์ฝ˜ํ…์ธ ๋กœ ๊ฑด๋„ˆ๋›ฐ๊ธฐ
Merck

Formulation approaches to improving the delivery of an antiviral drug with activity against seasonal flu.

Pharmaceutical development and technology (2013-11-14)
Srinivasa M Sammeta, Li Wang, Shravan K Mutyam, Kathleen O'Loughlin, Carol E Green, Milton H Werner, Terence Kelly, Gita N Shankar
์ดˆ๋ก

The main objective of the present study was to develop formulations of noscapine hydrochloride hydrate with enhanced solubility and bioavailability using co-solvent- and cyclodextrin-based approaches. Different combinations of co-solvents, which were selected on the basis of high-throughput solubility screening, were subjected to in vitro intestinal drug permeability studies conducted with Ussing chambers. Vitamin E tocopherol polyethylene glycol succinate and propylene glycol based co-solvent formulations provided the maximum permeability coefficient for the drug. Inclusion complexes of the drug were prepared using hydroxypropyl-ฮฒ-cyclodextrin and sulphobutylether cyclodextrins. Pharmacokinetic studies were carried out in male Sprague-Dawley rats for the selected formulations. The relative bioavailabilities of the drug with the co-solvent- and cyclodextrin-based formulations were found to be similar.

MATERIALS
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Sigma-Aldrich
Potassium chloride, ReagentPlusยฎ, โ‰ฅ99.0%
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Potassium chloride solution, BioUltra, ~1 M in H2O
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Potassium chloride, BioXtra, ≥99.0%
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Potassium chloride, anhydrous, free-flowing, Redi-Driโ„ข, ReagentPlusยฎ, โ‰ฅ99%
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Potassium chloride, tested according to Ph. Eur.
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Potassium chloride solution, conductance standard A acc. to ISO 7888, 0.1 M KCl
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ISA (ionic strength adjustment solution: 1 M KCl), 1 M KCl
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Potassium chloride solution, conductance standard B acc. to ISO 7888, 0.01 M KCl
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Potassium chloride, puriss., meets analytical specification of Ph. Eur., BP, USP, FCC, E508, 99-100.5% (AT), ≤0.0001% Al
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