Novel dry powder inhalation system based on dispersion of lyophilisates

Claus, Sarah; Schoenbrodt, Tilo; Weiler, Claudius; Frieß, Wolfgang

doi:10.1016/j.ejps.2011.03.005

Cited by 17 publications

(10 citation statements)

References 54 publications

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“…First, we added attachments for dispersion to the aerodynamic particle sizer (APS), as shown in Figure 1 , so that particles dispersed from a dosage form under the same condition as for MSLI measurement could be measured by APS. Then, we examined the correlation between MSLI and the APS with dispersion attachments using lyophilizate for dry powder inhalation (LDPI) formulations [ 27 , 28 , 29 , 30 , 31 ] as formulations with porous particles. In the LDPI system, porous particles suitable for pulmonary administration are generated on inhalation.…”

Section: Introductionmentioning

confidence: 99%

Simple Method to Measure the Aerodynamic Size Distribution of Porous Particles Generated on Lyophilizate for Dry Powder Inhalation

et al. 2020

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Recently, statistical techniques such as design of experiments are being applied for efficient optimization of oral formulations. To use these statistical techniques for inhalation formulations, efficient methods for rapid determination of the aerodynamic particle size distribution of many samples are needed. Therefore, we aimed to develop a simple method to measure aerodynamic particle size distribution that closely agrees with the results of inhalation characteristic tests. We added attachments for dispersion to the aerodynamic particle sizer (APS) so that formulations could be dispersed under the same condition as for multi-stage liquid impinger (MSLI) measurement. Then, we examined the correlation between MSLI and APS using lyophilizate for dry powder inhalation formulations that generate porous particles just on inhalation. It is difficult to obtain the accurate aerodynamic particle size distribution of porous particles by APS because the particle density is difficult to estimate accurately. However, there was a significant correlation between MSLI and APS when the particle density settings for APS measurement was calculated by a conversion factor based on the result of MSLI. The APS with dispersion attachments and this conversion factor can measure a number of samples in a short time, thereby enabling more efficient optimization of dry powder inhalers.

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Section: Introductionmentioning

confidence: 99%

Simple Method to Measure the Aerodynamic Size Distribution of Porous Particles Generated on Lyophilizate for Dry Powder Inhalation

et al. 2020

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“…Such powders are frequently highly voluminous because of their extreme porosity, particularly when being prepared by freeze drying [120], spray-freeze drying [98,121], or spray drying with volatile or blowing agents [94,122]. The excipients used furthermore increase the dose weight to be administered, and for high-dose drugs, this may also increase the number of inhalations per dose.…”

Section: Formulation Of High-dose Drugsmentioning

confidence: 99%

Dry powder inhalation: past, present and future

Boer

Hagedoorn

Hoppentocht

et al. 2016

Expert Opinion on Drug Delivery

221

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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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“…Excipients play an important role in the generation of particles suitable for inhalation in the LDPI system [45]. In comparison to saccharides, which are widely used as excipients for freeze-dried preparations, amino acids (especially hydrophobic amino acids) showed high aerosolization performance as excipients for LDPI formulations [39,45,55]. Therefore, we performed the screening study focusing not on saccharides but on hydrophobic amino acids.…”

Section: Selection Of Excipientsmentioning

confidence: 99%

Systemic Delivery of hGhrelin Derivative by Lyophilizate for Dry Powder Inhalation System in Monkeys

et al. 2021

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Ghrelin is the peptide that increases the hunger sensation and food intake and is expected to be clinically applied for treatment of diseases such as cachexia and anorexia nervosa. In the clinical application of ghrelin, injections are problematic in that they are invasive and inconvenient. Thus, we aimed to develop a formulation that can eliminate the need for injections and can be applied clinically. We prepared formulations of an hGhrelin derivative, in which the octanoyl group essential for expression of activity is modified to avoid rapid des-acylation, using lyophilizate for a dry powder inhalation (LDPI) system. The formulation of hGhrelin derivative was optimized by the addition of phenylalanine, of which the fine particle fraction of 5 µm or less was 41.7 ± 3.8%. We also performed pharmacokinetic/pharmacodynamic tests in monkeys using the optimum formulation that can be applied clinically. The absolute bioavailability of inhaled hGhrelin derivative with respect to that intravenously injected was 16.9 ± 2.6%. An increase in growth hormone was shown as an effect of the inhaled hGhrelin derivative similar to intravenous injection. The LDPI formulation can deliver the hGhrelin derivative systemically, and it is expected to be applied clinically as a substitute for injections.

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Novel dry powder inhalation system based on dispersion of lyophilisates

Cited by 17 publications

References 54 publications

Simple Method to Measure the Aerodynamic Size Distribution of Porous Particles Generated on Lyophilizate for Dry Powder Inhalation

Simple Method to Measure the Aerodynamic Size Distribution of Porous Particles Generated on Lyophilizate for Dry Powder Inhalation

Dry powder inhalation: past, present and future

Systemic Delivery of hGhrelin Derivative by Lyophilizate for Dry Powder Inhalation System in Monkeys

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