Applying surface energy derived cohesive–adhesive balance model in predicting the mixing, flow and compaction behaviour of interactive mixtures

Mangal, Sharad; Meiser, Felix; Tan, Guojin; Gengenbach, Thomas R.; Morton, David Alexander Vodden; Larson, Ian

doi:10.1016/j.ejpb.2016.04.021

Cited by 21 publications

(11 citation statements)

References 42 publications

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“…By contrast, an opposite behavior was observed for CFI/DCPA tablets (tensile strength increasing with caffeine content). This is in accordance with the literature [18,24] and attests that the choice of the ingredients is essential and could have many consequences on the quality of the final tablets.…”

Section: Resultssupporting

confidence: 91%

“…Nevertheless, Wu et al's model could not be applied for binary mixtures composed of CFI/DCPA, because it has been impossible to manufacture pure tablets of DCPA due to important binding and sticking phenomena occurring during the direct tableting process. This problem highlighted a restriction of this model, since some pharmaceutical powders, especially API, do not have the required compression properties such as fluidity and compressibility to form pure tablets [24,25]. Moreover, the predicted data calculated from equation 2 and from the model developed in [14] were slightly underestimated compared to the experimental ones, for the two mixtures studied.…”

Section: Comparison With Models From Literaturementioning

confidence: 94%

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Experimental study of tensile strength of pharmaceutical tablets: effect of the diluent nature and compression pressure

et al. 2017

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In the pharmaceutical field, tablets are the most common dosage form for oral administration in the world. Among different manufacturing processes, direct compression is widely used because of its economics interest and it is a process which avoids the steps of wet granulation and drying processes. Tablets are composed of at least two ingredients: an active pharmaceutical ingredient (API) which is mixed with a diluent. The nature of the powders and the processing conditions are crucial for the properties of the blend and, consequently, strongly influence the mechanical characteristics of tablets. Moreover, tablets have to present a suitable mechanical strength to avoid crumbling or breaking when handling, while ensuring an appropriate disintegration after administration. Accordingly, this mechanical property is an essential parameter to consider. Experimental results showed that proportion of the diluent, fragmentary (DCPA) or plastic (MCC), had a large influence on the tensile strength evolution with API content as well as the compression load applied during tableting process. From these results a model was developed in order to predict the tensile strength of binary tablets by knowing the compression pressure. The validity of this model was demonstrated for the two studied systems and a comparison was made with two existing models.

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Section: Resultssupporting

confidence: 91%

Section: Comparison With Models From Literaturementioning

confidence: 94%

Experimental study of tensile strength of pharmaceutical tablets: effect of the diluent nature and compression pressure

et al. 2017

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“…In carrier-based DPI formulations, it is desired that the fine drug particles adhere homogeneously to the surface of the carrier, yielding nonsegregating adhesive mixtures . However, it is also required that during aerosol delivery, these fine particles completely detach from the surface of the carrier (via shear and turbulence induced by the dispersion mechanism of the DPI device and patients’ inspiratory airflow) .…”

Section: Introductionmentioning

confidence: 99%

Assessment of Dry Powder Inhaler Carrier Targeted Design: A Comparative Case Study of Diverse Anomeric Compositions and Physical Properties of Lactose

et al. 2018

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The pulmonary administration landscape has rapidly advanced in recent years. Targeted design of particles by spray-drying for dry powder inhaler development offers an invaluable tool for engineering of new carriers. In this work, different formulation and process aspects of spray-drying were exploited to produce new lactose carriers. Using an integrated approach, lactose was spray-dried in the presence of polyethylene glycol 200 (PEG 200), and the in vitro performance of the resulting particles was compared with other grades of lactose with varying anomeric compositions and/or physical properties. The anomeric composition of lactose in lactose-PEG 200 feed solutions of variable compositions was analyzed via polarimetry at different temperatures. These results were correlated with the solid-state and anomeric composition of the resulting spray-dried particles using modulated differential scanning calorimetry and wide-angle X-ray scattering. The distinct selected grades of lactose were characterized in terms of their micromeritic properties using laser diffraction, helium pycnometry, and gas adsorption, and their particle surface morphologies were evaluated via scanning electron microscopy. Adhesive mixtures of the different lactose carriers with inhalable-sized salbutamol sulfate, as a model drug, were prepared in low doses and evaluated for their blend homogeneity and aerodynamic performance using a Next Generation Impactor. Characterization of the spray-dried particles revealed that predominantly crystalline (in an anomeric ratio 0.8:1 of α to β) spherical particles with a mean size of 50.9 ± 0.4 μm could be produced. Finally, it was apparent that micromeritic, in particular, the shape, and surface properties (inherent to solid-state and anomeric composition) of carrier particles dominantly control DPI delivery. This provided an insight into the relatively inferior performance of the adhesive blends containing the spherical spray-dried lactose-PEG 200 composites.

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“…Meropenem has relatively lower water solubility (approximately 16.4 mg/mL) (Choi et al, 2012), and usually less water soluble component can accumulate on the particle surfaces during drying as the compound with lower solubility will reach supersaturation and precipitate quicker on the surface than the compound with higher solubility (Vehring et al, 2007). However, surfactant-like molecules such as colistin can self-assemble at the air-water interface (Lawrence, Alpar, McAllister, & Brown, 1993; Mestres et al, 1998; Wallace et al, 2010) leading to shell formation (Mangal et al, 2015; Mangal et al, 2016). Spray-dried colistin particles exhibits a lower surface energy than the jet-milled colistin (Jong et al, 2016), attributed to the self-assembly of colistin at the air water interface with a specific orientation with low energy hydrophobic tail facing outwards (Jong et al, 2016).…”

Section: Discussionmentioning

confidence: 99%

Composite particle formulations of colistin and meropenem with improved in-vitro bacterial killing and aerosolization for inhalation

Mangal

Park

et al. 2018

International Journal of Pharmaceutics

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Antibiotic combination therapy is promising for the treatment of lower respiratory tract infections caused by multi-drug resistant Gram-negative pathogens. Inhaled antibiotic therapy offers the advantage of direct delivery of the drugs to the site of infection, as compared to the parenteral administrations. In this study, we developed composite particle formulations of colistin and meropenem. The formulations were characterized for particle size, morphology, specific surface area, surface chemical composition, in-vitro aerosolization performance and in-vitro antibacterial activity. The combinations demonstrated enhanced antibacterial activity against clinical isolates of Acinetobacter baumannii N16870 and Pseudomonas aeruginosa 19147, when compared with antibiotic monotherapy. Spray-dried meropenem alone showed a poor aerosolization performance as indicated by a low fine particle fraction (FPF) of 32.5 ± 3.3%. Co-spraying with colistin improved the aerosolization of meropenem with up to a two-fold increase in the FPF. Such improvements in aerosolization can be attributed to the enrichment of colistin on the surface of composite particles as indicated by X-ray photoelectron spectroscopy (XPS) and time-of-flight secondary ion mass spectrometry (ToF-SIMS), and the increases in particle porosity. Intermolecular interactions between colistin and meropenem were observed for the combination formulations as measured by FT-IR. In conclusion, our results show that co-spray drying with colistin improves the antibacterial activity and aerosol performance of meropenem and produces a formulation with synergistic bacterial killing.

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Applying surface energy derived cohesive–adhesive balance model in predicting the mixing, flow and compaction behaviour of interactive mixtures

Cited by 21 publications

References 42 publications

Experimental study of tensile strength of pharmaceutical tablets: effect of the diluent nature and compression pressure

Experimental study of tensile strength of pharmaceutical tablets: effect of the diluent nature and compression pressure

Assessment of Dry Powder Inhaler Carrier Targeted Design: A Comparative Case Study of Diverse Anomeric Compositions and Physical Properties of Lactose

Composite particle formulations of colistin and meropenem with improved in-vitro bacterial killing and aerosolization for inhalation

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