The Effect of Mechanical Processing on Surface Stability of Pharmaceutical Powders: Visualization by Atomic Force Microscopy

Begat, Philippe; Young, Paul M.; Edge, Stephen; Kaerger, Joerg; Price, Robert

doi:10.1002/jps.10320

Cited by 46 publications

(29 citation statements)

References 14 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Particle surface roughness (Donovan and Smyth, 2010;Hooton et al, 2006a;Kaialy and Nokhodchi, 2013b) Degradation during storage or processing (Begat et al, 2003) Crystal growth (Durbin and Carlson, 1992;Price and Young, 2004) Crystallinity (Begat et al, 2003;Ward et al, 2005) Polymorphism (Danesh et al, 2000;Hooton et al, 2006a) 3D imaging of the particle (Hooton et al, 2006a) Nanoindentation Elastic modulus (local)…”

Section: Phase Imagingmentioning

confidence: 99%

“…This is particularly useful for analysing milled powders, e.g. milled salbutamol sulphate particles (Begat et al, 2003). When a material is subjected to a high-energy milling process, amorphous regions are created which then affect the material's stability.…”

Section: Topographical Imagingmentioning

confidence: 99%

“…When a material is subjected to a high-energy milling process, amorphous regions are created which then affect the material's stability. Begat et al (2003) compared the structure of crystals before and after micronisation using cross-sectional AFM surface analysis (scanning cross sections of processed and unprocessed crystals) and observed the emergence of additional amorphous regions. Increasing the milling times lowered the ratio of crystalline to amorphous areas (Begat et al, 2003).…”

Section: Topographical Imagingmentioning

confidence: 99%

“…Begat et al (2003) compared the structure of crystals before and after micronisation using cross-sectional AFM surface analysis (scanning cross sections of processed and unprocessed crystals) and observed the emergence of additional amorphous regions. Increasing the milling times lowered the ratio of crystalline to amorphous areas (Begat et al, 2003). This agreed with moisture sorption data which showed a higher degree of moisture uptake by milled particles, indicating an increasing amount of amorphous material on the surface.…”

Section: Topographical Imagingmentioning

confidence: 99%

See 3 more Smart Citations

Characterisation of dry powder inhaler formulations using atomic force microscopy

Weiss

McLoughlin

Cathcart

2015

International Journal of Pharmaceutics

View full text Add to dashboard Cite

A B S T R A C TInhalation formulations are a popular way of treating the symptoms of respiratory diseases. The active pharmaceutical ingredient (API) is delivered directly to the site of action within the deep lung using an inhalation device such as the dry powder inhaler (DPI).The performance of the formulation and the efficiency of the treatment depend on a number of factors including the forces acting between the components. In DPI formulations these forces are dominated by interparticulate interactions. Research has shown that adhesive and cohesive forces depend on a number of particulate properties such as size, surface roughness, crystallinity, surface energetics and combinations of these. With traditional methods the impact of particulate properties on interparticulate forces could be evaluated by examining the bulk properties. Atomic force microscopy (AFM), however, enables the determination of local surface characteristics and the direct measurement of interparticulate forces using the colloidal probe technique. AFM is considered extremely useful for evaluating the surface topography of a substrate (an API or carrier particle) and even allows the identification of crystal faces, defects and polymorphs from high-resolution images. Additionally, information is given about local mechanical properties of the particles and changes in surface composition and energetics. The assessment of attractive forces between two bodies is possible by using colloidal probe AFM.This review article summarises the application of AFM in DPI formulations while specifically focussing on the colloidal probe technique and the evaluation of interparticulate forces.2015 Elsevier B.V. All rights reserved.

show abstract

Section: Phase Imagingmentioning

confidence: 99%

Section: Topographical Imagingmentioning

confidence: 99%

Section: Topographical Imagingmentioning

confidence: 99%

Section: Topographical Imagingmentioning

confidence: 99%

See 2 more Smart Citations

Characterisation of dry powder inhaler formulations using atomic force microscopy

Weiss

McLoughlin

Cathcart

2015

International Journal of Pharmaceutics

View full text Add to dashboard Cite

show abstract

“…4) AFM was also used to investigate adhesion problems during tablet manufacturing relative to run time on the tablet press and the influence of mechanical milling time on the surface stability of salbutamol sulfate. 5,6) Therefore, we investigated the morphological surface structures of the three tablets using SEM and AFM and found that SEM and AFM image analyses can be used to correlate surface structure and dissolution rates. …”

mentioning

confidence: 99%

Evaluation of Correlation between Dissolution Rates of Loxoprofen Tablets and Their Surface Morphology Observed by Scanning Electron Microscope and Atomic Force Microscope

Yoshikawa

Murata

Shida

et al. 2010

CHEMICAL & PHARMACEUTICAL BULLETIN

View full text Add to dashboard Cite

It was recently reported that there is a significant difference in dissolution rates between brand-name and generic drugs, although most generic versions passed the official dissolution test standards. 1) We examined the dissolution rates of 60 mg tablets of Loxonin ® , Loxot ® , and Lobu ® and confirmed a significant difference among them. The dissolution rate of an active pharmaceutical ingredient greatly depends on the surface structure and the constituent particle size of the tablet. These three tablets include loxoprofen sodium hydrate, C 15 H 17 NaO 3 · 2H 2 O, so dihydration is the same.The atomic force microscope (AFM) can be used to obtain 3D images with nanometer resolution and quantitatively measure surface morphology. Furthermore, AFM was recently used to measure adhesion force between glidants and pharmaceutical fillers and particle friction in a pharmaceutical system. 2,3) The mechanism of drug particle formation has also been investigated by scanning electron microscope (SEM) and AFM. 4) AFM was also used to investigate adhesion problems during tablet manufacturing relative to run time on the tablet press and the influence of mechanical milling time on the surface stability of salbutamol sulfate. 5,6) Therefore, we investigated the morphological surface structures of the three tablets using SEM and AFM and found that SEM and AFM image analyses can be used to correlate surface structure and dissolution rates. ExperimentalMaterials The samples used in this study were Loxonin ® , Loxot ® , and Lobu ® tablets. The dissolution rate and behavior of loxoprofen sodium were examined by following the dissolution test manual and the loxoprofen sodium tables of the Japanese Pharmaceutical Codex (JPC), part 3. The apparatus used for the dissolution test was an NTR-6200AC (Toyama Industry Co, Toyama, Japan). Briefly, the dissolution test was conducted with 900 ml of aqueous solution at 37°C with stirring at 50 rpm by the paddle method. About 20 ml of the eluate was promptly filtered with a 0.45-mm membrane filter (Millipore, Bedford, MA, U.S.A.); the first 10 ml of eluate was removed, the remaining 10 ml was diluted to the regulation quantity, and was prepared to measure absorbance. The same process was performed at a time interval of 5 min. The absorbance of the loxoprofen sodium was measured at 5 min intervals at wavelengths of 223 nm and 340 nm with a U-1900 spectrophotometer (Hitachi, Japan).AFM The AFM instrument was a NanoScope IIIa (Digital Instruments, Santa Barbara, CA, U.S.A.). 7,8) A tablet sample fixed with adhesive tape on a stainless steel plate was placed on the scanner unit of the instrument. AFM images were measured using the tapping mode in air. A cantilever (SSS-NCH-50) made of n ϩ -silicon was used. The scan rate was 0.5-0.7 Hz, and the tapping frequency was about 330 kHz.SEM SEM images and the elemental analysis of the tablet surface were conducted with an S-800 (Hitachi) and JSM-5200 (JEOL, Tokyo, Japan) equipped with an energy-dispersible X-ray (EDX) diffractometer JED 2001, respectively....

show abstract

Nanocrystals Production, Characterization, and Application for Cancer Therapy

Hollis

2013

Pharmaceutical Sciences Encyclopedia

View full text Add to dashboard Cite

The delivery of synthesized drugs exhibiting poor solubility in water is extremely difficult, limiting bioavailability and causing adverse effects when solubilized. A need was determined for developing a formulation to deliver poorly water‐soluble drugs without indiscriminately reaching healthy organs and tissues. Therefore, nanocrystal formulations have been a significant focus for delivering poorly water‐soluble drugs via oral, paraenteral, and alternative routes. Using nanocrystal formulations avoids potential side effects and instability related to many existing delivery systems. Currently, few cancer therapy products are approved by the Food and Drug Administration (FDA) in which poorly soluble drugs are formulated by nanoparticles. In this chapter, the production of nanocrystals of pharmaceutical organic compounds is reviewed. Thereafter, the chapter will focus on the application of nanocrystals for cancer therapy.

show abstract

The Effect of Mechanical Processing on Surface Stability of Pharmaceutical Powders: Visualization by Atomic Force Microscopy

Cited by 46 publications

References 14 publications

Characterisation of dry powder inhaler formulations using atomic force microscopy

Characterisation of dry powder inhaler formulations using atomic force microscopy

Evaluation of Correlation between Dissolution Rates of Loxoprofen Tablets and Their Surface Morphology Observed by Scanning Electron Microscope and Atomic Force Microscope

Nanocrystals Production, Characterization, and Application for Cancer Therapy

Contact Info

Product

Resources

About