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Columbus, OH, United States

Purpose: To compare physiochemical properties of mono-, di- and triglycerides of medium chain fatty acids for development of oral pharmaceutical dosage forms of poorly water-soluble drugs using phase diagrams, drug solubility, and drug dispersion experiments. Methods: Phase diagrams were prepared using a monoglyceride (glycerol monocaprylocaprate: CapmulMCM® EP), a diglyceride (glycerol dicaprylate) and two triglycerides (glycerol tricaprylate: Captex 8000®; caprylic/capric triglycerides: Captex 355 EP/NF®) in combination with a common surfactant (PEG-35 castor oil: Cremophor EL®) and water. Psuedoternary phase diagrams using mixtures of monoglyceride with either diglyceride or triglyceride were constructed to determine any potential advantage of using lipid mixtures. Result: The monoglyceride gave microemulsion (clear or translucent liquid) and emulsion phases, whereas di- and triglycerides exhibited an additional gel phase. Among individual mono-, di- and triglycerides, the oil-in-water microemulsion region was the largest for the diglyceride. Gel phase region within diglyceride and triglyceride phase diagrams could be practically eliminated and microemulsion regions expanded by mixing monoglyceride with di- or tri-glycerides (1:1). Addition of a model drug, danazol, had no effect on particle sizes of microemulsions formed. Dispersion of drug in aqueous media from mixtures of mono- and diglyceride or mono- and triglyceride was superior to individual lipids. Conclusion: Systematic study on comparison of mono-, diand triglyceride of medium chain fatty acids will help formulators select components for optimal lipid-based formulation. © The Author(s) 2011.

Prajapati H.N.,St. Johns University | Patel D.P.,St. Johns University | Patel N.G.,St. Johns University | Dalrymple D.M.,ABITEC Corporation | Serajuddin A.T.M.,St. Johns University
Journal of Excipients and Food Chemicals | Year: 2011

Lipids consisting of medium chain fatty acids are commonly used in the development of lipid-based self-emulsifying and self-microemulsifying drug delivery systems. However, no systematic approach to selecting one lipid over another has been reported in the literature. In this study, propylene glycol (PG) monoester (PG monocaprylate, Capmul PG-8 ®) and PG diester (PG dicaprylocaprate, Captex 200P ®) of C 8-fatty acids were compared with PG monoester (PG monolaurate, Capmul PG-12 ®) and PG diester (PG dilaurate, Capmul PG-2L ®) of C 12-fatty acids with respect to their phase diagrams, and especially for their ability to form microemulsions in the presence of a common surfactant, Cremophor EL ®, and water. The solubility of two model drugs, danazol and probucol, in the lipids and lipid/surfactant mixtures were also compared. The effect of the chain length of medium-chain fatty acids (C 8 versus C 12) on the phase diagrams of the lipids was minimal. Both shorter and longer chain lipids formed essentially similar microemulsion and emulsion regions in the presence of Cremophor EL ® and water, although the C 12-fatty acid esters formed larger gel regions in the phase diagrams than the C 8-fatty acid esters. When monoesters were mixed with their respective diesters at 1:1 ratios, larger microemulsion regions with lower lipid particle sizes were observed compared to those obtained with individual lipids alone. While the solubility of both danazol and probucol increased greatly in all lipids studied, compared to their aqueous solubility, the solubility in C 12-fatty acid esters was found to be lower than in C 8-fatty acid esters when the lipids were used alone. This difference in solubility due to the difference in fatty acid chain length, practically disappeared when the lipids were combined with the surfactant. © IPEC-Americas Inc.

Patel N.,St. Johns University | Dalrymple D.M.,ABITEC Corporation | Serajuddin A.T.M.,St. Johns University
Journal of Excipients and Food Chemicals | Year: 2012

Solid self-emulsifying drug delivery systems (SEDDS) for medium chain triglycerides (Captex® 355, ABITEC) were developed using stearoyl polyoxyl glycerides (Acconon® C-50, ABITEC and Gelucire® 50/13, Gattefosse) as both solidifying and emulsifying agents. Different mixtures of the lipid and each solidifying agent were heated to 65°C until homogenously mixed clear liquids were formed. Probucol was dissolved as the model drug. The molten mass was then filled into hard gelatin capsules, which upon cooling to room temperature converted to a solid mass inside capsules. The triglyceride could be incorporated into the system to a concentration as high as 80% w/w, still maintaining the solid or semisolid consistency of the system. Powder XRD, DSC, microscopy (cross-polarization and confocal fluorescence techniques), dispersion test and particle size analysis of the solid systems with, and without, drug were conducted to characterize different formulations. The solidifying agents maintained their crystallinity in solid systems, while the lipids were interspersed in between crystalline regions. The drug remained solubilized in the lipid phase. The formulations dispersed almost completely in 2 hours with particle size of the dispersed lipid in the range of 250 to 500 nm when the lipid content in the formulation was up to 50% w/w. Thus, a novel method of developing solid formulations of liquid triglycerides by incorporating lipids in stearoyl polyoxyl glycerides has been developed. © IPEC-Americas Inc.

Patel N.,St. Johns University | Prajapati H.N.,St. Johns University | Dalrymple D.M.,ABITEC Corporation | Serajuddin A.T.M.,St. Johns University
Journal of Excipients and Food Chemicals | Year: 2012

Self-emulsifying drug delivery systems (SEDDS) are usually isotropic liquids consisting of drugs, lipids, surfactants and/or co-surfactants that spontaneously form fine oil-in-water emulsions in contact with water. Since a solid dosage form has better patient acceptance than a liquid, it was investigated whether liquid SEDDS containing medium-chain lipids (mono- or tri-glycerides) may be converted to solids or semisolids using lauroyl polyoxyl glycerides (Acconon® C-44, ABITEC, and Gelucire® 44/14, Gattefosse) as solidifying agents. Acconon® C-44 and Gelucire® 44/14 were melted at 65EC. The liquid lipids or the liquid lipidsurfactant mixtures, with and without dissolved drug (probucol), were mixed with the melts, and the hot liquid solutions were filled into hard gelatin capsules. The solutions solidified inside the capsules when cooled to room temperature. Acconon® C-44 and Gelucire® 44/14 had a greater propensity for solidifying the triglyceride of medium chain fatty acids (Captex® 355, ABITEC) rather than the monoglyceride. Powder XRD, DSC and microscopic analyses indicated that the lauroyl polyoxyl glycerides crystallized at room temperature, while the lipid or the lipid-surfactant mixtures present in the formulations remained interspersed in between solids as a separate liquid phase. The drug remained dissolved in the liquid phase and there was no crystallization of the drug. Although Acconon® C-44 and Gelucire® 44/14 are themselves surface active, the dispersion testing using the USP apparatus II at 50 rpm and 37EC using 250 ml of 0.01N HCl as the dispersion medium showed that a second surfactant (Cremophor® EL®, BASF) was required in the solid formulation to maximize drug release and dispersion. Formulations containing 1:1 and 3:1 w/w ratios of Captex® 355 and Cremophor® EL produced lipid particles in the range of 200 to 450 nm. Thus, a novel approach of preparing solid SEDDS resulting in submicron emulsions with particle size <500nm is presented. © IPEC-Americas Inc.

Abitec Corporation | Date: 2012-06-26

Chemicals for use in the manufacture of goods in the nature of ethoxylated fatty amines and amine derivatives used as emulsifiers and surfactants in household, industrial and institutional applications for products such as lotions, shampoos, oil field, metalworking, and asphalt enhancers.

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