跳转至内容
Merck
  • Microbeads: a novel multiparticulate drug delivery technology for increasing the solubility and dissolution of celecoxib.

Microbeads: a novel multiparticulate drug delivery technology for increasing the solubility and dissolution of celecoxib.

Pharmaceutical development and technology (2013-11-29)
Bernard F McDonald, Ivan S Coulter, Ian W Marison
摘要

The purpose of this study was to develop a novel multipaticulate drug delivery technology suitable for the delivery of pre-solubilized celecoxib to the gastrointestinal tract and more specifically to the colon. The solubility of celecoxib in a range of oils, surfactants and co-solvents was evaluated. Celecoxib was solubilized in mixtures of these vehicles to produce liquid formulations. The in vitro dissolution of these liquid formulations was assessed and the data obtained was used to design microbead formulations containing celecoxib dissolved within an emulsion/micellar solution core. Microbead formulations were optimized to increase drug loading, avoid precipitation and to achieve good in vitro dissolution performance. An optimized formulation with a celecoxib loading of 6% w/w was produced and yielded an in vitro dissolution result of 80% over 6 h. The structure of these microbead formulations was characterized using light microscopy to reveal a correlation between droplet size and dissolution performance.

材料
货号
品牌
产品描述

Sigma-Aldrich
十二烷基硫酸钠, BioReagent, suitable for electrophoresis, for molecular biology, ≥98.5% (GC)
Sigma-Aldrich
十二烷基硫酸钠, ≥99.0% (GC), dust-free pellets
Sigma-Aldrich
十二烷基硫酸钠 溶液, BioUltra, for molecular biology, 10% in H2O
Sigma-Aldrich
十二烷基硫酸钠 溶液, BioUltra, for molecular biology, 20% in H2O
Sigma-Aldrich
十二烷基硫酸钠, BioUltra, for molecular biology, ≥99.0% (GC)
Sigma-Aldrich
DL-α-生育酚乙酸酯, ≥96% (HPLC)
Supelco
十二烷基硫酸钠, dust-free pellets, suitable for electrophoresis, for molecular biology, ≥99.0% (GC)
Supelco
DL-α-生育酚乙酸酯, analytical standard
Sigma-Aldrich
十二烷基硫酸钠, ≥98.0% (GC)
Sigma-Aldrich
十二烷基硫酸钠, ACS reagent, ≥99.0%
Sigma-Aldrich
(+)-α-生育酚乙酸酯, oil or semi-solid, ~1360 IU/g
USP
生育酚乙酸酯, United States Pharmacopeia (USP) Reference Standard
Sigma-Aldrich
(+)-α-生育酚乙酸酯, BioReagent, suitable for insect cell culture, ~1360 IU/g
Sigma-Aldrich
十二烷基硫酸钠, ReagentPlus®, ≥98.5% (GC)
Sigma-Aldrich
十二烷基硫酸钠, tested according to NF, mixture of sodium alkyl sulfates consisting mainly of sodium dodecyl sulfate
Supelco
DL-α-生育酚醋酸酯, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
十二烷基硫酸钠, BioXtra, ≥99.0% (GC)
Sigma-Aldrich
十二烷基硫酸钠, 92.5-100.5% based on total alkyl sulfate content basis
Supelco
十二烷基硫酸钠, suitable for ion pair chromatography, LiChropur, ≥99.0%
Sigma-Aldrich
十二烷基硫酸钠, ≥90% ((Assay))
月桂基硫酸钠, European Pharmacopoeia (EP) Reference Standard
αα-生育酚醋酸酯, European Pharmacopoeia (EP) Reference Standard
Sigma-Aldrich
DL-α-生育酚乙酸酯, tested according to Ph. Eur.
生育酚醋酸酯, European Pharmacopoeia (EP) Reference Standard
Sigma-Aldrich
十二烷基硫酸钠, BioReagent, suitable for electrophoresis, for molecular biology, ≥98.5% (GC), free-flowing, Redi-Dri