Deposition and pharmacokinetics of budesonide from the Miat Monodose inhaler, a simple dry powder device

Ball, Denise J.; Hirst, Peter H.; Newman, Stephen P.; Sonet, Bernard; Streel, Bruno; Vanderbist, Francis

doi:10.1016/s0378-5173(02)00338-1

Cited by 27 publications

(8 citation statements)

References 23 publications

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“…Pulmonary scintigraphy is a noninvasive method for visualizing deposition pattern and quantifying the amount of drug deposited and concept of proof of bioavailability (13,(80)(81)(82). The study was carried out at Radiation Medicine Centre (BARC), Tata Hospital, Mumbai, based on protocol approved by the Ethical Committee of the Department of Clinical Pharmacology, TNMC and BYL Nair Charitable Hospital, Mumbai, 400 008, India (IEC/20/04).…”

Section: In Vivo Pulmonary Deposition Pattern Of Developed Conventionmentioning

confidence: 99%

Development of Budesonide Microparticles Using Spray-Drying Technology for Pulmonary Administration: Design, Characterization, In Vitro Evaluation, and In Vivo Efficacy Study

et al. 2009

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Abstract. The purpose of this research was to generate, characterize, and investigate the in vivo efficacy of budesonide (BUD) microparticles prepared by spray-drying technology with a potential application as carriers for pulmonary administration with sustained-release profile and improved respirable fraction. Microspheres and porous particles of chitosan (drug/chitosan, 1:2) were prepared by spray drying using optimized process parameters and were characterized for different physicochemical parameters. Mass median aerodynamic diameter and geometric standard deviation for conventional, microspheres, and porous particles formulations were 2.75, 4.60, and 4.30 µm and 2.56, 1.75, and 2.54, respectively. Pharmacokinetic study was performed in rats by intratracheal administration of either placebo or developed dry powder inhalation (DPI) formulation. Pharmacokinetic parameters were calculated (Ka, Ke, T max , C max , AUC, and Vd) and these results indicated that developed formulations extended half life compared to conventional formulation with onefold to fourfold improved local and systemic bioavailability. Estimates of relative bioavailability suggested that developed formulations have excellent lung deposition characteristics with extended T 1/2 from 9.4 to 14 h compared to conventional formulation. Anti-inflammatory activity of BUD and developed formulations was compared and found to be similar. Cytotoxicity was determined in A549 alveolar epithelial cell line and found to be not toxic. In vivo pulmonary deposition of developed conventional formulation was studied using gamma scintigraphy and results indicated potential in vitro-in vivo correlation in performance of conventional BUD DPI formulation. From the DPI formulation prepared with porous particles, the concentration of BUD increased fourfold in the lungs, indicating pulmonary targeting potential of developed formulations.

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Section: In Vivo Pulmonary Deposition Pattern Of Developed Conventionmentioning

confidence: 99%

Development of Budesonide Microparticles Using Spray-Drying Technology for Pulmonary Administration: Design, Characterization, In Vitro Evaluation, and In Vivo Efficacy Study

et al. 2009

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“…13,14 An additional increase in absorption of peptides from the lungs can result from methods of administration that target the large and highly vascularized alveolar region. 7,15,16 The aim of this study was to optimize the pulmonary delivery of PTH by defining factors favoring its transport from the airspaces into the bloodstream. We simultaneously conducted pharmacokinetic and regional lung deposition studies in vivo in the rat following intratracheal administration of PTH in dry powder or solution form.…”

Section: Introductionmentioning

confidence: 99%

Impact of formulation and methods of pulmonary delivery on absorption of parathyroid hormone (1–34) from rat lungs

Codrons

Vanderbist²,

Ucakar

et al. 2004

Journal of Pharmaceutical Sciences

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“…The FPF is a maximum at 1 min at 70.07 ± 4.71%. Comparing this to the commercial budesonide turbuhaler DPI, the FPF is reported to be 44% (Ball et al 2002;Bisgaard et al 1998;Thorsson et al 1994;Borgstrom et al 1994). While FPF is almost similar at 10 and 30 min drug loading, at 55.91 ± 6.81% and 55.97 ± 5.97%, respectively.…”

Section: Drug Dispersionmentioning

confidence: 86%

Micronized Drug Adhesion and Detachment from Surfaces: Effect of Loading Conditions

Selvam

Marek

Truman

et al. 2011

Aerosol Science and Technology

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Drug loading and processing conditions in a dry powder inhaler system are critical for performance of the system since it is these forces that must be overcome to properly redisperse respirable particles. In this work, we have investigated the effects of different loading forces for adhering micronized drug onto surfaces on the drug adhesion, detachment, and aerosol performance under controlled conditions. Drug loading onto a standardized surface was performed under three different loading conditions using turbulamixer to actively induce powder-surface interactions. It was seen the drug loading increased with increased processing time. The presence of external press-on force also increased drug loading. Drug detachment studies performed using centrifugation method indicated that adhesion forces were the lowest at lower mixing time and increased with increasing press-on forces. Drug aerosolization performance from the surface was assessed using a prototype DPI and confirmed that external forces during drug loading and coating processing played an important role in drug dispersion. It was seen that the respirability of drug particles correlated with mixing times as well as the press-on forces.

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Deposition and pharmacokinetics of budesonide from the Miat Monodose inhaler, a simple dry powder device

Cited by 27 publications

References 23 publications

Development of Budesonide Microparticles Using Spray-Drying Technology for Pulmonary Administration: Design, Characterization, In Vitro Evaluation, and In Vivo Efficacy Study

Development of Budesonide Microparticles Using Spray-Drying Technology for Pulmonary Administration: Design, Characterization, In Vitro Evaluation, and In Vivo Efficacy Study

Impact of formulation and methods of pulmonary delivery on absorption of parathyroid hormone (1–34) from rat lungs

Micronized Drug Adhesion and Detachment from Surfaces: Effect of Loading Conditions

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