Which sort of drug candidates are not suitable for sustain release formulation ?

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Zeba's picture

Answer: 

They should have the follwing things like Molecular weight/size < 1000 Daltons, Solubility > 0.1 mg/ml for pH 1 to pH 7.8, Apparent partition coefficient High, Absorption mechanism Diffusion, General absorbability from all GI segments, Release should not be influenced by pH and enzymes, Elimination half-life preferably between 2 to 8 hrs, Total clearance should not be dose dependent, Elimination rate constant required for design, Apparent volume of distribution (Vd) The larger Vd and MEC, the larger will be the required dose size, Absolute bioavailability should be 75% or more, Intrinsic absorption rate must be greater than release rate

Reference: http://www.pharmatutor.org/articles/review-sustained-release-dosage-forms

 

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