Analyzing the impact of different excipients on drug release behavior in hot-melt extrusion formulations using FTIR spectroscopic imaging

被引：31

作者：

Pudlas, Marieke ^{[1
]}

Kyeremateng, Samuel O. ^{[1
]}

Williams, Leonardo A. M. ^{[2
]}

Kimber, James A. ^{[2
]}

van Lishaut, Holger ^{[1
]}

Kazarian, Sergei G. ^{[2
]}

Woehrle, Gerd H. ^{[1
]}

机构：

[1] AbbVie Deutschland GmbH & Co KG, D-67061 Ludwigshafen, Germany

[2] Univ London Imperial Coll Sci Technol & Med, Dept Chem Engn, London SW7 2AZ, England

来源：

EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES | 2015年 / 67卷

基金：

欧洲研究理事会;

关键词：

Hot-melt extrusion; FT-IR imaging; Drug release; Drug-polymer interactions; Soluplus (R); Copovidone; AMORPHOUS SOLID DISPERSIONS; WATER-SOLUBLE POLYMERS; TABLET DISSOLUTION; PHASE-BEHAVIOR; DOSAGE FORMS; IBUPROFEN; SOLUBILITY; ENHANCEMENT; TECHNOLOGY; MATRICES;

D O I：

10.1016/j.ejps.2014.10.012

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The drug release performance of hot-melt extrudate formulations is mainly affected by its composition and interactions between excipients, drug and the dissolution media. For targeted formulation development, it is crucial to understand the role of these interactions on the drug release performance of extrudate formulations. Attenuated total reflection Fourier transform infrared (ATR-FTIR) spectroscopic imaging was used with an in-situ flow-cell device to analyze the impact of different excipients on drug release from extrudates. The compositions differed in the type of polymer (copovidone and Soluplus (R)), the salt or acid form of ibuprofen and the addition of sodium carbonate. For comparison, conventional USP (United States Pharmacopeia) Apparatus 2 dissolution studies were performed. FTIR imaging revealed that differences in the drug release rate were mainly due to drug polymer interactions. Ibuprofen acid showed interactions with the matrix polymer and exhibited a slower drug release compared to non-interacting ibuprofen salt. Addition of sodium carbonate to the ibuprofen acid containing formulations enhanced the drug release rate of these systems by interfering with the drug polymer interactions. In addition, drug release rates also depended on the polymer type, showing faster drug release rates for extrudate formulations containing copovidone compared to Soluplus (R). FTIR imaging revealed that the stronger the drug polymer interaction in the formulations, the slower the drug release. The addition of sodium carbonate improved release as it reduces drug polymer interactions and allows for the formation of the more water-soluble ibuprofen salt. (C) 2014 Elsevier B.V. All rights reserved.

引用

页码：21 / 31

页数：11

共 44 条

[21] Xanthan gum to tailor drug release of sustained-release ethylcellulose mini-matrices prepared via hot-melt extrusion: in vitro and in vivo evaluation [J].

Verhoeven, E. ;

Vervaet, C. ;

Remon, J. P. .

EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2006, 63 (03) :320-330

[22] Extended release delivery system of metoprolol succinate using hot-melt extrusion: effect of release modifier on methacrylic acid copolymer [J].

Kiran P. Sawant ;

Ritesh Fule ;

Mohammed Maniruzzaman ;

Purnima D. Amin .

Drug Delivery and Translational Research, 2018, 8 :1679-1693

[23] Impact of Drug Loading Method on Drug Release from 3D-Printed Tablets Made from Filaments Fabricated by Hot-Melt Extrusion and Impregnation Processes [J].

Thanawuth, Kasitpong ;

Sutthapitaksakul, Lalinthip ;

Konthong, Srisuda ;

Suttiruengwong, Supakij ;

Huanbutta, Kampanart ;

Dass, Crispin R. ;

Sriamornsak, Pornsak .

PHARMACEUTICS, 2021, 13 (10)

[24] Characterisation of solid dispersions of paracetamol and EUDRAGIT® E prepared by hot-melt extrusion using thermal, microthermal and spectroscopic analysis [J].

Qi, Sheng ;

Gryczke, Andreas ;

Belton, Peter ;

Craig, Duncan Q. M. .

INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2008, 354 (1-2) :158-167

[25] Physicochemical properties and mechanism of drug release from ethyl cellulose matrix tablets prepared by direct compression and hot-melt extrusion [J].

Crowley, MM ;

Schroeder, B ;

Fredersdorf, A ;

Obara, S ;

Talarico, M ;

Kucera, S ;

McGinity, JW .

INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2004, 269 (02) :509-522

[26] Influence of a lipophilic thermal lubricant on the processing conditions and drug release properties of chlorpheniramine maleate tablets prepared by hot-melt extrusion [J].

Zhu, Y ;

Shah, NH ;

Malick, AW ;

Infeld, MH ;

McGinity, JW .

JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY, 2004, 14 (04) :313-318

[27] New investigation of distribution imaging and content uniformity of very low dose drugs using hot-melt extrusion method [J].

Park, Jun-Bom ;

Kang, Chin-Yang ;

Kang, Wie-Soo ;

Choi, Han-Gon ;

Han, Hyo-Kyung ;

Lee, Beom-Jin .

INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2013, 458 (02) :245-253

[28] In vitro and in vivo behavior of ground tadalafil hot-melt extrudates: How the carrier material can effectively assure rapid or controlled drug release [J].

Krupa, Anna ;

Cantin, Oriane ;

Strach, Beata ;

Wyska, Elzbieta ;

Tabor, Zbislaw ;

Siepmann, Juergen ;

Wrobel, Andrzej ;

Jachowicz, Renata .

INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2017, 528 (1-2) :498-510

[29] Chronotherapeutic Drug Delivery of Ketoprofen and Ibuprofen for Improved Treatment of Early Morning Stiffness in Arthritis Using Hot-Melt Extrusion Technology [J].

Dumpa, Nagi Reddy ;

Sarabu, Sandeep ;

Bandari, Suresh ;

Zhang, Feng ;

Repka, Michael A. .

AAPS PHARMSCITECH, 2018, 19 (06) :2700-2709

[30] Chronotherapeutic Drug Delivery of Ketoprofen and Ibuprofen for Improved Treatment of Early Morning Stiffness in Arthritis Using Hot-Melt Extrusion Technology [J].

Nagi Reddy Dumpa ;

Sandeep Sarabu ;

Suresh Bandari ;

Feng Zhang ;

Michael A. Repka .

AAPS PharmSciTech, 2018, 19 :2700-2709

← 1 2 3 4 5 →