Medium Chain Triglycerides as Vehicle for Palatable Oral Liquids

Bahal, Surendra M.; Romansky, Jamie M.; Álvarez, Francisco J.

doi:10.1081/pdt-120017518

Cited by 17 publications

(11 citation statements)

References 1 publication

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“…The three treatments were: 6·2 g/d n- 3 PUFA (3·7 g EPA and 2·5 g DHA), 3·1 g/d n- 3 PUFA (1·8 g EPA and 1·3 g DHA) (INCROMEGA TM TG4030; Croda International Plc) and placebo (CRODAMOL TM GTCC medium chain TAG; Croda International Plc) (Table 2). CRODAMOL TM GTCC was chosen as it is readily oxidised in the liver so has little impact on human health-related biomarkers ( 29 , 30 ) . Measurements were taken at days 0 and 21 of each treatment period.…”

Section: Methodsmentioning

confidence: 99%

Comparable reductions in hyperpnoea-induced bronchoconstriction and markers of airway inflammation after supplementation with 6·2 and 3·1 g/d of long-chainn-3 PUFA in adults with asthma

et al. 2017

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Although high dose n-3 PUFA supplementation reduces exercise- and hyperpnoea-induced bronchoconstriction (EIB/HIB), there are concurrent issues with cost, compliance and gastrointestinal discomfort. It is thus pertinent to establish the efficacy of lower n-3 PUFA doses. Eight male adults with asthma and HIB and eight controls without asthma were randomly supplemented with two n-3 PUFA doses (6·2 g/d (3·7 g EPA and 2·5 g DHA) and 3·1 g/d (1·8 g EPA and 1·3 g DHA)) and a placebo, each for 21 d followed by 14 d washout. A eucapnic voluntary hyperpnoea (EVH) challenge was performed before and after treatments. Outcome measures remained unchanged in the control group. In the HIB group, the peak fall in forced expiratory volume in 1 s (FEV1) after EVH at day 0 (-1005 (sd 520) ml, -30 (sd 18) %) was unchanged after placebo. The peak fall in FEV1 was similarly reduced from day 0 to day 21 of 6·2 g/d n-3 PUFA (-1000 (sd 460) ml, -29 (sd 17) % v. -690 (sd 460) ml, -20 (sd 15) %) and 3·1 g/d n-3 PUFA (-970 (sd 480) ml, -28 (sd 18) % v. -700 (sd 420) ml, -21 (sd 15) %) (P<0·001). Baseline fraction of exhaled nitric oxide was reduced by 24 % (P=0·020) and 31 % (P=0·018) after 6·2 and 3·1 g/d n-3 PUFA, respectively. Peak increases in 9α, 11β PGF2 after EVH were reduced by 65 % (P=0·009) and 56 % (P=0·041) after 6·2 and 3·1 g/d n-3 PUFA, respectively. In conclusion, 3·1 g/d n-3 PUFA supplementation attenuated HIB and markers of airway inflammation to a similar extent as a higher dose. Lower doses of n-3 PUFA thus represent a potentially beneficial adjunct treatment for adults with asthma and EIB.

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Section: Methodsmentioning

confidence: 99%

Comparable reductions in hyperpnoea-induced bronchoconstriction and markers of airway inflammation after supplementation with 6·2 and 3·1 g/d of long-chainn-3 PUFA in adults with asthma

et al. 2017

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“…A commercial medium-chain triglyceride solution of EFV has shown lower oral bioavailability than the solid form. Preclinical studies indicated that the encapsulation of EFV in poloxamine micelles increases the C max and the area-under-thecurve (AUC) [11] compared to the conventional triglyceride-based liquid formulation [16]. However, when the release profile was tested in vitro using the dialysis membrane method in intestine-like mimicking medium over 24 h, only 40% of the drug was released from the micellar reservoir.…”

Section: Introductionmentioning

confidence: 99%

N-alkylation of poloxamines modulates micellar assembly and encapsulation and release of the antiretroviral efavirenz

Chiappetta

Alvarez‐Lorenzo

Rey‐Rico

et al. 2010

European Journal of Pharmaceutics and Biopharmaceutics

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“…In addition to solid dosage forms, the pharmaceutical development of oral liquid dosage forms of EFV for use in pediatrics or in adults with difficulty in swallowing is challenging. Not only is the solubility of EFV very low, but it imparts a strong and prolonged burning sensation to the mouth and throat when incorporated in water containing liquid formulations (2). CDs can be used to reduce the GI irritation and unpleasant taste of drugs (12).…”

Section: Introductionmentioning

confidence: 99%

“…1). It is a crystalline lipophilic solid (log octanol water partition coefficient of 5.4) with a molecular mass of 315.68 and an aqueous solubility of 9.0 μg/ml (1,2). This is a class II drug (low solubility, high permeability) according to the biopharmaceutical classification system guidance by the Food and Drug Administration (3,4).…”

Section: Introductionmentioning

confidence: 99%

Physicochemical Characterization of Efavirenz–Cyclodextrin Inclusion Complexes

et al. 2009

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Abstract. Efavirenz (EFV) is an oral antihuman immunodeficiency virus type 1 drug with extremely poor aqueous solubility. Thus, its gastrointestinal absorption is limited by the dissolution rate of the drug. The objective of this study was to characterize the inclusion complexes of EFV with β-cyclodextrin (β-CD), hydroxypropyl β-CD (HPβCD), and randomly methylated β-CD (RMβCD) to improve the solubility and dissolution of EFV. The inclusion complexation of EFV with cyclodextrins in the liquid state was characterized by phase solubility studies. The solid-state characterization of various EFV and CD systems was performed by X-ray diffraction, differential scanning calorimetry, and scanning electron microscopy analyses. Dissolution studies were carried out in distilled water using US Pharmacopeia dissolution rate testing equipment. Phase solubility studies provided an A L -type solubility diagram for β-CD and A P -type solubility diagram for HPβCD and RMβCD. The phase solubility data enabled calculating stability constants (K s ) for EFV-βCD, EFV-HPβCD, and EFV-RMβCD systems which were 288, 469, and 1,073 M −1 , respectively. The physical and kneaded mixtures of EFV with CDs generally provided higher dissolution of EFV as expected. The dissolution of EFV was substantially higher with HPβCD and RMβCD inclusion complexes prepared by the freeze drying method. Thus, complexation with HPβCD and RMβCD could possibly improve the dissolution rate-limited absorption of EFV.

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Medium Chain Triglycerides as Vehicle for Palatable Oral Liquids

Cited by 17 publications

References 1 publication

Comparable reductions in hyperpnoea-induced bronchoconstriction and markers of airway inflammation after supplementation with 6·2 and 3·1 g/d of long-chainn-3 PUFA in adults with asthma

Comparable reductions in hyperpnoea-induced bronchoconstriction and markers of airway inflammation after supplementation with 6·2 and 3·1 g/d of long-chainn-3 PUFA in adults with asthma

N-alkylation of poloxamines modulates micellar assembly and encapsulation and release of the antiretroviral efavirenz

Physicochemical Characterization of Efavirenz–Cyclodextrin Inclusion Complexes

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