Characterization, stability, and pharmacokinetics of Sibutramine (cas 106650-56-0)/β-cyclodextrin inclusion complex
-
Add time:08/08/2019 Source:sciencedirect.com
β-Cyclodextrin (β-CD) is widely used to increase the stability, solubility, and bioavailability of poorly soluble drugs because of the appropriate size of its cavity. Sibutramine is a neurotransmitter reuptake inhibitor that has been investigated as an oral anorexiant. Here we report the complexation of sibutramine base with β-CD and the stability, dissolution, and pharmacokinetic properties of the sibutramine/CD complex. The formation of sibutramine/β-CD inclusion complexes is confirmed using differential scanning calorimetry, X-ray diffractometry, and 1H nuclear magnetic resonance. The thermal and photochemical stability of sibutramine is significantly improved by the complexation with β-CD, and the pharmacokinetic parameters (e.g., the plasma concentration, area under the curve, and maximum concentration of two active metabolites) for humans are comparable with those of the commercialized standard product (Reductil®). Our study suggests that sibutramine/β-CD complexation can be of great use to increase the stability and biological efficacy of sibutramine base.
We also recommend Trading Suppliers and Manufacturers of Sibutramine (cas 106650-56-0). Pls Click Website Link as below: cas 106650-56-0 suppliers
Prev:Influence of acute treatment with Sibutramine (cas 106650-56-0) on the sympathetic neurotransmission of the young rat vas deferens
Next:Effects of CYP3A5, CYP2C19, and CYP2B6 on the clinical efficacy and adverse outcomes of Sibutramine (cas 106650-56-0) therapy: A crucial role for the CYP2B6*6 allele) - 【Back】【Close 】【Print】【Add to favorite 】
- Related Information
- Effects of CYP3A5, CYP2C19, and CYP2B6 on the clinical efficacy and adverse outcomes of Sibutramine (cas 106650-56-0) therapy: A crucial role for the CYP2B6*6 allele08/09/2019
- Influence of acute treatment with Sibutramine (cas 106650-56-0) on the sympathetic neurotransmission of the young rat vas deferens08/07/2019
- Detection of Sibutramine (cas 106650-56-0) in adulterated dietary supplements using attenuated total reflectance-infrared spectroscopy08/06/2019
- Sibutramine (cas 106650-56-0) characterization and solubility, a theoretical study08/05/2019
- A simple and fast-portable method for the screening of the appetite-suppressant drug Sibutramine (cas 106650-56-0) in natural products and multivitamins supplements08/04/2019
- Sibutramine (cas 106650-56-0) provokes apoptosis of aortic endothelial cells through altered production of reactive oxygen and nitrogen species08/03/2019
- Sibutramine (cas 106650-56-0), a serotonin–norepinephrine reuptake inhibitor, causes fibrosis in rats08/02/2019
- A rapid ATR-FTIR spectroscopic method for detection of Sibutramine (cas 106650-56-0) adulteration in tea and coffee based on hierarchical cluster and principal component analyses08/01/2019
- Sibutramine (cas 106650-56-0) facilitates apoptosis and contraction of aortic smooth muscle cells through elevating production of reactive oxygen species07/31/2019
-
Health and Chemical more >