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Physicochemical properties of direct compression tablets with spray dried and ball milled solid dispersions of tadalafil in PVP-VA.
Eur J Pharm Biopharm. 2016 Dec; 109:14-23.EJ

Abstract

The aim of this research was to develop immediate release tablets comprising solid dispersion (IRSDTs) of tadalafil (Td) in a vinylpyrrolidone and vinyl acetate block copolymer (PVP-VA), characterized by improved dissolution profiles. The solid dispersion of Td in PVP-VA (Td/PVP-VA) in a weight ratio of 1:1 (w/w) was prepared using two different processes i.e. spray drying and ball milling. While the former process has been well established in the formulation of IRSDTs the latter has not been exploited in these systems yet. Regardless of the preparation method, both Td/PVP-VA solid dispersions were amorphous as confirmed by PXRD, DSC and FTIR. However, different morphology of particles (SEM) resulted in differences in water apparent solubility and disk intrinsic dissolution rate (DIDR). Both solid dispersions and crystalline Td were successfully made into directly compressible tablets at three doses of Td, i.e. 2.5mg, 10mgand20mg, yielding nine different formulations (D1-D9). Each of the lots met the requirements set by Ph.Eur. and was evaluated with respect to appearance, diameter, thickness, mass, hardness, friability, disintegration time and content of Td. IRSDTs performed as supersaturable formulations and had significantly improved water dissolution profiles in comparison with equivalent tablets containing crystalline Td and the marketed formulations. Tablets with both spray dried and ball milled Td/PVP-VA revealed the greatest improvement in dissolution depending on the investigated doses, i.e. 2.5mgand20mg, respectively. Also, dissolution of Td from Td/PVP-VA delivered in different forms occurred in the following order: powders>tablets>capsules.

Authors+Show Affiliations

Medical University of Gdansk, Department of Physical Chemistry, Hallera 107, 80-416 Gdansk, Poland. Electronic address: kamil.wlodarski@gumed.edu.pl.Trinity College Dublin, School of Pharmacy and Pharmaceutical Sciences, College Green, Dublin 2, Ireland.Medical University of Gdansk, Department of Physical Chemistry, Hallera 107, 80-416 Gdansk, Poland.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

27658987

Citation

Wlodarski, K, et al. "Physicochemical Properties of Direct Compression Tablets With Spray Dried and Ball Milled Solid Dispersions of Tadalafil in PVP-VA." European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, vol. 109, 2016, pp. 14-23.
Wlodarski K, Tajber L, Sawicki W. Physicochemical properties of direct compression tablets with spray dried and ball milled solid dispersions of tadalafil in PVP-VA. Eur J Pharm Biopharm. 2016;109:14-23.
Wlodarski, K., Tajber, L., & Sawicki, W. (2016). Physicochemical properties of direct compression tablets with spray dried and ball milled solid dispersions of tadalafil in PVP-VA. European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, 109, 14-23. https://doi.org/10.1016/j.ejpb.2016.09.011
Wlodarski K, Tajber L, Sawicki W. Physicochemical Properties of Direct Compression Tablets With Spray Dried and Ball Milled Solid Dispersions of Tadalafil in PVP-VA. Eur J Pharm Biopharm. 2016;109:14-23. PubMed PMID: 27658987.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Physicochemical properties of direct compression tablets with spray dried and ball milled solid dispersions of tadalafil in PVP-VA. AU - Wlodarski,K, AU - Tajber,L, AU - Sawicki,W, Y1 - 2016/09/20/ PY - 2016/01/19/received PY - 2016/05/17/revised PY - 2016/09/18/accepted PY - 2016/9/24/pubmed PY - 2017/3/30/medline PY - 2016/9/24/entrez KW - Amorphous solid dispersion KW - Ball milling KW - Direct compression tablets KW - Dissolution KW - Spray drying KW - Supersaturable formulation KW - Tadalafil SP - 14 EP - 23 JF - European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V JO - Eur J Pharm Biopharm VL - 109 N2 - The aim of this research was to develop immediate release tablets comprising solid dispersion (IRSDTs) of tadalafil (Td) in a vinylpyrrolidone and vinyl acetate block copolymer (PVP-VA), characterized by improved dissolution profiles. The solid dispersion of Td in PVP-VA (Td/PVP-VA) in a weight ratio of 1:1 (w/w) was prepared using two different processes i.e. spray drying and ball milling. While the former process has been well established in the formulation of IRSDTs the latter has not been exploited in these systems yet. Regardless of the preparation method, both Td/PVP-VA solid dispersions were amorphous as confirmed by PXRD, DSC and FTIR. However, different morphology of particles (SEM) resulted in differences in water apparent solubility and disk intrinsic dissolution rate (DIDR). Both solid dispersions and crystalline Td were successfully made into directly compressible tablets at three doses of Td, i.e. 2.5mg, 10mgand20mg, yielding nine different formulations (D1-D9). Each of the lots met the requirements set by Ph.Eur. and was evaluated with respect to appearance, diameter, thickness, mass, hardness, friability, disintegration time and content of Td. IRSDTs performed as supersaturable formulations and had significantly improved water dissolution profiles in comparison with equivalent tablets containing crystalline Td and the marketed formulations. Tablets with both spray dried and ball milled Td/PVP-VA revealed the greatest improvement in dissolution depending on the investigated doses, i.e. 2.5mgand20mg, respectively. Also, dissolution of Td from Td/PVP-VA delivered in different forms occurred in the following order: powders>tablets>capsules. SN - 1873-3441 UR - https://www.unboundmedicine.com/medline/citation/27658987/Physicochemical_properties_of_direct_compression_tablets_with_spray_dried_and_ball_milled_solid_dispersions_of_tadalafil_in_PVP_VA_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0939-6411(16)30574-4 DB - PRIME DP - Unbound Medicine ER -