- HYPERSULFATED GLUCOPYRANOSIDES
-
Hypersulfated disaccharides, preferably octasulfated sucrose, with utility in asthma or asthma related disorders are disclosed. The compounds may optionally be formulated with pharmaceutically acceptable excipients or delivery agents. The delivery agents are selected from the group consisting of natural or synthetic polymers, aerosols or other vehicles that facilitate the delivery or administration of the drug. The hypersulfated disaccharides are made from carbohydrate starting materials. Ion exchange or other suitable synthetic processes may be utilized to prepare the pharmaceuticals. The hypersulfated disaccharides are useful as anti-inflammatory agents.
- -
-
Page/Page column 10; 11
(2011/10/13)
-
- Tissue distribution of [14C]sucrose octasulfate following oral administration to rats.
-
PURPOSE: Aluminum sucrose octasulfate (SOS) is used clinically to prevent ulcers. Under physiologic conditions, the sodium salt of this drug can be formed. Our objective was to determine whether sodium SOS was absorbed when administered orally. In addition to furthering our understanding of aluminum SOS, this study also aimed to clarify how other polyanionic drugs, such as heparin and low-molecular-weight heparins, are absorbed. METHODS: [14C]-labeled and cold sodium SOS (60 mg/kg) were given to rats by stomach tube. Radioactivity was counted in gut tissue, gut washes, and nongut tissue (i.e., lung, liver, kidney, spleen, endothelial, and plasma samples) at 3 min, 6 min, 15 min, 30 min, 60 min, 4 h, and 24 h, and in urine and feces accumulated over 4 h and 24 h. RESULTS: Peak radioactivity was found in the tissue and washes of the stomach, ileum, and colon at 6 min, 60 min, and 4 h, respectively, showing progression through the gut. Gut recovery accounted for 84% of the dose at 6 min but only 12% of the dose at 24 h, including counts from feces. Radioactivity was recovered from nongut tissue (averaging 8.6% of the dose) and accumulated urine (18% of the dose at 24 h). When total body distribution was considered, the recovery of radioactivity was greater for the endothelium than for plasma (peak percentage of the dose was 65% at 15 min, 20% at 3 min, 5% from 20 to 240 min for the vena cava, aortic endothelium, and plasma, respectively). CONCLUSIONS: Results indicate that sodium SOS is absorbed, agreeing with previous studies demonstrating the oral absorption of other sulfated polyanions. Endothelial concentrations must be considered when assessing the pharmacokinetics of these compounds. The measured plasma drug concentrations reflect the much greater amounts of drug residing with the endothelium.
- Hiebert, Linda M,Wice, Sandra M,Ping, Tidly,Hileman, Ronald E,Polat, Tfilay,Linhardt, Robert J
-
p. 838 - 844
(2007/10/03)
-
- Method for preparing high potency sucralfate
-
Sucralfate is prepared in good yields and in newly useful form first by reacting sucrose with chlorosulfonic acid in 2-picoline. The amonium salt is then formed and reacted with aluminum chlorohydrate in specific sequence and alcoholic solvent. The two distinct products have unexpected pharmaceutical and physical characteristics. The oral liquid suspensions also must be critically formulated.
- -
-
-
