scholarly journals Single- and Multiple-Dose Pharmacokinetics of a Novel Tetramethylpyrazine Reservoir-Type Transdermal Patch versus Tetramethylpyrazine Phosphate Oral Tablets in Healthy Normal Volunteers, and in Vitro/in Vivo Correlation

2013 ◽  
Vol 36 (6) ◽  
pp. 931-937 ◽  
Author(s):  
Teng Shen ◽  
Huinan Xu ◽  
Weiyu Weng ◽  
Jianfang Zhang
2018 ◽  
pp. e4459 ◽  
Author(s):  
Liangyu Xia ◽  
Shunchen Qiu ◽  
Zhenqi Liu ◽  
Meiying Ning

2007 ◽  
Vol 337 (1-2) ◽  
pp. 88-101 ◽  
Author(s):  
Ji-Hui Zhao ◽  
Ji-Hua Fu ◽  
Shu-Ming Wang ◽  
Chang-Hai Su ◽  
Ying Shan ◽  
...  

1987 ◽  
Vol 21 (6) ◽  
pp. 514-517 ◽  
Author(s):  
James J. Heusner ◽  
George E. Dukes ◽  
Douglas E. Rollins ◽  
Keith G. Tolman ◽  
Raymond E. Galinsky

Ketoconazole, a nitrogen-substituted imidazole, has been shown to be a potent in vitro inhibitor of cytochrome P-450-mediated metabolic processes. Conflicting reports exist concerning the in vivo effect of ketoconazole on concomitantly administered drugs that require these metabolic processes for clearance. Therefore, the effect of multiple-dose ketoconazole on the elimination of theophylline, a drug metabolized by cytochrome P-450, in ten healthy, nonsmoking males (aged 18–40 years) was evaluated. Each subject received aminophylline 6 mg/kg iv before and at the end of seven days of ketoconazole 200 mg/d po. Theophylline serum concentrations were determined by fluorescence polarization immunoassay (TDx) at 12 time points over the 24-hour period following each infusion. No statistical difference (two-tailed t-test) in half-life (mean ± SD 7.8 ± 1.8 vs. 8.2 ± 1.9 h) or clearance (0.797 ± 0.201 vs. 0.722 ± 0.133 ml/min/kg) could be demonstrated for theophylline before or after ketoconazole administration. Theophylline dosage adjustment is probably not necessary for concomitant theophylline and ketoconazole drug therapy.


2009 ◽  
Vol 382 (1-2) ◽  
pp. 165-171 ◽  
Author(s):  
Yinghua Sun ◽  
Liang Fang ◽  
Meng Zhu ◽  
Wei Li ◽  
Ping Meng ◽  
...  

2020 ◽  
Vol 11 (SPL4) ◽  
pp. 997-1005
Author(s):  
Kondapuram Parameshwar ◽  
Suvendu Kumar Sahoo ◽  
Rabinarayan Parhi ◽  
Ravi Kumar V ◽  
Ahad Ahmed kodipad ◽  
...  

The prime objective behind this investigation was to plan a Letrozole enclosed adhesive transdermal patch; since the transdermal route is an outright attractive option concerning its route, convenience and safety. Letrozole, a non-steroidal type II aromatase inhibitor, is reported for treating breast tumours and in postmenopausal women. In this study, few factors confined to formulation such as drug-in-adhesive, enhancers and amount of drug-loaded were investigated. The procedure used supposedly involves, the incarnation of the LET in phospholipids exploiting to a spray dryer. FTIR, X-RD, and DSC techniques which are used to evaluate entrapment efficiency were employed to LET spray-dried powder (LT-SDP). The molecule size, polydispersity file, and the EE were allegedly found to be 284.0 nm, 0.247 and 59.08%. On adding LT-SDP to a cream base with peppermint and olive oil as regular infiltration, the optimized formulation showed superior skin targeting in both in vitro and in vivo observations post-study.In vivo bioavailability studies showed just about four-fold increment in the plasma whereas the mean residence time and half-life were reasonably higher as compared to the LET cream in plain. The in vivo results observed remarkable patch concurrence with the plasma fixations anticipated from the in vitro infiltration. As an outpatient convenience, avoidance of gastrointestinal incompatibility provides suitability for self-administration for breast cancer prevention and treatment.


1973 ◽  
Vol 30 (03) ◽  
pp. 597-601 ◽  
Author(s):  
Peter C. Ungaro ◽  
Thomas M. Beck ◽  
William M. McCaa ◽  
Edward J. Hershgold

SummaryThe effect of antihistamines on platelet aggregation was studied by examining the platelet rich plasma of subjects taking three representative classes of these drugs, as well as by studying the effect of direct addition of antihistamine to platelet rich plasma. Inhibition of aggregation by in vitro addition was obtained only with drug concentrations much greater than would usually be found in vivo. Platelet aggregation was unimpaired in normal volunteers taking standard doses of antihistamines.


2017 ◽  
Vol 12 (2) ◽  
Author(s):  
Kalpana G. Patel ◽  
Vaishali T. Thakkar ◽  
Kartik H. Dudhat ◽  
Mitesh H. Motisariya ◽  
Purvi A. Shah ◽  
...  

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