The use of different sugars as fine and coarse carriers for aerosolised salbutamol sulphate

Tee, S.K.; Marriott, Christopher; Zeng, Xian Ming; Martin, Gary P.

doi:10.1016/s0378-5173(00)00553-6

Cited by 111 publications

(44 citation statements)

References 28 publications

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“…This indicates that the co-spray-dried formulations are more cohesive, promoting the adhesion of these particles to the capsules and device. Interestingly, previous studies have demonstrated that SS generally has low aerosolisation efficiency with approximately FPF of 10%, but this was seen to be marginally improved in the presence of mannitol as a carrier (26,27). In this study, however, the cospray-dried MA-SS as one particle will change the surface chemistry (and consequently the surface energy) and subsequent particle interactions and cohesion forces of the formulations, resulting in an improved aerosol efficiency.…”

Section: In Vitro Aerosol Performance Studiesmentioning

confidence: 62%

Combined Inhaled Salbutamol and Mannitol Therapy for Mucus Hyper-secretion in Pulmonary Diseases

Ong

Traini

Ballerin

et al. 2014

AAPS J

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Abstract. This study focuses on the co-engineering of salbutamol sulphate (SS), a common bronchodilator, and mannitol (MA), a mucolytic, as a potential combination therapy for mucus hypersecretion. This combination was chosen to have a synergic effect on the airways: the SS will act on the β 2 -receptor for relaxation of smooth muscle and enhancement of ciliary beat frequency, whilst mannitol will improve the fluidity of mucus, consequently enhancing its clearance from the lung. A series of co-spray-dried samples, containing therapeutically relevant doses of SS and MA, were prepared. The physico-chemical characteristics of the formulations were evaluated in terms of size distribution, morphology, thermal and moisture response and aerosol performance. Additionally, the formulations were evaluated for their effects on cell viability and transport across air interface Calu-3 bronchial epithelial cells, contractibility effects on bronchial smooth muscle cells and cilia beat activity using ciliated nasal epithelial cells in vitro. The formulations demonstrated size distributions and aerosol performance suitable for inhalation therapy. Transport studies revealed that the MA component of the formulation enhanced penetration of SS across the complex mucus layer and the lung epithelia cells. Furthermore, the formulation in the ratios of SS 10 −6 and MA 10 −3 M gave a significant increase in cilia beat frequency whilst simultaneously preventing smooth muscle contraction associated with mannitol administration. These studies have established that co-spray dried combination formulations of MA and SS can be successfully prepared with limited toxicity, good aerosol performance and the ability to increase ciliary beat frequency for improving the mucociliary clearance in patients suffering from hyper-secretory diseases, whilst simultaneously acting on the underlying smooth muscle.

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Section: In Vitro Aerosol Performance Studiesmentioning

confidence: 62%

Combined Inhaled Salbutamol and Mannitol Therapy for Mucus Hyper-secretion in Pulmonary Diseases

Ong

Traini

Ballerin

et al. 2014

AAPS J

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show abstract

“…Other sugars and polyols have been tested as potential carriers and fine excipients in DPIs, such as mannitol, glucose, trehalose, dextrose, maltose, sorbitol, maltitol and xylitol [4,66,170,191,[216][217][218][219]. Anhydrous glucose is already used as a carrier in the marketed product, The mean adhesive forces were significantly different for each of the sugars with the following decreasing order: sorbitol > lactose > mannitol > glucose [170].…”

Section: Alternatives To Lactose In Dry Powder Formulations For Inhalmentioning

confidence: 99%

Lactose characteristics and the generation of the aerosol

Pilcer¹,

Wauthoz²,

Amighi³

2012

Advanced Drug Delivery Reviews

179

113

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“…17 LAC is selected as one of the crystalline excipients as it has been widely used in the pharmaceutical industry as carrier and diluent, especially in the formulation of powder mixtures for inhalation. 19 Fine lactose has been reported as improving the aerosolization properties of a cohesive drug and controlling drug dispersion from drug-lactose mixtures of inhalation. [20][21] AA is selected because it is a single polymorph 22 and a common pharmaceutical excipient, used as an acidulent in effervescent tablets or lubricant in tablets.…”

Section: Introductionmentioning

confidence: 99%

Influence of excipients in comilling on mitigating milling-induced amorphization or structural disorder of crystalline pharmaceutical actives

Balani

Tan

et al. 2010

Journal of Pharmaceutical Sciences

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The use of different sugars as fine and coarse carriers for aerosolised salbutamol sulphate

Cited by 111 publications

References 28 publications

Combined Inhaled Salbutamol and Mannitol Therapy for Mucus Hyper-secretion in Pulmonary Diseases

Combined Inhaled Salbutamol and Mannitol Therapy for Mucus Hyper-secretion in Pulmonary Diseases

Lactose characteristics and the generation of the aerosol

Influence of excipients in comilling on mitigating milling-induced amorphization or structural disorder of crystalline pharmaceutical actives

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