8. MODIFIED-RELEASE DOSAGE FORMS AND DRUG DELEVERY SYSTEMS ●●●●● ●●●● ●●。●●
8. MODIFIED-RELEASE DOSAGE FORMS AND DRUG DELEVERY SYSTEMS
●●●●● CONTENTS ●●●● ●●0 ●●● ●●●● I. The rationale for extended-release pharmaceuticals ll. Terminology II. Extended-release oral dosage forms IV Delayed-release oral dosage forms V USP requirements and FDA Guidance for modified-release dosage forms VI Clinical considerations in the use of oral modified-release dosage form VI. Packaging and storing modified-release tablets and capsules
CONTENTS I. The rationale for extended-release pharmaceuticals II. Terminology III. Extended-release oral dosage forms IV. Delayed-release oral dosage forms V. USP requirements and FDA Guidance for modified-release dosage forms VI. Clinical considerations in the use of oral modified-release dosage form VII. Packaging and storing modified-release tablets and capsules
●●●●● ●●●● ●●0 ●●● ●●●● o In contrast to conventional forms, modified-release products provide either delayed-release or extended release of drug Delayed-release products usually are enteric-coated tablets or capsules designed to pass through the stomach unaltered. later to release their medication within the intestinal tract
⚫ In contrast to conventional forms, modified-release products provide either delayed-release or extendedrelease of drug. ⚫ Delayed-release products usually are enteric-coated tablets or capsules designed to pass through the stomach unaltered, later to release their medication within the intestinal tract
●●●●● ●●●● ●●0 ●●● ●●●● ● Extended- release products are designed to release their medication in controlled manner. at predetermined rate, duration and location to achieve and maintain optimum therapeutic blood levels of rug
⚫ Extended-release products are designed to release their medication in a controlled manner, at a predetermined rate, duration and location to achieve and maintain optimum therapeutic blood levels of drug
I The rationale for extended- ●●●●● ●●●● ●●0 release pharmaceuticals ●●● ●●●● e Extended-release tablets and capsules are commonly taken only once or twice daily compared with counterpart conventional forms that may have to be taken three or four times daily to achieve the same therapeutic effect
I. The rationale for extendedrelease pharmaceuticals ⚫ Extended-release tablets and capsules are commonly taken only once or twice daily, compared with counterpart conventional forms that may have to be taken three or four times daily to achieve the same therapeutic effect
●●●●● ●●●● ●●0 ●●● ●●●● Typically, extended-release products provide an immediate release of drug that promptly produces the desired therapeutic effect, followed by gradual release of additional amounts of drug to maintain this effect over predetermined period
⚫ Typically, extended-release products provide an immediate release of drug that promptly produces the desired therapeutic effect, followed by gradual release of additional amounts of drug to maintain this effect over a predetermined period
MTC MEC Conventional dosage form 0 2 6 8 1012 Time(hr) Hypothetical drug blood level-time curves for a con ventional solid dosage form and a multiple-action product
MTC Controlled released product Conventional 1— dosage forr MEC Ti Ime Hypothetical drug blood level-time curves for a con ventional solid dosage form and a controlled release product
Advantages of Extended-Release Dosage Forms Over Conventional Forms advantas Explanation Reduction in drug blood By controlling the rate of drug release, "peaks and valleys"of drug-blood level fluctuations levels are eliminated Frequency reduction in dosing Extended-release products deliver frequently more than a single dose of medication and thus they may be taken less often than conventional fo ced patient convenience With less frequency of dose administration, a patient is less apt to neglect and compliance taking a dose. There is also greater patient and/or caregiver convenience with daytime and nighttime medication administration Reduction in adverse side effects Because there are fewer drug blood level peaks outside of the drug's therapeutic range and into the toxic range, adverse side effects occur less frequently. Reduction in overall health care costs Although the initial cost of extended-release dosage forms may be greater than that for conventional dosage forms, the overall cost of treatment may be less due to enhanced therapeutic benefit, fewer side-effects, and reduced time required of health care personnel to dispense and administer drugs and monitor patients
●●●●● ●●●● l Terminology ●●0 ●●● ●●●● o Modified-release use to describe dosage forms having drug release features based on time, course, and /or location which are designed to accomplish therapeutic or convenience objectives not offered by conventional or immediate -release forms
II. Terminology ⚫ Modified-release use to describe dosage forms having drug release features based on time, course, and /or location which are designed to accomplish therapeutic or convenience objectives not offered by conventional or immediate-release forms
