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

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
초록

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-β-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
Product Number
브랜드
제품 설명

Propylene glycol, European Pharmacopoeia (EP) Reference Standard
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Potassium chloride solution, conductance standard C acc. to ISO 7888, 0.001 M KCl
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(±)-α-Tocopherol, tested according to Ph. Eur.
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(±)-α-Tocopherol, analytical standard
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Alpha Tocopherol, Pharmaceutical Secondary Standard; Certified Reference Material
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(±)-α-Tocopherol, synthetic, ≥96% (HPLC)
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Potassium chloride, ReagentPlus®, ≥99.0%
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Potassium chloride solution, BioUltra, ~3 M in H2O
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Potassium chloride solution, conductance standard B acc. to ISO 7888, 0.01 M KCl
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Phosphate Standard for IC, TraceCERT®, 1000 mg/L phosphate in water (nominal concentration)
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Boric acid-11B, ≥99 atom % 11B
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Sodium phosphate dibasic solution, BioUltra, 0.5 M in H2O
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Sodium hydroxide, BioXtra, ≥98% (acidimetric), pellets (anhydrous)
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Sodium hydroxide solution, 49-51% in water, eluent for IC
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Sodium hydroxide, puriss., meets analytical specification of Ph. Eur., BP, NF, E524, 98-100.5%, pellets
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Sodium hydroxide solution, 50% in H2O
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Sodium hydroxide, reagent grade, 97%, flakes
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Sodium hydroxide solution, 5.0 M
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Glycerol solution, 83.5-89.5% (T)
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Glycerin, United States Pharmacopeia (USP) Reference Standard
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Glycerin, Pharmaceutical Secondary Standard; Certified Reference Material
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Sodium hydroxide concentrate, 0.1 M NaOH in water (0.1N), Eluent concentrate for IC
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Sodium hydroxide, reagent grade, ≥98%, pellets (anhydrous)
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Sodium hydroxide, BioUltra, ≥98.0% (T), pellets
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Sodium hydroxide, ACS reagent, ≥97.0%, pellets
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Sodium hydroxide, pellets, semiconductor grade, 99.99% trace metals basis
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Propylene glycol, United States Pharmacopeia (USP) Reference Standard
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Propylene Glycol, meets USP testing specifications
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Sodium hydroxide, anhydrous, free-flowing, Redi-Dri, reagent grade, ≥98%, pellets
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Sodium hydroxide solution, 1.0 N, BioReagent, suitable for cell culture