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Essay / Oral route and drug therapy - 1017
INTRODUCTION: The oral route is the most important route for drug therapy (Roger E). Water-insoluble drugs have poor oral bioavailability, so more attention has been paid to lipid-based formulation. Lipids are the delivery vehicles for drugs that have low water solubility (Pouton CW). Various lipid-based formulations like SEDDS and SMEDDS are used to improve the absorption as well as bioavailability of poorly water-soluble drugs (Yi T et al). Lipid vehicles play an important role in design and can lead to successful drug delivery, thereby controlling the rate of drug absorption. When evaluating lipids as vehicles, their digestibility must also be considered. SMEDDS present good thermodynamically stable preparations and have optical transparency, this formulation is simple and it is the mixture of oil, surfactant, co-surfactant, co-solvents, these lipid based excipients are commonly called permeability activators (Schwendener RA). For the design of SEDDS/SMEDDS, these require several excipients, in order to evaluate the relative solubility and affinity of the drug for each component. These excipients have the ability to form a fine oil-in-water microemulsion. The droplet size of the emulsion present in the intestine and the type of surfactants, lipid metabolic pathway, changes in gastric motility are due to the presence of lipids. These excipients can inhibit both presystemic metabolism and P-gp-mediated intestinal efflux, leading to increased oral absorption of cytotoxic drugs (Dintaman JM) (Chervinsky DS). FACTORS TO CONSIDER IN DESIGNING A LIPID-BASED FORMULATION:• Solvent capacity• Properties of lipid excipients• Lipophilicity of surfactants• Ex...... middle of paper ......nt, BHT, and thus by the addition of these excipients, the soft gelatin formulation exhibits improved bioavailability.Bexarotene is a derivative of benzoic acid and is a selective activator of the retinoid X receptor indicated for the treatment of T-cell lymphoma. It is formulated in the form of a soft gelatin capsule, i.e. Targetin®. The free acid form of bexarotene exhibits solubilization in a mixture of polysorbate20 and PEG 400 in combination with povidone and BHA as an antioxidant in Targetin® 75 mg soft gelatin capsules. Lopinavir and ritonavir have been formulated together as Kaletra® tablets and Kaletra oral solution, Span 20 is the lipid component present in this formulation. The fixed dose combination of the product contains 80 mg/ml lopinavir and 20 mg/ml ritonavir which are solubilized in propylene glycol, 42% ethanol, water, glycerin, cremophor surfactant RH 40 and peppermint oil..