Formulation characteristics and in vitro release testing of cyclosporine ophthalmic ointments.


:The aim of the present study was to investigate the relationship between formulation/process variables versus the critical quality attributes (CQAs) of cyclosporine ophthalmic ointments and to explore the feasibility of using an in vitro approach to assess product sameness. A definitive screening design (DSD) was used to evaluate the impact of formulation and process variables. The formulation variables included drug percentage, percentage of corn oil and lanolin alcohol. The process variables studied were mixing temperature, mixing time and the method of mixing. The quality and performance attributes examined included drug assay, content uniformity, image analysis, rheology (storage modulus, shear viscosity) and in vitro drug release. Of the formulation variables evaluated, the percentage of the drug substance and the percentage of corn oil in the matrix were the most influential factors with respect to in vitro drug release. Conversely, the process parameters tested were observed to have minimal impact. An evaluation of the release mechanism of cyclosporine from the ointment revealed an interplay between formulation (e.g. physicochemical properties of the drug and ointment matrix type) and the release medium. These data provide a scientific basis to guide method development for in vitro drug release testing of ointment dosage forms. These results demonstrate that the in vitro methods used in this investigation were fit-for-purpose for detecting formulation and process changes and therefore amenable to assessment of product sameness.


Int J Pharm


Dong Y,Qu H,Pavurala N,Wang J,Sekar V,Martinez MN,Fahmy R,Ashraf M,Cruz CN,Xu X




Has Abstract


2018-06-10 00:00:00














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    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章,评审


    authors: Mandić J,Zvonar Pobirk A,Vrečer F,Gašperlin M

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  • Acid-base interactions in amorphous solid dispersions of lumefantrine prepared by spray-drying and hot-melt extrusion using X-ray photoelectron spectroscopy.

    abstract::This study investigates drug-excipient interactions in amorphous solid dispersions (ASDs) of the model basic compound lumefantrine (LMN), with five acidic polymers. X-ray photoelectron spectroscopy (XPS) was used to measure the extent of the protonation of the tertiary amine in LMN by the five acidic polymers. The ext...

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    authors: Song Y,Zemlyanov D,Chen X,Su Z,Nie H,Lubach JW,Smith D,Byrn S,Pinal R

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    abstract::The simultaneous skin permeation of drug and penetration enhancer have been studied in vitro. Simple formulations of mefenamic acid in PEG400 incorporating various proportions of ethanol or 1,8-cineole were prepared and applied to porcine ear skin in diffusion cells under infinite conditions. Receptor phases were assa...

    journal_title:International journal of pharmaceutics

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    journal_title:International journal of pharmaceutics

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    authors: Traini D,Young PM,Rogueda P,Price R

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    abstract::Periplogenin (PPG), a cardiac glycoside prepared from Cortex periplocae, with similar structure to bufalin, has been found to induce apoptosis in many tumor cells. However, lots of cardiac glycosides possessing strong antitumor activity in vitro have still not passed phase I clinical trials, mostly due to poor tumor s...

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    authors: Marras-Marquez T,Peña J,Veiga-Ochoa MD

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    authors: Kamel R,Abbas H,Shaffie NM

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    abstract::A novel modification of tamoxifen [(Z)-2-[4-(1,2-diphenyl-1-butenyl) phenoxy]-N,N-dimethylethylamine] citrate, tamoxifen hemicitrate hydrate was prepared. The crystalline form was identified and characterized by powder and single crystal X-ray diffractometries, differential scanning calorimetry (DSC), thermal gravimet...

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    pub_type: 杂志文章


    authors: Valenta C,Janisch M

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    pub_type: 杂志文章


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    pub_type: 杂志文章


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    pub_type: 杂志文章


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    pub_type: 杂志文章


    authors: Ma N,Zhang B,Liu J,Zhang P,Li Z,Luan Y

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