Korea, South Korea
Korea, South Korea

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PubMed | Korea United Pharm. INC., Sungkyunkwan University, Catholic University of Korea and Hanyang University
Type: Journal Article | Journal: Pharmaceutical research | Year: 2016

We developed a new nanoparticle formulation comprised of human serum albumin (HSA) for co-delivery of doxorubicin (Dox) and tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) with the goal of apoptotic synergy in the treatment of colon cancer.TRAIL (0.2, 0.4, 1.0%)- and Dox-loaded HSA nanoparticles (TRAIL/Dox HSA NPs) were prepared by using the nab(TM) technology. Morphological and physicochemical characterizations were investigated by dynamic light scattering and transmission electron microscopy. Synergistic cytotoxicity, apoptotic activity, and potential penetration into mass tumor were determined in HCT116 cell-based systems. Furthermore, antitumor efficacy and tumor targeting were also investigated.TRAIL/Dox HSA NPs were uniformly spherical with sizes of 60~120 nm. The encapsulation efficacy of Dox and TRAIL was 68.9-77.2% and 80.4-86.0%, respectively. TRAIL 1.0%/Dox HSA NPs displayed the best inhibition of HCT116 colon cancer cells; inhibition was 6 times higher than achieved with Dox HSA NPs. The TRAIL 1.0%/Dox HSA NPs formulation was studied further. Flow cytometry analysis and TUNEL assay revealed that TRAIL 1.0%/Dox HSA NPs had markedly greater apoptotic activity than Dox HSA NPs. In HCT116 tumor-bearing BALB/c nu/nu mice, TRAIL 1.0%/Dox HSA NPs had significantly higher antitumor efficacy than Dox HSA NPs (tumor volume; 933.4 mm(3) vs. 3183.7 mm(3), respectively). TRAIL 1.0%/Dox HSA NPs penetrated deeply into tumor masses in a HCT116 spheroid model and localized in tumor sites after tail vein injection.Data indicate that TRAIL 1.0%/Dox HSA NPs offer advantages of co-delivery of Dox and TRAIL in tumors, with potential synergistic apoptosis-based anticancer therapy.


Lee S.-H.,Korea United Pharm. Inc. | Lee J.-H.,Korea United Pharm. Inc. | Cho S.,Korea United Pharm. Inc. | Do S.-H.,Korea University | Woo Y.-A.,Korea United Pharm. Inc.
Archives of Pharmacal Research | Year: 2012

This study showed near Infrared (NIR) and Raman spectroscopy with a multivariate calibration approach were very effective to determine blend uniformity end-point. A set of 36 trimebutine samples containing magnesium stearate, stearic acid, colloidal silicon oxide, talc as excipients (0.9%~1.8%) was acquired from six positions during blending processing with U-type blender from 0 to 30 min. Principle component analysis (PCA) with NIR and Raman spectral data was used to confirm the end-point of blending. After 30 min, the scores of principle component (PC) 1 and principle component (PC) 2 for samples moved into one point, which clearly indicated the mixture of sample became homogenous. In addition, NIR and Raman spectroscopy has been applied to the quantitative analysis of 20 trimebutine samples containing 2~40% in mixture granules, which divided into a calibration set of 15 samples and a prediction set of 5 samples for NIR spectral data. The standard error of calibration (SEC) and standard error of prediction (SEP) are 0.15% and 0.13%, respectively using NIR while SEC and SEP of 0.95% and 0.91% are obtained using Raman spectroscopy. The results showed the NIR and Raman spectroscopy with a multivariate calibration such as PCA and PLS provide the possibility of real time monitoring of homogeneity and content uniformity during blending process.


Lee Y.,Hanyang University | Kim J.,Hanyang University | Lee S.,Hanyang University | Woo Y.-A.,Korea United Pharm. Inc. | Chung H.,Hanyang University
Talanta | Year: 2012

Direct transmission Raman measurements for analysis of pharmaceuticals in capsules are advantageous since they can be used to determine active pharmaceutical ingredient (API) concentrations in a non-destructive manner and with much less fluorescence background interference from the capsules themselves compared to conventional back-scattering measurements. If a single calibration model such as developed from spectra simply collected in glass vials could be used to determine API concentrations of samples contained in capsules of different colors rather than constructing individual models for each capsule color, the utility of transmission measurements would be further enhanced. To evaluate the feasibility, transmission Raman spectra of binary mixtures of ambroxol and lactose were collected in a glass vial and a partial least squares (PLS) model for the determination of ambroxol concentration was developed. Then, the model was directly applied to determine ambroxol concentrations of samples contained in capsules of 4 different colors (blue, green, white and yellow). Although the prediction performance was slightly degraded when the samples were placed in blue or green capsules, due to the presence of weak fluorescence, accurate determination of ambroxol was generally achieved in all cases. The prediction accuracy was also investigated when the thickness of the capsule was varied. © 2011 Elsevier B.V. All rights reserved.


Non-destructive and rapid determination methods were developed for aceclofenac controlled release (CR) tablets. The tablet is composed of two layers, rapid release and controlled release (CR) layers. The pharmaceutical manufacturing process for CR granules is very critical for dissolution control of CR tablets. During processing, a rapid and nondestructive method to test content uniformity of aceclofenac granules is required. Chemometrics using near-infrared (NIR) and Raman spectroscopy have found significant uses in quantitative analysis of pharmaceutical products in complex matrixes. Most of the pharmaceutical products can be measured directly with little or no sample preparation using these spectroscopic methods. This study showed NIR and wide area illumination Raman spectroscopy with partial least squares (PLS) was very effective for the content uniformity of granules while high performance liquid chromatography (HPLC), a conventional method, was time-consuming and ineffective for real time control. This study showed that on-line control of content uniformity control of aceclofenac CR tablets can be achieved using NIR and Raman spectroscopy.


Disclosed herein is a sustained-release tablet of levodropropizine comprising: an immediate-release layer containing levodropropizine; and a sustained-release layer containing levodropropizine and a release-controlling polymer.


Provided is a controlled-release preparation administered orally once a day that exhibits an optimum pharmacological clinical effect, prepared in the form of a bilayered tablet, a dual tablet, or a multilayered tablet including an immediate-release layer containing aceclofenac, a water-soluble additive, an insoluble additive, a solubilizer, a disintegrating agent and a filler, and a slow-release layer containing aceclofenac, a slow-release base, a disintegrating agent, a binder, a filler, a fluidizer, a solubilizer, and a lubricant.


The formulation for oral administration of the present invention containing Mosapride or its salt is a double layer formulation consisting of a fast-release layer for rapid release of a drug and a sustained-release layer for slow release in order to simultaneously satisfy the rapid exhibition of pharmacological activities and sustained maintenance of pharmacological activities for 24 hours, wherein the high-viscosity hydroxypropyl methylcellulose (HPMC) and the low-viscosity HPMC are used in mixture such that the content of a high viscosity HPMC as a controlled-release matrix within the sustained-release layer has a higher content, thereby capable of controlling the dissolution rate in the regions having different pH values within the gastrointestinal tract and/or the retention time in the gastrointestinal tract. Additionally, the formulation of the present invention is a small-sized preparation with a total weight of 200 mg or less, preferably from 150 mg to 160 mg, thus capable of improving drug compliance of patients.


The formulation for oral administration of the present invention containing Mosapride or its salt is a double layer formulation consisting of a fast-release layer for rapid release of a drug and a sustained-release layer for slow release in order to simultaneously satisfy the rapid exhibition of pharmacological activities and sustained maintenance of pharmacological activities for 24 hours, wherein the high-viscosity hydroxypropyl methylcellulose (HPMC) and the low-viscosity HPMC are used in mixture such that the content of a high viscosity HPMC as a controlled-release matrix within the sustained-release layer has a higher content, thereby capable of controlling the dissolution rate in the regions having different pH values within the gastrointestinal tract and/or the retention time in the gastrointestinal tract. Additionally, the formulation of the present invention is a small-sized preparation with a total weight of 200 mg or less, preferably from 150 mg to 160 mg, thus capable of improving drug compliance of patients.


The present invention relates to a solid preparation including a Pelargonium sidoides extract and a silicic acid compound, which is allowed to be formulated in a solid form by direct adsorption of the Pelargonium sidoides extract onto a silicic acid compound, and a preparation method thereof. Since the solid preparation including the Pelargonium sidoides extract and the silicic acid compound of the present invention has higher stability than a liquid preparation such as syrup, and has no additives such as sugars, there is no concern about microbial contamination or spoilage of the preparation. In addition, it is possible to pack the solid preparation individually. Since the solid preparation is smaller in volume than the liquid preparation, it is highly portable, and there is also a convenience that no additional tools are needed to take the drug. Further, the active ingredient can be taken at the equal amount every time.


Provided is a slow-release tablet including cilostazol as a pharmacologically active component, which is efficacious in suppressing aggregation of blood platelets and promoting vascular relaxation by inhibiting phosphodiesterase types. The slow-release cilostazol tablet has an extended elution time so that the slow-release cilostazol tablet can be taken once daily for convenience of drug use, and minimizes the manifestation of headache which is one side effect caused when women, the elderly and children take conventional cilostazol preparations so that the convenience of drug use can be improved. Also, the slow-release cilostazol tablet exhibits a stable elution pattern with no variation in elution rate according to changes in pH in the stomach and intestines, as well as an effect of delaying the release of a drug, using a mixture of hydroxypropyl methylcellulose and a carbomer as a release-controlling polymer.

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