Glipizide is used to treat high blood sugar levels caused by a type of diabetes mellitus called type 2 diabetes. It is classified as a second generation sulfonylurea, which means that it undergoes enterohepatic circulation. Mechanism of action is produced by blocking potassium channels in the beta cells of the islets of Langerhans. By partially blocking the potassium channels, the cell remains depolarized, increasing the time the cell spends in the calcium release stage, which results in signaling leading to calcium influx. The increase in calcium will initiate more insulin release from each beta cell. Sulfonylureas may also cause the decrease of serum glucagon and potentiate the action of insulin at the extrapancreatic tissues[3]. Glipizide treatment decreased dilated renal tubule number, improved glomerulus integrity, and reduced inflammatory infiltration. Glipizide blocks renal interstitial fibrosis by inhibiting AKT signaling pathway[4]. Glipizide release from mucoadhesive microcapsules was slow and extended over longer periods of time and depended on composition of the coat. In the in vivo evaluation, alginate-Carbopol microcapsules could sustain the hypoglycemic effect of glipizide over a 14-hour period[5].
Glipizide/格列吡嗪 细胞实验
Cell Line
Concentration
Treated Time
Description
References
DU145 cells
50–200 µM
48 hours or 72 hours
Glipizide showed no significant effect on DU145 cell proliferation
Sci Rep. 2016 Jun 13;6:27819.
PC-3 cells
50–200 µM
48 hours or 72 hours
Glipizide showed no significant effect on PC-3 cell proliferation
Sci Rep. 2016 Jun 13;6:27819.
Glipizide/格列吡嗪 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Dogs
Healthy dogs
Oral
10 mg/day
Once daily for 10 to 20 days
To examine the effects of chronic glipizide treatment on insulin-mediated glucose disposal. Results showed that glipizide treatment significantly increased insulin-mediated overall glucose disposal (Rd) but had no significant effect on insulin suppression of hepatic glucose production (Ra).
J Clin Invest. 1981 Apr;67(4):1016-23
Sprague-Dawley rats and Swiss Albino Mice
STZ-induced diabetic mice model
Oral
2 mg/kg
Single dose (rats) and 28 days continuous administration (mice)
To evaluate the long-term glucose-lowering effect of glipizide microspheres in diabetic models. Results showed that compared to immediate-release formulations, the microspheres provided a more sustained reduction in blood glucose and showed persistent effects even after cessation of treatment.
Saudi Pharm J. 2011 Jul;19(3):143-52
Beagle dogs
Healthy male Beagle dogs
Oral
5 mg
Single dose, with a washout period of one week
Evaluate the impact of particle size on in vivo absorption. Results showed that formulations with API particle sizes in the range of 2–5 μm exhibited similar oral absorption compared to the reference product.
Asian J Pharm Sci. 2019 Mar;14(2):165-173
TRAMP mice ([C57BL/6 × FVB]F1 background)
Spontaneous prostate adenocarcinoma model
Intraperitoneal injection
5 mg/kg
Every three days for 8 weeks
Glipizide significantly suppresses prostate cancer growth and metastasis by inhibiting tumor-induced angiogenesis rather than tumor cell proliferation
Sci Rep. 2016 Jun 13;6:27819.
Wistar rats
Normal and diabetic rat models
Oral
5 mg/kg
7 or 28 days
To evaluate the effects of APE and AND on the pharmacokinetic parameters of glipizide. APE significantly improved the Cmax and AUC0–t/AUC0–∞ values of GLZ in normal and diabetic rats (p < 0.05). AND significantly reduced the bioavailability of GLZ in diabetic rats, as indicated by decreased values of T1/2, Cmax, and AUC0–t/AUC0–∞ (p < 0.05).
China, Beijing
... 展开 >> Beijing Tiantan Hospital
Beijing, Beijing, China, 100050
Xuanwu Hospital Capital Medical University
Beijing, Beijing, China, 100053
Peking Union Medical College Hospital
Beijing, Beijing, China, 100730
China, Chongqing
Southwest Hospital
Chongqing, Chongqing, China, 400038
Daping Hospital
Chongqing, Chongqing, China, 400042
China, Jiangsu
Nanjing General Hospital of Nanjing Military Command
Nanjing, Jiangsu, China, 210002
China, Jilin
Jilin University
Changchun, Jilin, China, 130021
China, Shanghai
Huashan Hospital Fudan University
Shanghai, Shanghai, China, 200040
China, Sichuan
West China Center of Medical Sciences
Chengdu, Sichuan, China, 610041
China, Tianjin
The General Hospital Under Tianjin Medical Sciences University
Tianjin, Tianjin, China, 300052 收起 <<
Diabetes Mellitus Type 2
... 展开 >> Severe Hyperglycemia - Blood Glucose Level >300mg/dl. 收起 <<
Phase 4
Unknown
December 2012
United States, Illinois
... 展开 >>
John Stroger Hospital of Cook County
Not yet recruiting
Chicago, Illinois, United States, 60612
Contact: Ambika Babu, M.D. 312-864-0543 Ambika_Babu@rush.edu
Contact: Leon Fogelfeld, M.D. 312-864-0539 lfogelfe@cchil.org
Principal Investigator: Ambika Babu, M.D.
John Stroger Hospital of Cook County
Recruiting
Chicago, Illinois, United States, 60612
Contact: Ambika Babu, M.D. 312-864-0543 aamblee@hotmail.com
Contact: Leon Fogelfeld, M.D. 312-864-0539 lfogelfe@cchil.org
Principal Investigator: Ambika Babu, M.D. 收起 <<
United States, Minnesota
... 展开 >>
PRACS Institute Ltd.
East Grand Forks, Minnesota, United States, 56721
United States, North Dakota
PRACS Institute, Ltd.
Fargo, North Dakota, United States, 58104 收起 <<
United States, Massachusetts
... 展开 >>
Massachusetts General Hospital
Boston, Massachusetts, United States, 02114
Brigham and Women's Hospital
Boston, Massachusetts, United States, 02116
Joslin Diabetes Center
Boston, Massachusetts, United States, 02116 收起 <<
United States, Minnesota
... 展开 >>
PRACS Institute Ltd.
East Grand Forks, Minnesota, United States, 56721
United States, North Dakota
PRACS Institute, Ltd.
Fargo, North Dakota, United States, 58104 收起 <<
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