An investigation into the structure and bioavailability of α-tocopherol dispersions in Gelucire 44/14

Barker, S. A.; Yap, Siew Ping; Yuen, Kah Hay; McCoy, Colin; Murphy, John R.; Craig, Duncan Q.M.

doi:10.1016/s0168-3659(03)00261-x

Cited by 74 publications

(43 citation statements)

References 16 publications

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“…Gelucire® 44/14, with HLB value of 14, is a mixture of monoesters, diesters and triesters of glycerol, and monoesters and diesters of polyethylene glycols [28] that belongs to the lauryl polyoxylglycerides (macroglycerides) family. Because of its numerous pharmaceutical applications, such as self-emulsification [29], and biocompatibility [27,30], this material was investigated as an adjuvant to modulate the drug release properties from the transdermal patch systems.…”

Section: Introductionmentioning

confidence: 99%

Hot melt extruded transdermal films based on amorphous solid dispersions in Eudragit RS PO: The inclusion of hydrophilic additives to develop moisture-activated release systems

Albarahmieh

Craig

2016

International Journal of Pharmaceutics

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A series of Eudragit RS PO-based hot melt extruded films were evaluated as potential transdermal systems, with particular emphasis on the inclusion of hydrophilic excipients to allow water sorption, which in turn would allow drug release on application to the skin. More specifically, sucrose, methyl cellulose, xanthan gum (Xantural®75), poloxamer (Pluronic®F127), Gelucire 44/14 were added to Eudragit RS PO and assessed in terms of physical structure (modulated temperature DSC (MTDSC), thermogravimetric analysis (TGA), powder XRD (PXRD), scanning electron microscopy(SEM)) and in vitro drug release and permeation properties. In addition, the effect of prior hydration on drug permeation was studied for selected systems. Phase separation was noted for sucrose, methylcellulose (high loading), xanthan gum (high loading), poloxamer and Gelucire 44/14 (high loading) using both visual observation and MTDSC. PXRD studies indicated drug crystallization within the phase separated systems. SEM studies broadly followed the same pattern. Dissolution studies indicated that the hydrophilic excipients considerably enhanced the release rate, while Franz diffusion cell studies showed a much greater variability in effectiveness, which we ascribe to the paucity of water of hydration present which would not allow swellable additives such as xanthan to release the drug. However, films containing Gelucire 44/14 emerged as the most satisfactory systems, despite the higher additive loaded systems showing drug phase separation. This may be related to emulsification rather than swelling on contact with water, as noted for the permeation studies involving prehydration. This strategy therefore presents a promising approach for triggered transdermal drug delivery, activated by hydration from the skin itself.

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Section: Introductionmentioning

confidence: 99%

Hot melt extruded transdermal films based on amorphous solid dispersions in Eudragit RS PO: The inclusion of hydrophilic additives to develop moisture-activated release systems

Albarahmieh

Craig

2016

International Journal of Pharmaceutics

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“…The gelucires containing only PEG ester 50/13 are generally used in the preparation of fast or rapidly dissolving formulations (Mahmoud et al, 2009). It is a class of hydrophilic lipid with HLB 13 and melting point 50 C. That containing only glycerides or mixtures of glycerides and PEG esters such as 43/01 is used in the preparation of sustained release (Barker et al, 2003) and gastroretentive formulations (Jain & Jagdale, 2009). Gelucire 43/01 is a class of highly hydrophobic lipid with HLB 1 and melting point 43 C. Gelucire 43/01 comprises of a mixture of saturated triglycerides of different fatty acids C8 (3%), C10 (2%), C12 (29%), C14 (2%), C16 (17%), and C18 (36%) melting at 43 C. Extreme hydrophobicity of gelucire 43/01 is attributed to the absence of PEG esters, which in turn provide releaseretarding ability.…”

Section: Introductionmentioning

confidence: 99%

Design and characterization of cefuroxime axetil biphasic floating minitablets

et al. 2014

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Biphasic floating minitablets of cefuroxime axetil were prepared by melt granulation technique using two different grades of gelucire namely 50/13 and 43/01 to maintain constant plasma drug concentration. Loading dose of cefuroxime axetil was formulated as immediate release (IR) minitablets by using hydrophilic grade of gelucire 50/13. Maintenance dose was formulated as floating sustained release (SR) minitablets by using hydrophobic grade of gelucire 43/01. The prepared IR and SR granules were subjected to micromeritic studies and scanning electron microscopy. Fourier transform infrared spectroscopy (FT-IR) study revealed that drug and selected carriers were compatible. In vitro dissolution study of optimized IR minitablets showed more than 85% of loading dose dissolved within 30 min. Optimized SR minitablets showed zero lag time with floating duration more than 12 h. The drug release from SR minitablets was linear with square root of time with non-Fickian diffusion-controlled release. The optimized batch of minitablets was filled into 0 size hard gelatin capsule. In vitro dissolution study for capsule showed an immediate burst release followed by SR up to 12 h. There is no significant change in dissolution data after storage at 40 C and 75% RH for three months. Microbiological assay of dissolution samples of optimized minitablets filled in capsules showed proportionate increase in inhibition of growth against Escherichia coli up to 12 h samples. In vivo bioavailability study in albino rabbits showed three times improvement in oral bioavailability.

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“…Gelucire 50/13 is obtained by PEGylation of stearoyl glycerides and has considerably higher molecular volume as compared to Gelucire 44/14 which may be the reason for less solubilization potential. Gelucire 44/14 was selected as an oil phase for further investigation due to its solubilizing potential for NM and also due to its well established bioavailability enhancing properties (17,18) which would be helpful in case of NM. Amongst various surfactants that were screened, Labrasol exhibited highest solubilizing potential for NM whereas amongst various co-surfactants, Transcutol P and Plurol (Fig.…”

Section: Solubility Studiesmentioning

confidence: 99%

“…Interestingly, NM micellar solution and oily solution showed mean relative bioavailability of 299.42% and 241.14% as compared to NM suspension (P< 0.05). This increase in the bioavailability can be attributed to the absorption enhancing properties of Gelucire 44/14 (used in oily solution), Labrasol and Transcutol P (used in micellar solution) which are well established (17,18,21). Furthermore, Labrasol has recently been shown to improve the absorption of digoxin which is a CYP3A substrate like NM (14).…”

Section: Bioavailability Studymentioning

confidence: 99%

Design and Evaluation of Self-Emulsifying Drug Delivery Systems (SEDDS) of Nimodipine

Kale

Patravale

2008

AAPS PharmSciTech

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Abstract. The ability of self-emulsifying drug delivery systems (SEDDS) to improve solubility, dissolution rate and bioavailability of a poorly water-soluble calcium channel blocker, nimodipine (NM) was evaluated in the present investigation. Solubility of NM in various oils, surfactants and cosurfactants was determined. The influence of the ratio of oil to surfactant + cosurfactant, pH of aqueous phase on mean globule size of resulting emulsions was studied by means of photon correlation spectroscopy. The NM loaded SEDDS selected for the in vitro and in vivo studies exhibited globule size less than 180 nm. In vitro dissolution studies indicated that NM loaded SEDDS could release complete amount of NM irrespective of the pH of the dissolution media. Pharmacokinetics of NM suspension, NM oily solution, NM micellar solution and NM SEDDS were evaluated and compared in rabbits. Relative bioavailability of NM in SEDDS was significantly higher than all the other formulations. NM loaded SEDDS were subjected to various conditions of storage as per ICH guidelines for 3 months. NM SEDDS successfully withstood the stability testing.KEY WORDS: in vitro drug release; low oral bioavailability; nimodipine; pharmacokinetics; selfemulsifying drug delivery systems (SEDDS).

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An investigation into the structure and bioavailability of α-tocopherol dispersions in Gelucire 44/14

Cited by 74 publications

References 16 publications

Hot melt extruded transdermal films based on amorphous solid dispersions in Eudragit RS PO: The inclusion of hydrophilic additives to develop moisture-activated release systems

Hot melt extruded transdermal films based on amorphous solid dispersions in Eudragit RS PO: The inclusion of hydrophilic additives to develop moisture-activated release systems

Design and characterization of cefuroxime axetil biphasic floating minitablets

Design and Evaluation of Self-Emulsifying Drug Delivery Systems (SEDDS) of Nimodipine

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