Oily (Lipophilic) Solutions and Suspensions

Larsen, Susan Weng; Thing, Mette; Larsen, Claus

doi:10.1007/978-1-4614-0554-2_7

Cited by 8 publications

(7 citation statements)

References 75 publications

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“…Vegetable oils (such as castor, sesame, cottonseed, etc. ), medium chain triglycerides and fatty acid monoesters, or their mixtures normally play the role of a solvent in these products [ 8 ]. Following their application (usually intramuscular), the oil forms a depot, from which a prolonged drug release (and some excipients) occurs.…”

Section: Introductionmentioning

confidence: 99%

“…However, these cosolvents allow higher partitioning of the drug into the aqueous phase, which might shorten the release time of the drug, thus decreasing its value as a sustained release formulation. Therefore, the amount of cosolvent added to the solution must be carefully determined in order to balance out its positive effects on drug solubility and solution viscosity while maintaining the partitioning of the drug adequate for prolonged drug release [ 8 ].…”

Section: Introductionmentioning

confidence: 99%

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Development of fiber optic in vitro release testing method for dexamethasone release from the oil solutions

et al. 2022

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For many parenteral drugs, there is still no standardized method for in vitro release (IVR) testing available. This article presents the development of a new IVR method for oil solutions using a dialysis membrane and USP II apparatus coupled to a fiber optic UV-Vis spectrometer. Experiments were performed using dexamethasone formulations containing castor oil as a solvent with the addition of cosolvents, 20 % (v/v) of isopropanol or Capryol® 90. Based on solubility testing results, castor oil was chosen as the best solvent amongst other vegetable oils, while a significant increase in solubility was obtained by adding either of the two cosolvents. Partitioning experiments were performed to ensure these formulations could achieve prolonged drug release. IVR testing was performed with model formulations and critical test parameters were varied in order to examine the method’s sensitivity. The developed method was sensitive to temperature and stirring rate, while coupling the USP II apparatus with a fiber optic UV-Vis spectrometer enabled complete automation. Moreover, due to the interference of excipients on fiber optic detection of dexamethasone during the release testing, derivative spectroscopy was successfully introduced for the elimination of the interference. The developed IVR method described herein could be useful in preformulation investigations and the early development of novel formulations.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Development of fiber optic in vitro release testing method for dexamethasone release from the oil solutions

et al. 2022

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“…These ''depots'' can be defined as dosage forms where drugs are formulated as an aqueous suspension or as an oily/non-aqueous solutions or suspension. They offer numerous advantages, such as prolonged drug action, ease of manufacture and improved patient adherence [4]. Antipsychotic drugs and steroidal hormones have been successfully commercialized as long-acting therapeutic alternatives [4].…”

Section: Introductionmentioning

confidence: 99%

“…They offer numerous advantages, such as prolonged drug action, ease of manufacture and improved patient adherence [4]. Antipsychotic drugs and steroidal hormones have been successfully commercialized as long-acting therapeutic alternatives [4]. With the advances in the areas of biomaterials and polymer science, innovative LADDS have been developed and entered the preclinical and clinical phases of drug development.…”

Section: Introductionmentioning

confidence: 99%

Polymeric long-acting drug delivery systems (LADDS) for treatment of chronic diseases: Inserts, patches, wafers, and implants

Abdelkader

Fathalla

Seyfoddin

et al. 2021

Advanced Drug Delivery Reviews

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“…Oil suspension is simple to prepare, having lower irritation and higher safety than other injections, promoting it into a traditional form of sustained-release formulation (Larsen, Thing, & Larsen, 2012;Duong, Maeng, Duong, Maeng, & Chi, 2019). In the meantime, it has the advantage of sustained-release so that prolongs the action time of the drug and reduces the frequency of drug delivery, determining the feasibility of the dosage form in the veterinary clinic.…”

mentioning

confidence: 99%

Pharmacokinetics and relative bioavailability of meloxicam oil suspension in pigs after intramuscular administration

Liu

Guo

Jiang

et al. 2019

Vet Pharm & Therapeutics

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This study aimed to develop one novel meloxicam (MEL) oil suspension for sustained‐release and compare the pharmacokinetic characteristics of it with MEL conventional formulation in pigs after a single intramuscular administration. Six healthy pigs were used for the study by a crossover design in two periods with a withdrawal interval of 14 days. Plasma concentrations of MEL were measured by ultra‐performance liquid chromatography–tandem mass spectrometry (UPLC‐MS/MS). Pharmacokinetic parameters were calculated by noncompartmental methods. The difference was statistically significant (p < .05) between MEL oil suspension and MEL conventional formulation in pharmacokinetic parameters of mean residence time (6.16 ± 4.04) hr versus (2.66 ± 0.55) hr, peak plasma concentration (Cmax) (0.82 ± 0.12) µg/ml versus (1.12 ± 0.22) µg/ml, time needed to reach Cmax (Tmax) (2.33 ± 0.82) hr versus (0.59 ± 0.18) hr, and terminal elimination half‐life (t1/2λz) (3.74 ± 2.66) hr versus (1.55 ± 0.37) hr. The mean area under the concentration–time curve (AUC0–∝) of MEL oil suspension and MEL conventional formulation was 5.35 and 3.43 hr µg/ml, respectively, with a relative bioavailability of 155.98%. Results of the present study demonstrated that the MEL oil suspension could prolong the effective time of drugs in blood, thereby reducing the frequency of administration on a course of treatment. Therefore, the novel MEL oil suspension seems to be of great value in veterinary clinical application.

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Oily (Lipophilic) Solutions and Suspensions

Cited by 8 publications

References 75 publications

Development of fiber optic in vitro release testing method for dexamethasone release from the oil solutions

Development of fiber optic in vitro release testing method for dexamethasone release from the oil solutions

Polymeric long-acting drug delivery systems (LADDS) for treatment of chronic diseases: Inserts, patches, wafers, and implants

Pharmacokinetics and relative bioavailability of meloxicam oil suspension in pigs after intramuscular administration

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