Effect of the Moisture Content in Aerosol on the Spray Performance of Stmerin&lt;sup&gt;&amp;reg;&lt;/sup&gt; D Hydrofluoroalkane Preparations (2)

Murata, Saburo; Izumi, Takashi; Ito, Hideki

doi:10.1248/cpb.60.593

Cited by 5 publications

(3 citation statements)

References 6 publications

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“…Presence of water can greatly affect the product stability as water may initiate and enhance the hydrolytic degradation of the active constituent and may cause changes in particle size distribution or aggregation leading to reduction in the suspension homogeneity (Williams & Hu, 2000a). Furthermore, the moisture strongly affects the particle size distribution after actuation because it reduces the propellant evaporation rate and increases the apparent particle size (Murata et al., 2012) and consequently may affect the FPF of the formulation (Williams & Hu, 2000b). Therefore, water should be strictly limited to prevent these changes.…”

Section: Resultsmentioning

confidence: 99%

In-vitro and in-vivo respiratory deposition of a developed metered dose inhaler formulation of an anti-migraine drug

Abdou

Kandil²,

morsi

et al. 2019

Drug Delivery

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Enhancement of zolmitriptan bioavailability through development of micronized zolmitriptan pressurized metered dose inhaler (MDI) as an alternative to its traditional drug delivery systems. A reversed phase HPLC method for zolmitriptan determination was developed and evaluated. Micronized zolmitriptan MDI formulations were prepared using two different propellants. The prepared formulations were evaluated for mean shot weight, drug content, and leakage rate in addition to in-vitro deposition using next generation impactor where mass median aerodynamic diameter (MMAD), geometric standard deviation (GSD), fine particle dose, fine particle fraction (FPF), emitted dose (ED), and dispersibility were determined. The selected formulation was evaluated for in-vivo bronchial absorption in rats. The physicochemical characters of the prepared formulations were found to be dependent mainly on the vapor pressure of the used propellant. MDI formulation prepared with HFA 134a propellant was found to have the lowest MMAD (3.47 ± 0.65) with GSD of 2.3 ± 0.4. It also had the highest FPF (41.9), ED (89.26 ± 2.35) with dispersibility of 46.9%. This formulation, when applied to rats, resulted in faster T max (27 ± 5 min) with higher C max (1236 ± 116 ng/mL) and AUC (0-12) (3375 ± 482 ng/mL·h) over the oral tablet. Its relative bioavailability was 72.7% which was 1.25 times higher than the oral tablet relative bioavailability. Zolmitriptan MDI formulation was developed using micronized zolmitriptan powder without further modification or particle engineering. The developed formulation using HFA 134a propellant could be favorable alternative, with enhanced bioavailability, to zolmitriptan oral tablet for acute migraine treatment.

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Section: Resultsmentioning

confidence: 99%

In-vitro and in-vivo respiratory deposition of a developed metered dose inhaler formulation of an anti-migraine drug

Abdou

Kandil²,

morsi

et al. 2019

Drug Delivery

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“…Another consideration for the stability of suspensions is the effect of low levels of water in the formulation. For instance, an accelerated stability study of isoproterenol sulfate and atropine methylbromide HFA MDIs at 40°C/75% relative humidity compared to 40°C/ambient humidity for 3 months reveals that at higher levels of humidity, the emitted doses were not uniform and the FPF was significantly reduced; however, moisture ingress can be limited with selected sealing gasket materials and controlled manufacturing conditions (143,144). However, the inclusion of water does not always have a detrimental effect on the suspension HFA formulation.…”

Section: Stabilizing and Suspending Agentsmentioning

confidence: 99%

Advances in Metered Dose Inhaler Technology: Formulation Development

2014

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Pressurized metered dose inhalers (MDIs) are a long-standing method to treat diseases of the lung, such as asthma and chronic obstructive pulmonary disease. MDIs rely on the driving force of the propellant, which comprises the bulk of the MDI formulation, to atomize droplets containing drug and excipients, which ideally should deposit in the lungs. During the phase out of chlorofluorocarbon propellants and the introduction of more environmentally friendly hydrofluoroalkane propellants, many improvements were made to the methods of formulating for MDI drug delivery along with a greater understanding of formulation variables on product performance. This review presents a survey of challenges associated with formulating MDIs as solution or suspension products with one or more drugs, while considering the physicochemical properties of various excipients and how the addition of these excipients may impact overall product performance of the MDI. Propellants, volatile and nonvolatile cosolvents, surfactants, polymers, suspension stabilizers, and bulking agents are among the variety of excipients discussed in this review article. Furthermore, other formulation approaches, such as engineered excipient and drug-excipient particles, to deliver multiple drugs from a single MDI are also evaluated.

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“…Under the same conditions, TPU‐4 was recovered with a molecular weight twice as high as TPU‐3, using the double amount of isocyanate derivative in the prepolymer preparation step. Therefore, to obtain a high M n of TPUs, the prepolymer formation should be prepared with PTHF and MDI at a temperature not below 90°C, using an excess of MDI considering the high sensitivity to water which may lead to its inactivation 61 …”

Section: Resultsmentioning

confidence: 99%

Thermoplastic polyurethanes for biomedical application: A synthetic, mechanical, antibacterial, and cytotoxic study

Nakib

Toncheva

Fontaine

et al. 2021

J of Applied Polymer Sci

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Thermoplastic polyurethanes (TPUs) bear tunable chemistry offering the possibility to develop a rich palette of physio‐mechanical properties, making the materials suitable for various fields of application. The great variety in TPUs properties comes from the choices of the monomers and the reaction conditions. Herein, the mechanical properties of the developed TPUs are tailored, while fine‐tuning the hard and soft segment molar ratio, as well as the reaction conditions. TPUs are synthesized from 4,4′‐methylenebis(phenyl isocyanate), poly(tetrahydrofuran), and 1,4‐butanediol, and their thermal and mechanical properties are fully characterized. The sample with the most appropriate mechanical properties that are suitable for catheter fabrication, is selected for the biomedical application. Quaternary ammonium salt is synthesized, and 0.5 mol% is incorporated in the TPU to confer antibacterial properties to the material while preserving its mechanical strength. The microbiological tests reveal the antibacterial effect of the developed materials against Staphylococcus aureus and Pseudomonas aeruginosa, as well as 80% SiHa cell viability, after 72 h of exposure, as part of the performed cytotoxicity studies. Finally, TPUs catheter prototypes fabrication is also proposed, applying an extrusion or injection molding approach for the production of biomedical devices with desirable mechanical properties.

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Effect of the Moisture Content in Aerosol on the Spray Performance of Stmerin<sup>®</sup> D Hydrofluoroalkane Preparations (2)

Cited by 5 publications

References 6 publications

In-vitro and in-vivo respiratory deposition of a developed metered dose inhaler formulation of an anti-migraine drug

In-vitro and in-vivo respiratory deposition of a developed metered dose inhaler formulation of an anti-migraine drug

Advances in Metered Dose Inhaler Technology: Formulation Development

Thermoplastic polyurethanes for biomedical application: A synthetic, mechanical, antibacterial, and cytotoxic study

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