Quantitative determination of micronization-induced changes in the solid state of lactose

Bella, Andrea Della; Müller, Michele; Soldati, L De; Elviri, Lisa; Bettini, Ruggero

doi:10.1016/j.ijpharm.2016.04.015

Cited by 13 publications

(11 citation statements)

References 29 publications

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“…The solid-state of lactose carriers (Lα·H 2 O, Lα H , and Lα S ) and fine micronized lactose was previously investigated by XRPD and DSC [29]. Micronized lactose was characterized by a lower degree of crystallinity compared to the coarse Lα·H 2 O used as starting material for the micronization process.…”

Section: Resultsmentioning

confidence: 99%

“…The thermal dehydration process used to prepare the anhydrous forms of lactose led to the formation of limited amounts of β-lactose. In all the other cases, the percentage of β-form was negligible and revealed that micronization in the reported conditions did not induce mutarotation [29].…”

Section: Resultsmentioning

confidence: 99%

“…Lα H was prepared following a procedure reported elsewhere [29] by heating Lacto-Sphere ® MM50 at 120 °C for 9 h under a dry nitrogen flow. After production, Lα H was always handled in a glove-box filled with dry nitrogen (RH < 5%) in order to prevent possible rehydration.…”

Section: Methodsmentioning

confidence: 99%

“…Lα S was prepared as described in a previous work [29] by heating Lacto-Sphere ® MM50 at 145 °C for 6 h under a dry nitrogen flow.…”

Section: Methodsmentioning

confidence: 99%

“…In a previous work, we have put into evidence the effect of the micronization process on the solid-state properties of the lactose fines underlying the pseudo-polymorphic transition of the micronized lactose with partial formation of hygroscopic anhydrous α-lactose rather than amorphous lactose [29].…”

Section: Introductionmentioning

confidence: 99%

See 4 more Smart Citations

Effect of Lactose Pseudopolymorphic Transition on the Aerosolization Performance of Drug/Carrier Mixtures

Bella

Müller²,

Danani

et al. 2019

Pharmaceutics

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Physico-chemical properties of lactose are key factors in adhesive mixtures used as dry powder inhaler (DPI). Despite the abundant literature on this topic, the effect of the polymorphism and pseudo-polymorphism of lactose has been seldom investigated and discussed although often lactose used in DPI is subjected to unit operations, which may alter its solid-state properties. Here, we studied the aerosolization performance of salbutamol sulphate (SS) or budesonide (BUD) formulations by investigating the effect of lactose pseudopolymorphism in ternary (coarse lactose/fine lactose/drug) and binary (coarse lactose/drug) mixtures. An improvement of the aerosolization performance of SS formulations with the increase of the amount of fine micronized lactose up to 30% (fine particle fraction (FPF) = 57%) was observed. Micronized lactose contained hygroscopic anhydrous α-lactose, which converted to α-lactose monohydrate at ambient conditions. This implied that the positive effect of fines on the aerosolization performance decreased and eventually disappeared with the formulation aging. Positive effect on SS deposition was observed also with binary mixtures with anhydrous lactose, whereas the opposite occurred with budesonide-containing formulations. The collected data demonstrated the crucial role of the carrier crystal form on the positive effect of fines on the deposition.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

“…Lα S was prepared as described in a previous work [29] by heating Lacto-Sphere ® MM50 at 145 °C for 6 h under a dry nitrogen flow.…”

Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%