The Role of Force Control Agents in High-Dose Dry Powder Inhaler Formulations

Begat, Philippe; Morton, David Alexander Vodden; Shur, Jagdeep; Kippax, Paul; Staniforth, John N.; Price, Robert

doi:10.1002/jps.21629

Cited by 77 publications

(27 citation statements)

References 25 publications

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“…This concept has been elaborated into the PowderHale ® technology by the University of Bath and Vectura, using magnesium stearate or leucine as additives, later referred to as Force Control Agents (FCAs). The technology, based on a dry mechanical fusion (mechanofusion) process [82,83], is licensed by Vectura to GlaxoSmithKline (for the formulations in the Ellipta ® ) [84] and Novartis (for the Breezhaler ® ) [85]. Also the Chiesi powder formulation for beclomethasone dipropionate and formoterol fumarate (Foster, or Fostair), administered with the NEXThaler ® device, contains magnesium stearate.…”

Section: 'Repair Actions' For Design Weaknesses Of Early Dpi Conceptsmentioning

confidence: 99%

Dry powder inhalation: past, present and future

Boer

Hagedoorn

Hoppentocht

et al. 2016

Expert Opinion on Drug Delivery

226

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Introduction: Early dry powder inhalers (DPIs) were designed for low drug doses in asthma and COPD therapy. Nearly all concepts contained carrier-based formulations and lacked efficient dispersion principles. Therefore, particle engineering and powder processing are increasingly applied to achieve acceptable lung deposition with these poorly designed inhalers. Areas covered: The consequences of the choices made for early DPI development with respect of efficacy, production costs and safety and the tremendous amount of energy put into understanding and controlling the dispersion performance of adhesive mixtures are discussed. Also newly developed particle manufacturing and powder formulation processes are presented as well as the challenges, objectives, and new tools available for future DPI design. Expert opinion: Improved inhaler design is desired to make DPIs for future applications cost-effective and safe. With an increasing interest in high dose drug delivery, vaccination and systemic delivery via the lungs, innovative formulation technologies alone may not be sufficient. Safety is served by increasing patient adherence to the therapy, minimizing the use of unnecessary excipients and designing simple and self-intuitive inhalers, which give good feedback to the patient about the inhalation maneuver. For some applications, like vaccination and delivery of hygroscopic formulations, disposable inhalers may be preferred. ARTICLE HISTORY

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Section: 'Repair Actions' For Design Weaknesses Of Early Dpi Conceptsmentioning

confidence: 99%

Dry powder inhalation: past, present and future

Boer

Hagedoorn

Hoppentocht

et al. 2016

Expert Opinion on Drug Delivery

226

View full text Add to dashboard Cite

show abstract

“…To emphasize that dispersion enhancing particle engineering is indeed not necessary when an effective inhaler design is used, we compared the dispersion and retention performance of pure spray dried tobramycin in the modified inhaler concept with that of co-spray dried tobramycin with 5% L-leucine. Co-spray drying of this excipient is known to modify the particle structure in a beneficial way for dispersion and retention [19,20].…”

Section: Salt Choice and Production Processmentioning

confidence: 99%

The Cyclops for pulmonary delivery of aminoglycosides; a new member of the Twincer™ family

Hoppentocht

Akkerman

Hagedoorn

et al. 2015

European Journal of Pharmaceutics and Biopharmaceutics

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“…Different approaches have been investigated to increase the deagglomeration properties of the drug powders by decreasing the interaction between particles. The use of ternary components such as fine lactose (Louey and Stewart, 2002;Zeng et al, 1998), force control agents such as magnesium stearate (MgSt) and leucine (Begat et al, 2009), and modification of carrier surface (Islam et al, 2004) are a few examples of the approaches explored. A comprehensive list of these approaches can be found in a review (Xu et al, 2011).…”

Section: Introductionmentioning

confidence: 99%

The Kinetics of De-agglomeration of Magnesium Stearate Dry-Coated Salbutamol Sulphate Powders

Shi

Das

Morton

et al. 2015

KONA

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The objective was to investigate the effect of dry coating of salbutamol sulphate (SS) with magnesium stearate (MgSt) on the kinetics of powder de-agglomeration. The relative de-agglomeration of the MgSt coated SS powders was higher than uncoated SS at all air flow rates; the SS coated with 2 % MgSt showed the highest extent of de-agglomeration (> 5 % MgSt coated SS > 1 % MgSt coated SS). Rate of de-agglomeration was described by a cumulative de-agglomerated versus time profile. Profiles fitted a mono-exponential model and the deagglomeration rate constant (k d ) was estimated. No significant differences existed between any of the uncoated and coated powders. The significance of this study relates to the improved aerosolization and de-agglomeration performance of the MgSt coated SS powders with optimum performance of 2 % MgSt coated SS. More significant is the finding that no change existed in de-agglomeration rate constants between the coated and uncoated powders, with the potential implications that their aerosol plume concentration and deposition patterns were similar.

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The Role of Force Control Agents in High-Dose Dry Powder Inhaler Formulations

Cited by 77 publications

References 25 publications

Dry powder inhalation: past, present and future

Dry powder inhalation: past, present and future

The Cyclops for pulmonary delivery of aminoglycosides; a new member of the Twincer™ family

The Kinetics of De-agglomeration of Magnesium Stearate Dry-Coated Salbutamol Sulphate Powders

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