1.Ion-sensitive nanoemulsion-in situ gel system for ophthalmic delivery of flurbiprofen axetil.
Jinqiu SHEN ; Yong GAN ; Li GAN ; Chunliu ZHU ; Jiabi ZHU
Acta Pharmaceutica Sinica 2010;45(1):120-5
The aim of the study is to prepare flurbiprofen axetil nanoemulsion-in situ gel system (FBA/NE-ISG) and observe its ocular pharmacokinetics, rheological behavior, TEM images, irritation and cornea retention. Production of nanoemulsion was based on high-speed shear and homogenization process, and then mixed with gellan gum to prepare FBA/NE-ISG. Rheological study showed that FBA/NE-ISG possesses strong gelation capacity and its viscosity and elastic modulus increases by 2 Pa*s and 5 Pa respectively when mixed with artificial tear at the ratio of 40 : 7. TEM images suggested no significant changes in particle morphology of the pre and post gelation. Good ocular compatibility of FBA/NE-ISG was testified by the irritation test based on histological examination. In vivo fluorescence imaging system was applied to investigate the characteristics of cornea retention, and the results indicated that the nanoemulsion-in situ gel (NE-ISG) prolonged the cornea retention time significantly since K(NE-ISG) (0.008 5 min(-1) was much lower compared with flurbiprofen sodium eye drops (FB-Na, 0.03% w/v) of which the K(Eye drops) was 0.105 2 min(-1), indicated that the cornea retention time of NE-ISG was prolonged significantly. Pharmacokinetics of FBA/NE-ISG in rabbit aqueous humor was studied by cornea puncture, the MRT (12.3 h) and AUC(0-12h) (126.8 microg x min x mL(-1)) of FBA/NE-ISG was 2.7 and 2.9 times higher than that of the flurbiprofen sodium eye drops respectively, which meant that the ocular bioavailability was improved greatly by the novel preparation. Therefore, FBA/NE-ISG can enhance the ocular bioavailability by prolonging drug corneal retention significantly. What's more, encapsulated by emulsion droplets prodrug flurbiprofen (FBA) instead of flurbiprofen (FB) can reduce the ocular irritation.
2.Ion-sensitive nanoemulsion-in situ gel system for ophthalmic delivery of flurbiprofen axetil
Jinqiu SHEN ; Yong GAN ; Li GAN ; Chunliu ZHU ; Jiabi ZHU
Acta Pharmaceutica Sinica 2010;0(01):-
The aim of the study is to prepare flurbiprofen axetil nanoemulsion-in situ gel system (FBA/NE- ISG) and observe its ocular pharmacokinetics, rheological behavior, TEM images, irritation and cornea retention. Production of nanoemulsion was based on high-speed shear and homogenization process, and then mixed with gellan gum to prepare FBA/NE-ISG. Rheological study showed that FBA/NE-ISG possesses strong gelation capacity and its viscosity and elastic modulus increases by 2 Pa?s and 5 Pa respectively when mixed with artificial tear at the ratio of 40∶7. TEM images suggested no significant changes in particle morphology of the pre and post gelation. Good ocular compatibility of FBA/NE-ISG was testified by the irritation test based on histological examination. In vivo fluorescence imaging system was applied to investigate the characteristics of cornea retention, and the results indicated that the nanoemulsion-in situ gel (NE-ISG) prolonged the cornea retention time significantly since KNE-ISG (0.008 5 min-1) was much lower compared with flurbiprofen sodium eye drops (FB-Na, 0.03% w/v) of which the KEye drops was 0.105 2 min-1, indicated that the cornea retention time of NE-ISG was prolonged significantly. Pharmacokinetics of FBA/NE-ISG in rabbit aqueous humor was studied by cornea puncture, the MRT (12.3 h) and AUC0→12 h (126.8 ?g?min?mL-1) of FBA/NE-ISG was 2.7 and 2.9 times higher than that of the flrubiprofen sodium eye drops respectively, which meant that the ocular bioavailabilitywas improved greatly by the novel preparation. Therefore, FBA/NE-ISG can enhance the ocular bioavailability by prolonging drug corneal retention significantly. What’s more, encapsulated by emulsion droplets prodrug flurbiprofen (FBA) instead of flurbiprofen (FB) can reduce the ocular irritation.
3.Ocular pharmacokinetics of dexamethasone cubosomes in rabbit aqueous humor
Li GAN ; Yong GAN ; Jinqiu SHEN ; Jiabi ZHU
Journal of China Pharmaceutical University 2009;40(4):327-331
Aim: To prepare novel cubosome system for effective ocular drug delivery with dexamethasone(DEX) as model drug, and investigate its pharmacokinetic profile in rabbit aqueous humor. Methods: DEX cubosomes was prepared by the method of high-pressure homogenization, and its particle size was determined by the laser particle sizer, and the microstructure observed by cryo-TEM. In addition, Draize method was used to evaluate the ocular irritation of DEX cubosomes. Finally, aqueous humor microdialysis was utilized to evaluate its pharmacokinetics in rabbits. Results: Average diameter of DEX cubosomes was about 200 nm, and the cubic structure of the particles was evident under the cryo-TEM. It was indicated by Draize scores that this dosage form exhibited excellent ocular tolerance. Results of pharmacokinetic profiles in aqueous humor showed that AUC_(0→240) and c_(max) of the rabbit group administered with DEX cubosomes were significantly higher than those of the control group( DEX sodium phosphate eye drops), with AUC_(0→240) of the formulation Fl( 10% oil content) and F2(20% oil content) is being about 1. 8 and 2. 9 times higher than those of the control group, respectively( P <0. 05). Conclusion: The novel ocular drug delivery system of DEX cubosomes was capable of increasing significantly the drug concentration in aqueous humor, and improving the ocular bioavailability.
4.Depression and life satisfaction among residential elderly in Xiamen city,China and Daejeon city, Korea
Yiqiang GUO ; In-Sook PARK ; Benlan YE ; Qu SHEN ; Jinqiu YANG ; Yang LIU
Chinese Mental Health Journal 2018;32(1):49-54
Objective:To compare the differences between Chinese and Korean residential elderly depression status,life satisfaction and relatedfactors in Xiamen China and Daejeon Korea.Methods:A survey was conducted on 201 elder people (≥60 years old) in Xiamen,China and 206 elder ones in Daejeon,Korea.The Geriatric Depression Scale,Life Satisfaction Index-A Scale and self-designed demographic questions were used.Data were analyzed with t-test and multiple stepwise regression analysis.Results:The LSI-A scores were higher in Korean elderly than in Chinese elderly (P <0.05).In Chinese elderly,social activities (β =0.37),living status (β =-0.30) and education level (β =0.16) were associated with GDS scores,and social activity (β =-0.36) and living status (β=0.17) were associated with LSI-A scores.In Korea elderly,health status (β =-0.33),social activity (β =0.24)and living status (β =-0.13) were associated with GDS scores,and health status (β =0.32),social activity (β =-0.15) and living status (β =0.16) were associated with LSI-A scores.Conclusion:It indicates that Korea elderly have better life satisfaction than Chinese elderly.