Abstract：
:The use of experimental design for the robustness testing of a flow-through dissolution method (Ph Eur/USP Apparatus 4) for atovaquone, one of the drug substances in a dual-active anti-malarial tablet formulation, Malarone tablets, is described. This procedure was developed to overcome the suppression of the atovaquone solubility, caused by the presence of the co-drug proguanil hydrochloride and potential imprecision due to the poor solubility of the coating material in the basic dissolution media employed. For this testing a quarter fractional two-level factorial design was applied, assessing six factors in sixteen experiments, with a further six centre points to assess natural experimental variation. Results demonstrate that the method is robust to small changes in all the main factors evaluated at sample times of 30 min or greater. At 15 min, variations in the concentration of sodium hydroxide in the dissolution media, peristaltic pump speed and flow rate were assessed as statistically significant. This observation is a result of the initial steepness of the dissolution release curve and hence these factors are now controlled routinely in the method. Release of this poorly soluble drug is limited at the 45 min time point (Q=75%) according to pharmacopoeial guidelines. The approach may be applied for other dissolution procedures.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Bloomfield MS,Butler WCdoi
10.1016/s0378-5173(00)00509-3keywords:
subject
Has Abstractpub_date
2000-09-25 00:00:00pages
55-61issue
1-2eissn
0378-5173issn
1873-3476pii
S0378517300005093journal_volume
206pub_type
杂志文章abstract：:It has been reported that the degree of particle agglomeration in fluidized bed coating is greatly affected by the spray mist size of coating solution. However, the mist size has generally been measured in open air, and few reports have described the measurement of the mist size in a chamber of the fluidized bed, in w...
journal_title：International journal of pharmaceutics
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更新日期：2001-09-11 00:00:00
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更新日期：1999-11-10 00:00:00
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更新日期：2013-11-01 00:00:00
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更新日期：2009-05-08 00:00:00
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更新日期：2010-08-30 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 评论,杂志文章
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更新日期：2004-01-09 00:00:00
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pub_type： 杂志文章,评审
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更新日期：2005-01-20 00:00:00
