|
|
|
| Preparation and evaluation of nebulized inhalation preparation of nitanib ethanesulfonate |
| LI Qide1, MI Cuilan2, XU Leyuan1, ZHU Shun1, ZHOU Zaijun1, SHEN Song1 |
| (1. School of Pharmacy, Jiangsu University, Zhenjiang Jiangsu 212013; 2. Bishuilantian Community Health Service Center of Yinchuan Hospital of Traditional Chinese Medicine, Yinchuan Ningxia 750010, China) |
|
|
|
Abstract Objective： To study the optimized formulation of nidanib ethanesulfonate (NE) solution for inhalation and evaluate the formulation in vitro and in vivo. Methods： The prescription of NE solution was studied by optimizing the amount of the antioxidants, osmotic pressure regulators and pH value. The dynamic particle size of NE nebulized inhalation formulations was measured. The in vivo pharmacokinetics of NE nebulized inhalation formulations was determined by high performance liquid chromatography. Lung function, hydroxyproline (HYP), tumor necrosis factor-α(TNF-α), transforming growth factor-β1 (TGF-β1) were used as indicators to evaluate the therapeutic effect in vivo. Results： Optimized prescription was obtained: NE: 10 mg, sodium bisulfite: 4 mg, propylene glycol: 50 mg, water: 2 mL. The pH of the solution was adjusted to 4.0. The average particle size of NE nebulized inhalation was about 3.3 μm. The in vivo pharmacokinetic results in SD rats showed that the elimination half-life of NE inhalation preparation was 5.27 h. The bioavailability was significantly improved, reaching 63.71%. Pulmonary function parameters (tracheal contraction parameters, 50% tidal volume expiratory flow rate, respiratory rate) and lung dry/wet weight ratio, HYP, TNF-α in mice with pulmonary fibrosis model after inhalation administration had been significantly improved. Conclusion： NE inhalation can greatly improve lung function parameters and increase its bioavailability.
［Key words］nidanib ethanesulfonate; inhalation preparations; nebulized inhalation; pharmacokinetics; idiopathic pulmonary fibrosis
|
|
Received: 01 March 2024
|
|
|
|
| [1] |
. [J]. Journal of Jiangsu University(Medicine Edition), 2021, 31(01): 44-50. |
|
|
|
|
