Role of wetting agents and disintegrants in development of danazol nanocrystalline tablets

Saikishore Meruva; Prajwal Thool; Yuchuan Gong; Shyam Karki; William E. Bowen; Sumit Kumar

doi:10.1016/j.ijpharm.2020.119026

Role of wetting agents and disintegrants in development of danazol nanocrystalline tablets

Saikishore Meruva, Prajwal Thool, Yuchuan Gong, Shyam Karki, William E. Bowen, Sumit Kumar

In: International Journal of Pharmaceutics · 2020 · vol. 577 , pp. 119026 · doi:10.1016/j.ijpharm.2020.119026 · PMID:31940456 · W2999851628

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This study investigated how wetting agents and disintegrants affect the development of danazol nanocrystalline tablets, assessing their impact on tablet properties.

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Abstract

Poor wetting and/or particle aggregation are the shortcomings of the dried nanocrystalline suspensions, which subsequently might hinder the superior dissolution performance of the nano-crystalline suspensions. The objective of this study was to evaluate the effect of wetting agents and disintegrants on the dissolution performance of dried nanocrystals of an active pharmaceutical ingredient (API) with poor wetting property. Danazol, a BCS Class II compound with high LogP and low polar surface area, was chosen as a model compound for this study. Danazol nanocrystalline suspension was prepared by wet-media milling and converted into powder via spray granulation either with mannitol or microcrystalline cellulose as carriers at a drug: carrier ratio of 1:9 w/w. Danazol nanocrystalline suspension showed a superior dissolution performance compared to an un-milled danazol suspension. Dried danazol nanocrystals suffered from poor wetting leading to hindered dissolution performance i.e. ~ 40% and ~ 15% drug dissolution within 15 min for the mannitol and microcrystalline cellulose-based granules, respectively. Addition of a lipophilic surfactant (i.e. docusate sodium) at a surfactant: drug ratio of 0.015: 1 w/w during granulation helped in retaining the superior drug dissolution rates i.e. more than 80% drug dissolution within 15 min for mannitol-based granules by enhancing the wettability of dried danazol nanocrystals when compared to a hydrophilic surfactant (i.e. poloxamer 188) or disintegrant (i.e. sodium starch glycolate or croscarmellose sodium). The fast-dissolving mannitol-based granules containing danazol nanocrystals and docusate sodium were compressed into a tablet dosage form. The tablets containing danazol nanocrystals with docusate sodium showed a superior dissolution performance compared to a tablet containing un-milled danazol with docusate sodium.

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Formulation and Performance of Danazol Nano-crystalline Suspensions and Spray Dried Powders via openalex
Rapid dissolving high potency danazol powders produced by spray freezing into liquid process via openalex
Solubilization and Wetting Effects of Bile Salts on the Dissolution of Steroids via openalex
Surface treatment of the hydrophobic drug danazol to improve drug dissolution via openalex
doi:10.1016/s0928-0987(96)00256-4 via openalex
doi:10.1002/jps.2600670716 via openalex
doi:10.2174/1381612821666150901100417 via openalex
doi:10.1016/j.ejpb.2009.05.006 via openalex
doi:10.1016/0378-5173(95)00033-f via openalex
doi:10.1021/ma00111a026 via openalex
doi:10.1208/pt0801009 via openalex
doi:10.1016/j.ejps.2007.06.005 via openalex
doi:10.1016/j.ejpb.2016.03.007 via openalex
doi:10.1016/j.ijpharm.2007.02.005 via openalex
doi:10.1016/j.ijpharm.2009.04.038 via openalex
doi:10.1016/j.ejpb.2008.06.014 via openalex
doi:10.1002/jps.24155 via openalex
doi:10.1016/j.ijpharm.2019.118509 via openalex
doi:10.1016/s0378-5173(97)00311-6 via openalex
doi:10.1016/j.ejps.2008.06.009 via openalex
doi:10.1016/j.addr.2007.05.003 via openalex
doi:10.3390/pharmaceutics10030131 via openalex
doi:10.1016/j.addr.2006.09.017 via openalex
doi:10.1016/0021-9797(82)90128-x via openalex
doi:10.1201/b14005-13 via openalex
doi:10.1016/j.ijpharm.2019.03.007 via openalex
doi:10.1016/j.ijpharm.2014.05.060 via openalex
doi:10.1248/cpb.58.230 via openalex
doi:10.1080/03639045.2016.1178770 via openalex
doi:10.1016/b978-0-323-51255-8.00010-0 via openalex
doi:10.1016/j.ijpharm.2014.11.043 via openalex
doi:10.1002/jps.24426 via openalex
doi:10.1208/s12249-016-0604-1 via openalex
doi:10.1016/j.ijpharm.2019.04.050 via openalex
doi:10.1016/j.ijpharm.2004.09.007 via openalex
doi:10.1016/j.ejps.2012.04.020 via openalex
doi:10.3390/pharmaceutics10030134 via openalex
doi:10.1080/03639040500216097 via openalex
doi:10.1016/j.ijpharm.2014.01.013 via openalex
doi:10.1016/j.ijpharm.2005.05.014 via openalex
doi:10.1201/9780849374555-4 via openalex
doi:10.3109/10837450.2014.982822 via openalex
doi:10.1016/0378-5173(86)90226-7 via openalex

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[1] Solubilization and Wetting Effects of Bile Salts on the Dissolution of Steroids 1991

[2] Surface treatment of the hydrophobic drug danazol to improve drug dissolution 1998

[3] Formulation and Performance of Danazol Nano-crystalline Suspensions and Spray Dried Powders 2014

[4] Rapid dissolving high potency danazol powders produced by spray freezing into liquid process 2003