and total degradation without hazardous by-products (14).…”

Section: Introductionmentioning

confidence: 99%

Wax-incorporated Emulsion Gel Beads of Calcium Pectinate for Intragastric Floating Drug Delivery

et al. 2008

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Abstract. The purpose of this study was to prepare wax-incorporated pectin-based emulsion gel beads using a modified emulsion-gelation method. The waxes in pectin-olive oil mixtures containing a model drug, metronidazole, were hot-melted, homogenized and then extruded into calcium chloride solution. The beads formed were separated, washed with distilled water and dried for 12 h. The influence of various types and amounts of wax on floating and drug release behavior of emulsion gel beads of calcium pectinate was investigated. The drug-loaded gel beads were found to float on simulated gastric fluid if the sufficient amount of oil was used. Incorporation of wax into the emulsion gel beads affected the drug release. Water-soluble wax (i.e. polyethylene glycol) increased the drug release while other waterinsoluble waxes (i.e. glyceryl monostearate, stearyl alcohol, carnauba wax, spermaceti wax and white wax) significantly retarded the drug release. Different waxes had a slight effect on the drug release. However, the increased amount of incorporated wax in the formulations significantly sustained the drug release while the beads remained floating. The results suggest that wax-incorporated emulsion gel beads could be used as a carrier for intragastric floating drug delivery.

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“…They have been extensively used for encapsulation of enzymes and cells [1], in drug delivery [2], as scaffolds in tissue engineering [3], biosensors and actuators [4], sorbents [5], etc. The conventional methods for mass production of hydrogel microbeads are atomisation [6] and emulsification using conventional high-pressure valve homogenisers or rotor-stator systems [7].…”

Section: Introductionmentioning

confidence: 99%

Manufacture of chitosan microbeads using centrifugally driven flow of gel-forming solutions through a polymeric micronozzle

Mark

Haeberle

Zengerle

et al. 2009

Journal of Colloid and Interface Science

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A centrifugally driven pulse-free flow has been used for generation of tripolyphosphate (TPP)-gelated chitosan beads with tunable diameters ranging from 148 to 257 µm. The production process requires a single motor as the sole actively actuated component. The 2 % (w/w) chitosan solution was extruded through a polymeric nozzle with an inner diameter of 127 µm in the centrifugal field ranging from 93 to 452 g and the drops were collected in an Eppendorf tube containing 10 % (w/w) TPP solution at pH 4.0. The reproducibility of the bead diameters out of different nozzles was very good with overall CVs of the bead diameters down to 15 % and the production rate was 45 beads per second per nozzle at 44 Hz rotor frequency. The production rate was proportional to the sixth power of the rotor frequency, which was explained by the non-Newtonian behaviour of the chitosan solution with a flow behaviour index of 0.466. An analytical model for the bead diameter and production rate has been presented and validated by the experimental data. The shrinkage of chitosan drops during gelation was estimated from the observations and the theoretical model. 2

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Calcium pectinate gel beads for controlled release drug delivery:

Cited by 147 publications

References 9 publications

Effect of degree of esterification of pectin and calcium amount on drug release from pectin-based matrix tablets

Effect of degree of esterification of pectin and calcium amount on drug release from pectin-based matrix tablets

Wax-incorporated Emulsion Gel Beads of Calcium Pectinate for Intragastric Floating Drug Delivery

Manufacture of chitosan microbeads using centrifugally driven flow of gel-forming solutions through a polymeric micronozzle

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