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目的研制成骨生长肽(OGP)鼻喷剂并考察其吸收特性。方法采用大鼠鼻腔灌流模型,以成骨生长肽在大鼠鼻腔的下降量为指标,运用正交试验,筛选吸收促进剂;优化蛋白酶抑制剂及其剂量,考察并验证最佳处方及其稳定性。并采用扫描电镜观察经成骨生长肽鼻喷剂灌流4 h后大鼠鼻黏膜纤毛形态的改变,进行局部安全性评价。结果成骨生长肽鼻喷剂的最佳处方为含成骨生长肽0.2 mg·mL-1、枸橼酸5 mg·mL-1、羟丙基-β-环糊精10 mg·mL-1、聚山梨酯-80 30 mg·mL-1及杆菌肽锌5 mg·mL-1的pH3邻苯二甲酸氢钾缓冲溶液;该鼻喷剂对鼻黏膜刺激性较小。结论成骨生长肽鼻喷剂在大鼠鼻腔具有良好的吸收、质量稳定。
OBJECTIVE To develop osteogenesis peptide (OGP) nasal spray and investigate its absorption characteristics. Methods Rat nasal perfusion model was used to determine the descent amount of osteogenic growth peptide in the rat nasal cavity as an index. The orthogonal test was used to screen the absorption enhancers. The optimized protease inhibitor and its dosage were investigated and validated. Sex. Scanning electron microscopy was used to observe the morphological changes of the nasal mucosa in rats after 4 h perfusion of the osteogenic growth peptide nasal spray for local safety evaluation. Results The best prescription of osteoporosis peptide nasal spray was osteoblast growth peptide 0.2 mg · mL-1, citrate 5 mg · mL-1, hydroxypropyl-β-cyclodextrin 10 mg · mL-1 , Polysorbate-80 30 mg · mL-1 and bacitracin zinc 5 mg · mL-1 pH3 potassium hydrogen phthalate buffer; the nasal spray less irritating to the nasal mucosa. Conclusion Osteogenic growth peptide nasal spray has a good absorption in rat nasal cavity and its quality is stable.