Objective To investigate the clinical curative effect and security of Kanglaite injection in combination with low power ultrasound microbubble agents (cavitation) in the treatment of vascular embolization therapy.Methods Thirty-eight patients with abdominal malignant tumor,in accordance with the random number table,were divided into two groups:treatment group (Kanglaite combined with ultrasonic cavitation,21 cases) and control group (Kanglaite,17 cases).Intravenous drip with Kanglaite injection for 21 days,200 ml per day.Ultrasonic cavitation therapy treatment for three weeks,5 days a week and once a day.Tumors size,Karnofsky score,grade of the degree of pain and blood biochemical indicator detection were measyred before and after treatment.Results There was no complete remission,4 cases with partial remission,10 cases with stable disease in the treatment group,and the clinical benefit rate was 66.7％ (14/21).There was no complete remission,1 case with partial remission,3 cases with stable diseasein in control group,and the clinical benefit rate was 23.5％ (4/17).The treatment group was better than control group in clinical benefit rate (66.7％ ∶ 23.5％),pain improvement (76.2％ ∶ 41.2％),Karnofsky score [(66.67 ± 5.77) ∶ (82.86 ± 6.44);(64.12 ±5.07) ∶ (69.41 ±6.59)],and one year survival rate (57.1％ ∶23.5％) (x2 =7.012,P =0.008;x2 =4.821,P=0.028;t=4.575,P＜0.001;x2 =4.354,P=0.037).Conclusion Kanglaite injection in combination with cavitation shows higher clinical efficient,tolerated adverse recations,and significant improvement of quality of life.

Objective To prepare asenapine maleate microemulsion gel(ASPM-Emulgel)and evaluate its brain targeting by nasal administration.Methods The prescription composition and dosage of asenapine maleate microemulsion(ASPM-Emul)was determined according to the equilibrium solubility of asenapine maleate(ASPM)in different oils,emulsifiers,co-emulsifiers and the compatibility results of excipients,and ASPM-Emul was prepared into a gel with carbomer 940 as the gel matrix.The particle size distribution and microstructure of ASPM-Emul were investigated.The in vitro release rates and permeability in sheep nasal mucosa of ASPM-Emul and ASPM Emulgel were compared using the Franz diffusion cell method.The nasal ciliary toxicity of ASPM-Emulgel was investigated using the in vivo toad maxillary model method.Brain targeting of ASPM-Emulgel by nasal administration in rats was evaluated.Results According to the results of equilibrium solubility and compatibility,Maisine 35-1,Tween 80 and Transcutol P were selected as the oil phase,emulsifier and co-emulsifier of ASPM-Emul,respectively,with the ratio of 4 ∶ 4 ∶ 2.ASPM-Emul was a light blue semi-transparent microemulsion with a particle size of(73.6±7.4)nm.The microemulsion was regularly spherical and uniformly dispersed under transmission electron microscopy.The results of in vitro release and permeation showed that the release rate of ASPM-Emul was relatively fast,while the release rate of ASPM-Emulgel remained stable.However,the permeability of the two formulations in sheep nasal mucosa was basically similar.ASPM-Emul and ASPM-Emulgel showed no significant toxicity to nasal cilia of toad.Compared with the tail vein ASPM group,the drug content in the brain of ASPM-Emul and ASPM-Emulgel significantly increased after nasal administration,both exhibiting significant brain targeting,and the drug targeting efficiency(DTE)of ASPM-Emulgel was higher.Conclusion The preparation of ASPM into microemulsion gel can significantly improve the brain targeting after nasal administration,and is expected to improve the clinical therapeutic effect of ASPM.