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PREPARATION PROCESS FOR ORAL DISSOLVING FILM OF GINKGOLIDE B FOR TREATMENT OF ALZHEIMER'S DISEASE  ( SCI-EXPANDED收录)  

文献类型:期刊文献

英文题名:PREPARATION PROCESS FOR ORAL DISSOLVING FILM OF GINKGOLIDE B FOR TREATMENT OF ALZHEIMER'S DISEASE

作者:Zhou, Juntong[1];Xu, Qinmei[1];Wang, Yue[1,2];Wang, Zhenpeng[3];Li, Jiayang[4,5];Yu, Shan[1];Liu, Kexin[1];Li, Chi[1];Li, Shuhui[1];Zhang, Yuan[1];Qu, Xintong[1];Tian, Ye[1];Feng, Zhaoxuan[1];Huo, Qing[1,2]

第一作者:Zhou, Juntong

通讯作者:Huo, Q[1];Huo, Q[2]

机构:[1]Beijing Union Univ, Biochem Engn Coll, Beijing, Peoples R China;[2]Beijing Key Lab Biomass Waste Resource Utilizat, Beijing, Peoples R China;[3]Chinese Acad Sci, Inst Chem, Beijing, Peoples R China;[4]Natl Ctr Nanosci & Technol China, CAS Key Lab Biomed Effects Nanomat & Nanosafety, Beijing, Peoples R China;[5]Natl Ctr Nanosci & Technol China, CAS Ctr Excellence Nanosci, Beijing, Peoples R China

第一机构:北京联合大学生物化学工程学院

通讯机构:[1]corresponding author), Beijing Union Univ, Biochem Engn Coll, Beijing, Peoples R China;[2]corresponding author), Beijing Key Lab Biomass Waste Resource Utilizat, Beijing, Peoples R China.|[1141726]北京联合大学生物化学工程学院;[11417]北京联合大学;

年份:2020

卷号:36

期号:2

起止页码:1223-1230

外文期刊名:ACTA MEDICA MEDITERRANEA

收录:;Scopus(收录号:2-s2.0-85083346307);WOS:【SCI-EXPANDED(收录号:WOS:000526121600077)】;

基金:This work was financially supported by National Natural Science Foundation of China (Grant No. 11475020 and No. 11975048), project of Chaoyang district collaborative innovation (No. XC1608).

语种:英文

外文关键词:Alzheimer's Disease; oral dissolving film; ginkgolide B; pharmacokinetics

摘要:Objective: Ginkgolide B (GB) has been applied to cardiovascular diseases in clinic with its anti-oxidative and anti-aging effects. GB plays a neuroprotective role in models of various diseases. A study showns that A beta 1-42 induces oxidative damage to the cellular biomolecules, which are associated with AD pathology, and are protected by the pre-treatment of GB against A beta-toxicity. We prepared the oral dissolving film (ODF) of GB by tape casting. The influence of film forming material, plasticizer and defoamer on the performance of the ODF of GB was studied. ODF has better adherence and is easy to take, which provides certain reference value for future nerve agents. Methods: The preparation parameters were as follows: 35mg GB was dissolved with 70ml of distilled water and mixed well, which was followed by the addition of 0.5g of glycerol as the plasticizer. After complete dissolution, 2g of hydroxypropyl methylcellulose was added as the film forming material. An ODF solution was formed by mixing, during which two to three drops of edible defoamer were added. After defoaming, the solution was coated onto the carrier sheet and left to stand until complete drying. Then the film was cut into a proper size. Results: Experiments showed that the ODF of GB could completely dissolve in 280s and 80% of GB was released in 1min. The degree of release reached100% in 3min. This drug was pasted onto the supralingual area of 0.6x1.3min with a single dose of 1mg/kg for the rats. Pharmacokinetic parameters were measured, and the clearance rate CL (Llh ) was calculated as 2.156, Cmax (ng.mL(-1)): 13.52, Tmax: 4h. Conclusion: The AUC for the ODF of GB was larger by about 1.77-fold as compared with the intragastric administration of GB. The bioavailability of ODF of the drug was higher than other conventional oral preparations.

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