pharma-and-clinical-pharmacy-congress-2016_posters

9 / 21

Notes:
Page 59
Pharma & Clinical Pharmacy Congress 2016
November 07-09, 2016
Volume 5 Issue 4(Suppl) Clin Pharmacol Biopharm
ISSN: 2167-065X CPB, an open access journal
conferenceseries .com
November 07-09, 2016 Las Vegas, Nevada, USA
4th International
Pharma & Clinical Pharmacy Congress
Cristina Helena Dos Reis Serra et al., Clin Pharmacol Biopharm 2016, 5:4(Suppl)
Solubility characterization of didanosine using shake flask and intrinsic dissolution methods:
Application for biopharmaceutical classification
Cristina Helena Dos Reis Serra, Andre Bersani Dezani, Julie Caroline Ferrari Ferreira and Thaisa Marinho Dezani
University of Sao Paulo, Brazil
The solubilization of a drug orally administered is a mandatory step for its permeation. Two methods have been described
in the literature for solubility characterization: shake flask and intrinsic dissolution. Although some values of solubility
can be found in the literature, this characterization is not clear for didanosine (ddI). Thus, the solubility of ddI was evaluated
using the shake flask and intrinsic dissolution methods. Buffer solutions were prepared at pH 1.2, pH 4.5, pH 6.8, pH 7.5 and
purified water. In the shake flask method, ddI was added in each media (150 rpm at 37°C for 72h). For intrinsic dissolution
method, the compound was compacted into the wood’s apparatus matrix and subjected to dissolution in each media (50 rpm
at 37°C up to 150 min). The results obtained in shake flask method showed that 139.37 mL (pH 1.2), 87.72 mL (pH 4.5), 12.54
mL (pH 6.8), 4.09 mL (pH 7.5) and 7.65 mL (purified water) were necessary for drug solubilization. In addition, a very fast
intrinsic dissolution rate was obtained for each media: 0.1 mg/min/cm² (pH 1.2), 0.2 mg/min/cm² (pH 4.5), 0.2 mg/min/
cm² (pH 6.8), 0.1 mg/min/cm² (pH 7.5) and 0.1 mg/min/cm² (purified water). Results from both methods are in accordance,
but some differences in dose strength can explain divergences in the solubility. For intrinsic dissolution, the dose strength
is not considered and does not interfere on the dissolution profile. Based on these results, ddI is highly soluble, considering
dose:solubility ratio <250 mL and dose number (D0) ≤1 for shake flask method and intrinsic dissolution rate greater than
0.1 mg/min/cm2. Furthermore, the intrinsic dissolution method can be used for early drug development regarding solubility
characterization.
Biography
Cristina Helena Dos Reis Serra is an expert in Pharmacy with emphasis on bio-pharmaceutics considering the following topics: “Gastrointestinal drug absorption,
drug solubility and permeability, bioequivalence and oral bioavailability, in vitro-in vivo correlation (IVIVC) and pharmaceutical development”. Currently, she is a
Professor at Faculty of Pharmaceutical Sciences, University of Sao Paulo, Brazil.