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Effect of aminoalkyl methacrylate copolymer E/HCl on in vivo absorption of poorly water-soluble drug.
Drug Dev Ind Pharm. 2013 Nov; 39(11):1698-705.DD

Abstract

This study aimed to investigate in vivo absorption of tacrolimus formulated as a solid dispersion using Eudragit E®/HCl (E-SD). E-SD is an aminoalkyl methacrylate copolymer that can be dissolved under neutral pH conditions. E-SD was used alone as a solid dispersion carrier and/or was mixed with tacrolimus primarily dispersed with hydroxypropylmethylcellulose (HPMC). Tacrolimus was formulated with E-SD at several different ratios. Formulations with tacrolimus/E-SD ratio of 1/3 showed higher in vivo absorption, compared to tacrolimus dispersed in the excipients (primarily HPMC) found in commercially available tacrolimus capsules, using a rat in situ closed loop method. Good correlation was observed between in vitro drug solubility and in vivo drug absorption. In vitro solubility tests and rat oral absorption studies of tacrolimus/HPMC solid dispersion formulations were also conducted after mixing the HPMC dispersion with several ratios of E-SD. E-SD/tacrolimus/HPMC formulations yielded high in vitro drug solubility but comparatively low in vivo absorption. Dog oral absorption studies were conducted using capsules containing a formulation of tacrolimus/E-SD at a ratio of 1/5. The E-SD formulation-containing capsule showed higher in vivo drug absorption than tacrolimus dispersed in the standard HPMC capsule. These studies report enhancement of the in vivo absorption of a poorly water-soluble drug following dispersion with E-SD when compared to formulation in HPMC.

Authors+Show Affiliations

Pharmaceutical Research and Technology Labs , Astellas Pharma, Inc., 180 Ozumi, Yaizu, Shizuoka , Japan.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

23062024

Citation

Yoshida, Takatsune, et al. "Effect of Aminoalkyl Methacrylate Copolymer E/HCl On in Vivo Absorption of Poorly Water-soluble Drug." Drug Development and Industrial Pharmacy, vol. 39, no. 11, 2013, pp. 1698-705.
Yoshida T, Kurimoto I, Yoshihara K, et al. Effect of aminoalkyl methacrylate copolymer E/HCl on in vivo absorption of poorly water-soluble drug. Drug Dev Ind Pharm. 2013;39(11):1698-705.
Yoshida, T., Kurimoto, I., Yoshihara, K., Umejima, H., Ito, N., Watanabe, S., Sako, K., & Kikuchi, A. (2013). Effect of aminoalkyl methacrylate copolymer E/HCl on in vivo absorption of poorly water-soluble drug. Drug Development and Industrial Pharmacy, 39(11), 1698-705. https://doi.org/10.3109/03639045.2012.730525
Yoshida T, et al. Effect of Aminoalkyl Methacrylate Copolymer E/HCl On in Vivo Absorption of Poorly Water-soluble Drug. Drug Dev Ind Pharm. 2013;39(11):1698-705. PubMed PMID: 23062024.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effect of aminoalkyl methacrylate copolymer E/HCl on in vivo absorption of poorly water-soluble drug. AU - Yoshida,Takatsune, AU - Kurimoto,Ippei, AU - Yoshihara,Keiichi, AU - Umejima,Hiroyuki, AU - Ito,Naoki, AU - Watanabe,Shunsuke, AU - Sako,Kazuhiro, AU - Kikuchi,Akihiko, Y1 - 2012/10/15/ PY - 2012/10/16/entrez PY - 2012/10/16/pubmed PY - 2014/5/16/medline SP - 1698 EP - 705 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 39 IS - 11 N2 - This study aimed to investigate in vivo absorption of tacrolimus formulated as a solid dispersion using Eudragit E®/HCl (E-SD). E-SD is an aminoalkyl methacrylate copolymer that can be dissolved under neutral pH conditions. E-SD was used alone as a solid dispersion carrier and/or was mixed with tacrolimus primarily dispersed with hydroxypropylmethylcellulose (HPMC). Tacrolimus was formulated with E-SD at several different ratios. Formulations with tacrolimus/E-SD ratio of 1/3 showed higher in vivo absorption, compared to tacrolimus dispersed in the excipients (primarily HPMC) found in commercially available tacrolimus capsules, using a rat in situ closed loop method. Good correlation was observed between in vitro drug solubility and in vivo drug absorption. In vitro solubility tests and rat oral absorption studies of tacrolimus/HPMC solid dispersion formulations were also conducted after mixing the HPMC dispersion with several ratios of E-SD. E-SD/tacrolimus/HPMC formulations yielded high in vitro drug solubility but comparatively low in vivo absorption. Dog oral absorption studies were conducted using capsules containing a formulation of tacrolimus/E-SD at a ratio of 1/5. The E-SD formulation-containing capsule showed higher in vivo drug absorption than tacrolimus dispersed in the standard HPMC capsule. These studies report enhancement of the in vivo absorption of a poorly water-soluble drug following dispersion with E-SD when compared to formulation in HPMC. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/23062024/Effect_of_aminoalkyl_methacrylate_copolymer_E/HCl_on_in_vivo_absorption_of_poorly_water_soluble_drug_ L2 - https://www.tandfonline.com/doi/full/10.3109/03639045.2012.730525 DB - PRIME DP - Unbound Medicine ER -