Tags

Type your tag names separated by a space and hit enter

In vitro and in vivo correlation of disintegration and bitter taste masking using orally disintegrating tablet containing ion exchange resin-drug complex.
Int J Pharm. 2013 Oct 15; 455(1-2):31-9.IJ

Abstract

Although the taste-masking of bitter drug using ion exchange resin has been recognized, in vitro testing using an electronic tongue (e-Tongue) and in vivo bitterness test by human panel test was not fully understood. In case of orally disintegrating tablet (ODT) containing bitter medicine, in vitro and in vivo disintegration is also importance for dosage performance. Donepezil hydrochloride was chosen as a model drug due to its bitterness and requires rapid disintegration for the preparation of ODT. In this study, ion exchange resin drug complex (IRDC) at three different ratios (1:2, 1:1, 2:1) was prepared using a spray-drying method and then IRDC-loaded ODT containing superdisintegrants (crospovidone, croscarmellose sodium, and sodium starch glycolate) were prepared by the direct compression method. The physical properties and morphologies were then characterized by scanning electron microscopy (SEM), X-ray powder diffraction (PXRD) and electrophoretic laser scattering (ELS), respectively. The in vitro taste-masking efficiency was measured with an electronic tongue (e-Tongue). In vivo bitterness scale was also evaluated by human volunteers and then we defined new term, "bitterness index (BI)" to link in vitro e-Tongue. There was a good correlation of IRDC between in vitro e-Tongue values and in vivo BI. Furthermore, IRDC-loaded ODT showed good in vitro/in vivo correlation in the disintegration time. The optimal IRDC-loaded ODTs displayed similar drug release profiles to the reference tablet (Aricept(®) ODT) in release media of pH 1.2, pH 4.0, pH 6.8 and distilled water but had significantly better palatability in vivo taste-masking evaluation. The current IRDC-loaded ODT according to the in vitro and in vivo correlation of disintegration and bitter taste masking could provide platforms in ODT dosage formulations of donepezil hydrochloride for improved patient compliances.

Authors+Show Affiliations

Korea United Pharm., Inc., Seoul 135-010, Republic of Korea.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

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

Language

eng

PubMed ID

23933050

Citation

Kim, Jong-Il, et al. "In Vitro and in Vivo Correlation of Disintegration and Bitter Taste Masking Using Orally Disintegrating Tablet Containing Ion Exchange Resin-drug Complex." International Journal of Pharmaceutics, vol. 455, no. 1-2, 2013, pp. 31-9.
Kim JI, Cho SM, Cui JH, et al. In vitro and in vivo correlation of disintegration and bitter taste masking using orally disintegrating tablet containing ion exchange resin-drug complex. Int J Pharm. 2013;455(1-2):31-9.
Kim, J. I., Cho, S. M., Cui, J. H., Cao, Q. R., Oh, E., & Lee, B. J. (2013). In vitro and in vivo correlation of disintegration and bitter taste masking using orally disintegrating tablet containing ion exchange resin-drug complex. International Journal of Pharmaceutics, 455(1-2), 31-9. https://doi.org/10.1016/j.ijpharm.2013.07.072
Kim JI, et al. In Vitro and in Vivo Correlation of Disintegration and Bitter Taste Masking Using Orally Disintegrating Tablet Containing Ion Exchange Resin-drug Complex. Int J Pharm. 2013 Oct 15;455(1-2):31-9. PubMed PMID: 23933050.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - In vitro and in vivo correlation of disintegration and bitter taste masking using orally disintegrating tablet containing ion exchange resin-drug complex. AU - Kim,Jong-Il, AU - Cho,Sang-Min, AU - Cui,Jing-Hao, AU - Cao,Qing-Ri, AU - Oh,Euichaul, AU - Lee,Beom-Jin, Y1 - 2013/08/07/ PY - 2013/04/06/received PY - 2013/07/18/revised PY - 2013/07/27/accepted PY - 2013/8/13/entrez PY - 2013/8/13/pubmed PY - 2014/3/26/medline KW - Bitterness index KW - Donepezil hydrochloride KW - Electronic tongue KW - In vitro/in vivo correlation KW - Ion exchange-resin drug complex KW - Orally disintegrating tablet SP - 31 EP - 9 JF - International journal of pharmaceutics JO - Int J Pharm VL - 455 IS - 1-2 N2 - Although the taste-masking of bitter drug using ion exchange resin has been recognized, in vitro testing using an electronic tongue (e-Tongue) and in vivo bitterness test by human panel test was not fully understood. In case of orally disintegrating tablet (ODT) containing bitter medicine, in vitro and in vivo disintegration is also importance for dosage performance. Donepezil hydrochloride was chosen as a model drug due to its bitterness and requires rapid disintegration for the preparation of ODT. In this study, ion exchange resin drug complex (IRDC) at three different ratios (1:2, 1:1, 2:1) was prepared using a spray-drying method and then IRDC-loaded ODT containing superdisintegrants (crospovidone, croscarmellose sodium, and sodium starch glycolate) were prepared by the direct compression method. The physical properties and morphologies were then characterized by scanning electron microscopy (SEM), X-ray powder diffraction (PXRD) and electrophoretic laser scattering (ELS), respectively. The in vitro taste-masking efficiency was measured with an electronic tongue (e-Tongue). In vivo bitterness scale was also evaluated by human volunteers and then we defined new term, "bitterness index (BI)" to link in vitro e-Tongue. There was a good correlation of IRDC between in vitro e-Tongue values and in vivo BI. Furthermore, IRDC-loaded ODT showed good in vitro/in vivo correlation in the disintegration time. The optimal IRDC-loaded ODTs displayed similar drug release profiles to the reference tablet (Aricept(®) ODT) in release media of pH 1.2, pH 4.0, pH 6.8 and distilled water but had significantly better palatability in vivo taste-masking evaluation. The current IRDC-loaded ODT according to the in vitro and in vivo correlation of disintegration and bitter taste masking could provide platforms in ODT dosage formulations of donepezil hydrochloride for improved patient compliances. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/23933050/In_vitro_and_in_vivo_correlation_of_disintegration_and_bitter_taste_masking_using_orally_disintegrating_tablet_containing_ion_exchange_resin_drug_complex_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(13)00708-4 DB - PRIME DP - Unbound Medicine ER -