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Preliminary observations on dissolution and bioavailability of triamterene–hydrochlorothiazide combination products

✍ Scribed by Vinod P. Shah; Mark A. Walker; Vadlamani K. Prasad; Julianne Lin; Gene Knapp; Bernard E. Cabana


Publisher
John Wiley and Sons
Year
1984
Tongue
English
Weight
464 KB
Volume
5
Category
Article
ISSN
0142-2782

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✦ Synopsis


The dissolution profiles of two brands of triamterene-hydrochlorothiazide (TRM-HCT) combination tablets and two brands of TRM-HCT combination capsules were studied using the USP paddle method at 100revmin-' in acid medium (0.1N). The tablets represent two products marketed in Germany, whereas the capsules represent the approved innovator's product and an unapproved generic product. The tablets dissolved almost 100 per cent in 15min whereas the capsules dissolved less than 25 per cent in 60min. A pilot bioavailability study was carried out in four normal healthy male volunteers. Urine samples were collected over a 48 h period and analysed for TRM, its major metabolite TRM-sulfate, and HCT using HPLC methods. The dissolution characteristics of TRM can be associated with the total drug excretion (absorption) of the product. On the other hand, the excretion (absorption) of HCT was independent of dissolution characteristics of the products. However, in TRM-HCT combination product, there appears to be a 50 per cent reduction in HCT excretion (absorption) when compared to the reported excretion (absorption) from a marketed single-entity product.