Usually, drugs with these properties should not be formulated into a sustained release dosage form:
- Drugs with a half life shorter than 2 hours
- Drugs with a half life longer than 5 hours
- Drugs with a short half life but a long duration of action
- Drugs which have a poor absorption
- Drugs with a narrow therapeutic index
- Drugs weighing more than 1g
- Drugs with a solubility lower than 0.1mg/mL
- Drugs with a very low partition coefficient
sustained release dosage form follows first order kinetics.
Sustained-release capsules.
25 mg daily dose
Factors influencing oral sustained-release dosage form design include drug properties (such as solubility, stability, and half-life), desired release profile, site of absorption in the gastrointestinal tract, manufacturing feasibility, patient compliance, and regulatory requirements. Additionally, considerations such as cost-effectiveness, formulation complexity, and technology advancement may also impact the design of sustained-release dosage forms.
They include:Biological half-lifeCompounds with a half-life which is shorter than 8 hours and shorter than 2 hours are good for sustained release formulations. On the other hand, drugs with a short half life yet long duration of action are not suitable for sustained release formulations.AbsorptionThe rate of release should be slower than the rate of absorption. In other words, the overall absorption rate of the drug should be consistent with the rate of release of the drug from the dosage form. Drugs which have a poor absorption are not suitable for sustained released formulations.MetabolismMetabolism can occur in the intestine. When compared with a bolus dose, sustained release increases the chances of the drugs being metabolised as they are released one by one.Margin of safety and therapeutic effectsDrugs with a narrow therapeutic window are dangerous candidates as failure of choosing the correct dosage form may lead to accidental overdose.
They include:Dose size: For orally administered drugs, there is usually an upper limit for the size of the dose. It is usually 1g for tablets. If the size is over this limit, an alternative solution may be needed (eg. taking more than one tablet instead).Ionisation and solubility: Compounds which a solubility less than 0.01mg/mL will be sustained. The lower solubility limit for drugs formulated for sustained release is around 0.1mg/mL.Partition coefficient: Compounds with a poor availability include those with a low partition coefficient.Stability: Some drugs are not stable in the acidic environment of the stomach and will be released there. It is hence ideal to delay the release of these drugs so that they are released in the small intestine for more absorption.
Control release dosage forms involves the calculated release of an administered drug. For example, most aspirins have a time release formula configured after the stomach digests the drug.
You didn't specify which drug so we cannot answer this.
Most drugs are metabolised or flushed from your system within hours, except slow-release drugs designed to provide a sustained dosage over a longer period. Trace amounts of most drugs remain detectable (particularly in hair follicles) for far longer.
Dark Justice - 1991 Incorrect Dosage 3-12 was released on: USA: 2 July 1993
Apparatus 3 Modified a dissolution apparatus used to study in-vitro dissolution behaviour of solid dosage forms, particularly modified release dosage forms.
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