Effect of Liquid Load Level and Binder Type on the Tabletability of Mesoporous Silica Based Liquisolids.


Journal

AAPS PharmSciTech
ISSN: 1530-9932
Titre abrégé: AAPS PharmSciTech
Pays: United States
ID NLM: 100960111

Informations de publication

Date de publication:
21 Oct 2024
Historique:
received: 16 05 2024
accepted: 24 09 2024
medline: 22 10 2024
pubmed: 22 10 2024
entrez: 21 10 2024
Statut: epublish

Résumé

Mesoporous silica offers an easy way to transform liquids into solids, due to their high loading capacity for liquid or dissolved active ingredients and the resulting enhanced dissolution properties. However, the compression of both unloaded and loaded mesoporous silica bulk material into tablets is challenging, due to poor/non-existing binding capacity. This becomes critical when high drug loads are to be achieved and the fraction of additional excipients in the final tablet formulation needs to be kept at a minimum. Our study aimed to investigate the mechanism of compression and tabletability dependent on the Liquid Load Level of the silica and type of filler/binder in binary tabletting mixtures. To this end, Vivapur® 101, FlowLac® 90, Pearlitol® 200 SD and tricalcium citrate tetrahydrate were selected and mixed with Syloid® XDP 3050 at various Liquid Load Levels. Compaction characteristics were analysed using the StylOne® Classic 105 ML compaction simulator. Additionally, the Overall Liquid Load (OLL) was defined as a new critical quality attribute for liquisolid tablets. The Overall Liquid Load allows straightforward, formulation-relevant comparisons between various fillers/binders, liquid components, and silica types. Results indicate strong binding capacity and high plasticity of the fillers/binders as key components for successful high liquid load silica tablet formulation. A volumetric combination of 30% Vivapur® 101 and 70% 0.75 mL/g loaded Syloid® XDP 3050 proved to be the most effective mixture, achieving an Overall Liquid Load of 36-41% [v/v] and maintaining a tensile strength of 1.5 N/mm

Identifiants

pubmed: 39433659
doi: 10.1208/s12249-024-02958-9
pii: 10.1208/s12249-024-02958-9
doi:

Substances chimiques

Tablets 0
Silicon Dioxide 7631-86-9
Excipients 0

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

246

Informations de copyright

© 2024. The Author(s).

Références

Spireas SS, Jarowski CI, Rohera BD. Powdered Solution Technology: Principles and Mechanism. Pharm Res. 1992;9(10):1351–8.
pubmed: 1448438 doi: 10.1023/A:1015877905988
Sun WJ, Aburub A, Sun CC. A mesoporous silica based platform to enable tablet formulations of low dose drugs by direct compression. Int J Pharm. 2018;539(1–2):184–9.
pubmed: 29414125 doi: 10.1016/j.ijpharm.2018.01.049
McCarthy CA, Ahern RJ, Dontireddy R, Ryan KB, Crean AM. Mesoporous silica formulation strategies for drug dissolution enhancement: a review. Expert Opin Drug Deliv. 2016;13(1):93–108.
pubmed: 26549623 doi: 10.1517/17425247.2016.1100165
Limnell T, Santos HA, Mäkilä E, Heikkilä T, Salonen J, Murzin DYu, et al. Drug Delivery Formulations of Ordered and Nonordered Mesoporous Silica: Comparison of Three Drug Loading Methods. J Pharm Sci. 2011;100(8):3294–306.
pubmed: 21520084 doi: 10.1002/jps.22577
Spireas S, inventor; Liquisolid systems and methods of preparing same. United States patent US6423339B1, 2002 [cited 2023 Oct 12]. Available from: https://patents.google.com/patent/US6423339B1/en
Lipinski CA, Lombardo F, Dominy BW, Feeney PJ. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings1PII of original article: S0169–409X(96), 00423–1. Adv Drug Deliv Rev. 1997;23(1):3–25 (2001 Mar 1;46(1):3–26).
doi: 10.1016/S0169-409X(96)00423-1
Tabboon P, Pongjanyakul T, Limpongsa E, Jaipakdee N. In Vitro Release, Mucosal Permeation and Deposition of Cannabidiol from Liquisolid Systems: The Influence of Liquid Vehicles. Pharmaceutics. 2022;14(9):1787.
pubmed: 36145536 pmcid: 9503133 doi: 10.3390/pharmaceutics14091787
Tiong N, Elkordy AA. Effects of liquisolid formulations on dissolution of naproxen. Eur J Pharm Biopharm. 2009;73(3):373–84.
pubmed: 19679184 doi: 10.1016/j.ejpb.2009.08.002
Akinlade B, Elkordy AA, Essa EA, Elhagar S. Liquisolid Systems to Improve the Dissolution of Furosemide. Sci Pharm. 2010;78(2):325–44.
pubmed: 21179350 pmcid: 3002790 doi: 10.3797/scipharm.0912-23
Javadzadeh Y, Jafari-Navimipour B, Nokhodchi A. Liquisolid technique for dissolution rate enhancement of a high dose water-insoluble drug (carbamazepine). Int J Pharm. 2007;341(1):26–34.
pubmed: 17498898 doi: 10.1016/j.ijpharm.2007.03.034
Elkordy AA, Tan XN, Essa EA. Spironolactone release from liquisolid formulations prepared with Capryol™ 90, Solutol® HS-15 and Kollicoat® SR 30 D as non-volatile liquid vehicles. Eur J Pharm Biopharm. 2013;83(2):203–23.
pubmed: 22960707 doi: 10.1016/j.ejpb.2012.08.004
Spireas S, Sadu S. Enhancement of prednisolone dissolution properties using liquisolid compacts. Int J Pharm. 1998;166(2):177–88.
doi: 10.1016/S0378-5173(98)00046-5
Hentzschel CM, Alnaief M, Smirnova I, Sakmann A, Leopold CS. Enhancement of griseofulvin release from liquisolid compacts. Eur J Pharm Biopharm. 2012;80(1):130–5.
pubmed: 21846502 doi: 10.1016/j.ejpb.2011.08.001
Khaled KA, Asiri YA, El-Sayed YM. In vivo evaluation of hydrochlorothiazide liquisolid tablets in beagle dogs. Int J Pharm. 2001;222(1):1–6.
pubmed: 11404027 doi: 10.1016/S0378-5173(01)00633-0
Badawy MA, Kamel AO, Sammour OA. Use of biorelevant media for assessment of a poorly soluble weakly basic drug in the form of liquisolid compacts: in vitro and in vivo study. Drug Deliv. 2016;23(3):808–17.
doi: 10.3109/10717544.2014.917442
Hentzschel CM, Sakmann A, Leopold CS. Suitability of various excipients as carrier and coating materials for liquisolid compacts. Drug Dev Ind Pharm. 2011;37(10):1200–7.
pubmed: 21449826 doi: 10.3109/03639045.2011.564184
Liao CC, Jarowski CI. Dissolution rates of corticoid solutions dispersed on silicas. J Pharm Sci. 1984;73(3):401–3.
pubmed: 6325660 doi: 10.1002/jps.2600730330
Lamprecht A, Grizic D, inventors; Pharmaceutical formulations using propylene carbonate. German patent DE102015008534A1, 2017 [cited 2023 Oct 12]. Available from: https://patents.google.com/patent/DE102015008534A1/en
Yadav V, Yadav A. Enhancement of solubility and dissolution rate of BCS class II pharmaceuticals by nonaqueous granulation technique. Int J Pharma Res Dev–Online. 2010;1:1.
Javadzadeh Y, Siahi MR, Asnaashari S, Nokhodchi A. An Investigation of Physicochemical Properties of Piroxicam Liquisolid Compacts. Pharm Dev Technol. 2007;12(3):337–43.
pubmed: 17613897 doi: 10.1080/10837450701247574
Gubbi S, Jarag R. Liquisolid Technique for Enhancement of Dissolution Properties of Bromhexine Hydrochloride. Res J Pharm Technol. 2009;2(2):382–6.
Lam M, Ghafourian T, Nokhodchi A. Liqui-Pellet: the Emerging Next-Generation Oral Dosage Form Which Stems from Liquisolid Concept in Combination with Pelletization Technology. AAPS PharmSciTech. 2019;20(6):231.
pubmed: 31236781 doi: 10.1208/s12249-019-1441-9
Choudhari Y, Reddy U, Monsuur F, Pauly T, Hoefer H, McCarthy W. Comparative evaluation of porous silica based carriers for lipids and liquid drug formulations. Open Mater Sci. 2014;1(1). Available from: https://www.degruyter.com/document/doi/10.2478/mesbi-2014-0004/html
Lam M, Ghafourian T, Nokhodchi A. Liquisolid System and Liqui-Mass System Are Not the Same. AAPS PharmSciTech. 2020;21(3):105.
pubmed: 32180042 doi: 10.1208/s12249-020-01650-y
Pezzini BR, Beringhs AO, Ferraz HG, Silva MAS, Stulzer HK, Sonaglio D. Liquisolid Pellets and Liqui-Pellets Are Not Different. AAPS PharmSciTech. 2020;21(2):72.
pubmed: 31953566 doi: 10.1208/s12249-019-1590-x
Lu M, Xing H, Jiang J, Chen X, Yang T, Wang D, et al. Liquisolid technique and its applications in pharmaceutics. Asian J Pharm Sci. 2017;12(2):115–23.
pubmed: 32104320 doi: 10.1016/j.ajps.2016.09.007
Wagner KG, Lamprecht A, Krome AK, Grizic D, Becker T, inventors; Liquisolid pharmaceutical formulation and process for manufacturing. European patent EP 3 903 770 A1.
European Pharmacopoeia. 10th ed. Deutscher Apotheker Verlag; 2019.
Fell JT, Newton JM. Determination of Tablet Strength by the Diametral-Compression Test. J Pharm Sci. 1970;59(5):688–91.
pubmed: 5446428 doi: 10.1002/jps.2600590523
Hunter JD. Matplotlib: A 2D Graphics Environment. Comput Sci Eng. 2007;9(3):90–5.
doi: 10.1109/MCSE.2007.55
Kawakita K, Lüdde KH. Some considerations on powder compression equations. Powder Technol. 1971;4(2):61–8.
doi: 10.1016/0032-5910(71)80001-3
Alderborn G, Nyström C. Pharmaceutical powder compaction technology. Marcel Dekker; 1996.
Nordström J, Klevan I, Alderborn G. A Particle Rearrangement Index Based on the Kawakita Powder Compression Equation. J Pharm Sci. 2009;98(3):1053–63.
pubmed: 18704952 doi: 10.1002/jps.21488
Pitt KG, Heasley MG. Determination of the tensile strength of elongated tablets. Powder Technol. 2013;1(238):169–75.
doi: 10.1016/j.powtec.2011.12.060
Sabri AH, Hallam CN, Baker NA, Murphy DS, Gabbott IP. Understanding tablet defects in commercial manufacture and transfer. J Drug Deliv Sci Technol. 2018;1(46):1–6.
Xi Y, Liangying Z, Sasa W. Pore size and pore-size distribution control of porous silica. Sens Actuators B Chem. 1995;25(1):347–52.
doi: 10.1016/0925-4005(95)85078-3
Burra S, Yamsani M, Vobalaboina V. The Liquisolid technique: an overview. Braz J Pharm Sci. 2011;47:475–82.
doi: 10.1590/S1984-82502011000300005
Hummler H, Stillhart C, Meilicke L, Grimm M, Krause E, Mannaa M, et al. Impact of Tablet Size and Shape on the Swallowability in Older Adults. Pharmaceutics. 2023;15(4):1042.
pubmed: 37111528 pmcid: 10145850 doi: 10.3390/pharmaceutics15041042
W.R. Grace. SYLOID® XDP silica for conversion of oily actives into powders. 2020 [cited 2023 Nov 7]. Available from: https://www.youtube.com/watch?v=KsfBYL-7mGQ
Nyström C, Alderborn G, Duberg M, Karehill PG. Bonding Surface area and Bonding Mechanism-Two Important Factors fir the Understanding of Powder Comparability. Drug Dev Ind Pharm. 1993;19(17–18):2143–96.
doi: 10.3109/03639049309047189
Osei-Yeboah F, Chang SY, Sun CC. A critical Examination of the Phenomenon of Bonding Area - Bonding Strength Interplay in Powder Tableting. Pharm Res. 2016;33(5):1126–32.
pubmed: 26767997 doi: 10.1007/s11095-016-1858-8
Leuenberger H, Jetzer W. The compactibility of powder systems - a novel approach. Powder Technol. 1984;37(1):209–18.
doi: 10.1016/0032-5910(84)80018-2
Schönfeld BV, Westedt U, Wagner KG. Compression Modulus and Apparent Density of Polymeric Excipients during Compression—Impact on Tabletability. Pharmaceutics. 2022;14(5):913.
pubmed: 35631499 pmcid: 9147214 doi: 10.3390/pharmaceutics14050913
Klinzing GR, Troup GM. Modeling the Air Pressure Increase Within a Powder Bed During Compression—A Step Toward Understanding Tablet Defects. J Pharm Sci. 2019;108(6):1991–2001.
pubmed: 30639739 doi: 10.1016/j.xphs.2019.01.002
Elastic Moduli Data for Polycrystalline Ceramics, R. G. Munro, NISTIR 6853. National Institute of Standards and Technology, Gaithersburg, Maryland 20899. 2022. Available from: https://srdata.nist.gov/CeramicDataPortal/Elasticity/SiO2
Lyapin AG, Gromnitskaya EL, Danilov IV, Brazhkin VV. Elastic properties of the hydrogen-bonded liquid and glassy glycerol under high pressure: comparison with propylene carbonate. RSC Adv. 2017;7(53):33278–84.
doi: 10.1039/C7RA06165J
Çelik M. Overview of Compaction Data Analysis Techniques. Drug Dev Ind Pharm. 1992;18(6–7):767–810.
doi: 10.3109/03639049209058560
Çelik M, Marshall K. Use of a Compaction Simulator System in Tabletting Research. Drug Dev Ind Pharm. 1989;15(5):759–800.
doi: 10.3109/03639048909058530
Thomas I. Algorithm description - ContourPy documentation. [cited 2023 Oct 19]. Available from: https://contourpy.readthedocs.io/en/v1.1.1/description.html
Mamidi HK, Mishra SM, Rohera BD. Determination of maximum flowable liquid-loading potential of Neusilin® US2 and investigation of compressibility and compactibility of its liquisolid blends with PEG (400). J Drug Deliv Sci Technol. 2019;1(54):101285.
doi: 10.1016/j.jddst.2019.101285
Molaei MA, Osouli-Bostanabad K, Adibkia K, Shokri J, Asnaashari S, Javadzadeh Y. Enhancement of ketoconazole dissolution rate by the liquisolid technique. Acta Pharm. 2018;68(3):325–36.
pubmed: 31259692 doi: 10.2478/acph-2018-0025
El-Houssieny BM, Wahman LF, Arafa NMS. Bioavailability and biological activity of liquisolid compact formula of repaglinide and its effect on glucose tolerance in rabbits. Biosci Trends. 2010;4(1):17–24.
pubmed: 20305340
Thoorens G, Krier F, Leclercq B, Carlin B, Evrard B. Microcrystalline cellulose, a direct compression binder in a quality by design environment—A review. Int J Pharm. 2014;473(1):64–72.
pubmed: 24993785 doi: 10.1016/j.ijpharm.2014.06.055
Li XH, Zhao LJ, Ruan KP, Feng Y, Xu DS, Ruan KF. The application of factor analysis to evaluate deforming behaviors of directly compressed powders. Powder Technol. 2013;1(247):47–54.
doi: 10.1016/j.powtec.2013.06.040
Hagelstein V, Gerhart M, Wagner KG. Tricalcium citrate – a new brittle tableting excipient for direct compression and dry granulation with enormous hardness yield. Drug Dev Ind Pharm. 2018;44(10):1631–41.
pubmed: 29916271 doi: 10.1080/03639045.2018.1483389
Vromans H, Bolhuis GK, Lerk CF, van de Biggelaar H, Bosch H. Studies on tableting properties of lactose. VII. The effect of variations in primary particle size and percentage of amorphous lactose in spray dried lactose products. Int J Pharm. 1987;35(1):29–37.
doi: 10.1016/0378-5173(87)90071-8

Auteurs

Jan Appelhaus (J)

Department of Pharmaceutics, University of Bonn, Gerhard-Domagk-Str. 3, 53121, Bonn, Germany.

Kristina E Steffens (KE)

Department of Pharmaceutics, University of Bonn, Gerhard-Domagk-Str. 3, 53121, Bonn, Germany.

Karl G Wagner (KG)

Department of Pharmaceutics, University of Bonn, Gerhard-Domagk-Str. 3, 53121, Bonn, Germany. karl.wagner@uni-bonn.de.

Articles similaires

Silicon Dioxide Water Hot Temperature Compressive Strength X-Ray Diffraction
Calcium Carbonate Sand Powders Construction Materials Materials Testing
Animals Rumen Methane Fermentation Cannabis
Inclusion Bodies Solubility Recombinant Proteins Detergents Protein Denaturation

Classifications MeSH