中国药师
中國藥師
중국약사
CHINA PHARMACIST
2014年
11期
1849-1852
,共4页
盐酸倍他洛尔%N-三甲基壳聚糖%脂质体%眼压%心率%血压
鹽痠倍他洛爾%N-三甲基殼聚糖%脂質體%眼壓%心率%血壓
염산배타락이%N-삼갑기각취당%지질체%안압%심솔%혈압
Betaxolol hydrochloride%N-trimethyl chitosan%Liposomes%Intraocular pressure%Heart rate%Blood pressure
目的：研究盐酸倍他洛尔( BH)眼用阳离子脂质体对家兔眼压( IOP)、血压( BP)及心率( HR)的影响,为BH新型眼用制剂的研发奠定实验基础。方法：采用N-三甲基壳聚糖(TMC60)为包衣材料,制备BH阳离子脂质体(TMC60-BHL)；以24只健康家兔为实验动物,按数字法随机分为4组,均行单侧颈动脉插管后连接于生理记录仪。分别单侧眼滴入50μl 的TMC60-BHL,未包衣BHL,市售BH滴眼液(阳性对照)及灭菌蒸馏水(阴性对照)。在预定时间内用眼压计测定家兔双侧眼压,生理记录仪测定血压及心率的变化。结果：滴入TMC60-BHL及未包衣BHL的家兔眼压最大降幅分别为为23.00%及26.65%,对侧眼压最大降幅分别为18.54%及24.33%。与阳性对照组(最大降幅分别为19.01%,15.19%)比较,差异均有统计学意义(P<0.05)；与BHL组比较,TMC60-BHL的降IOP作用更为显著而持久(P<0.05)。各给药组可引起心率减慢及血压的下降,但与阴性对照组比较,差异无统计学意义(P>0.05)。结论：TMC60-BHL降眼压作用明显,且对心率及血压无显著影响,值得进一步研究。
目的：研究鹽痠倍他洛爾( BH)眼用暘離子脂質體對傢兔眼壓( IOP)、血壓( BP)及心率( HR)的影響,為BH新型眼用製劑的研髮奠定實驗基礎。方法：採用N-三甲基殼聚糖(TMC60)為包衣材料,製備BH暘離子脂質體(TMC60-BHL)；以24隻健康傢兔為實驗動物,按數字法隨機分為4組,均行單側頸動脈插管後連接于生理記錄儀。分彆單側眼滴入50μl 的TMC60-BHL,未包衣BHL,市售BH滴眼液(暘性對照)及滅菌蒸餾水(陰性對照)。在預定時間內用眼壓計測定傢兔雙側眼壓,生理記錄儀測定血壓及心率的變化。結果：滴入TMC60-BHL及未包衣BHL的傢兔眼壓最大降幅分彆為為23.00%及26.65%,對側眼壓最大降幅分彆為18.54%及24.33%。與暘性對照組(最大降幅分彆為19.01%,15.19%)比較,差異均有統計學意義(P<0.05)；與BHL組比較,TMC60-BHL的降IOP作用更為顯著而持久(P<0.05)。各給藥組可引起心率減慢及血壓的下降,但與陰性對照組比較,差異無統計學意義(P>0.05)。結論：TMC60-BHL降眼壓作用明顯,且對心率及血壓無顯著影響,值得進一步研究。
목적：연구염산배타락이( BH)안용양리자지질체대가토안압( IOP)、혈압( BP)급심솔( HR)적영향,위BH신형안용제제적연발전정실험기출。방법：채용N-삼갑기각취당(TMC60)위포의재료,제비BH양리자지질체(TMC60-BHL)；이24지건강가토위실험동물,안수자법수궤분위4조,균행단측경동맥삽관후련접우생리기록의。분별단측안적입50μl 적TMC60-BHL,미포의BHL,시수BH적안액(양성대조)급멸균증류수(음성대조)。재예정시간내용안압계측정가토쌍측안압,생리기록의측정혈압급심솔적변화。결과：적입TMC60-BHL급미포의BHL적가토안압최대강폭분별위위23.00%급26.65%,대측안압최대강폭분별위18.54%급24.33%。여양성대조조(최대강폭분별위19.01%,15.19%)비교,차이균유통계학의의(P<0.05)；여BHL조비교,TMC60-BHL적강IOP작용경위현저이지구(P<0.05)。각급약조가인기심솔감만급혈압적하강,단여음성대조조비교,차이무통계학의의(P>0.05)。결론：TMC60-BHL강안압작용명현,차대심솔급혈압무현저영향,치득진일보연구。
Objective: To study the effects of betaxolol hydrochloride (BH) cationic liposomes on intraocular pressure (IOP), blood pressure ( BP) and heart rate ( HR) in rabbits to lay foundation for the development of new BH eye preparations. Methods:N-trimethyl chitosan (TMC60) was used as the coating material, the BH-loaded cationic liposomes (TMC60-BHL) were prepared. Total-ly 24 healthy rabbits were randomly divided into 4 groups using number method. Unilateral carotid artery intubation was carried out in the rabbits and connected a physiological recorder. TMC60-BHL, uncoated BHL, the marketed BH eye drops ( the positive control) and sterilized distilled water ( the negative control) with the volume of 50 μl was respectively used in one eye of the rabbits. IOP was detected by an ophthalmotonometer, and BP and HR were determined by the physiological recorder at the predetermined time intervals. Results:In the ipsilateral eyes, the maximum decrease in IOP for uncoated BHL and TMC60-BHL was 23. 00% and 26. 65%, respec-tively. In the contralateral eyes, the maximum decrease in IOP for uncoated BHL and TMC60-BHL was 18. 54% and 24. 33%, respec-tively. Compared with that of the positive control (19. 01%,15. 19%), the IOP decrease effect of uncoated BHL and TMC60-BHL was significant higher(P<0. 05), and that of TMC60-BHL was the highest(P<0. 05). BP and HR were both reduced in the various BH groups, while there was no notable difference when compared with those in the negative group(P>0. 05). Conclusion:TMC60-BHL shows significant IOP decrease effect without notable effect on BP and HR, which is valuable to be studied further.
