Tablets based on compressed zein microspheres for sustained oral administration

Design, pharmacokinetics, and clinical study

Sheng Ju Gong, Shi Xuan Sun, Qing Shen Sun, Jin Ye Wang, Xinming Liu, Guo Yan Liu

Research output: Contribution to journalArticle

18 Citations (Scopus)

Abstract

In our previous study, we reported a novel tablet based on compressed zein microspheres as a universal drug delivery system using the hydrophobic protein zein, which shows zero-order release in the presence of pepsin. However, this formulation had difficulty with disintegration under physiological conditions within 48 h, and thus could not be used directly for oral administration. In the present study, a formulation of ivermectin (IVM) tablets based on compressed zein microspheres was improved as a new dosage form. The plasma disposition pharmacokinetics of IVM tablets based on compressed zein microspheres after oral administration was studied over a 7-day period with six dogs (Canis familiaris), using a commercial IVM tablet (5 mg/piece, Yilijia®) as a control. Clinical efficacy was tested using 270 dogs presented as veterinary patients for the treatment of demodicidosis. A formulation with disintegration time within 15 min could be obtained. The acquired C max, Tmax, and AUC were 9.89 ± 0.34 ng/mL, 11.33 ± 2.63 h, and 883.87 ng h/mL for IVM tablets based on compressed zein microspheres and 9.64 ± 1.05 ng/mL, 7.26 ± 2.09 h, and 666.30 ng h/mL for Yilijia®, respectively. The bioavailability of the tablets based on compressed zein microspheres was 132.65% that of Yilijia ®. Efficacy for the dogs in all the IVM tablets based on compressed zein microspheres-treated groups reached 100% at 7, 14, and 21 days post administration.

Original languageEnglish (US)
Pages (from-to)195-208
Number of pages14
JournalJournal of Biomaterials Applications
Volume26
Issue number2
DOIs
StatePublished - Aug 1 2011

Fingerprint

Zein
Pharmacokinetics
Microspheres
Tablets
Ivermectin
Disintegration
Pepsin A
Dosage Forms
Proteins
Plasmas

Keywords

  • ivermectin
  • oral administration.
  • pharmacokinetics
  • tablets based on compressed zein microspheres
  • zein

ASJC Scopus subject areas

  • Biomaterials
  • Biomedical Engineering

Cite this

Tablets based on compressed zein microspheres for sustained oral administration : Design, pharmacokinetics, and clinical study. / Gong, Sheng Ju; Sun, Shi Xuan; Sun, Qing Shen; Wang, Jin Ye; Liu, Xinming; Liu, Guo Yan.

In: Journal of Biomaterials Applications, Vol. 26, No. 2, 01.08.2011, p. 195-208.

Research output: Contribution to journalArticle

Gong, Sheng Ju ; Sun, Shi Xuan ; Sun, Qing Shen ; Wang, Jin Ye ; Liu, Xinming ; Liu, Guo Yan. / Tablets based on compressed zein microspheres for sustained oral administration : Design, pharmacokinetics, and clinical study. In: Journal of Biomaterials Applications. 2011 ; Vol. 26, No. 2. pp. 195-208.
@article{bdbc6ff4478349c3902cd7b1da3cde81,
title = "Tablets based on compressed zein microspheres for sustained oral administration: Design, pharmacokinetics, and clinical study",
abstract = "In our previous study, we reported a novel tablet based on compressed zein microspheres as a universal drug delivery system using the hydrophobic protein zein, which shows zero-order release in the presence of pepsin. However, this formulation had difficulty with disintegration under physiological conditions within 48 h, and thus could not be used directly for oral administration. In the present study, a formulation of ivermectin (IVM) tablets based on compressed zein microspheres was improved as a new dosage form. The plasma disposition pharmacokinetics of IVM tablets based on compressed zein microspheres after oral administration was studied over a 7-day period with six dogs (Canis familiaris), using a commercial IVM tablet (5 mg/piece, Yilijia{\circledR}) as a control. Clinical efficacy was tested using 270 dogs presented as veterinary patients for the treatment of demodicidosis. A formulation with disintegration time within 15 min could be obtained. The acquired C max, Tmax, and AUC were 9.89 ± 0.34 ng/mL, 11.33 ± 2.63 h, and 883.87 ng h/mL for IVM tablets based on compressed zein microspheres and 9.64 ± 1.05 ng/mL, 7.26 ± 2.09 h, and 666.30 ng h/mL for Yilijia{\circledR}, respectively. The bioavailability of the tablets based on compressed zein microspheres was 132.65{\%} that of Yilijia {\circledR}. Efficacy for the dogs in all the IVM tablets based on compressed zein microspheres-treated groups reached 100{\%} at 7, 14, and 21 days post administration.",
keywords = "ivermectin, oral administration., pharmacokinetics, tablets based on compressed zein microspheres, zein",
author = "Gong, {Sheng Ju} and Sun, {Shi Xuan} and Sun, {Qing Shen} and Wang, {Jin Ye} and Xinming Liu and Liu, {Guo Yan}",
year = "2011",
month = "8",
day = "1",
doi = "10.1177/0885328210363504",
language = "English (US)",
volume = "26",
pages = "195--208",
journal = "Journal of Biomaterials Applications",
issn = "0885-3282",
publisher = "SAGE Publications Ltd",
number = "2",

}

TY - JOUR

T1 - Tablets based on compressed zein microspheres for sustained oral administration

T2 - Design, pharmacokinetics, and clinical study

AU - Gong, Sheng Ju

AU - Sun, Shi Xuan

AU - Sun, Qing Shen

AU - Wang, Jin Ye

AU - Liu, Xinming

AU - Liu, Guo Yan

PY - 2011/8/1

Y1 - 2011/8/1

N2 - In our previous study, we reported a novel tablet based on compressed zein microspheres as a universal drug delivery system using the hydrophobic protein zein, which shows zero-order release in the presence of pepsin. However, this formulation had difficulty with disintegration under physiological conditions within 48 h, and thus could not be used directly for oral administration. In the present study, a formulation of ivermectin (IVM) tablets based on compressed zein microspheres was improved as a new dosage form. The plasma disposition pharmacokinetics of IVM tablets based on compressed zein microspheres after oral administration was studied over a 7-day period with six dogs (Canis familiaris), using a commercial IVM tablet (5 mg/piece, Yilijia®) as a control. Clinical efficacy was tested using 270 dogs presented as veterinary patients for the treatment of demodicidosis. A formulation with disintegration time within 15 min could be obtained. The acquired C max, Tmax, and AUC were 9.89 ± 0.34 ng/mL, 11.33 ± 2.63 h, and 883.87 ng h/mL for IVM tablets based on compressed zein microspheres and 9.64 ± 1.05 ng/mL, 7.26 ± 2.09 h, and 666.30 ng h/mL for Yilijia®, respectively. The bioavailability of the tablets based on compressed zein microspheres was 132.65% that of Yilijia ®. Efficacy for the dogs in all the IVM tablets based on compressed zein microspheres-treated groups reached 100% at 7, 14, and 21 days post administration.

AB - In our previous study, we reported a novel tablet based on compressed zein microspheres as a universal drug delivery system using the hydrophobic protein zein, which shows zero-order release in the presence of pepsin. However, this formulation had difficulty with disintegration under physiological conditions within 48 h, and thus could not be used directly for oral administration. In the present study, a formulation of ivermectin (IVM) tablets based on compressed zein microspheres was improved as a new dosage form. The plasma disposition pharmacokinetics of IVM tablets based on compressed zein microspheres after oral administration was studied over a 7-day period with six dogs (Canis familiaris), using a commercial IVM tablet (5 mg/piece, Yilijia®) as a control. Clinical efficacy was tested using 270 dogs presented as veterinary patients for the treatment of demodicidosis. A formulation with disintegration time within 15 min could be obtained. The acquired C max, Tmax, and AUC were 9.89 ± 0.34 ng/mL, 11.33 ± 2.63 h, and 883.87 ng h/mL for IVM tablets based on compressed zein microspheres and 9.64 ± 1.05 ng/mL, 7.26 ± 2.09 h, and 666.30 ng h/mL for Yilijia®, respectively. The bioavailability of the tablets based on compressed zein microspheres was 132.65% that of Yilijia ®. Efficacy for the dogs in all the IVM tablets based on compressed zein microspheres-treated groups reached 100% at 7, 14, and 21 days post administration.

KW - ivermectin

KW - oral administration.

KW - pharmacokinetics

KW - tablets based on compressed zein microspheres

KW - zein

UR - http://www.scopus.com/inward/record.url?scp=80052676037&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=80052676037&partnerID=8YFLogxK

U2 - 10.1177/0885328210363504

DO - 10.1177/0885328210363504

M3 - Article

VL - 26

SP - 195

EP - 208

JO - Journal of Biomaterials Applications

JF - Journal of Biomaterials Applications

SN - 0885-3282

IS - 2

ER -