平其能
长期致力口服药物缓释及控释剂型研究、微粒给药系统研究透皮给药研究、难溶性药物剂型及制剂研究、药物给药途径及吸收研究等。
个性化签名
- 姓名:平其能
- 目前身份:
- 担任导师情况:
- 学位:
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学术头衔:
博士生导师
- 职称:-
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学科领域:
药剂学
- 研究兴趣:长期致力口服药物缓释及控释剂型研究、微粒给药系统研究透皮给药研究、难溶性药物剂型及制剂研究、药物给药途径及吸收研究等。
平其能,1946年8月生,教授、博士生导师,中国药科大学药学院院长。中国药学会理事兼药剂专业委员会副主任、江苏省药学会常务理事兼药剂专业委员会主任、中国军事医学科学院药物与毒物研究所客座教授,国家新药审评专家以及英国"药学与药理学杂志"(Journal of Pharmacy and Pharmacology)、美国非胃肠给药协会(PDA)"PDA药学科学与技术杂志"(PDA Journal of Pharmaceutical Science and Technology)、"药学学报""中国药学杂志"、"中国药学(英文版)"、"中国新药杂志"、"中国新药与临床"、"中国药科大学学报"等国内外药学刊物编委。曾任国家自然科学基金委员会生命科学部评审委员、江苏省学位委员会委员。
1993年起享受国务院颁发政府特殊津贴。1995年获得吴阶平-保罗.杨森医药学研究三等奖。1995年获国家人事部和国家教委颁发"全国优秀教师"荣誉称号和奖章。2001年主持的"药剂学教学改革新体系的建设"获江苏省教育厅优秀教学成果一等奖,国家教育部优秀教学成果二等奖。2002年获江苏省优秀博士生导师称号。1999年主编"现代药剂学"荣获国家科技进步奖(图书类)二等奖。2001年主持的国家"九五"攻关项目"液体缓控释制剂技术研究" 和承担的"生脉散细粒剂研究"获国家教育部科技成果证书(分别排名第一和第三)。1996"事后避孕药"项目研究获国家计划生育委员会颁发"科研工作表彰荣誉证书"。24小时盐酸曲马多缓释片(2001)并通过重庆市主持科技成果鉴定(2003)和取得科技成果证书。
长期致力口服药物缓释及控释剂型研究、微粒给药系统研究透皮给药研究、难溶性药物剂型及制剂研究、药物给药途径及吸收研究等。主持研究国家自然科学基金重点项目2项、面上项目、教育部科技重点项目及江苏省自然科学基金重点项目各1项,主持完成国家自然科学基金面上项目3项。国家七五、八五、九五攻关项目4项和863项目2项,国家新药基金项目2项。编著、主编出版"药剂学实验与指导"(中国医药科技出版社,1992)、"药用聚合物的理论和实践"(中国医药科技出版社,1994)、"现代药剂学"(中国医药科技出版社,1998)、"药剂学发展与展望"(化学工业出版社,2002),"制剂工程学"(电子教材,南京大学出版社,2003),副主编"药剂学"(参考书,人民卫生出版社,2003)。参编"药剂学"(人民卫生出版社,第4版,1998)、"药剂学"(中国医药科技出版社,第1版,2003),"药用高分子材料学"(中国医药科技出版社,1992,2000)和"经皮给药制剂"(中国医药科技出版社,1992)等。参编"国家药物制剂发展指南"第一辑、第二辑、第三辑。在国内外刊物发表论文200余篇。9个药物制剂取得国家新药证书并取得重要经济社会效益。
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成果数
8
【期刊论文】Chitosan-coated liposomes: characterization and interaction with leuprolide
平其能, J. Guoa, b, Q. Ping a, *, G. Jiang b, L. Huanga, Y. Tong a
International Journal of Pharmaceutics 260(2003)167-173,-0001,():
-1年11月30日
The objective of the present work was to investigate the effect of chitosan concentration and lipid type on the characteristics of chitosan-coated liposomes and their interactions with leuprolide. Liposomes from lipid of high purity and low purity were prepared and coated by chitosan. Physical properties, drug entrapment efficiency, and stability upon dilution were respectively compared. Results showed that the particle size increment of liposomes from low purity lipid was larger than that from high purity lipid, indicating a thicker coating layer. The high zeta potential of particles from low purity lipid was thought to play an important role in the resistance to flocculation. As to particles from high purity lipid, polymer bridging caused flocculation at low polymer concentration while at high concentration, the adsorbed chitosan molecule led to steric stabilization. Drug entrapment efficiency decreased as chitosan was added to liposomes, showing the disturbance of bilayers. Upon dilution, the leakage of leuprolide from low purity liposomes was larger than that from high purity liposomes. In conclusion, low purity lipid possessed more negative charge and formed thicker adsorptive layer by stronger electrostatic attraction with chitosan. The interaction between chitosan and the polar head groups on the surface of phospholipid bilayers may interfere with leuprolide entrapped in liposomes and result in the leakage of leuprolide.
Chitosan-coated liposomes, Leuprolide, Characterization, Flocculation, Interaction
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【期刊论文】The absorption behavior of cyclosporin A lecithin vesicles in rat intestinal tissue
平其能, Ying Chen, Qineng Ping*, Jianxin Guo, Wenli Lv, Jing Gao
International Journal of Pharmaceutics 261(2003)21-26,-0001,():
-1年11月30日
The purpose of the study was to investigate the absorption behavior of lecithin vesicles of cyclosporin A (CsA-VES), prepared by the rotary evaporation method and treated further with sonication. The everted gut sac technique and in situ circulation method were used to examine: (1) relationship between the CsA-VES absorption velocity and the CsA-VES content; (2) the influence of the intestinal mucus, blank vesicles, concentration of Na+, energy inhibitor and P-gp inhibitor on the absorption of CsA-VES; and (3) the respective accumulated content of CsA in the incubating medium and the sacs after incubation with Sandimmum Neoral
Lecithin vesicles, Cyclosporin A, Everted gut sac technique, In situ circulation method, Absorption behavior
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【期刊论文】Hypoglycemic efficacy of chitosan-coated insulin liposomes after oral administration in mice1
平其能, Zheng-hong WU, Qi-neng PING, Yi WEI, Jia-ming LAI
,-0001,():
-1年11月30日
AIM: To evaluate the hypoglycemic efficacy of insulin liposomes coated by chitosan with different molecular weights and concentrations after oral administration in mice. METHODS: Insulin-liposomes were prepared by reversed-phase evaporation. Chitosan coating was carried out by incubation of the liposomal suspensions with the chitosan solution. The hypoglycemic efficacies of chitosan-coated insulin liposomes were investigated by monitoring the blood glucose level using the glucose oxidase method after oral administration to healthy mice. RESULTS: In all the insulin liposomes, the insulin liposomes coated by 0.2% chitosan (Mr 1000 kDa) showed a better hypoglycemic efficacy as compared with the other liposomes coated by chitosan. The minimum blood glucose level was 15.1%
chitin, chitosan, insulin, liposomes, blood glucose, oral administration
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【期刊论文】Transport of leuprolide across rat intestine, rabbit intestine and Caco-2 cell monolayer
平其能, J. Guoa, Q. Ping a, *, G. Jiang b, J. Donga, S. Qia, L. Feng a, Z. Lic, C. Lic
International Journal of Pharmaceutics 278(2004)415-422,-0001,():
-1年11月30日
The purpose of this study was to investigate the transport mechanisms and causes of low bioavailability of leuprolide. The everted gut sac technique and Caco-2 cell monolayer were used to examine: (1) transport properties, enzyme degradation and apparent permeation coefficient (Papp); (2) the influence of trypsin inhibitor, EDTA, chitosan and alginate on drug transport; and (3) the effect of animal species on the intestinal transport. Results showed flux increased with increasing concentration of drug, showing a passive diffusion pathway. The enzyme degradation in rabbit gut was the highest. The Papp of (4.19±1.33)×10-5cm/s in rat gut was the largest and the Papp of (5.20±0.20)×10−7cm/s in Caco-2 cell the smallest. At a low concentration of drug, trypsin inhibitor had strong enhancement effect on the Papp by protecting enough drug for permeation. Chitosan had no effect on the activity of α-chymotrypsin. The increase in Papp was due to opening of the tight junctions and interaction with cells. In conclusion, both inhibition of proteolytic enzymes and opening the tight junctions to allow for paracellular transport improved the intestinal absorption. At low drug concentration, reduction of enzyme degradation is the most important factor.
Leuprolide, Transport, Trypsin inhibitor, Chitosan, Everted gut sac technique, Caco-2 cell
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平其能, 吕文莉, 郭健新, 平其能*
,-0001,():
-1年11月30日
目的:制备灯盏花素脂质体并测定其包封率等理化性质。方法:采用薄膜蒸发法和冷冻干燥法制备灯盏花素脂质体。冻干品水合后,RP-HPLC法测定脂质体含量;并用透析法结合紫外分光光度法测定其包封率;利用马尔文测定仪测定脂质体的粒径、Zeta电位;并考查脂质体胶体溶液在0.9%氯化钠注射液中的释放度。结果:脂质体的载药量为20.%±0.88% (n=3),包封率为81.1%±1.1%(n=3);冻干脂质体再分散后的粒径为50±12nm(n=3),Zeta电位为-24±9mV(n=3);脂质体胶体溶液在氯化钠注射液中2h的释放度为17.2%±0.8%(n=3),8h的释放度为26.1%±0.7%(n=3),24h的释放度为29.9%±0.8%(n=3)。结论:灯盏花素脂质体的载药量和包封率较高,粒径在纳米大小范围,可望实现体内的长循环和靶向给药。
灯盏花素, 脂质体, 包封率, 透析
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【期刊论文】酪蛋白和鱼精蛋白对胰岛素酶降解和口服降血糖作用的影响
平其能, 祁荣, 平其能*, 徐瑞阳, 石勇平
药学学报Acta Pharmaceutica Sinica 2004, 39(10): 844-848,-0001,():
-1年11月30日
目的 研究酪蛋白和鱼精蛋白对酶降解胰岛素(INS)的保护作用及对大鼠灌胃给予INS溶液和微球后降血糖作用的影响。方法 采用:HPI止法测定α-糜蛋白酶和胰蛋白酶溶液中INS的残余量+考察酪蛋白和鱼精蛋白对体外酶陴解INS的保护作用;制各INS溶液及肠溶傲球。在促吸荆N-[8-(2-羟基苯甲酰幕)氮基]辛酸钠(SNAC)存在下,太鼠灌胃给药研究酷蛋白和鱼精蛋白单独腰合并使用对INS溶液和徽球降血糖作用的影响。结果 酪蛋白对α-糜蛋白酶体外降解INS有较好的抑制作用,鱼精蛋白不能抑制α-靡蛋白酶对INS的降解,但对胰蛋白酶降解INS的抑制作用忧于酪蛋白。鱼精蛋白和酪蛋白均可增加I№溶液和肠溶微球的降血糖作用,两者台用嫂果更佳。在SNAC、鱼精蛋白和酪蛋白存在下。INS肠溶豫球比INS籍液有更强而持久的降血糖作用。结论 酪蛋白和鱼精蛋白可通过竞争性与酶结音机制增加INS在肠道消化酶中的稳定性。对INS口服吸收有利。
酪置白, 鱼精置白, 胰岛索, α-靡蛋白酶, 胰蛋白酶, N-[8-(, 2-羟基苯甲酰基), 氨基]辛酸钠, 肠溶散球
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【期刊论文】新型两亲性N-辛基-N-PEG化壳聚糖衍生物的合成与表征
平其能, 张灿, 丁娅, 平其能*
中国乐科大学学报,2005,36(3):201~204,-0001,():
-1年11月30日
目的:制备新型的两亲性N-辛基-N-PEG化壳聚糖衍生物。方法:以天然聚合物壳聚糖为原料,其2-NH-与辛醛形成Schiff's碱,用KBH4还原得到N-辛基壳聚糖,然后在其剩余2-NH-与MeO-PEG-CHO反应,再用KBH4还原制备了N-辛基-N-PEG化壳聚糖衍生物,结构经FTIR、13CNMR、1HNMR得到了表征。用DSC实验对其物理性质进行了分析。结果与结论:制得了新型的辛基、PEG取代度分别为36,64%的两亲性N-辛基-N-PEG化壳聚糖衍生物,有望作为难溶性药物增溶的载体。
壳聚糖, 两亲性, 聚合物胶束, 合成
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【期刊论文】Investigation of lectin-modified insulin liposomes as carriers for oral administration
平其能, Na Zhang a, Qi N. Ping b, Gui H. Huanga, Wen F. Xu a, *
International Journal of Pharmaceutics 294(2005)247-259,-0001,():
-1年11月30日
The aim of this study was to design and characterize lectin-modified liposomes containing insulin and to evaluate the potential of these modified colloidal carriers for oral administration of peptide and protein drugs. Wheat germ agglutinin (WGA), tomato lectin (TL), or Ulex europaeus agglutinin 1 (UEA1) were conjugated by coupling their amino groups to carbodiimideactivated carboxylic groups of N-glutaryl-phosphatidylethanolamine (N-glut-PE). Insulin liposomes dispersions were prepared by the reverse-phase evaporation technique and modified with the lectin-N-glut-PE conjugates. Lectin-modified liposomes were characterized according to particles size, zeta potential and entrapment efficiency. The hypoglycemic effect indicated by pharmacological bioavailability of insulin liposomes modified with WGA, TL and UEA1 were 21.40, 16.71 and 8.38% in diabetic mice as comparison with abdominal cavity injection of insulin, respectively. After oral administration of the insulin liposomes modified with WGA, TL and UEA1 to rats, the relative pharmacological bioavailabilities were 8.47, 7.29 and 4.85%, the relative bioavailability were 9.12, 7.89 and 5.37% in comparison with subcutaneous injection of insulin, respectively. In the two cases, no remarkable hypoglycemic effects were observed with the conventional insulin liposomes. These results confirmed that lectin-modified liposomes promote the oral absorption of insulin due to the specific-site combination on GI cell membrane.
Wheat germ agglutinin, Tomato lectin, Ulex europaeus agglutinin 1, Insulin, Liposomes, Oral administration
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