Lu J.,China Pharmaceutical University |
Kan S.,Jiangsu Aosaikang Pharmaceutical Co. |
Zhao Y.,China Pharmaceutical University |
Zhang W.,China Pharmaceutical University |
Liu J.,China Pharmaceutical University
Drug Development and Industrial Pharmacy | Year: 2016
The purpose of this study was to develop the novel naproxen/esomeprazole magnesium compound pellets (novel-NAP/EMZ) depending on EMZ acid-independent mechanism which has been proved to be predominate in the mechanism of co-therapy with nonsteroidal anti-inflammatory drug. The novel-NAP/EMZ compound pellets, composed of NAP colon-specific pellets (NAP-CSPs) and EMZ modified-release pellets (EMZ-MRPs), were prepared by fluid-bed coating technology with desired in vitro release profiles. The resulting pellets were filled into hard gelatin capsules for in vivo evaluation in rats and compared with the reference compound pellets, consisted of NAP enteric-coated pellets (NAP-ECPs) and EMZ immediate-release pellets (EMZ-IRPs). The reference compound pellets were prepared simulating the drug delivery system of VIMOVO®. In vivo pharmacokinetics, EMZ-MRPs had significantly larger AUC0– t (p < 0.01), 1.67 times more than that of EMZ-IRPs, and prolonged mean residence time (7.55 ± 0.12 h) than that of IRPs (1.46 ± 0.39 h). NAP-CSPs and NAP-ECPs showed similar AUC0– t. Compared to the reference compound pellets, the novel-NAP/EMZ compound pellets did not show distinct differences in histological mucosal morphology. However, biochemical tests exhibited enhanced total antioxidant capacity, increased nitric oxide content and reduced malondialdehyde level for novel-NAP/EMZ compound pellets, indicating that the acid-independent action took effect. The gastric pH values of novel-NAP/EMZ compound pellets were at a low and stable level, which could ensure normal physiological range of human gastric pH. As a result, the novel-NAP/EMZ compound pellets may be a more suitable formulation with potential advantages by improving bioavailability of drug and further reducing undesirable gastrointestinal damages. © 2016 Taylor & Francis Source
Dong J.,China Pharmaceutical University |
Gong Y.,China Pharmaceutical University |
Liu J.,China Pharmaceutical University |
Chen X.,Jiangsu Aosaikang Pharmaceutical Co. |
And 2 more authors.
Bioorganic and Medicinal Chemistry | Year: 2014
All eight stereoisomers of saxagliptin have been synthesized and evaluated for their inhibitory activity against DPP-IV. It was unambiguously confirmed that the configuration of saxagliptin was critical to potent inhibition of DPP-IV. Docking study was performed to elucidate the configuration-activity relationship of saxagliptin stereoisomers. Tyr662 and Tyr470 have been suggested as the key residues of DPP-IV interacting with the inhibitors. This work provides valuable information for further inhibitor design against DPP-IV. © 2014 Elsevier Ltd. All rights reserved. Source
Jiangsu Aosaikang Pharmaceutical; Co. | Date: 2012-10-24
Medicines for human purposes for the treatment of gastrointestinal diseases; dietetic food preparations, namely, crackers adapted for medical purposes; tonics medicine for human purposes for the treatment of gastrointestinal diseases; milk powder for infants; dental lacquer; disinfecting paper tissue impregnated with disinfecting chemicals or compounds therefor for use on railings, countertops and toilet seats; first aid kits; depuratives for the body; preparations for destroying vermin. Chemical research; cosmetic research; chemical analysis; chemistry services, namely, laboratory analysis in the field of chemistry; biological research; bacteriological research; new product research and development for others; industrial design; computer software consultancy. Health care; physical therapy; pharmaceutical advice; services of a psychologist, namely, psychological counseling; guidance on diet nutrition; landscape gardening; animal breeding; pharmacists services to make up prescriptions; health spa services, namely, health spa services for health and wellness of the body and spirit; telemedicine services.
Chen X.-F.,Jiangsu Aosaikang Pharmaceutical Co. |
Ma J.-J.,Jiangsu Aosaikang Pharmaceutical Co.
Chinese Journal of New Drugs | Year: 2011
As a new generation of anti-cancer drugs, bendamustine has an obvious effect on a wide range of cancers. The clinical practice indicated that its monotherapy or combination therapy has a curative effect on non-Hodgkin's lymphoma, multiple myeloma, chronic lymphocytic leukemia and breast carcinoma. Besides, bendamustine significantly reduces the relapse rate and mortality with lower adverse reactions. It is safe and worthy of a wide use for cancer patients. This article summarized its pharmacology and the clinical research. Source
Zhao J.,Jiangsu Aosaikang Pharmaceutical Co. |
Ma J.-J.,Jiangsu Aosaikang Pharmaceutical Co.
Chinese Journal of New Drugs | Year: 2012
Miriplatin is a third-generation platinum compound developed to treat hepatocellular carcinoma (HCC). It is administered via the hepatic artery using the carrier lipiodol that consists of ethyl esters of iodized poppy seed oil. Miriplatin has a high affinity for lipiodol and it is anticipated to exert antitumor effects with prolonged retention along with local lipiodol at the tumor site. Therefore, it is suggested that the active compound released from miriplatin/lipiodol can bind to DNA and produce a cytotoxic effect. The clinical research shows that miriplatin has beneficial curative effect and safety in the treatment of hepatocellular carcinoma. This article will summarize its pharmacology, pharmacokinetics, clinical research, and safety evaluation. Source