Nifedipine ????????????

1
Nifedipine ????????????

• ?????????,??????????????????????
• ???????????????????,????????????
• ????,?????????????????????(Nifedipine)
• ,???????????(PEG 400,PEG 600, PEG 6000)??????(
• SLS),??????????(MCC)?????,??????,???
• ??(Aerosil)?????????????????????????
• ?????????,???Nifedipine ?????????????
• ??????PEG 6000??,?PEG 400?PEG 600??????????
• ??????(90mg)?????????(1mg)?,?????????
• ????????Nifedipine??????????????(80mg,
• 70mg)???
• ????????????,?????????????,?????
• ????????????????????????????????
• ????,?????????????? (tangential spraying) ?
• ?????????,??????????????????????
• ?????????????,??????????????????
• ????????????????????????????????
• ,???????,???????????????????????
• ,???????Pluronic F68 ?SLS,????????,????

2
The Formulation Studies og Nifeeipine Dosage
Forms Instant Release and Controlled-Release

• Because of limited aqueous solubility in body
  fluids, the
• dissolution rate of the poorly soluble drugs
  becomes the rate
• limiting step in the absorption process. The
  adsorption of
• soluble form of poorly soluble drugonto the
  surface of
• excipients could maintain its solubilization and
  plays a
• valuable way to enhance the drug release. In the
  first part of
• thisstudy, soluble form of Nifedipine in the
  medium containing
• various amountsof PEG derivatives (PEG 400, PEG
  600, PEG 6000)
• and SLS was compounded aand then was adsorbed on
  the mixture of
• microcrystalline cellulose (MCC) andAerosil-200
  to become powder
• forms. The dissolution of Nifedipine demonstrated
  to be
• independent of the ratios of powder mixture of
  MCC and
• Aerosil-200.The results also showed that the
  amounts of water
• soluble carriers and surfactants increased, the
  dissolution
• rate of Nifedipine was increased expectedly. With
  sufficient
• amount of surfactant, the release rate of
  Nifedipine from three
• samples followed the order of PEG 6000 gt PEG 600
  PEG 400. When
• the formulations employ high concentration (90mg)
  of carrier but
• low amount (1mg) of surfactants, the dissolution
  rate of

3
The Formulation Studies og Nifeeipine Dosage
Forms Instant Release and Controlled-Release

• increased, the dissolution rate was also
  increased. The
• combination of PluronicF68 and SLS in the solid
  dispersion
• showed higher enhancement on dissolution rate of
  Nifedipine than
• that with only one surfactant. The surfactants
  may act to
• inhibit the crystal growth of Nifedipine during
  the formation of
• solid dispersion on the pellet surface.
  Increasing wettability,
• dispersibility and solubilization of drug to
  enhance dissolution
• rate of Nifedipine from the soliddispersion are
  among the
• possible reasons.
• Pellet capsule dosage form has shown many
  advantages and
• flexibility in theway of enhancing the
  therapeutic safety and
• potency or in term of processing and formulation
  design.
• Especially, multilayered pellet dosage forms may
  include many
• different kinds or different release rates of
  drugs in the same
• pellet. In this study, a multilayered pellet
  dosage form was
• developed with reference to Cortance (SB).
  Basically, a
• Nifedipine solid dispersion was adhered onto
  nu-pareil seeds in
• a fluidized-bed system as the first layer. Then
  cellulose ether
• of ethylcellulose (Surelease, 25 ethylcellulose
  aqueous