Formulation factors affecting drug absorption

Drug absorption is defined as the process of movement of unchanged drug from the site of
administration to systemic circulation.

Non-drug components which are added during formulation of drug are called excipients. 
Excipients are added during drug formulation
Despite their inertness & utility in the dosage form, excipients can influence absorption of drug.
More number of excipients in a dosage form, the more complex it is & greater potential for absorption &
bioavailability problems. Excipients are added to ensure 1.Stability 2.Uniformity 3.Functionability
4.Bioavailability 5.Acceptability
1. VEHICLE: Absrption depend to a large extent on its miscibility with biological fluids
2. DILUENTS are commonly added to tablet (and capsule) formulations if the required dose is
inadequate to produce the necessary bulk e.g. of drug-diluent interaction resulting in poor bioavailability is
that of tetracycline & DCP
3. BINDERS & GRANULATING AGENTS: Promote cohesive compacts before & after
compression e.g. polymeric materials like starch, cellulose derivatives, acacia, PVP, etc.
4. COLOURANTS: Very low concentration of water-soluble dye inhibitory effect on dissolution.
Dye molecules get adsorbed onto the crystal faces & inhibit drug dissolution e.g. brilliant blue retards
dissolution of sulfathiazole
5. LUBRICANTS: aid flow of granules. Reduce interparticle friction and Sticking of particles to
dies & punches e.g. Hydrophobic in nature (several metallic stearates & waxes)
6. COATINGS: Deleterious effect of various coatings on drug dissolution from a tablet dosage
form is enteric coat > sugar coat > nonenteric film coat e.g. Shellac coated tablets, on prolonged storage,
dissolve more slowly in the GIT
7. DISINTEGRANTS: Agents overcome cohesive strength of tablet & break them up on contact
with water which is an important prerequisite to tablet dissolution. These're hydrophilic in nature e.g. MCC
8. BUFFERS: They create right atmosphere for dissolutio n e.g. buffered aspirin tablets. Buffer
containing potassium cations inhibit the drug absorption e.g. vitamin B2 & sulphanilamide
9. SURFACTANTS: They may enhance or retard drug absorption: 1. Promotion of wetting &
dissolution of drugs 2. Better membrane contact of drug for absorption 3. Enhanced membrane permeability
of the drug.
10. SUSPENDING AGENTS/VISCOSITY IMPARTERS: Hydrophilic polymers like vegetable
gums, semisynthetic gums & synthetic gums. Stabilize drug particles by reducing their rate of settling & by
increasing viscosity of the medium they also affect palatability & pourability of solution dosage forms e.g.
Na-CMC complex amphetamine increases drug absorption.
11. CRYSTAL GROWTH INHIBITORS: e.g. crystal growth inhibitors like PVP & PEG inhibit
conversion of a high energy metastable polymorph into stable.
12. COMPLEXING AGENTS: These agent alters stability, solubility, molecular size, partition
coefficient & diffusion coefficient. Pharmacologically inert & must dissociate either at the absorption site or
following absorption into the systemic circulation. Complexation has been used to enhance dissolution
through formation of a soluble complex e.g. ergotamine tartarate-caffeine complex. Enhanced lipophilicity
for better membrane permeability e.g. caffeine-PABA complexand Enhanced membrane permeability e.g.
enhanced GI absorption of heparin.
Nature types of dosage form

SOLUTIONS: Solutions is most rapidly absorbed its Drug dissolution is absent and Factors influencing
absorption of solution is: viscosity, surfactant, solubilizers, stabilizer and stability.
EMULSIONS: Superior to suspensions in administering poorly aqueous soluble lipophilic drugs.
Absorption increases 3 fold over its aqueous suspension. Factors influencing drug absorption of emulsion
are Surface area, Interfacial tension, Droplet size, Surfactants and Lipophilicity
SUSPENSIONS: Drug dissolution which is generally rapid due to the large surface area of the particles .
Factors influencing are particle size, polymorphism, wetting agent, viscosity of medium and suspending
agent.
POWDERS: Though powders are superior to tablets & capsules. They are not in use nowadays due to
handling & palatability problems. Factors to be considered in the absorption of drug from powders are
particle size, Polymorphism and wettability.
CAPSULES: Powders & granules are administered in hard gelatin capsules whereas viscous fluid s & oils
in soft elastic shells. Factors of importance in case of hard gel is Drug particle size, Density,
Polymorphism, Intensity of packing, Influence of diluents & excipients. Factors of importance in case of
soft gel Between the drug & the diluent and Between drug & gelatin shell
TABLETS: Compressed Tablets > Film Coated Tablets > Sugar Coated Tablets > Enteric Coated Tablets
> Sustained Release Products Factors to be considered in the absorption of drug are effective surface area,
dissolution, deaggregation, permeability, excipients/ API and type of tablet

Thank you…

By: Miami Arif & Noor Mohammed

Group: B3