Tailoring α/β Ratio of Pollen-Like Anhydrous Lactose as Ingredient Carriers for Controlled Dissolution Rate

Jia Xiang,Chuanpin Chen,Songwen Tan,Le Fu,Bo Wang,Wenjie Liu

doi:10.3390/cryst11091049

Abstract

Lactose is a commonly used excipient with two isomers. Different isomers have different properties, especially in terms of solubility. This work is mainly to explore the influence of different a/β ratio lactose on drug dissolution. This work has developed novel mesoporous pollen-like lactose anhydrous with tailored α/β ratios as ingredient carriers for controlled dissolution rate. The produced lactose carriers are pollen-like with a particle size of ~15 μm and a mean pore width of ~30 nm. β-lactose anhydrous has a unique FTIR-peak at 948 cm−1, whereas α-lactose anhydrous shows a unique FTIR-peak at 855 cm−1. DSC analysis suggests that the pollen-like α/β-lactose crystals are polymorphs with unique peaks of melting points. XRD analysis suggests that (5:5)α/β-lactose polymorph has high crystalline purity. The loading efficiency (30.6–33.4% w/w) of acetamidophenol within the nanoporous lactose particles is dependent on the surface structure and pore volumes—the pore volumes were found to be 0.0209–0.0380 cm3/g. The release rates of acetamidophenol are lower for lactose with high α/β ratios. The lactose solubility and the first-order release constant can be tailored by changing the proportion of β-lactose in the pollen-like lactose carriers.

Highlights

IntroductionAs reported by Young, et al [1], each 100 g regular milk (aqueous) contains about 4.7 g lactose, 3.2 g protein and 3.6 g fat
The α/β ratio of lactose is important for any food or pharmaceutical applications since the solubility, stability and morphology are different for and αlactose [16,23], affecting the dissolution, taste, storage and inspection of products
A method of antisolvent precipitation in DMSO-ethanol was employed to produce the pollen-like anhydrous lactose, where no water was involved in synthesis to avoid mutarotation of lactose

Summary

Introduction

As reported by Young, et al [1], each 100 g regular milk (aqueous) contains about 4.7 g lactose, 3.2 g protein and 3.6 g fat. Their weight fractions generally change within certain ranges regarding factors of breed, gene, health, environment, management practices and diet [2], where the concentration of lactose keeps relatively constant [3]. Regarding the high and constant concentration of lactose in milk, lactose has been purely isolated in the industry from nanofiltered whey solutions with assistance of activated carbons at adjusted pHs. Lactose has been widely used in food [4]

Methods

Results

Conclusion