Optimization of Budesonide Compression-Coated Tablets for Colonic Delivery

Yehia, Soad A.; Elshafeey, Ahmed Hassen; Sayed, Ibrahim El Tantawy El; Shehata, Ahmed H.

doi:10.1208/s12249-009-9188-3

Cited by 26 publications

(19 citation statements)

References 27 publications

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“…Although several polysaccharides such as guar gum, pectin, sodium alginate, locust bean gum, chitosan, boswellia gum, and xanthan gum have been used as compressioncoating material (16)(17)(18)(19)(20), carboxymethyl xanthan gum (CMXG), neither alone nor in combination with other polysaccharides, has been explored to assess its suitability for the development of compression-coated colon-targeted tablets. In a previous study, we evaluated Ca +2 ion cross-linked CMXG (Ca-CMXG) matrix tablets for colon delivery of prednisolone (PDL) (21).…”

Section: Introductionmentioning

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: Introductionmentioning

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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“…Polymethacrylates are widely used in pharmaceutical delivery systems for sustained drug delivery, 10) hot melt extrusion, 11,12) microencapsulation, 13) nanoparticle, 14,15) antiretroviral drug delivery, 15,16) floating microspheres, 17) colon delivery 18,19) and transdermal drug delivery. 20) In our previous studies we showed the effect of thermal treating on the release of indomethacin 8) and diclofenac sodium 9) from acrylic matrix tablets and mechanistically studied the effect of heat-treating on physicochemical structure of tablet.…”

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confidence: 99%

Thermal Treating of Acrylic Matrices as a Tool for Controlling Drug Release

Hasanzadeh

Ghaffari

Monajjemzadeh

et al. 2009

CHEMICAL & PHARMACEUTICAL BULLETIN

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The purpose of the present study was to investigate the effect of thermal-treating on the release of ibuprofen from the granules prepared using aqueous dispersions of Eudragit. To accomplish this goal, different formulations were prepared using wet granulation method containing two different types of Eudragit aqueous dispersions, RS30D, RL30D and Avicel as filler. Tablets were prepared using direct compression method. The prepared tablets were thermally treated at 50 and 70°C for 24 h. The drug release from tablets was assessed before and after thermal-treating. The results of release study showed that, thermally-treating the tablets at the temperatures higher than glass transition temperature (Tg) of the polymer can decrease the drug release from matrices. For mechanistic evaluation of the effect of thermal-treating, powder X-ray diffraction (XPD), scanning electron microscopy (SEM), differential scanning calorimeter (DSC), Fourier transform infrared (FT-IR) and helium pycnometer have been employed. The SEM graphs showed that the tablets have smoother surface with less porosity after thermal-treating. FT-IR spectra showed no change in the spectrum of thermally-treated tablet compared to control. In DSC graphs, no crystalline change was seen in the heat-treated samples of ibuprofen tablets, but decreased and widened peak size were related to the probable formation of solid solution of ibuprofen in Eudragit matrix. The results of helium pycnometer showed a significant decrease in the total porosity of some heat-treated samples. This study revealed the importance of thermal treating on the drug release from sustained release tablets containing Eudragit polymer.

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“…These results may be explained on the basis that the release retardation imparted by tablets coated with 10% HPMC provided minimal gastric and intestinal absorption but allowed high drug release in the colon. The successful use of compression coated tablets of budesonide in treatment of ulcerative colitis has been documented [30]. …”

Section: Histopathological Evaluation Of Rabbit Colonmentioning

confidence: 99%