Aguiar João P, Fernandes Tânia A P, Nese Carlotta, Fernandes Ana I, Pinto João F
CiiEM - Centro de Investigação Interdisciplinar Egas Moniz, Instituto Superior de Ciências da Saúde Egas Moniz, Caparica, Portugal.
iMed.ULisboa - Dep. Farmácia Galénica e Tecnologia Farmacêutica, Faculdade de Farmácia, Universidade de Lisboa, Lisboa, Portugal.
J Pharm Pharmacol. 2017 May;69(5):554-566. doi: 10.1111/jphp.12612. Epub 2016 Aug 3.
This work evaluates the potential of using fresh milk to deliver theophylline to children.
Theophylline-fresh milk systems were prepared using different solids ratios (0 : 1-1 : 0) and three fat contents in commercial milks (low, medium and high), which were spray-dried at different inlet air temperatures (T - 105, 130 and 150 °C). The process was evaluated for yield and the resulting powders for moisture content (MC), particle size and shape, density and wettability. Theophylline-milk potential interactions (differential scanning calorimetry (DSC) and FT-IR) and chemical (theophylline content) and microbiological stability of powders (shelf and in-use) were also evaluated.
The production yield (13.6-76.0%), MC (0.0-10.3%) and contact angles in water (77.29-93.51°) were significantly (P < 0.05) affected by T , but no differences were found concerning the mean particle size (3.0-4.3 μm) of the different powders. The milk fat content significantly (P < 0.05) impacted on the density (1.244-1.552 g/cm ). Theophylline content remained stable after 6 months of storage, before extemporaneous reconstitution. After reconstitution in water, low-fat milk samples (stored at 4 °C) met the microbial pharmacopoeia criteria for up to 7 days. No theophylline-milk components interaction was observed.
Spray-dried milk-composed powders may be used as vehicles for theophylline delivery in paediatrics following further characterization and in-vivo evaluation.
本研究评估使用鲜牛奶向儿童递送茶碱的潜力。
使用不同的固液比（0:1 - 1:0）以及市售牛奶中的三种脂肪含量（低、中、高）制备茶碱 - 鲜牛奶体系，并在不同的进风温度（105、130和150℃）下进行喷雾干燥。对该过程的产率进行评估，并对所得粉末的水分含量（MC）、粒径和形状、密度及润湿性进行测定。还评估了茶碱与牛奶的潜在相互作用（差示扫描量热法（DSC）和傅里叶变换红外光谱法（FT - IR））以及粉末的化学稳定性（茶碱含量）和微生物稳定性（货架期和使用期）。
产率（13.6 - 76.0%）、MC（0.0 - 10.3%）和在水中的接触角（77.29 - 93.51°）受进风温度显著影响（P < 0.05），但不同粉末的平均粒径（3.0 - 4.3μm）未发现差异。牛奶脂肪含量对密度（1.244 - 1.552 g/cm³）有显著影响（P < 0.05）。在临时复溶前，茶碱含量在储存6个月后保持稳定。在水中复溶后，低脂牛奶样品（4℃储存）在长达7天内符合微生物药典标准。未观察到茶碱与牛奶成分的相互作用。
经进一步表征和体内评估后，喷雾干燥的牛奶组成粉末可作为儿科中递送茶碱的载体。
