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Sugar-branched-cyclodextrins as injectable drug carriers in mice.
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- Author(s): Shinoda T;Shinoda T; Kagatani S; Maeda A; Konno Y; Hashimoto H; Hara K; Fujita K; Sonobe T
- Source:
Drug development and industrial pharmacy [Drug Dev Ind Pharm] 1999 Nov; Vol. 25 (11), pp. 1185-92.- Publication Type:
Journal Article- Language:
English - Source:
- Additional Information
- Source: Publisher: Informa Healthcare Country of Publication: England NLM ID: 7802620 Publication Model: Print Cited Medium: Print ISSN: 0363-9045 (Print) Linking ISSN: 03639045 NLM ISO Abbreviation: Drug Dev Ind Pharm Subsets: MEDLINE
- Publication Information: Publication: London : Informa Healthcare
Original Publication: New York, Dekker. - Subject Terms:
- Abstract: The purpose of this study was to investigate stable complexation of drug in blood by sugar-branched-beta-cyclodextrins (beta-CDs) such as glucose (glu)- or galactose (gal)-branched-beta-CDs and the pharmacokinetic disposition of drug in sugar-branched-beta-CD complex. Complexation of steroidal drugs in sugar-branched-beta-CDs and their replacement by cholesterol were measured. The complexes of dexamethasone/glucosyl-beta-CDs (dexamethasone/glu-beta-CD or dexamethasone/glu-glu-beta-CD) were not replaced by cholesterol, which is a representative endogenous compound, whereas the complex of dexamethasone/beta-CD was replaced by cholesterol. The same results were obtained in steroidal drugs such as hydrocortisone, triamcinolone, and prednisolone. Thus, the use of glu-beta-CD and glu-glu-beta-CD permitted the stable complexation of the drug in water. Stability constants of dexamethasone/glu-glu-beta-CD and dexamethasone/gal-glu-beta-CD complexes are the same, which means that the sugar moiety of the side chain in beta-CD has little effect on stability constants. After the dexamethasone/gal-glu-beta-CD complex or the dexamethasone/glu-glu-beta-CD complex (dexamethasone: 1 mg/body) was administered intravenously to mice, dexamethasone concentrations in liver tissue and blood were measured. The dexamethasone/gal-glu-beta-CD complex (66.1 +/- 1.7 micrograms as dexamethasone/gram of liver tissue) was distributed to liver tissue significantly more than the dexamethasone/glu-glu-beta-CD (beta-CD) complex (59.9 +/- 1.0 micrograms as dexamethasone/gram of liver) at 30 min after administration (p < .05). Sugar-branched-beta-CD gave a water-soluble and stable complex for dexamethasone and changed the disposition of dexamethasone. Sugar-branched-beta-CDs are potentially excellent carriers for a steroidal injectable formulation.
- Accession Number: 0 (Carbohydrates)
0 (Cyclodextrins)
0 (Drug Carriers)
0 (Steroids)
7S5I7G3JQL (Dexamethasone)
97C5T2UQ7J (Cholesterol) - Publication Date: Date Created: 19991222 Date Completed: 20000111 Latest Revision: 20190921
- Publication Date: 20240104
- Accession Number: 10.1081/ddc-100102286
- Accession Number: 10596356
- Source:
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