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Colonic release and reduced intestinal tissue damage of coated tablets containing naproxen inclusion complex.
Int J Pharm. 2008 Feb 28; 350(1-2):205-11.IJ

Abstract

A colonic-release delivery system containing naproxen inclusion complex with 2-hydroxypropyl-beta-cyclodextrin (2-HPbetaCD) was originally proposed. The core tablets consisting of the naproxen inclusion complex and disintegrants (Ac-Di-Sol), Primojel), Avicel) or Polyplasdone) were formed by direct compression, and then coated with the polymers, either pH-dependent Eudragit S100 and/or pH-independent Eudragit RS100 with plasticizers like dibutyl sebacate (DBS) and aluminum tristearate (AT). The in vitro release characteristics were evaluated in simulated gastric fluid for 2h and then subsequently in simulated intestinal fluid for 12h. The potential histological changes were also evaluated after direct dosing of suspensions of naproxen alone and powdered mixtures of inclusion complex-loaded tablet into rat intestinal segments. No distinct colonic release was observed when disintegrants were excluded in the single-layered coated tablets regardless of coated structures, giving a zero-order fashion over 12h. The coated tablet with double-layered structures of Eudragit S100 and Eudragit RS100 was not also applicable. In contrast, colonic release was achieved when the core tablet containing inclusion complex and disintegrant was coated with only Eudragit S100 in a single-layered structure. The colonic-release tablet was resistant in gastric fluid for 2h and for 2-4h in intestinal fluid, followed by rapid release of the drug after a total of 4-6h of lag time depending on the type of disintegrants. The lag time was advanced in case of DBS while delayed in case of AT. On histological examination, the inclusion complex-loaded suspension caused less intestinal tissue damage than naproxen alone. Based on these findings, the colonic-release tablet with enteric coatings which contains inclusion complex and disintegrants could be useful to deliver drugs like naproxen to the lower small intestine and upper colon with increased dissolution and reduced intestinal tissue damage.

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Authors+Show Affiliations

Piao ZZ
National Research Laboratory for Bioavailability Control, College of Pharmacy, Kangwon National University, Chuncheon 200-701, Republic of Korea.
Lee MK
No affiliation info available
Lee BJ
No affiliation info available

MeSH

2-Hydroxypropyl-beta-cyclodextrinAcrylic ResinsAnimalsChemistry, PharmaceuticalColonHydrogen-Ion ConcentrationIntestinesMaleNaproxenPolymethacrylic AcidsRatsRats, Sprague-DawleySolubilityTablets, Enteric-Coatedbeta-Cyclodextrins

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

17928177

Citation

Piao, Zong-Zhu, et al. "Colonic Release and Reduced Intestinal Tissue Damage of Coated Tablets Containing Naproxen Inclusion Complex." International Journal of Pharmaceutics, vol. 350, no. 1-2, 2008, pp. 205-11.
Piao ZZ, Lee MK, Lee BJ. Colonic release and reduced intestinal tissue damage of coated tablets containing naproxen inclusion complex. Int J Pharm. 2008;350(1-2):205-11.
Piao, Z. Z., Lee, M. K., & Lee, B. J. (2008). Colonic release and reduced intestinal tissue damage of coated tablets containing naproxen inclusion complex. International Journal of Pharmaceutics, 350(1-2), 205-11.
Piao ZZ, Lee MK, Lee BJ. Colonic Release and Reduced Intestinal Tissue Damage of Coated Tablets Containing Naproxen Inclusion Complex. Int J Pharm. 2008 Feb 28;350(1-2):205-11. PubMed PMID: 17928177.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Colonic release and reduced intestinal tissue damage of coated tablets containing naproxen inclusion complex. AU - Piao,Zong-Zhu, AU - Lee,Mi-Kyung, AU - Lee,Beom-Jin, Y1 - 2007/08/31/ PY - 2007/05/14/received PY - 2007/07/26/revised PY - 2007/08/26/accepted PY - 2007/10/12/pubmed PY - 2008/4/9/medline PY - 2007/10/12/entrez SP - 205 EP - 11 JF - International journal of pharmaceutics JO - Int J Pharm VL - 350 IS - 1-2 N2 - A colonic-release delivery system containing naproxen inclusion complex with 2-hydroxypropyl-beta-cyclodextrin (2-HPbetaCD) was originally proposed. The core tablets consisting of the naproxen inclusion complex and disintegrants (Ac-Di-Sol), Primojel), Avicel) or Polyplasdone) were formed by direct compression, and then coated with the polymers, either pH-dependent Eudragit S100 and/or pH-independent Eudragit RS100 with plasticizers like dibutyl sebacate (DBS) and aluminum tristearate (AT). The in vitro release characteristics were evaluated in simulated gastric fluid for 2h and then subsequently in simulated intestinal fluid for 12h. The potential histological changes were also evaluated after direct dosing of suspensions of naproxen alone and powdered mixtures of inclusion complex-loaded tablet into rat intestinal segments. No distinct colonic release was observed when disintegrants were excluded in the single-layered coated tablets regardless of coated structures, giving a zero-order fashion over 12h. The coated tablet with double-layered structures of Eudragit S100 and Eudragit RS100 was not also applicable. In contrast, colonic release was achieved when the core tablet containing inclusion complex and disintegrant was coated with only Eudragit S100 in a single-layered structure. The colonic-release tablet was resistant in gastric fluid for 2h and for 2-4h in intestinal fluid, followed by rapid release of the drug after a total of 4-6h of lag time depending on the type of disintegrants. The lag time was advanced in case of DBS while delayed in case of AT. On histological examination, the inclusion complex-loaded suspension caused less intestinal tissue damage than naproxen alone. Based on these findings, the colonic-release tablet with enteric coatings which contains inclusion complex and disintegrants could be useful to deliver drugs like naproxen to the lower small intestine and upper colon with increased dissolution and reduced intestinal tissue damage. SN - 0378-5173 UR - https://www.unboundmedicine.com/medline/citation/17928177/Colonic_release_and_reduced_intestinal_tissue_damage_of_coated_tablets_containing_naproxen_inclusion_complex_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(07)00739-9 DB - PRIME DP - Unbound Medicine ER -