Enhancement of oral bioavailability of fenofibrate by solid self-microemulsifying drug delivery systems. 2013

Gun Gook Kim, and Bijay K Poudel, and Nirmal Marasini, and Dong Won Lee, and Tran Tuan Hiep, and Kwan Yeol Yang, and Jong Oh Kim, and Chul Soon Yong, and Han-Gon Choi
College of Pharmacy, Yeungnam University, 214-1, Dae-Dong, Gyongsan 712-749, South Korea.

A solid form of self-microemulsifying drug delivery system (Solid SMEDDS) was developed by spray-drying with dextran as the inert solid carrier, to improve the oral bioavailability of a poorly water-soluble drug, fenofibrate. The optimized liquid SMEDDS, composed of Labrafil M 1944 CS/Labrasol/Capryol PGMC (15/75/10%v/v) with 10% w/v fenofibrate gave a z-average diameter of around 240 nm. There was no significant difference in the mean droplet size and size distribution of the emulsions obtained from the liquid and solid forms of SMEDDS. Solid state characterizations of solid SMEDDS showed that the crystal state of fenofibrate in solid SMEDDS was converted from crystalline to amorphous form. Solid SMEDDS had significantly higher dissolution rates than the drug powder, due to its fast self-emulsification in the dissolution media. Furthermore, the AUC value of solid SMEDDS was twofold greater than that of the powder, indicating this formulation greatly improved the oral bioavailability of drug in rats. Thus, these results suggest that solid SMEDDS could be used as an effective oral solid dosage form to improve dissolution and oral bioavailability of fenofibrate.

UI MeSH Term Description Entries
D008297 Male Males
D009930 Organic Chemicals A broad class of substances containing carbon and its derivatives. Many of these chemicals will frequently contain hydrogen with or without oxygen, nitrogen, sulfur, phosphorus, and other elements. They exist in either carbon chain or carbon ring form. Organic Chemical,Chemical, Organic,Chemicals, Organic
D011092 Polyethylene Glycols Polymers of ETHYLENE OXIDE and water, and their ethers. They vary in consistency from liquid to solid depending on the molecular weight indicated by a number following the name. They are used as SURFACTANTS, dispersing agents, solvents, ointment and suppository bases, vehicles, and tablet excipients. Some specific groups are NONOXYNOLS, OCTOXYNOLS, and POLOXAMERS. Macrogols,Polyoxyethylenes,Carbowax,Macrogol,Polyethylene Glycol,Polyethylene Oxide,Polyethyleneoxide,Polyglycol,Glycol, Polyethylene,Glycols, Polyethylene,Oxide, Polyethylene,Oxides, Polyethylene,Polyethylene Oxides,Polyethyleneoxides,Polyglycols,Polyoxyethylene
D011108 Polymers Compounds formed by the joining of smaller, usually repeating, units linked by covalent bonds. These compounds often form large macromolecules (e.g., BIOPOLYMERS; PLASTICS). Polymer
D011345 Fenofibrate An antilipemic agent which reduces both CHOLESTEROL and TRIGLYCERIDES in the blood. Procetofen,Antara Micronized Procetofen,Apo-Feno-Micro,Apo-Fenofibrate,CiL,Controlip,Fenobeta,Fenofanton,Fenofibrat AL,Fenofibrat AZU,Fenofibrat AbZ,Fenofibrat FPh,Fenofibrat Heumann,Fenofibrat Hexal,Fenofibrat Stada,Fenofibrat-ratiopharm,Fénofibrate Debat,Fénofibrate MSD,Gen-Fenofibrate,LF-178,Lipanthyl,Lipantil,Liparison,Lipidil,Lipidil-Ter,Livesan,Lofibra,MTW-Fenofibrat,Normalip,Novo-Fenofibrate,Nu-Fenofibrate,PMS-Fenofibrate Micro,Phenofibrate,Procetofene,Secalip,Supralip,Tricor,durafenat,fenofibrat von ct,AZU, Fenofibrat,Apo Feno Micro,Apo Fenofibrate,Debat, Fénofibrate,Fenofibrat ratiopharm,Gen Fenofibrate,Heumann, Fenofibrat,Hexal, Fenofibrat,LF 178,LF178,Lipidil Ter,MTW Fenofibrat,Micronized Procetofen, Antara,Novo Fenofibrate,Nu Fenofibrate,PMS Fenofibrate Micro,Procetofen, Antara Micronized,Stada, Fenofibrat
D011409 Propylene Glycols Derivatives of propylene glycol (1,2-propanediol). They are used as humectants and solvents in pharmaceutical preparations. Propanediols,Glycols, Propylene
D002210 Caprylates Derivatives of caprylic acid. Included under this heading are a broad variety of acid forms, salts, esters, and amides that contain a carboxy terminated eight carbon aliphatic structure. Caprylate,Octanoates,Caprylic Acids,Octanoic Acids,Acids, Caprylic,Acids, Octanoic
D003911 Dextrans A group of glucose polymers made by certain bacteria. Dextrans are used therapeutically as plasma volume expanders and anticoagulants. They are also commonly used in biological experimentation and in industry for a wide variety of purposes. Dextran,Dextran 40,Dextran 40000,Dextran 70,Dextran 75,Dextran 80,Dextran B-1355,Dextran B-1355-S,Dextran B1355,Dextran B512,Dextran Derivatives,Dextran M 70,Dextran T 70,Dextran T-40,Dextran T-500,Hemodex,Hyskon,Infukoll,Macrodex,Polyglucin,Promit,Rheodextran,Rheoisodex,Rheomacrodex,Rheopolyglucin,Rondex,Saviosol,Dextran B 1355,Dextran B 1355 S,Dextran T 40,Dextran T 500
D004355 Drug Stability The chemical and physical integrity of a pharmaceutical product. Drug Shelf Life,Drugs Shelf Lives,Shelf Life, Drugs,Drug Stabilities,Drugs Shelf Life,Drugs Shelf Live,Life, Drugs Shelf,Shelf Life, Drug,Shelf Live, Drugs,Shelf Lives, Drugs
D004655 Emulsions Colloids formed by the combination of two immiscible liquids such as oil and water. Lipid-in-water emulsions are usually liquid, like milk or lotion. Water-in-lipid emulsions tend to be creams. The formation of emulsions may be aided by amphiphatic molecules that surround one component of the system to form MICELLES. Emulsion

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