Influence of Solid Phase and Formulation Processing on Stability of Abbott-232 Tablet Formulations

Wardrop, Jacqueline; Law, Devalina; Qiu, Yihong; Engh, Kevin; Faitsch, L.; Ling, Chris D.

doi:10.1002/jps.20679

Cited by 34 publications

(18 citation statements)

References 18 publications

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“…[11][12][13] During pharmaceutical unit operations, processinduced stresses originate from temperature (e.g., drying phase), mechanical activation (e.g., milling, compression), or water/solvate (e.g., wet granulation). The anhydrate-to-hydrate conversion of theophylline during wet granulation has been reported, 14,15 while Wardrop et al 16 observed an anhydrate-to-amorphous conversion of the uroselective a 1A antagonist, Abbott-232. Changes in the degree of crystallinity as a result of compression and milling have also been widely reported.…”

Section: Introductionmentioning

confidence: 99%

Towards Effective Solid Form Screening

Allesø

Tian

Cornett

et al. 2010

Journal of Pharmaceutical Sciences

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Section: Introductionmentioning

confidence: 99%

Towards Effective Solid Form Screening

Allesø

Tian

Cornett

et al. 2010

Journal of Pharmaceutical Sciences

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“…This study showed that these techniques allowed rapid and non‐invasive monitoring of solid‐state transformations during pharmaceutical manufacturing. In another work, solid‐state transformations, including amorphisation during wet granulation, were described for the API Abbott‐232 using a range of analytical methods including XRPD, polarising light microscopy, DSC, thermogravimetric analysis and Raman spectroscopy 139 . The amorphisation of paracetamol in polymeric mixtures containing the drug and microcrystalline cellulose, hydroxypropyl methylcellulose or cross‐linked polyvinyl pyrrolidone after melting and cooling has been observed using a range of techniques, including DSC, hot‐stage microscopy, micro FTIR spectroscopy and scanning electron microscopy 140 .…”

Section: Introductionmentioning

confidence: 99%

Analysis of solid-state transformations of pharmaceutical compounds using vibrational spectroscopy

Heinz

Strachan

Gordon

et al. 2009

Journal of Pharmacy and Pharmacology

196

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Objectives Solid-state transformations may occur during any stage of pharmaceutical processing and upon storage of a solid dosage form. Early detection and quantification of these transformations during the manufacture of solid dosage forms is important since the physical form of an active pharmaceutical ingredient can significantly influence its processing behaviour, including powder flow and compressibility, and biopharmaceutical properties such as solubility, dissolution rate and bioavailability. Key findings Vibrational spectroscopic techniques such as infrared, near-infrared, Raman and, most recently, terahertz pulsed spectroscopy have become popular for solidstate analysis since they are fast and non-destructive and allow solid-state changes to be probed at the molecular level. In particular, Raman and near-infrared spectroscopy, which require no sample preparation, are now commonly used coupled to fibreoptic probes and are able to characterise solid-state conversions in-line. Traditionally, uni-or bivariate approaches have been used to analyse spectroscopic data sets; however, recently the simultaneous detection of several solid-state forms has been increasingly performed using multivariate approaches where even overlapping spectral bands can be analysed. Summary This review discusses the applications of different vibrational spectroscopic techniques to detect and monitor solid-state transformations possible for crystalline polymorphs, hydrates and amorphous forms of pharmaceutical compounds. In this context, the theoretical basis of solid-state transformations and vibrational spectroscopy and common experimental approaches are described, including recent methods of data analysis.

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“…The tensile strength (TS), used as an index of hardness of tablets, was determined from: 26) TS = (2) where F is the crushing force of the tablet in the diametrical direction, D is the diameter, and w is the thickness of the tablet. In convex tablets, w is the length of thickest part of the tablet.…”

Section: Determination Of Tensile Strengthmentioning

confidence: 99%

“…1) In addition, direct compression is easy to adopt when the active pharmaceutical ingredient (API) is unstable in water or to thermal drying. 2) It is beneficial if we can provide the optimal formulation of preliminary mixed powders (premix powders) in advance for tableting use. Such knowledge can be applicable to the development of an initial trial of tablet formulation containing APIs.…”

mentioning

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Optimization of Premix Powders for Tableting Use

Todo

Sato

Takayama

et al. 2018

CHEMICAL & PHARMACEUTICAL BULLETIN

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SummaryDirect compression is a popular choice as it provides the simplest way to prepare the tablet.It can be easily adopted when the active pharmaceutical ingredient (API) is unstable in water or to thermal drying. An optimal formulation of preliminary mixed powders (premix powders) is beneficial if prepared in advance for tableting use. The aim of this study was to find the optimal formulation of the premix powders composed of lactose (LAC), cornstarch (CS), and microcrystalline cellulose (MCC) by using statistical techniques. Based on the "Quality by Design" concept, a (3,3)-simplex lattice design consisting of three components, LAC, CS, and MCC was employed to prepare the model premix powders. Response surface method incorporating a thin-plate spline interpolation (RSM-S) was applied for estimation of the optimum premix powders for tableting use. The effect of tablet shape identified by the surface curvature on the optimization was investigated. The optimum premix powder was effective when the premix was applied to a small quantity of API, although the function of premix was limited in the case of the formulation of large amount of API. Statistical techniques are valuable to exploit new functions of well-known materials such as LAC, CS, and MCC.Key words tablet; direct compression; premix powder; quality by design; simplex lattice design; thin-plate spline Chemical and Pharmaceutical Bulletin Advance PublicationA compressed tablet is one of the most popular and widely used dosage forms for drug administration. They are easy to swallow and the proper dose is countable by the number of tablets. Compared with the other solid dosage forms such as powders, granules, and capsules, tableting requires rather long and complex manufacturing process, i.e., milling, sieving, mixing, granulation, drying, and compression via a tableting machine. Direct compression is the simplest method and a popular choice to prepare the tablet. 1)In addition, direct compression is easy to adopt when the active pharmaceutical ingredient (API) is unstable in water or to thermal drying.2)It is beneficial if we can provide the optimal formulation of preliminary mixed powders (premix powders) in advance for tableting use. Such knowledge can be applicable to the development of an initial trial of tablet formulation containing APIs.The aim of this study was to find the optimal formulation of the premix powders composed of lactose (LAC), cornstarch (CS), and microcrystalline cellulose (MCC) by using a series of statistical techniques. [3][4][5][6][7][8][9][10][11][12] LAC is used as a filler-binder and CS as a filler and possible disintegrating agent. 13)MCC is a filler and used mostly as a binder for direct compression. 14)These components are the most common and effective tableting materials. 15) In recent years, the application of statistical techniques to pharmaceutical product development has been implemented to allow the "Quality by Design" concept proposed by the International Council for Harmonization of Technical Requirements for Pharm...

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Influence of Solid Phase and Formulation Processing on Stability of Abbott-232 Tablet Formulations

Cited by 34 publications

References 18 publications

Towards Effective Solid Form Screening

Towards Effective Solid Form Screening

Analysis of solid-state transformations of pharmaceutical compounds using vibrational spectroscopy

Optimization of Premix Powders for Tableting Use

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