Lactose modifications enhance its drug performance in the novel multiple dose Taifun® DPI

Harjunen, Päivi; Lehto, Vesa‐Pekka; Martimo, Krista; Suihko, Eero; Lankinen, Tapio; Paronen, Petteri; Järvinen, Kristiina

doi:10.1016/s0928-0987(02)00126-4

Cited by 39 publications

(13 citation statements)

References 23 publications

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“…Compared with conventional crystalline a-lactose monohydrate, spray-dried amorphous lactose showed no improvement in aerosol performance (49Y51), and in fact, its dispersion performance was poorer than those of the spray-dried crystalline lactose prepared with different polyethylene glycols (52). The major limitation with amorphous carrier is its strong tendency to undergo spontaneous recrystallization at ambient conditions (48) or higher RHs (51). Consequently current strategies in carrier engineering are targeted at reducing the amorphous content or increasing the crystallinity of the lactose carrier.…”

Section: Blending and Formulation With Lactosementioning

confidence: 99%

Particle Engineering for Pulmonary Drug Delivery

et al. 2007

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With the rapidly growing popularity and sophistication of inhalation therapy, there is an increasing demand for tailor-made inhalable drug particles capable of affording the most efficient delivery to the lungs and the most optimal therapeutic outcomes. To cope with this formulation demand, a wide variety of novel particle technologies have emerged over the past decade. The present review is intended to provide a critical account of the current goals and technologies of particle engineering for the development of pulmonary drug delivery systems. These technologies cover traditional micronization and powder blending, controlled solvent crystallization, spray drying, spray freeze drying, particle formation from liquid dispersion systems, supercritical fluid processing and particle coating. The merits and limitations of these technologies are discussed with reference to their applications to specific drug and/or excipient materials. The regulatory requirements applicable to particulate inhalation products are also reviewed briefly.

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Section: Blending and Formulation With Lactosementioning

confidence: 99%

Particle Engineering for Pulmonary Drug Delivery

et al. 2007

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“…Further details of these studies are given in Table I. Although salbutamol sulphate has been the most frequently investigated drug, a number of other drugs have also used: beclomethasone dipropionate (5,29), bovine serum albumin (3,4), budesonide (23,37), formoterol fumarate dihydrate (37), glucagon (33), liposomal amikacin (30), liposomal amphotericin B (31,32), salmeterol xinafoate (11,12,20,26,28,35,36) and a candidate NK1 receptor antagonist (FK888) (27).…”

Section: Adding Lactose Fines To a Formulationmentioning

confidence: 99%

The Influence of Fine Excipient Particles on the Performance of Carrier-Based Dry Powder Inhalation Formulations

2006

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The inclusion of a small amount of fine particle excipient in a carrier-based dry powder inhalation system is a well researched technique to improve formulation performance and is employed in the pharmaceutical industry. The removal of intrinsic fines from a lactose carrier has been found to decrease formulation performance, whereas adding fines of many different materials into formulations increased performance. Changing the particle size of these fines, the amount added and the technique by which they were prepared also affected formulation behaviour. Despite this body of research, there is disagreement as to the mechanism by which fines improved formulation performance, with two main hypotheses presented in the literature. The first hypothesis suggested that fines prevent the drug from adhering to the strongest binding sites on the carrier, whilst the second proposed that fine particles of drug and excipient form mixed agglomerates that are more easily dispersed and deaggregated during aerosolisation. The evidence in support of each hypothesis is limited and it is clear that future research should aim to produce stronger mechanistic evidence. The investigation of interparticulate interactions using techniques such as atomic force microscopy and inverse gas chromatography may prove useful in achieving this aim.

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“…Different studies are known in which the type and size of the adhesive forces between drug and carrier particles in adhesive mixtures for inhalation are described (e.g., [1][2][3][4][5]. Many parameters have been investigated that influence the size of these forces, for instance carrier payload (6)(7), mixing time (7)(8), relative humidity (9-10), tribocharge (11)(12), carrier type and grade (13)(14)(15)(16), and more, in particular the carrier surface morphology (17)(18). Modification of the carrier smoothness and purity has been explored to reduce the drug-to-carrier interaction force, thereby enhancing drug redispersion during inhalation (19)(20)(21)(22).…”

Section: Introductionmentioning

confidence: 99%