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Effect of binders on the release rates of direct molded verapamil tablets using twin-screw extruder in melt granulation.
Int J Pharm. 2014 Mar 10; 463(1):89-97.IJ

Abstract

Conventional manufacturing of pharmaceutical tablets often involves single processes such as blending, granulation, milling and direct compression. A process that minimizes and incorporates all these in a single continuous step is desirable. The concept of omitting milling step followed by direct-molding of tablets utilizing a twin-screw extruder in a melt granulation process using thermoplastic binders was explored. The objective of this study was to investigate the effect of combining hydrophilic binder (HPMC K4M, PEO 1M), and hydrophobic binder (Compritol® ATO 888, Precirol® ATO 5) on the release profiles of direct-molded tablets and direct-compressed tablets from milled extrudates using a quality-by-design approach. It was identified that hydrophilic binder type and process significantly affects (p=0.005) the release profiles of verapamil. Moreover, two-way interaction analysis demonstrated that the combination of process with type of hydrophilic polymer (p=0.028) and the type of hydrophilic polymer with polymer ratio (p=0.033) significantly affected the release profiles. The formulation release kinetics correlated to Higuchi release model and the mechanism correlated to a non-Fickian release mechanism. The results of the present study indicated that direct-molded tablets with different release profiles can be manufactured without milling process and through a continuous melt granulation using twin-screw extruder with appropriate thermoplastic binder ratio.

Authors+Show Affiliations

AbbVie Pte Ltd, 11 Biopolis Way, Helios, #05-06, Singapore 138667, Singapore. Electronic address: cheng.tan@abbvie.com.AbbVie Pte Ltd, 11 Biopolis Way, Helios, #05-06, Singapore 138667, Singapore.AbbVie Pte Ltd, 11 Biopolis Way, Helios, #05-06, Singapore 138667, Singapore.AbbVie Pte Ltd, 11 Biopolis Way, Helios, #05-06, Singapore 138667, Singapore.AbbVie Pte Ltd, 11 Biopolis Way, Helios, #05-06, Singapore 138667, Singapore.AbbVie Pte Ltd, 11 Biopolis Way, Helios, #05-06, Singapore 138667, Singapore. Electronic address: rajeev.gokhale@abbvie.com.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

24406670

Citation

Tan, David Cheng Thiam, et al. "Effect of Binders On the Release Rates of Direct Molded Verapamil Tablets Using Twin-screw Extruder in Melt Granulation." International Journal of Pharmaceutics, vol. 463, no. 1, 2014, pp. 89-97.
Tan DC, Chin WW, Tan EH, et al. Effect of binders on the release rates of direct molded verapamil tablets using twin-screw extruder in melt granulation. Int J Pharm. 2014;463(1):89-97.
Tan, D. C., Chin, W. W., Tan, E. H., Hong, S., Gu, W., & Gokhale, R. (2014). Effect of binders on the release rates of direct molded verapamil tablets using twin-screw extruder in melt granulation. International Journal of Pharmaceutics, 463(1), 89-97. https://doi.org/10.1016/j.ijpharm.2013.12.053
Tan DC, et al. Effect of Binders On the Release Rates of Direct Molded Verapamil Tablets Using Twin-screw Extruder in Melt Granulation. Int J Pharm. 2014 Mar 10;463(1):89-97. PubMed PMID: 24406670.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effect of binders on the release rates of direct molded verapamil tablets using twin-screw extruder in melt granulation. AU - Tan,David Cheng Thiam, AU - Chin,William Wei Lim, AU - Tan,En Hui, AU - Hong,Shiqi, AU - Gu,Wei, AU - Gokhale,Rajeev, Y1 - 2014/01/07/ PY - 2013/10/08/received PY - 2013/12/04/revised PY - 2013/12/27/accepted PY - 2014/1/11/entrez PY - 2014/1/11/pubmed PY - 2014/9/23/medline KW - Direct mold KW - Hot melt extruder KW - Hydrophilic KW - Hydrophobic KW - Melt granulation KW - Modified release SP - 89 EP - 97 JF - International journal of pharmaceutics JO - Int J Pharm VL - 463 IS - 1 N2 - Conventional manufacturing of pharmaceutical tablets often involves single processes such as blending, granulation, milling and direct compression. A process that minimizes and incorporates all these in a single continuous step is desirable. The concept of omitting milling step followed by direct-molding of tablets utilizing a twin-screw extruder in a melt granulation process using thermoplastic binders was explored. The objective of this study was to investigate the effect of combining hydrophilic binder (HPMC K4M, PEO 1M), and hydrophobic binder (Compritol® ATO 888, Precirol® ATO 5) on the release profiles of direct-molded tablets and direct-compressed tablets from milled extrudates using a quality-by-design approach. It was identified that hydrophilic binder type and process significantly affects (p=0.005) the release profiles of verapamil. Moreover, two-way interaction analysis demonstrated that the combination of process with type of hydrophilic polymer (p=0.028) and the type of hydrophilic polymer with polymer ratio (p=0.033) significantly affected the release profiles. The formulation release kinetics correlated to Higuchi release model and the mechanism correlated to a non-Fickian release mechanism. The results of the present study indicated that direct-molded tablets with different release profiles can be manufactured without milling process and through a continuous melt granulation using twin-screw extruder with appropriate thermoplastic binder ratio. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/24406670/Effect_of_binders_on_the_release_rates_of_direct_molded_verapamil_tablets_using_twin_screw_extruder_in_melt_granulation_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(13)01129-0 DB - PRIME DP - Unbound Medicine ER -