Effect of Lactose Pseudopolymorphic Transition on the Aerosolization Performance of Drug/Carrier Mixtures
Abstract
:1. Introduction
2. Materials and Methods
2.1. Materials
2.2. Methods
2.2.1. Production of Micronized Lactose
2.2.2. Preparation of Hygroscopic Anhydrous α-Lactose (LαH)
2.2.3. Preparation of Stable Anhydrous α-lactose (LαS)
2.2.4. Differential Scanning Calorimetry (DSC)
2.2.5. Particle size Determination
2.2.6. Scanning Electron Microscopy (SEM)
2.2.7. Preparation of Drug/Carrier Mixtures
2.2.8. Salbutamol Sulphate Quantification
2.2.9. Budesonide Quantification
2.2.10. Homogeneity Test
2.2.11. In Vitro Deposition Tests
2.2.12. Statistical Analysis
3. Results and Discussion
3.1. Characterization of Lactose Samples
3.2. Effect of Lactose Solid-State on Drug Respirability
3.2.1. Ternary Mixtures
3.2.2. Binary Mixtures
4. Conclusions
Author Contributions
Funding
Conflicts of Interest
References
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Sample | dV10 (µm) | dV50 (µm) | dV90 (µm) |
---|---|---|---|
Lα·H2O | 10.2 ± 0.8 | 53.1 ± 2.0 | 103.3 ± 2.6 |
LαH | 18.8 ± 1.1 | 54.7 ± 0.7 | 104.9 ± 0.6 |
LαS | 20.7 ± 2.2 | 56.3 ± 0.4 | 105.7 ± 1.4 |
Mixture | Lα·H2O (%) | Micronized Lactose (%) | SS (%) |
---|---|---|---|
M-SS | 99 | - | 1 |
M-10 | 89 | 10 | 1 |
M-30 | 69 | 30 | 1 |
M-50 | 49 | 50 | 1 |
Mixture | ED (µg) | FPD (µg) | FPF (%) |
---|---|---|---|
M-SS | 177.1 ± 3.4 | 26.8 ± 1.9 | 15.1 ± 0.8 |
M-10 | 178.7 ± 4.6 | 84.3 ± 2.6 | 47.2 ± 0.7 |
M-30 | 180.9 ± 9.7 | 103.4 ± 7.3 | 57.2 ± 2.5 |
M-50 | 102.8 ± 5.5 | 34.9 ± 4.6 | 33.9 ± 2.8 |
Mixture | ED (µg) | FPD (µg) | FPF (%) |
---|---|---|---|
H-SS | 182.7 ± 11.6 | 76.2 ± 3.6 | 41.7 ± 1.9 |
S-SS | 173.0 ± 2.7 | 54.4 ± 2.2 | 31.5 ± 0.9 |
Mixture | ED (µg) | FPD (µg) | FPF (%) |
---|---|---|---|
M-BUD | 154.1 ± 4.3 | 27.9 ± 0.1 | 18.1 ± 0.5 |
S-BUD | 149.6 ± 4.0 | 17.9 ± 1.3 | 12.0 ± 0.5 |
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Della Bella, A.; Müller, M.; Danani, A.; Soldati, L.; Bettini, R. Effect of Lactose Pseudopolymorphic Transition on the Aerosolization Performance of Drug/Carrier Mixtures. Pharmaceutics 2019, 11, 576. https://doi.org/10.3390/pharmaceutics11110576
Della Bella A, Müller M, Danani A, Soldati L, Bettini R. Effect of Lactose Pseudopolymorphic Transition on the Aerosolization Performance of Drug/Carrier Mixtures. Pharmaceutics. 2019; 11(11):576. https://doi.org/10.3390/pharmaceutics11110576
Chicago/Turabian StyleDella Bella, Andrea, Michele Müller, Andrea Danani, Luciano Soldati, and Ruggero Bettini. 2019. "Effect of Lactose Pseudopolymorphic Transition on the Aerosolization Performance of Drug/Carrier Mixtures" Pharmaceutics 11, no. 11: 576. https://doi.org/10.3390/pharmaceutics11110576