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A Novel Approach to Flurbiprofen Pulsatile Colonic Release: Formulation and Pharmacokinetics of Double-Compression-Coated Mini-Tablets.
AAPS PharmSciTech. 2015 Dec; 16(6):1465-73.AP

Abstract

A significant plan is executed in the present study to study the effect of double-compression coating on flurbiprofen core mini-tablets to achieve the pulsatile colonic delivery to deliver the drug at a specific time as per the patho-physiological need of the disease that results in improved therapeutic efficacy. In this study, pulsatile double-compression-coated tablets were prepared based on time-controlled hydroxypropyl methylcellulose K100M inner compression coat and pH-sensitive Eudragit S100 outer compression coat. Then, the tablets were evaluated for both physical evaluation and drug-release studies, and to prove these results, in vivo pharmacokinetic studies in human volunteers were conducted. From the in vitro drug-release studies, F6 tablets were considered as the best formulation, which retarded the drug release in the stomach and small intestine (3.42 ± 0.12% in 5 h) and progressively released to the colon (99.78 ± 0.74% in 24 h). The release process followed zero-order release kinetics, and from the stability studies, similarity factor between dissolution data before and after storage was found to be 88.86. From the pharmacokinetic evaluation, core mini-tablets producing peak plasma concentration (C max) was 14,677.51 ± 12.16 ng/ml at 3 h T max and pulsatile colonic tablets showed C max = 12,374.67 ± 16.72 ng/ml at 12 h T max. The area under the curve for the mini and pulsatile tablets was 41,238.52 and 72,369.24 ng-h/ml, and the mean resident time was 3.43 and 10.61 h, respectively. In conclusion, development of double-compression-coated tablets is a promising way to achieve the pulsatile colonic release of flurbiprofen.

Authors+Show Affiliations

Department of Pharmacy, College of Medical and Health Sciences, Wollega University, Post Box No: 395, Nekemte, Ethiopia. vemulasatish15@gmail.com. Department of Pharmaceutics, Chaitanya College of Pharmaceutical Sciences, Hanamkonda, Warangal, Telangana, 506001, India. vemulasatish15@gmail.com. Department of Pharmaceutics, Jangaon Institute of Pharmaceutical Sciences, Yeshwanthapur, Jangaon, Warangal, Telangana, 506167, India. vemulasatish15@gmail.com.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

26017285

Citation

Vemula, Sateesh Kumar. "A Novel Approach to Flurbiprofen Pulsatile Colonic Release: Formulation and Pharmacokinetics of Double-Compression-Coated Mini-Tablets." AAPS PharmSciTech, vol. 16, no. 6, 2015, pp. 1465-73.
Vemula SK. A Novel Approach to Flurbiprofen Pulsatile Colonic Release: Formulation and Pharmacokinetics of Double-Compression-Coated Mini-Tablets. AAPS PharmSciTech. 2015;16(6):1465-73.
Vemula, S. K. (2015). A Novel Approach to Flurbiprofen Pulsatile Colonic Release: Formulation and Pharmacokinetics of Double-Compression-Coated Mini-Tablets. AAPS PharmSciTech, 16(6), 1465-73. https://doi.org/10.1208/s12249-015-0340-y
Vemula SK. A Novel Approach to Flurbiprofen Pulsatile Colonic Release: Formulation and Pharmacokinetics of Double-Compression-Coated Mini-Tablets. AAPS PharmSciTech. 2015;16(6):1465-73. PubMed PMID: 26017285.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - A Novel Approach to Flurbiprofen Pulsatile Colonic Release: Formulation and Pharmacokinetics of Double-Compression-Coated Mini-Tablets. A1 - Vemula,Sateesh Kumar, Y1 - 2015/05/28/ PY - 2015/03/11/received PY - 2015/05/18/accepted PY - 2015/5/29/entrez PY - 2015/5/29/pubmed PY - 2016/9/13/medline KW - core mini-tablets KW - double-compression coating KW - inner compression coat KW - outer compression coat KW - similarity factor SP - 1465 EP - 73 JF - AAPS PharmSciTech JO - AAPS PharmSciTech VL - 16 IS - 6 N2 - A significant plan is executed in the present study to study the effect of double-compression coating on flurbiprofen core mini-tablets to achieve the pulsatile colonic delivery to deliver the drug at a specific time as per the patho-physiological need of the disease that results in improved therapeutic efficacy. In this study, pulsatile double-compression-coated tablets were prepared based on time-controlled hydroxypropyl methylcellulose K100M inner compression coat and pH-sensitive Eudragit S100 outer compression coat. Then, the tablets were evaluated for both physical evaluation and drug-release studies, and to prove these results, in vivo pharmacokinetic studies in human volunteers were conducted. From the in vitro drug-release studies, F6 tablets were considered as the best formulation, which retarded the drug release in the stomach and small intestine (3.42 ± 0.12% in 5 h) and progressively released to the colon (99.78 ± 0.74% in 24 h). The release process followed zero-order release kinetics, and from the stability studies, similarity factor between dissolution data before and after storage was found to be 88.86. From the pharmacokinetic evaluation, core mini-tablets producing peak plasma concentration (C max) was 14,677.51 ± 12.16 ng/ml at 3 h T max and pulsatile colonic tablets showed C max = 12,374.67 ± 16.72 ng/ml at 12 h T max. The area under the curve for the mini and pulsatile tablets was 41,238.52 and 72,369.24 ng-h/ml, and the mean resident time was 3.43 and 10.61 h, respectively. In conclusion, development of double-compression-coated tablets is a promising way to achieve the pulsatile colonic release of flurbiprofen. SN - 1530-9932 UR - https://www.unboundmedicine.com/medline/citation/26017285/A_Novel_Approach_to_Flurbiprofen_Pulsatile_Colonic_Release:_Formulation_and_Pharmacokinetics_of_Double_Compression_Coated_Mini_Tablets_ DB - PRIME DP - Unbound Medicine ER -