Abstract：
:In this work calcium stearate (CaSt) multi-particulates loaded with codeine phosphate (COP) were developed in an attempt to provide extended release (ER) combined with alcohol dose dumping (ADD) resistance. The pellets were prepared via wet/extrusion spheronization and ER characteristics were obtained after fluid bed drying at 30°C. Pore blockers (i.e., xanthan, guar gum and TiO2) were integrated to control the uptake of ethanolic media, the CaSt swelling and consequently, the COP release. While all three pore blockers are insoluble in ethanol, xanthan dissolves, guar gum swells and TiO2 does not interact with water. The incorporation of 10 and 15% TiO2 still provided ER characteristics and yielded ADD resistance in up to 40v% ethanol. The in-vitro data were subjected to PK simulations, which revealed similar codeine plasma levels when the medication is used concomitantly with alcoholic beverages. Taken together the in-vitro and in-silico results demonstrate that the incorporation of appropriate pore blockers presents a promising strategy to provide ADD resistance of multi-particulate systems.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Schrank S,Jedinger N,Wu S,Piller M,Roblegg Edoi
10.1016/j.ijpharm.2016.05.049subject
Has Abstractpub_date
2016-07-25 00:00:00pages
219-228issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(16)30438-0journal_volume
509pub_type
杂志文章abstract：:This work investigated the permeation of primaquine across full-thickness excised human skin from two acrylate transdermal adhesives. Primaquine base was formulated with National Starch 387-2516 and 387-2287 to provide aluminium foil-backed 1-cm diameter patches, each loaded with 10 mg drug. Other patches were prepare...
journal_title：International journal of pharmaceutics
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pub_type： 杂志文章,随机对照试验
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journal_title：International journal of pharmaceutics
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pub_type： 临床试验,杂志文章
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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更新日期：2002-07-08 00:00:00
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journal_title：International journal of pharmaceutics
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更新日期：2017-10-30 00:00:00
