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Does the performance of wet granulation and tablet hardness affect the drug dissolution profile of carvedilol in matrix tablets?
Drug Dev Ind Pharm. 2018 Sep; 44(9):1543-1550.DD

Abstract

Wet granulation is mostly used process for manufacturing matrix tablets. Compared to the direct compression method, it allows for a better flow and compressibility properties of compression mixtures. Granulation, including process parameters and tableting, can influence critical quality attributes (CQAs) of hydrophilic matrix tablets. One of the most important CQAs is the drug release profile. We studied the influence of granulation process parameters (type of nozzle and water quantity used as granulation liquid) and tablet hardness on the drug release profile. Matrix tablets contained HPMC K4M hydrophilic matrix former and carvedilol as a model drug. The influence of selected HPMC characteristics on the drug release profile was also evaluated using two additional HPMC batches. For statistical evaluation, partial least square (PLS) models were generated for each time point of the drug release profile using the same number of latent factors. In this way, it was possible to evaluate how the importance of factors influencing drug dissolution changes in dependence on time throughout the drug release profile. The results of statistical evaluation show that the granulation process parameters (granulation liquid quantity and type of nozzle) and tablet hardness significantly influence the release profile. On the other hand, the influence of HPMC characteristics is negligible in comparison to the other factors studied. Using a higher granulation liquid quantity and the standard nozzle type results in larger granules with a higher density and lower porosity, which leads to a slower drug release profile. Lower tablet hardness also slows down the release profile.

Authors+Show Affiliations

a KRKA, d. d. , Novo Mesto , Slovenia. b Faculty of Pharmacy , University of Ljubljana , Ljubljana , Slovenia.a KRKA, d. d. , Novo Mesto , Slovenia.a KRKA, d. d. , Novo Mesto , Slovenia. b Faculty of Pharmacy , University of Ljubljana , Ljubljana , Slovenia.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

29848075

Citation

Košir, Darjan, et al. "Does the Performance of Wet Granulation and Tablet Hardness Affect the Drug Dissolution Profile of Carvedilol in Matrix Tablets?" Drug Development and Industrial Pharmacy, vol. 44, no. 9, 2018, pp. 1543-1550.
Košir D, Ojsteršek T, Vrečer F. Does the performance of wet granulation and tablet hardness affect the drug dissolution profile of carvedilol in matrix tablets? Drug Dev Ind Pharm. 2018;44(9):1543-1550.
Košir, D., Ojsteršek, T., & Vrečer, F. (2018). Does the performance of wet granulation and tablet hardness affect the drug dissolution profile of carvedilol in matrix tablets? Drug Development and Industrial Pharmacy, 44(9), 1543-1550. https://doi.org/10.1080/03639045.2018.1483394
Košir D, Ojsteršek T, Vrečer F. Does the Performance of Wet Granulation and Tablet Hardness Affect the Drug Dissolution Profile of Carvedilol in Matrix Tablets. Drug Dev Ind Pharm. 2018;44(9):1543-1550. PubMed PMID: 29848075.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Does the performance of wet granulation and tablet hardness affect the drug dissolution profile of carvedilol in matrix tablets? AU - Košir,Darjan, AU - Ojsteršek,Tadej, AU - Vrečer,Franc, Y1 - 2018/06/14/ PY - 2018/6/1/pubmed PY - 2018/10/17/medline PY - 2018/6/1/entrez KW - HPMC KW - drug dissolution profile KW - high shear mixer KW - matrix tablets KW - partial least squares analysis KW - wet granulation SP - 1543 EP - 1550 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 44 IS - 9 N2 - Wet granulation is mostly used process for manufacturing matrix tablets. Compared to the direct compression method, it allows for a better flow and compressibility properties of compression mixtures. Granulation, including process parameters and tableting, can influence critical quality attributes (CQAs) of hydrophilic matrix tablets. One of the most important CQAs is the drug release profile. We studied the influence of granulation process parameters (type of nozzle and water quantity used as granulation liquid) and tablet hardness on the drug release profile. Matrix tablets contained HPMC K4M hydrophilic matrix former and carvedilol as a model drug. The influence of selected HPMC characteristics on the drug release profile was also evaluated using two additional HPMC batches. For statistical evaluation, partial least square (PLS) models were generated for each time point of the drug release profile using the same number of latent factors. In this way, it was possible to evaluate how the importance of factors influencing drug dissolution changes in dependence on time throughout the drug release profile. The results of statistical evaluation show that the granulation process parameters (granulation liquid quantity and type of nozzle) and tablet hardness significantly influence the release profile. On the other hand, the influence of HPMC characteristics is negligible in comparison to the other factors studied. Using a higher granulation liquid quantity and the standard nozzle type results in larger granules with a higher density and lower porosity, which leads to a slower drug release profile. Lower tablet hardness also slows down the release profile. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/29848075/Does_the_performance_of_wet_granulation_and_tablet_hardness_affect_the_drug_dissolution_profile_of_carvedilol_in_matrix_tablets L2 - https://www.tandfonline.com/doi/full/10.1080/03639045.2018.1483394 DB - PRIME DP - Unbound Medicine ER -