Raman Map**-Based Reverse Engineering Facilitates Development of Sustained-Release Nifedipine Tablet
Abstract
:1. Introduction
2. Materials and Methods
2.1. Materials
2.2. Raman Map** of Adalat®-L
2.3. Preparation of Nifedipine Sustained-Release Tablets
2.4. Validation of the Prepared Tablets by Raman Map**
2.5. In Vitro Dissolution Studies
2.6. Bioequivalence Studies
3. Results and Discussion
3.1. Analysis of Adalat®-L by Laser Raman Spectroscopy
3.2. Comminution and Particle Size Control of Nifedipine
3.3. Validation by Raman Map** of Prepared Tablets
3.4. In Vitro Dissolution Studies
3.5. Bioequivalence Studies
4. Conclusions
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Conflicts of Interest
References
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Ingredients | Amount (mg) |
---|---|
Nifedipine | 20.0 |
Polysorbate 80 | 0.4 |
Microcrystalline cellulose | 26.0 |
Lactose | 8.0 |
Corn starch (for blending) | 12.4 |
Corn starch (for starch slurry) | 12.4 |
Magnesium stearate | 0.8 |
SUM | 80.0 |
D90 (μm) | D50 (μm) | D10 (μm) | |
---|---|---|---|
Nifedipine | 150 | 118 | 30.7 |
Components | Nifedipine | Microcrystalline Cellulose | Lactose | Corn Starch |
---|---|---|---|---|
Proportion (%) | 33.94 | 33.02 | 1.40 | 31.65 |
Batch | Particle Size | ||
---|---|---|---|
D (90) (μm) | D (50) (μm) | D (10) (μm) | |
A | 145.2 ± 0.6 | 69.3 ± 0.6 | 12.1 ± 0.5 |
B | 96.1 ± 0.7 | 38.2 ± 0.6 | 8.4 ± 0.6 |
C | 62.0 ± 0.6 | 26.3 ± 0.2 | 5.5 ± 0.3 |
D | 38.9 ± 0.5 | 18.8 ± 0.4 | 6.1 ± 0.4 |
Particle Size | |||
---|---|---|---|
D (90) (μm) | D (50) (μm) | D (10) (μm) | |
Adalat®-L | 150 | 118 | 30.7 |
Batch B | 173 | 118 | 52.2 |
Batch C | 147 | 121 | 47.5 |
Batch D | 108 | 103 | 32.7 |
Condition | Pharmacokinetic Parameters | Mean and Ratio | 90% Confidence Interval | ||
---|---|---|---|---|---|
Batch C (T) | Adalat®-L (R) | (T/R)% | |||
Fasting (N = 28) | Cmax (ng/mL) | 56.4 ± 15.4 | 54.9 ± 16.3 | 102.75 | 92.15~114.56 |
AUC0–t (ng/mL·h) | 443.4 ± 150.0 | 478.1 ± 156.2 | 92.73 | 86.67~99.21 | |
AUC0–∞ (ng/mL·h) | 501.6 ± 147.8 | 536.6 ± 162.8 | 93.48 | 87.55~99.80 | |
Fed (N = 28) | Cmax (ng/mL) | 107.5 ± 46.5 | 119.8 ± 44.1 | 89.67 | 81.95~98.11 |
AUC0–t (ng/mL·h) | 539.6 ± 303.4 | 569.3 ± 283.0 | 94.78 | 88.39~101.63 | |
AUC0–∞ (ng/mL·h) | 569.1 ± 314.9 | 597.3 ± 297.3 | 95.28 | 88.97~102.04 |
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Sun, N.; Chang, L.; Lu, Y.; Wu, W. Raman Map**-Based Reverse Engineering Facilitates Development of Sustained-Release Nifedipine Tablet. Pharmaceutics 2022, 14, 1052. https://doi.org/10.3390/pharmaceutics14051052
Sun N, Chang L, Lu Y, Wu W. Raman Map**-Based Reverse Engineering Facilitates Development of Sustained-Release Nifedipine Tablet. Pharmaceutics. 2022; 14(5):1052. https://doi.org/10.3390/pharmaceutics14051052
Chicago/Turabian StyleSun, Ningyun, Liang Chang, Yi Lu, and Wei Wu. 2022. "Raman Map**-Based Reverse Engineering Facilitates Development of Sustained-Release Nifedipine Tablet" Pharmaceutics 14, no. 5: 1052. https://doi.org/10.3390/pharmaceutics14051052