Predicting the critical quality attributes of ibuprofen tablets via modelling of process parameters for roller compaction and tabletting

Published on Jun 1, 2019in International Journal of Pharmaceutics4.213
· DOI :10.1016/j.ijpharm.2019.05.011
Antonio Matji2
Estimated H-index: 2
(Complutense University of Madrid),
Nicoletta Donato1
Estimated H-index: 1
(Complutense University of Madrid)
+ 6 AuthorsJuan J. Torrado24
Estimated H-index: 24
(Complutense University of Madrid)
We would like to thank Industrial Farmaceutica Cantabria (Torrejon, Spain) for their support and assistance to perform this work. This study was partially supported by the Complutense University of Madrid and a Science Foundation Ireland grant co-funded under the European Regional Development Fund (SFI/12/RC/2275) provided to Prof. A. M. Healy
  • References (32)
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Abstract The comparison of spray drying versus hot melt extrusion (HME) in order to formulate amorphous solid dispersions has been widely studied. However, to the best of our knowledge, the use of both techniques to form cocrystals within a carrier excipient has not previously been compared. The combination of ibuprofen (IBU) and isonicotinamide (INA) in a 1:1 M ratio was used as a model cocrystal. A range of pharmaceutical excipients was selected for processing - mannitol, xylitol, Soluplus and...
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The applications of Raman microspectroscopy have been extended in recent years into the field of clinical medicine, and specifically in cancer research, as a non-invasive diagnostic method in vivo and ex vivo, and the field of pharmaceutical development as a label-free predictive technique for new drug mechanisms of action in vitro. To further illustrate its potential for such applications, it is important to establish its capability to fingerprint drug mechanisms of action and different cellula...
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#1Antonio Matji (Complutense University of Madrid)H-Index: 2
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Last. Juan J. Torrado (Complutense University of Madrid)H-Index: 24
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Abstract Ibuprofen is an oral analgesic usually processed by wet granulation. In this manuscript a new roller compaction process for ibuprofen is reported. The low melting point of ibuprofen is a critical point to be considered during processing. Melting of ibuprofen and its posterior solidification leads to a lower soluble form. The hypothesis of this work is that crystallinity of ibuprofen may be a good indicator of the quality for both raw material selection and the granules obtained during r...
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Last. Anne Marie Healy (Trinity College, Dublin)H-Index: 27
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Abstract The development of solid dosage forms and manufacturing processes are governed by complex physical properties of the powder and the type of pharmaceutical unit operation the manufacturing processes employs. Suitable powder flow properties and compactability are crucial bulk level properties for tablet manufacturing by direct compression. It is also generally agreed that small scale powder flow measurements can be useful to predict large scale production failure. In this study, predictiv...
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Purpose The impact of granule densification in high-shear wet granulation on tabletting and product performance was investigated, at pharmaceutical production scale. Product performance criteria need to be balanced with the need to deliver manufacturability criteria to assure robust industrial scale tablet manufacturing processes. A Quality by Design approach was used to determine in-process control specifications for tabletting, propose a design space for disintegration and dissolution, and to ...
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#1Li Qu (Monash University)H-Index: 10
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Last. Qi (Tony) Zhou (Purdue University)H-Index: 17
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This study aims at testing the feasibility of a single-step coating process to produce a powder formulation of active and inactive ingredients for direct compression. A cohesive ibuprofen powder was coprocessed with a coating material, a binder (polyvinylpyrrolidone K25), and a superdisintegrant (crospovidone). Magnesium stearate (MgSt), l-leucine, and silica were selected as coating materials (1% w/w). A coprocessed powder without any coating material was employed as a control. Coating with MgS...
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#2Sharvil Patil (Poona College of Arts Science & Commerce)H-Index: 5
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AbstractContext: Most of the active pharmaceutical ingredients (APIs) suffer from a drawback of poor aqueous solubility. In addition to the same, some APIs show poor tabletting behavior creating problems in formulation development. Crystal engineering can be an efficient tool in rectification of such problems associated with the APIs. Thus present work deals with crystallization of ibuprofen (a model drug) onto the surface of dicalcium phosphate (DCP) particles using different techniques.Objecti...
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#1Changquan Calvin Sun (UMN: University of Minnesota)H-Index: 30
#2Peter Kleinebudde (HHU: University of Düsseldorf)H-Index: 43
In this mini-review, we have critically examined literature aimed at understanding the mechanisms to the frequently observed phenomenon of loss of tabletability of a powder after dry granulation by slugging or roll compaction. Impact of each mechanism on tabletability could be explained by considering their influence on either bonding area (BA) or bonding strength (BS). For plastically deforming materials, key mechanisms that influence tabletability of dry granulated powders include lubrication,...
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#1Jose R. Cerda (Complutense University of Madrid)
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Although not readily accessible yet to many community and hospital pharmacists, fuse deposition modelling (FDM) is a 3D printing technique that can be used to create a 3D pharmaceutical dosage form by employing drug loaded filaments extruded via a nozzle, melted and deposited layer by layer. FDM requires printable filaments, which are commonly manufactured by hot melt extrusion, and identifying a suitable extrudable drug-excipient mixture can sometimes be challenging. We propose here the use of ...
#1Antonio Matji (Complutense University of Madrid)H-Index: 2
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The bioequivalence of a new ibuprofen 600-mg film-coated tablet obtained by roller compaction was studied in a crossover study with 22 healthy volunteers. Bioequivalence was analyzed based on (a) the S-enantiomer, (b) the R-enantiomer, and (c) the sum of both enantiomers (representing the results of an achiral assay). The bioequivalence conclusion for ibuprofen products should be based not only on AUC and Cmax but also on tmax since tmax is related to the onset of action. However, it is not poss...
#1Takuya Oishi (University of Toyama)H-Index: 1
#2Yoshihiro Hayashi (University of Toyama)H-Index: 7
Last. Yoshinori Onuki (University of Toyama)H-Index: 15
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Abstract Our aim was to understand better the causal relationships between material attributes (MAs), process parameters (PPs), and critical quality attributes (CQAs) using an originally created large dataset and regularized linear regression models. In this study, we focused on the following three points: (1) creation of a dataset comprising several tablet production methods, (2) the influence of interaction terms of MAs and/or PPs, and (3) comparison of regularized linear regression models wit...
Abstract The present study aimed to establish a new model to evaluate the compressibility and compactibility of materials simultaneously. Eighteen types of pharmaceutical excipients were studied via direct compaction. The model was established as CR = y0 + Ae−bP, r2 ≥ 0.9684 (where CR is the compression ratio and P is the compaction force and y0, A, b is constant). The physical meaning of y0 and b were studied in the model. The results show that y0 has a strong correlation with the mean yield pr...