Influence of fine lactose and magnesium stearate on low dose dry powder inhaler formulations

Guchardi, R; Frei, M; John, Edgar; Kaerger, Joerg

doi:10.1016/j.ijpharm.2007.06.041

Cited by 85 publications

(40 citation statements)

References 17 publications

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“…With added lactose fines, the proportion of lactose delivered to the Stage 2 was even higher at approximately 80%. These data are in an agreement with previous studies, where it was reported that fine particle lactose is indeed delivered to the impactor stages (Guchardi et al, 2008;Karhu et al, 2000;Srichana et al, 1998b).…”

Section: Morphological and Chemical Characteristics Of Materials Depossupporting

confidence: 93%

“…However, some studies have also made an attempt of understanding the mechanisms by which the lactose fines govern the DPI performance by determining the deposition of lactose in the different parts of the impactor alongside the drug determination (Guchardi et al, 2008;Karhu et al, 2000;Srichana et al, 1998b). These studies proved that in addition to the drug, also fine lactose is deposited on the impactor stages.…”

Section: Introductionmentioning

confidence: 99%

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Extrinsic lactose fines improve dry powder inhaler formulation performance of a cohesive batch of budesonide via agglomerate formation and consequential co-deposition

Kinnunen

Hebbink²,

Peters³

et al. 2015

International Journal of Pharmaceutics

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Price, R. (2015) 'Extrinsic lactose nes improve dry powder inhaler formulation performance of a cohesive batch of budesonide via agglomerate formation and consequential co-deposition.', International journal of pharmaceutics., 478 (1). pp. 53-59. Further information on publisher's website:http://dx.doi.org/10.1016/j.ijpharm.2014.11.019Publisher's copyright statement: NOTICE: this is the author's version of a work that was accepted for publication in International Journal of Pharmaceutics. Changes resulting from the publishing process, such as peer review, editing, corrections, structural formatting, and other quality control mechanisms may not be re ected in this document. Changes may have been made to this work since it was submitted for publication. A de nitive version was subsequently published in International Journal of Pharmaceutics, 478, 1, 15 January 2015, 10.1016/j.ijpharm.2014 Additional information: Use policyThe full-text may be used and/or reproduced, and given to third parties in any format or medium, without prior permission or charge, for personal research or study, educational, or not-for-pro t purposes provided that:• a full bibliographic reference is made to the original source • a link is made to the metadata record in DRO • the full-text is not changed in any way The full-text must not be sold in any format or medium without the formal permission of the copyright holders.Please consult the full DRO policy for further details. AbstractThe aim of the study was to investigate how the fine particle content of lactose carriers prepared with different types of lactose fines regulates dry powder inhaler (DPI) formulation performance of a cohesive batch of micronised budesonide.Budesonide formulations (0.8 wt-% ) were prepared with three different lactose carriers (Lactohale (LH) LH100, 20 wt-% LH210 in LH100 and 20 wt-% LH300 in LH100 indicated that the more fine lactose particles were available the more agglomerates of budesonide and lactose were delivered to the Stage 2. These results suggest drug-fines agglomerate formation is an important mechanism for how lactose fines improve and regulate DPI formulation performance.

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Section: Morphological and Chemical Characteristics Of Materials Depossupporting

confidence: 93%

Section: Introductionmentioning

confidence: 99%

Extrinsic lactose fines improve dry powder inhaler formulation performance of a cohesive batch of budesonide via agglomerate formation and consequential co-deposition

Kinnunen

Hebbink²,

Peters³

et al. 2015

International Journal of Pharmaceutics

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“…One may assume that above 5% of fine lactose, the mechanism of influence on performance undergoes a change. Competing effects, such as the saturation of activated areas on the carrier surface or the formation of drug-fines agglomerates for easier lift-off, could offer an explanation for this behaviour (see Section 4.1.2.1) [195].…”

Section: Lactose In Ternary Mixturesmentioning

confidence: 99%

Lactose characteristics and the generation of the aerosol

Pilcer¹,

Wauthoz²,

Amighi³

2012

Advanced Drug Delivery Reviews

178

113

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“…18) We found that when magnesium stearate at 0.5% (w/w) was added to the selected formulation which contained lactose as cryoprotectant according to Table 2, the angle of repose decreased from 41.4Ϯ0.95 to 38.9Ϯ0.89°, and the FPF value of SBS increased from 6.34Ϯ0.98 to 16.26Ϯ 0.51%, indicating that magnesium stearate was a valuable addition. This benefit of adding magnesium stearate to the formulation was sometimes questioned due to the potential risk associated with delivery of this agent deep into the lungs.…”

Section: Development Of Liposomal Dry Powder Inhaler Formulationsmentioning

confidence: 82%

Development of Liposomal Salbutamol Sulfate Dry Powder Inhaler Formulation

Huang

Yang

et al. 2010

Biological & Pharmaceutical Bulletin

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The purpose of our study was to develop a formulation of liposomal salbutamol sulfate (SBS) dry powder inhaler (DPI) for the treatment of asthma. Liposomes of high encapsulation efficiency (more than 80%) were prepared by a vesicular phospholipid gel (VPG) technique. SBS VPG liposomes were subjected to lyophilization using different kinds of cryoprotectants in various mass ratios. Coarse lactose (63-106 m mm) in different mass ratios was used as a carrier. Magnesium stearate (0.5%) was added as a lubricator. The dry liposomal powders were then crushed by ball milling and sieved through a 400-mesh sieve to control the mean particle size at about 10 m mm. The effects of different kinds of cryoprotectants and the amount of lactose carrier on the fine particle fraction (FPF) of SBS were investigated. The results showed that the developed formulation of liposomal dry powder inhaler was obtained using lactose as a cryoprotectant with a mass ratio of lyophilized powder to carrier lactose at 1 : 5; 0.5% magnesium stearate was used as a lubricator. The value of FPF for SBS was 41.51؎ ؎2.22% for this formulation. Sustained release of SBS from the VPG liposomes was found in the in vitro release study. The study results offer the promising possibility of localized pulmonary liposomal SBS delivery in the anhydrous state.

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Influence of fine lactose and magnesium stearate on low dose dry powder inhaler formulations

Cited by 85 publications

References 17 publications

Extrinsic lactose fines improve dry powder inhaler formulation performance of a cohesive batch of budesonide via agglomerate formation and consequential co-deposition

Extrinsic lactose fines improve dry powder inhaler formulation performance of a cohesive batch of budesonide via agglomerate formation and consequential co-deposition

Lactose characteristics and the generation of the aerosol

Development of Liposomal Salbutamol Sulfate Dry Powder Inhaler Formulation

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