Gliclazide: Biopharmaceutics Characteristics to Discuss the Biowaiver of Immediate and Extended Release Tablets
Abstract
:Featured Application
Abstract
1. Introduction
2. Methods
3. Results and Discussion
3.1. Physical-Chemical Features
3.2. Biopharmaceutics Features and Waiver from Relative Bioavailability/Bioequivalence Studies for Tablets of Immediate Release Containing Gliclazide
3.2.1. Solubility
3.2.2. Permeability
3.2.3. Dissolution
3.3. Extended-Release Solid Oral Dosage Forms Containing Gliclazide
3.4. Waiver of RB/BE Studies for Extended-Release Solid Oral Dosage Forms Containing Gliclazide
4. Conclusions
Author Contributions
Funding
Acknowledgments
Conflicts of Interest
References
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Media | Temperature (°C) | Solubility (mg/mL) | RPM | Reference | Calculated D/S ** (mL) | Calculated D/S *** (mL) |
---|---|---|---|---|---|---|
pH 4.5 | 25 | 0.0337 | ------ | NA | NA | |
pH 5.5 | 0.0433 | Shaker | [47] | |||
pH 6.0 | 0.0619 | |||||
pH 6.4 | 0.1133 | |||||
pH 6.8 | 0.2164 | |||||
pH 7.0 | 0.2646 | |||||
pH 6.8 | 0.2774 | |||||
Distilled water | 25 | 0.0373 | ------ | [42] | NA | NA |
pH 2.67 | 0.0715 | Magnetic shaker | ||||
pH 3.69 | 0.0326 | |||||
pH 4.47 | 0.0338 | |||||
pH 5.73 | 0.0689 | |||||
pH 7.4 | 0.1751 | |||||
pH 8.24 | 0.7856 | |||||
pH 9.74 | 1.4754 | |||||
pH 4.5 | room temperature | 0.0578 | 250 | [48] | NA | NA |
pH 5.4 | 0.0742 | |||||
pH 6.8 | 0.2954 | |||||
pH 7.4 | 0.6375 | |||||
pH 1.2 | room temperature | 1.6940 | Mechanical agitation | [41] | NA | NA |
pH 4.5 | 0.0335 | |||||
Distilled water pH 7.0 | 0.3485 | |||||
pH 7.4 | 1.8415 | |||||
pH 1.2 | 37 | 0.4 * | 50 | [49] | 400 | 200 |
pH 4.5 | 0.1 * | Magnetic shaker | 1600 | 800 | ||
pH 5.8 | 0.1 * | 1600 | 800 | |||
pH 6.8 | 0.6 * | 267 | 133.3 | |||
pH 7.2 | 1.2 * | 134 | 66.7 | |||
pH 7.4 | 1.5 * | 107 | 53.33 | |||
pH 1.2 | 37 | 0.81 | ---- | [50] | 197.5 | 98.7 |
pH 1.1 | 37 | 0.8 * | 250 | [51] | 200 | 100 |
pH 6.8 | 0.3 * | (shake flask) | 533.3 | 266.7 | ||
pH 7.4 | 1.1 * | 145.5 | 72.7 | |||
Distilled water | 37 | 0.0526 | ---- | [40] | 3041.8 | 1520.9 |
pH 1.2 | 0.1242 | Shaker | 1288.2 | 644.1 | ||
pH 4.5 | 0.0404 | 3960.4 | 1980.2 | |||
pH 6.8 | 0.1824 | 877.2 | 438.6 |
Method | Reference Value | Results | Reference |
---|---|---|---|
Partition coefficient octanol-water (Log P) | High: ≥1.72 * | 1.97 | [54] |
Partition coefficient octanol-water (Log P) | High: ≥1.72 * | 1.73 | [49] |
Cell Caco-2 (Papp) | >1 × 10−6 cm/s ** | 25 × 10−6 cm/s | [55] |
Absolute bioavailability | High: ≥85% *** | 113.4% | [56] |
High: ≥85% *** | 86–89% | [57] |
Drug | Medium/Volume (mL) | USP | Temperature (°C) | Dissolved Quantity (%)/min | Reference |
---|---|---|---|---|---|
Apparatus/ | |||||
Stirring Speed (rpm) | |||||
Diamicron 80 mg | II/100 | 37 | <50/30 | [51] | |
Glioral 80 mg | pH 1.2/900 | <85/30 | |||
Glikosan 80 mg | <60/20 | ||||
Diamicron 80 mg | <30/30 | ||||
Glioral 80 mg | pH 4.0/900 | <60/30 | |||
Glikosan 80 mg | <30/30 | ||||
Diamicron80 mg | ≥85/30 | ||||
Glioral 80 mg | pH 7.2/900 | ≥85/30 | |||
Glikosan 80 mg | ≥85/30 | ||||
Diabezidum 80 mg | pH 7.4/900 | II/100 | 37 | 81.62/60 | [43] |
Diabrezide 80 mg | 88.83/20 | ||||
Diabezid 80 mg | pH 1.2/--- | II/100 | 37 | 50.95/15 | [56] |
Diabrezide 80 mg | 11.9/15 | ||||
Diamicron 80 mg | pH 1.2/900 | II/100 | 37 | <70/60 | [63] |
Diberin 80 mg | <80/60 | ||||
Diamicron 80 mg | pH 4.0/900 | <40/60 | |||
Diberin 80 mg | <50/60 | ||||
Diamicron 80 mg | pH 7.2/900 | ≥85/30 | |||
Diberin 80 mg | ≥85/30 | ||||
Diamicron 80 mg | pH 7.4/900 | II/100 | 37 | 90.43/20 | [64] |
Diamicron 80 mg | pH 7.4/900 | II/100 | 37 | 84.3/20 | [65] |
95.6/30 | |||||
Diamicron 80 mg | pH 7.4/500 | II/50 | 37 | 33/480 | [66] |
Drug | Concentration (mg) | Industry | Date of Registration | Commercial Name® |
---|---|---|---|---|
Reference (07/08/2020) * | 30 | Servier | 12/11/2012 21/1/2013 | Diamicron MR |
60 | ||||
Generic (05/08/2019) * | 30 | Ranbaxy | 24/09/2012 | --- |
30 | Torrent | 26/10/2015 | --- | |
30; 60 | Pharlab | 31/10/2016 | --- | |
30; 60 | EMS S/A | 23/04/2018 | --- | |
30; 60 | Germed | 02/07/2018 | --- | |
30; 60 | Legrand Pharma | 02/07/2018 | --- | |
30; 60 | Nova Química | 02/07/2018 | --- | |
Similar | 30 | Torrent | 27/07/2015 | Azukon MR |
30; 60 | Pharlab | 31/03/2016 | Dicazid MR | |
30 | Ranbaxy | 15/12/2014 | Tezara MR | |
(06/02/2020) * | 30; 60 | Nova Química | 30/11/2018 | Beteglid |
30; 60 | Germed | 30/11/2018 | Clazi XR | |
30; 60 | Legrand Pharma | 30/11/2018 | Dagli |
Drug | Medium/Volume (mL) | Apparatus USP/Stirring Speed (rpm) | Temperature (°C) | Dissolved Quantity (%)/time h | Reference |
---|---|---|---|---|---|
Azukon® MR 30 mg | pH 4.5/1000 | I/50 | 37 | 54.2/24 | [47] |
pH 6.4/1000 | 63.9/24 | ||||
pH 6.8/1000 | 67.1/24 | ||||
pH 4.5/1000 | I/100 | 37 | 75.7/24 | ||
pH 6.4/1000 | 104.8/24 | ||||
pH 6.8/1000 | 99.6/24 | ||||
pH 4.5/1000 | II/50 | 37 | 63.69/24 | ||
pH 6.4/1000 | 71.60/24 | ||||
pH 6.8/1000 | 74.97/24 | ||||
pH 4.5/1000 | II/100 | 37 | 100.62/24 | ||
pH 6.4/1000 | 101.34/24 | ||||
pH 6.8/1000 | 98.56/24 | ||||
Azukon® MR 30 mg | pH 6.8/1000 | II/100 | 37 | 73.8/24 | |
Diamicron® MR 30 mg | 37 | 98.6/24 | |||
Azukon® MR 30 mg | pH 4.5 por 1 h; | III (Bio-Dis) | 37 | ||
pH 5.5 por 1 h; | 10 dpm, 420 mesh | ||||
pH 6.0 por 1 h; | 73.03/24 | ||||
pH 7.0 por 1 h; | |||||
pH 6.4 por 1 h; | |||||
pH 6.8 por 1 h; /250 ml | |||||
pH 6.8/250 ml | |||||
72.13/24 | |||||
Diamicron® MR 30 mg | pH 7.4/900 | I/100 | 37 | 77/10 | [49] |
Diamicron® MR 30 mg | pH 1.2/900 | II/100 | 37 | 80/4 | |
pH 6.8/900 | 80/8 | ||||
pH 7.4/900 | 80/8 | ||||
pH 1.2 for 1 h; pH 4.5 for 2 h; | III(Bio-Dis)/ | 37 | 95.45/10 | ||
pH 5.8 for 1 h; | 30 dpm, 400 μm mesh | ||||
Diamicron® MR 30 mg | pH 6.8 for 5 h | ||||
pH 7.2 for 1 h; | |||||
/250 mL | |||||
pH 1.2 for 1 h; pH 4.5 for 2 h; | |||||
Azukon® 30 mg | pH 5.8 for 1 h; | ||||
pH 6.8 for 5 h | |||||
pH 7.2 for 1 h; | |||||
/250 mL | |||||
Diaprel 30 mg | pH 7.4/900 | II/100 | 37 | 59.64/6 | [43] |
Diaprel 80 mg | 67.35/8 | ||||
Diamicron® 30 mg | 37 | 90/5.8 | [41] | ||
Nuzide 30 mg | pH 1.2/900 | I/100 | 90/5.3 | ||
Azukon 30 mg | 90/3.3 | ||||
pH 4.5/900 | |||||
Diamicron® 30 mg | 90/26.8 | ||||
Nuzide 30 mg | 90/12.4 | ||||
Azukon 30 mg | pH 7.4/900 | 90/15.6 | |||
Diamicron® 30 mg | distilled water/900 | 90/12.8 | |||
Nuzide 30mg Azukon 30 mg | 90/13.0 | ||||
90/11.0 | |||||
Diamicron® 30 mg | |||||
Nuzide 30mg Azukon 30 mg | 90/10.2 | ||||
90/10.7 | |||||
90/11.7 | |||||
Glizid® MR 60 | pH 1.2/--- | I/-- | 90/9.1 | [73] | |
pH 7.4/--- | 90/7.7 | ||||
distilled water/--- | 90/16.9 | ||||
Gliclazide MR 30 mg | pH 4.5/900 | II/75 | 37 | 73/24 | [48] |
pH 6.8/900 | 89/24 | ||||
pH 7.4/900 | 99/24 |
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Mapa, B.d.C.; Araújo, L.U.; Silva-Barcellos, N.M.; Caldeira, T.G.; Souza, J. Gliclazide: Biopharmaceutics Characteristics to Discuss the Biowaiver of Immediate and Extended Release Tablets. Appl. Sci. 2020, 10, 7131. https://doi.org/10.3390/app10207131
Mapa BdC, Araújo LU, Silva-Barcellos NM, Caldeira TG, Souza J. Gliclazide: Biopharmaceutics Characteristics to Discuss the Biowaiver of Immediate and Extended Release Tablets. Applied Sciences. 2020; 10(20):7131. https://doi.org/10.3390/app10207131
Chicago/Turabian StyleMapa, Bruna de Carvalho, Lorena Ulhôa Araújo, Neila Márcia Silva-Barcellos, Tamires Guedes Caldeira, and Jacqueline Souza. 2020. "Gliclazide: Biopharmaceutics Characteristics to Discuss the Biowaiver of Immediate and Extended Release Tablets" Applied Sciences 10, no. 20: 7131. https://doi.org/10.3390/app10207131
APA StyleMapa, B. d. C., Araújo, L. U., Silva-Barcellos, N. M., Caldeira, T. G., & Souza, J. (2020). Gliclazide: Biopharmaceutics Characteristics to Discuss the Biowaiver of Immediate and Extended Release Tablets. Applied Sciences, 10(20), 7131. https://doi.org/10.3390/app10207131