Hydrophilic excipients modulate the time lag of time-controlled disintegrating press-coated tablets |
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Authors: | Shan-Yang Lin Mei-Jane Li Kung-Hsu Lin |
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Institution: | (1) Biopharmaceutical Laboratory, Department of Medical Research and Education, Veterans General Hospital-Taipei, Taipei, Taiwan, Republic of China |
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Abstract: | An oral press-coated tablet was developed by means of direct compression to achieve the time-controlled disintegrating or
rupturing function with a distinct predetermined lag time. This press-coated tablet containing sodium diclofenac in the inner
core was formulated with an outer shell by different weight ratios of hydrophobic polymer of micronized ethylcellulose (EC)
powder and hydrophilic excipients such as spray-dried lactose (SDL) or hydroxypropyl methylcellulose (HPMC). The effect of
the formulation of an outer shell comprising both hydrophobic polymer and hydrophilic excipients on the time lag of drug release
was investigated. The release profile of the press-coated tablet exhibited a time period without drug release (time lag) followed
by a rapid and complete release phase, in which the outer shell ruptured or broke into 2 halves. The lag phase was markedly
dependent on the weight ratios of EC/SDL or EC/HPMC in the outer shell. Different time lags of the press-coated tablets from
1.0 to 16.3 hours could be modulated by changing the type and amount of the excipients. A semilogarithmic plot of the time
lag of the tablet against the weight ratios of EC/SDL or EC/HPMC in the outer shell demonstrated a good linear relationship,
withr=0.976 andr=0.982, respectively. The predetermined time lag prior to the drug release from a press-coated tablet prepared by using a
micronized EC as a retarding coating shell can be adequately scheduled with the addition of hydrophilic excipients according
to the time or site requirements. |
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Keywords: | micronized ethylcellulose press-coated tablet time lag spray-dried lactose HPMC time-controlled disintegration weight ratio |
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