Spray-dried Amioca starch/Carbopol 974P mixtures as buccal bioadhesive carriers.
In the present study, spray-dried Amioca starch/Carbopol 974P mixtures were evaluated as potential buccal bioadhesive tablets. Carbopol (C 974P) concentrations from 5 to 75% were tested. All spray-dried mixtures showed a comparable or better bioadhesive capacity compared to a reference formulation (DDWM/C 974P 95/5). The bioadhesive capacities of Amioca/Carbopol 974P mixtures were improved by spray-drying. All spray-dried mixtures showed significantly higher work of adhesion values compared to their equivalent physical mixtures. The influence of Carbopol concentration on the in vivo adhesion time of placebo tablets and in vitro miconazole nitrate release was tested. The ratio Amioca/C 974P 70/30 showed the longest in vivo adhesion time (24.5+/-8.5 h). Lower and higher C 974P concentrations had a shorter in vivo adhesion time. The mixtures containing between 15 and 30% C 974P could all sustain the in vitro miconazole nitrate release over 20 h. Again, lower and higher C 974P concentrations showed a faster in vitro miconazole release. The drug loading capacity of a spray-dried mixture containing 20% C 974P was investigated in vivo in dogs using testosterone as model drug. The spray-dried mixture could be loaded with 60% drug without loosing its in vivo bioadhesive and pharmacokinetic properties.
Ameye
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Laboratory of Pharmaceutical Technology, Ghent University, Harelbekestraat 72, B-9000 Gent, Belgium.
Mus
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D
Foreman
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Remon
J P
JP
D000179:Acrylates / Q000737:chemistry*; D000278:Administration, Buccal; D000818:Animals; D001682:Biological Availability; D002610:Cheek; D002851:Chromatography, High Pressure Liquid; D004285:Dogs; D005079:Excipients / Q000737:chemistry*; D005612:Freeze Drying; D009061:Mouth Mucosa; D012995:Solubility; D013056:Spectrophotometry, Ultraviolet; D013213:Starch / Q000737:chemistry*; D013607:Tablets; D013739:Testosterone / Q000097:blood; D014014:Tissue Adhesives
D000179:Acrylates; D005079:Excipients; D013607:Tablets; D014014:Tissue Adhesives; C117167:carbopol 974P NF; D013739:Testosterone; D013213:Starch