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Outline
Helicide and rosmarinic acid possess sleep-improving properties but suffer from poor aqueous solubility. This study aimed to construct a dual-drug co-loaded amorphous system. Compatibility and intermolecular interactions were predicted using Hansen solubility parameters and molecular docking. Co-evaporates were prepared via the solvent co-evaporation method. Polarized light microscopy, X-ray diffraction, and differential scanning calorimetry analyses confirmed the formation of a single-phase binary co-amorphous system. Fourier-transform infrared spectroscopy, ultraviolet spectroscopy, and nuclear magnetic resonance analyses revealed that hydrogen bonds formed between the aromatic ketone carbonyl group of helicide and the carboxylic acid group of rosmarinic acid, while π-π stacking interactions occurred between their aromatic rings, constituting a stable intermolecular network. Co-amorphization significantly enhanced the apparent solubility of both drugs in pure water by 4.7-fold and 5.1-fold, respectively. In vitro dissolution studies indicated an initial rapid release phase, followed by limitations due to gelation. All animal experiments were conducted in strict accordance with the regulations of the Animal Experiment Ethics Committee of Yunnan University of Chinese Medicine, with approval number: YNUTCM-XMSS-G-20250059. Pharmacodynamic evaluation in a zebrafish insomnia model demonstrated that the co-amorphous system at low and medium doses prolonged total sleep time, increased the number of sleep bouts and average bout length, and shortened sleep latency compared to individual drugs or physical mixture. A combination index (CI) < 0.7 confirmed a synergistic sleep-promoting effect. The solvent co-evaporation method proved efficient and straightforward for preparing the co-amorphous system. This co-amorphous strategy demonstrates significant advantages in improving aqueous solubility and achieving synergistic hypnotic efficacy.
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| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |
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