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α-Glucosyl hesperidin induced an improvement in the bioavailability of pranlukast hemihydrate using high-pressure homogenization.

Abstract：

:The α-glucosyl hesperidin (Hsp-G)-induced improvement of both the dissolution and absorption properties of pranlukast hemihydrate (PLH) was achieved by means of a high-pressure homogenization (HPH) processing. The average particle size in the HPH-processed suspension was decreased significantly after 50 cycles of processing and reached a constant size of ca. 300 nm. The amount of dissolved PLH gradually increased with the pass number of HPH processing, and was extremely higher than the PLH solubility (0.8 μg/mL at 37°C) after the HPH processing. On a dissolution study of the freeze-dried sample of HPH-processed PLH/Hsp-G (1/10), the apparent solubility of PLH was at least 2.5-fold more than that of untreated PLH crystals. The transport study showed that the amount of PLH that had permeated through the Caco-2 cell monolayers was improved in the case of HPH-processed PLH/Hsp-G (1/10). The bioavailability of PLH from HPH-processed PLH/Hsp-G (1/10) showed a 3.9- and 2.2-fold improvement over the PLH crystal in terms of C(max) and AUC values, respectively. Hsp-G formed an associated structure in aqueous media. High-pressure homogenization provides a good opportunity for molecular-level interaction of PLH and the associated structure of Hsp-G to occur. The use of Hsp-G under HPH processing was a promising way to enhance the dissolution and absorption of PLH without using an organic solvent.

journal_name

Int J Pharm

journal_title

International journal of pharmaceutics

authors

Uchiyama H,Tozuka Y,Asamoto F,Takeuchi H

doi

10.1016/j.ijpharm.2011.03.017

subject

Has Abstract

pub_date

2011-05-30 00:00:00

pages

114-7

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(11)00219-5

journal_volume

410

pub_type

杂志文章

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