Preparation and characterisation of sustained-release ibuprofen-cetostearyl alcohol spheres

Wong, Lynn; Gilligan, C.A.; Po, A. Li Wan

doi:10.1016/0378-5173(82)90012-6

Cited by 19 publications

(5 citation statements)

References 23 publications

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“…In the ternary CET ALC-PCV-LYS mixture (Figure 7), the drug melting peak at 253 °C disappeared, which indicated complete solubilization of the PVC and LYS in the CET ALC. This result agreed with previous reports that showed strong interactions between CET ALC and prednicarbate [43], lapachol [48], and ibuprofen [49]. However, since CET ALC is a surfactant, solubilisation of the drugs in melted CET ALC does not necessarily represent incompatibility [43,48,49].…”

Section: Resultssupporting

confidence: 92%

Solid-State Characterization and Compatibility Studies of Penciclovir, Lysine Hydrochloride, and Pharmaceutical Excipients

et al. 2019

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The physical and chemical characterization of the solid-state properties of drugs and excipients is fundamental for planning new formulations and developing new strategies for the treatment of diseases. Techniques such as differential scanning calorimetry, thermogravimetry, X-ray powder diffraction, Fourier transform infrared spectroscopy, and scanning electron microscopy are among the most commonly used techniques for these purposes. Penciclovir and lysine are individually used to treat the herpes virus. As such, the development of a formulation containing both drugs may have therapeutic potential. Solid-state characterization showed that both penciclovir and lysine were crystalline materials with melting points at 278.27 °C and 260.91 °C, respectively. Compatibility studies of penciclovir and lysine indicated a possible interaction between these substances, as evidenced by a single melting point at 253.10 °C. The compatibility of several excipients, including ethylenediaminetetraacetic acid, cetostearyl alcohol, sodium lauryl sulphate, di-tert-butyl methyl phenol, liquid petrolatum, methylparaben, nonionic wax, paraffin, propylene glycol, and propylparaben, was evaluated in ternary (penciclovir-lysine-excipient) mixtures (1:1:1, w/w/w) to determine the optimal formulation. The developed formulation was stable under accelerated and ambient conditions, which demonstrated that the interaction between penciclovir and lysine was suitable for the development of a formulation containing both drugs.

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Section: Resultssupporting

confidence: 92%

Solid-State Characterization and Compatibility Studies of Penciclovir, Lysine Hydrochloride, and Pharmaceutical Excipients

et al. 2019

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“…The effect of the initial burst in the formulations was less pronounced. MTH release from the SLMs increased with decrease in particle sizes of the SLMs, consistent with earlier report (Wong et al, 1992). For instance, in batch A formulations, sub-batch A1 with the least particle size (33 mm) gave a maximum release of 74%, while sub-batch A3 with the highest particle size (47 mm) gave a maximum release of 64%.…”

Section: Physicochemical Properties Of Slmssupporting

confidence: 90%

Formulation and evaluation of novel solid lipid microparticles as a sustained release system for the delivery of metformin hydrochloride

2013

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The low encapsulation efficiency of conventional solid lipid microparticles (SLMs) especially for hydrophilic drugs has remained a challenge to drug formulation experts. This work seeks to address the issue of inefficient delivery of metformin hydrochloride (MTH), a potent hydrophilic oral antihyperglycemic agent, using novel SLMs based on solidified reverse micellar solutions (SRMS) prepared by melt-emulsification using a lipid derived from Capra hircus and Phospholipon® 90H. Characterization based on size, morphology, zeta potential, polydispersity index, encapsulation efficiency (EE%), loading capacity (LC) and time-resolved stability were carried out on the SLMs. The in vitro release of MTH from the SLMs was performed in phosphate buffer (pH 7.4) while the in vivo antidiabetic properties were investigated in alloxan-induced diabetic rats. Stable, spherical and smooth SLMs were obtained. Loading of MTH into the SLMs had no effect on the surface charge of the particles. The SLMs with 1.0%w/w PEG 4000 resulted in significantly (p < 0.05) higher EE% while those with 2.0%w/w gave the least. The LC values ranged from 20.3 to 29.1 and 14.6 to 24.1 for SLMs containing 500 mg and 250 mg of MTH, respectively. The in vitro release studies revealed significant release of MTH from the SLMs whereas the in vivo antidiabetic studies indicated that novel SLMs containing 500 mg of MTH gave significantly (p < 0.05) higher glucose reduction than glucophage®. This research has shown that SLMs based on SRMS offer a new and better approach of delivering MTH, thus encouraging further development of this formulation.

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“…Microspheres to encapsulate drugs can, of course, be synthesised from alternatives to stearic acid (13). For example ibuprofen has previously been incorporated within ceto-stearyl alcohol microspheres (14) but to date, drug release profiles based on dissolution studies have not been fully investigated.…”

Section: Ibuprofenmentioning

confidence: 99%

In vitro controlled drug release from loaded microspheres - dose regulation through formulation

Waters

Pavlakis

2007

J Pharm Pharm Sci

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ABSTRACT-Purpose. Drug release profiles were established for ibuprofen encapsulated within several types of microspheres and a range of dissolution buffer media to study the effect these variables have in controlling the rate and extent of drug release. Methods. Fatty acid microspheres containing ibuprofen were prepared by a process previously developed and refined to produce microspheres of a known size and composition, namely 80-125 μm diameter and an excipient to ibuprofen ratio of 3:1. Drug release profiles from these encapsulated formulations were compared with those obtained for the dissolution of ibuprofen alone under the same conditions. Results. Stearic acid microspheres were found to only partially retard the release of ibuprofen over a twenty minute period compared with the dissolution of ibuprofen alone. However, a significant retardation of ibuprofen release was observed with cetostearyl alcohol microspheres over the same period of time. Secondly, drug release profiles for encapsulated ibuprofen were determined using five distinct dissolution buffer media; sodium phosphate, potassium phosphate, citric acid and phosphate mix, MOPS and tris. Significant differences in the extent and rate of drug release were recorded between the different dissolution buffer solutions. These differences were also shown to be independent of variations in pH, temperature, buffer concentrations and the type of cations present. Conclusions. The presence and choice of microsphere formulation, and the choice of buffer present in the dissolution solution, can influence drug release in vitro, i.e. it is possible to achieve controlled drug release from microspheres. To explain the control achieved through the choice of buffer in solution it is proposed that the buffer anion exerts a stabilising influence on the ibuprofen-microsphere matrix. NOVELTY OF THE WORKThe research presented in this paper introduces a new formulation for pharmaceutical applications, namely encapsulating a drug within stearic acid and cetostearyl alcohol microspheres. Several interesting observations were made in that different microsphere formulations retarded drug release in vitro to differing degrees and surprisingly, the buffer anion appeared to dictate drug release. It is therefore now possible to produce a unique formulation with a highly controlled level of drug release, i.e. achieving dose regulation through formulation.

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Preparation and characterisation of sustained-release ibuprofen-cetostearyl alcohol spheres

Cited by 19 publications

References 23 publications

Solid-State Characterization and Compatibility Studies of Penciclovir, Lysine Hydrochloride, and Pharmaceutical Excipients

Solid-State Characterization and Compatibility Studies of Penciclovir, Lysine Hydrochloride, and Pharmaceutical Excipients

Formulation and evaluation of novel solid lipid microparticles as a sustained release system for the delivery of metformin hydrochloride

In vitro controlled drug release from loaded microspheres - dose regulation through formulation

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