• Journal of Pharmaceutical Investigation
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• 제40권2호
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• pp.117-123
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• 2010

Ibudilast, 3-isobutyryl-2-isopropyrazolo[1,5-a]pyridine, is a nonselective inhibitor of cyclic nucleotide phosphodiesterase (PDE). It preferentially inhibits PDE 3A, PDE4, PDE10 and PDE11 as well as a number of the other PDE families, albeit to a lesser extent. Ibudilast is used clinically to treat bronchial asthma and cerebrovascular disorders. Thes e clinical uses are based on the ability of ibudilast to inhibit platelet aggregation, improve cerebral blood flow and attenuate allergic reactions. The purpose of the present study was to evaluate the bioequivalence of two ibudilast capsules, Ketas capsule (Handok Pharmaceuticals Co., Ltd.) and Pinatos capsule (Sam Chun Dang Pharm. Co., Ltd.), according to the guidelines of the Korea Food and Drug Administration (KFDA). The in vitro release of ibudilast from the two ibudilast formulations was tested using KP Apparatus method with various dissolution media. Twenty six healthy male subjects, 23.31${\pm}$1.09 years in age and 70.45${\pm}$8.51 kg in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After a single capsule containing 10 mg as ibudilast was orally administered, blood samples were taken at predetermined time intervals and the concentrations of ibudilast in serum were determined using HPLC/UV detector. The dissolution profiles of two formulations were similar in all tested dissolution media. The pharmacokinetic parameters such as $AUC_t$, $C_{max}$ and $T_{max}$ were calculated, and computer programs (Equiv Test and K-BE Test 2002) were utilized for the statistical analysis of the parameters using logarithmically transformed $AUC_t$, $C_{max}$ and untransformed $T_{max}$. The results showed that the differences between two formulations based on the reference drug, Ketas, were 6.99%, -2.48% and 9.93% for $AUC_t$, $C_{max}$ and $T_{max}$, respectively. There were no sequence effects between two formulations in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log 0.8 to log 1.25 (e.g., log 0.8791~log 1.1861 and log 0.8347~log 1.1199 for $AUC_t$ and $C_{max}$, respectively). Thus, the criteria of the KFDA bioequivalence guideline were satisfied, indicating Pinatos capsule was bioequivalent to Ketas capsule.

• 약학회지
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• 제52권3호
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• pp.188-194
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• 2008

Fexofenadine, ($\pm$)-4-1-hydroxy-4-{4-(hydroxydiphenylmethyl)-1-piperidinyl}-butyl-a,a-dimethyl benzeneacetic acid, is a selective histamine $H_1$ receptor antagonist, and is clinically effective in the treatment of seasonal allergic rhinitis and chronic idiopathic urticaria as a first-line therapeutic agent. The purpose of the present study was to evaluate the bioequivalence of two fexofenadine hydrochloride tablets, $Allegra^{(R)}$ (Handok Pharmaceuticals Co., Ltd.) and Alecort (Samchundang Pharmaceutical Co., Ltd.), according to the guidelines of the Korea Food and Drug Administration (KFDA). The release of fexofenadine from the two fexofenadine hydrochloride formulations in vitro was tested using KP VIII Apparatus II method with various dissolution media. Twenty six healthy male subjects, 25.62$\pm$3.35 years in age and 70.05$\pm$11.71 kg in body weight, were divided into two groups and a randomized 2$\times$2 cross-over study was employed. After a single tablet containing 120 mg as fexofenadine hydrochloride was orally administered, blood samples were taken at predetermined time intervals and the concentrations of fexofenadine in serum were determined using HPLC with fluorescence detector. The dissolution profiles of two formulations were similar in all tested dissolution media. The harmacokinetic parameters such as $AUC_t$, $C_{max}$ and $T_{max}$ were calculated, and ANOVA test was utilized for the statistical analysis of the parameters using logarithmically transformed $AUC_t$, $C_{max}$ and untransformed $T_{max}$. The results showed that the differences between two formulations based on the reference drug, $Allegra^{(R)}$, were -1.37, 5.22 and 16.50% for $AUC_t$, $C_{max}$ and $T_{max}$, respectively. There were no sequence effects between two formulations in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log 0.8 to log 1.25 (e.g., log 0.83$\sim$log 1.08 and log 0.81$\sim$log 1.03 for $AUC_t$ and $C_{max}$, respectively). Thus, the criteria of the KFDA bioequivalence guideline were satisfied, indicating Alecort tablet was bioequivalent to $Allegra^{(R)}$ tablet.

• Bulletin of the Korean Chemical Society
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• 제30권9호
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• pp.2007-2010
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• 2009

Donepezil hydrochloride is a reversible acetylcholinesterase inhibitor that is used in the treatment of Alzheimer’s disease to improve the cognitive performance. It shows different crystalline forms including hydrates. Therefore, it is very important to confirm the polymorphic forms in the formulations of pharmaceutical materials because polymorphs of the same drug often exhibit significant differences in solubility, bioavailability, processability and physical/chemical stability. In this paper, four different forms of donepezil hydrochloride were prepared and characterized using X-ray powder diffraction, Fourier transform infrared, and solid-state nuclear magnetic resonance (NMR) spectroscopy. This study showed that solid-state NMR spectroscopy is a powerful technique for obtaining structural information and the polymorphology of pharmaceutical solids.

• Journal of Pharmaceutical Investigation
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• 제38권6호
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• pp.429-432
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• 2008

Drug delivery systems (DDS) have entered mainstream in the pharmaceutical industry in the recent years. Major pharmaceutical companies as well as small or medium-sized biotechnology companies are developing various DDS-based products. We have established Drug Delivery System Company Database, which is an online searchable database of companies that develop DDS-based products and technologies or supply formulations and/or materials. Company summary, products and key technologies are listed in the database. DDS technology fields also include administration routes and indications of drugs. DDS terminologies, Statistical analysis, Useful Links, Glossary and Comments pages are also provided.

• 고려인삼학회:학술대회논문집
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• 고려인삼학회 1998년도 Advances in Ginseng Research - Proceedings of the 7th International Symposium on Ginseng -
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• pp.138-145
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• 1998

A validated and reproducible HPLC method was developed for the profiling and quantitative analysis of ginsenosides in commercial products available in North America. Analysis of 280 Panax ginseng and Panax quinquefolius products showed profiles indicative of the presence of ginsenosides in the majority of these products. However, the quantitative contents of the products vary greatly, not only in products of different formulations, but also of products within each of the fromulations examined.

• Archives of Pharmacal Research
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• 제29권10호
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• pp.921-927
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• 2006

Prolonged release micro particles of clarithromycin (CL) were prepared using Eudragit RL 100 and RS 100 by spray-drying and casting-drying techniques. For the characterization of those microparticles, preparation yield, particle size distribution, X-ray diffraction, thermal behavior, active agent content and in vitro dissolution from the microparticles were performed. HPLC was used for the assay of clarithromycin and the assay method was validated. All the formulations obtained showed prolonged release when compared to pure clarithromycin. Microparticles prepared by spray-drying method had a slower release compared to those of casting drying method. Spray-drying method seems to be a more suitable method to prepare microparticles for prolongation in release.

• 약학회지
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• 제49권4호
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• pp.268-274
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• 2005

Paclitaxel is an effective antineoplastic agent against ovarian, colon and breast tumors. But there have been many difficulties to formulate this drug due to the extremely low aqueous solubility. Paclitaxel is currently formulated in a vehicle composed of Cremophor EL and absolute ethanol mixture which is $5\~20$ fold diluted in normal saline or $5\%$ dextrose solution before I.V. injection. However, this formulation has many problems such as allergic reactions and drug precipitation on aqueous dilution. To overcome these problems, we prepared the micelle and microemulsion systems for parenteral administration of paclitaxel by using glycofurol, $Soluto^{(R)}lHS$ 15 and oleic acid. Phase diagram, pH-rate stability, particle size distributions and pharmacokinetics of the systems were studied. Micelles and microemulsions formulated as nano-particle delivery system were physically and chemically stable. Therefore, these formulations might be the promising alternative candidate for the parenteral delivery of paclitaxel.

• Journal of Pharmaceutical Investigation
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• 제37권5호
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• pp.281-286
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• 2007

For transdermal delivery of porcine placenta extract (PPE), various emulsion formulations were prepared and evaluated. Polysorbate surfactants were used as emulsifiers and various C-18 unsaturated fatty acids as enhancers. The skin permeation of PPE was tested using a cellulose nitrate membrane-loaded Franz cell apparatus. Among emulsifiers, Tween 20 provided higher penetration effect than did Tween 80. Meanwhile, of various fatty acids, linolenic acid (18:3) revealed the highest skin permeation of PPE than the other C-18 unsaturated fatty acids. Stability of PPE emulsions was determined by cycles of freezing and thawing processes. The stability of emulsions depended on the percentage of Tween 20. Minimum 20% of Tween 20 was required to stabilize emulsions at room temperature for several days. Taken together, our results suggest that Tween 20 and linolenic acids might be key components to formulate PPE emulsion to provide the desirable skin permeability and stability.

• Journal of Pharmaceutical Investigation
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• 제36권5호
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• pp.293-297
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• 2006

Curcumin is a phytochemical compound with anticancer activity. Although curcumin has substantial pharmacological effect against various cancers, the low solubility of curcumin has hindered its development. For an organic solvent-free injectable formulation, we encapsulated curcumin in various liposomes. Due to its lipophilic property, curcumin was placed in the membrane region of liposomes. Curcumin was stably encapsulated in all formulations tested in this study. The cellular uptake of curcumin delivered in liposomal formulations or free form was measured in K562 human leukemia cell lines using a flow cytometry and MTT viability assay, respectively. Although all the liposomes could solubilize curcumin, the cellular levels and the anticancer effects of liposomal curcumin varied with the composition of liposomes. Moreover, liposomal curcumin down-regulated the expression of Notch-1, the molecule involved in the carcinogenesis, to the similar extent to free curcumin dissolved in dimethyl sulfoxide. These results warrant the development of liposomal curcumin as an injectable formulation for leukemia treatment.

• Journal of Pharmaceutical Investigation
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• 제38권5호
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• pp.325-329
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• 2008

To enhance the skin delivery of genistein (GT), a soybean isoflavone having anti oxidative activity, comparative formulation studies including liposomes were carried out. GT-loaded conventional and elastic liposomal gel showed the enhanced skin deposition and photoprotection effect as well, in comparison to GT suspension. Elastic liposomes composed of soybean phosphatidylcholine and sodium deoxycholate (85:15, w/w%) were superior to conventional liposomes and were of characteristics as follows: about 130 nm in size; 85% encapsulation efficiency of GT; 5.8% skin deposition of applied dose; 40% inhibition effect on UVB-induced $H_2O_2$ production. Photoprotection effect was closely related to skin deposition of GT. In conclusion, it is possible to suggest that elastic liposomes could be a promising nanocarrier system for efficient skin delivery.