Pharmaceutical Technology: Controlled Drug Release, Volume 2

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MULTIPARTICULATES [CH. 11 127 Fig. 1—Passage of ethylcellulose-coated pellets through the gastrointestinal tract in six healthy volunteers. The position of the foremost part of the dose has been numbered according to Table 1. Each point represents the mean±SD. **, p
128 CH. 11] THE EFFECT OF FOOD ON GASTROINTESTINAL TRANSIT AND DRUG ABSORPTION Table 2—Radiological evaluation of the time during which the majority of pellets were retained in the stomach Table 3—Radiological evaluation of the time during which the majority of the pellets had entered the colon most pellets into the colon was usually delayed from 4 to 12 h, but in one case (JO) for more than 18 h (Table 3). Fig. 2 shows the serum verapamil levels of each volunteer in both the fasted and the fed states, and the position of the majority of pellets at each blood sampling. Especially large differences in time-concentration curves were noted if in the fasted state the majority of pellets had already entered the intestine at 2 h but in the fed state remained in the stomach for more than 4 h (volunteers KM and TM). CONCLUSION We conclude that food, and especially a heavy meal, markedly enhances the gastric residence time of pellets administered in a hard gelatin capsule. Clearly most of the pellets were only swept out of the stomach by the migrating motor complex (‘housekeeper wave’). This delay in gastric emptying can cause a higher and earlier peak in blood drug concentration, leading to some side effects. Thus it is important that in the development of modified release formulations, both single unit and multiple unit, bioavailability studies should be carried out under both fasting and nonfasting conditions. Testing a light breakfast only may be misleading. According to the results of absorption studies, patients must also be informed on the proper timing of drug administration in relation to meals.
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PHARMACEUTICAL TECHNOLOGY Controlle
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3 TABLET MACHINE INSTRUMENTATION IN
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First published in 1991 by ELLIS HO
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7 10 Controlled delivery of theophy
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Slow and steady wins the race Poems
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1 Influence of drug solubility in t
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CH. 1] INFLUENCE OF DRUG SOLUBILITY
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24 MATRIX FORMULATIONS [CH. 2 MATER
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26 MATRIX FORMULATIONS [CH. 2 Fig.
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28 MATRIX FORMULATIONS [CH. 2 Table
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30 MATRIX FORMULATIONS [CH. 2 The e
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34 CH. 3] THE FORMULATION OF SUSTAI
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4 Statistical optimization of a con
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MATRIX FORMULATIONS [CH. 4 45 (4) G
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MATRIX FORMULATIONS [CH. 4 47 Fig.
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Columns 1-4 lead to the matrix of e
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MATRIX FORMULATIONS [CH. 4 51 Table
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MATRIX FORMULATIONS [CH. 4 53 Fig.
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Fig. 5—Linearization of the relea
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58 MATRIX FORMULATIONS [CH. 5 Pevik
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60 MATRIX FORMULATIONS [CH. 5 The d
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6 Controlled release matrix tablets
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CH. 6] CONTROLLED RELEASE MATRIX TA
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CH. 6] CONTROLLED RELEASE MATRIX TA
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Page 91 and 92: 90 CH. 8] TOPICAL RELEASE AND PERME
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Page 105 and 106: 104 MULTIPARTICULATES [CH. 9 parace
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Page 127: 126 CH. 11] THE EFFECT OF FOOD ON G
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Page 133 and 134: 132 CH. 12] BIODEGRADABLE POLYMERS
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Page 157 and 158: 156 OPHTHALMIC FORMULATION [CH. 14
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178 IMPLANTS [CH. 16 Fig. 1—The e
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180 IMPLANTS [CH. 16 Table 3—Tobr
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182
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184 CH. 17] SILICON MATRIX SYSTEMS
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192
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194 INDEX dry granulation, 43 elect
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Pharmaceutical Technology: Controlled Drug Release, Volume 2

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