• 대한화장품학회지
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• 제41권4호
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• pp.315-324
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• 2015

본 논문에서는 양친매성물질인 $C_{12-20}$ 알킬글루코사이드, $C_{14-22}$ 알코올 및 베헤닐알코올로 구성된 액정 에멀젼을 제조하고 그 특성 및 in vitro 피부 투과 연구를 수행하였다. 액정 에멀젼의 배합비 실험 결과, $C_{12-20}$ 알킬글루코사이드 0.8%, $C_{14-22}$ 알코올 3.2% 및 베헤닐알코올 4%에서 선명한 액정 구조가 관찰되었다. 액정 에멀젼과 비교군으로 O/W 에멀젼의 물리적 특성을 비교한 결과, 액정 에멀젼과 O/W 에멀젼의 점성은 각각 $1871.26{\sim}1.15Pa{\cdot}s$ 및 $1768.69{\sim}1.14Pa{\cdot}s$이었으며, 전단응력은 액정 에멀젼은 190.45 ~ 919.38 Pa, O/W 에멀젼은 178.68 ~ 909.18 Pa로 측정되었다. 저장 탄성률은 액정 에멀젼은 4487.82 ~ 8195.59 Pa, O/W 에멀젼은 3428.53 ~ 9157.45 Pa, 탄성에 대한 점성의 비인 tan (delta) 값은, 액정 에멀젼은 0.23 ~ 0.25, O/W 에멀젼은 0.43 ~ 0.19로 나타났다. 경피 수분 함량 측정 결과, 액정 에멀젼은 O/W 에멀젼에 비하여 사용 후 1 h부터 6 h까지 유의적으로 더 높은 피부 수분 함량을 나타냈으며, 경피 수분 손실에서는 30 min부터 4 h까지 유의적으로 수분 손실 억제 효과를 나타내었다. 글리시리직애씨드를 이용한 피부 투과 실험 결과, 24 h 동안 피부 투과량은 액정 에멀젼($64.58{\mu}g/cm^2$), O/W 에멀젼($37.07{\mu}g/cm^2$), 부틸렌글라이콜 용액($41.05{\mu}g/cm^2$) 순으로 나타났고, 시간별 투과능 관찰 결과는 8 h 이후부터 액정 제형에서 피부 투과능이 증가하는 것으로 나타났다. 결론적으로 액정 에멀젼은 피부의 보습 효과를 증진시킬 뿐만 아니라 기능성 소재의 효율적인 피부 전달체로서 응용 가능성이 있음을 시사한다.

• Journal of Pharmaceutical Investigation
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• 제36권6호
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• pp.393-399
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• 2006

This study was aimed to design, formulate and characterize the moisture-activated patches containing acyclovir for antiviral action. Gel intermediates for film-type patches were prepared with mucoadhesive polymer, viscosity builders, enhancers and acyclovir. Patches containing acyclovir were characterized by in vitro measurement of drug release rates through a cellulose barrier membrane, and of drug flux through the hairless mouse skin. Film-type patches obtained were uniform in the thickness and showed a mucoadhesive property when contacted with moisture. The formulation was optimized, which consisted of $Cantrez^{\circledR}$ AN-169(2%), $Kollidon^{\circledR}$ VA 64(1%), $Natrosol^{\circledR}$(1%), hydroxypropyl-$\beta$-cyclodextrin(1%) and dimethylsulfoxide(0.5%). Release rates of acyclovir patches increased dose-dependently. The addition of terpenes such as d-limonene or cineole increased release rates of acyclovir, but decreased permeation rates. The permeation rates were enhanced by 2 and 2.5 times by the addition of glycyrrhizic acid ammonium salt and sodium glycocholate, respectively, compared with that of no enhancer. These results suggest that it may be feasible to deliver acyclovir through the skin or gingival mucosa from the moisture-activated patches.

• Journal of Pharmaceutical Investigation
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• 제30권2호
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• pp.119-125
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• 2000

In an attempt to develop a non-aqueous liquid formulation of practically insoluble biphenyl dimethyl dicarboxylate (DDB), dissolution and permeation studies were performed. Various non-aqueous DDB solutions were formulated and filled into empty hard capsules. Dissolution rates of a new formulation were compared with those of commercially available DDB preparations using one and eight dose units. Dissolution rates after 2 hr of DDB tablets (DDB 25 mg), hard capsules (DDB 7.5 mg) and soft capsules (DDB 7.5 mg) on market and new formulation (DDB 7.5 mg) were 6.3, 15.0, 84.5 and 98.0%, respectively. Higher doses (8 units) resulted in a supersaturation within one hr of dissolution, and dissolved amounts were reduced markedly. Due to the saturation and precipitation, a directly proportional dose-dissolution relationship was not observed. The addition of copolyvidone and/or glycyrrhizic acid ammonium salt to DDB solution in polyethylene glycol 300 and 400 inhibited the formation of precipitates during dissolution and markedly enhanced the rabbit duodenal permeation of DDB. From the site-specific gastrointestinal permeation studies, it was found that permeation rates of DDB after mixing of non-aqueous DDB solutions with aqueous buffered solutions were faster in the order of $rectal\;<\;colonic\;{\risingdotseq}\;ileal\;{\risingdotseq}\;duodenal\;<\;jejunal\;<\;gastric$.

• Biomolecules & Therapeutics
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• 제7권3호
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• pp.263-270
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• 1999

The in vitro permeation of thyrotropin-releasing hormone (TRH) through rabbit nasal, rectal and duodenal mucosae was studied in the absence and presence of an enzyme inhibitor and permeation enhancer. TRH in the donor and receptor solutions was assayed by HPLC. When thimerosal (TM, 0.5 mM) was added to the donor cell as an inhibitor, the permeation rate of TRH (200 $\mu\textrm{g}$/ml) increased linearly as a function of time. Fluxes of TRH through the nasal, rectal and duodenal mucosae were found to be 33.3$\pm$5.9, 11.8$\pm$1.9 and 9.6$\pm$0.7 $\mu\textrm{g}$/$\textrm{Cm}^2$/hr, respectively. The addition of sodium glycocholate, glycyrrhizic acid ammonium salt, sodium taurodihydrofusidate or L-$\alpha$-lysophosphatidylcholine to the donor solution containing TM did not result in the significant increase of permeation flux except for the duodenal mucosa, comparing with that in the presence of TM alone. Consequently, it was suggested that the nasal route was advantageous for systemic delivery of TRH, and the addition of TM and/or an enhancer was necessary to maximize the transmucosal permeation of TRH.

• 동의생리병리학회지
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• 제33권1호
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• pp.39-47
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• 2019

Galgeun-tang (GGT) is a traditional herbal medicine generally used to treat cold, fever, headache, migraine and convulsion. To investigate the difference of ingredient and efficacy of GGT according to production method, mix extract powder and decoction, the quantities of index components, antioxidant and anti-inflammatory effects of two kinds of GGT formulation were compared. The contents of ten index components were simultaneously analyzed with HPLC. A HPLC method was developed and validated for the simultaneous determination. The GGT mix extract powder contained higher puerarin and daidzin content than the decoction, while the GGT decoction contained higher cinnamic acid and glycyrrhizic acid content than the mix extract powder. But ingredient of GGT mix extract powder and decoction was statistically very similar (r=0.8335). GGT decoction showed higher antioxidant effect than GGT mix extract powder, but the difference was low. The patterns of productions for NO, iNOS, COX-2, TNF-${\alpha}$, IL-$1{\beta}$ and IL-6 were decreased along the increasing dose of GGT formulation in LPS-induced RAW 264.7 macrophages. The inhibitory effects on NO, iNOS, COX-2, IL-$1{\beta}$ and IL-6 in Raw 264.7 cell were very similar to each other. The results obtained in this study could be used as fundamental data for verifying the equivalence and effectiveness of the herbal medicines.

• 생약학회지
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• 제38권4호
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• pp.299-304
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• 2007

The residual sulfur dioxide in the five herbal medicines dried with burning bituminous coal for 9 hours showed from 339 (Glycyrrhizae Radix) to 1,138 mg/kg (Zingiberis Rhizoma) measured right after drying. The residual sulfur dioxide, from 70.1 to 95.5%, was remained in the above five matrices even after 30 days passed. The marker components concentration in above five herbal medicines like glycyrrhizic acid, betaine et al., were almost same after drying in oven and with burning bituminous coal.

• 동의생리병리학회지
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• 제32권5호
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• pp.333-340
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• 2018

Gamiguibi-tang (GGBT) is a traditional herbal medicine generally used to treat anemia, insomnia, anxiety, and nervousness. GGBT is being commercially produced in the form of extract granule and the quality control methods are specified in the Korean Herbal Pharmacopeia (KHP). However, there is no method to simultaneously analyze compound preparations. In this study, a HPLC method was developed and validated for the simultaneous determination of marker compounds in GGBT. And the contents of marker components and biological activities of the commercial GGBT extract granules (GGBT-2 and GGBT-3) were compared with those of the GGBT decoction (GGBT-1). We confirmed the robustness of simultaneous analytical method by monitoring the contents of the commercial GGBT products and carrying out validation. The marker components of GGBT were geniposide ($8.03{\sim}12.70{\mu}g/mL$), paeoniflorin ($2.79{\sim}4.25{\mu}g/mL$) and glycyrrhizic acid ($5.06{\sim}6.30{\mu}g/mL$). DPPH and ABTS radical scavenging activities were 47.34~63.17% and 21.52~33.61% in the GGBT products concentration of $1,000{\mu}g/mL$, respectively. The GGBT products significantly decreased NO, iNOS and COX-2 production in lipopolysaccharide (LPS)-induced RAW 264.7 macrophages in a concentration-dependent manner. The GGBT-2 had higher contents of marker components and biological activities than GGBT-1 and GGBT-3. The research suggest that be used in developing quality control methods for enhancing the quality of herbal medicines.

• Journal of Pharmaceutical Investigation
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• 제24권2호
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• pp.57-65
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• 1994

To increase the dissolution rate of practically insoluble biphenyl dimethyl dicarboxylate (DDB), various solid dispersions were prepared with water soluble carriers, such as povidone (PVP K-30), poloxamer 407, sodium deoxycholate (SDC) and polyethylene glycol (PEG) 6000, at drug to carrier ratios of 1:3, 1:5 and 1:10 (w/w) by solvent or fusion method. Dissolution test was performed by the paddle method. The dissolution rate of DDB tablets (25 mg) on market was found to be very low (11.44, 9.02 and 6.42% at pH 1.2, 4.0 and 6.5 after 120 min, respectively). However, dissolution rates of DDB from various solid dispersions were very fast and reached supersaturation within 10 min. DDB-PEG 6000 solid dispersion appeared to be better in enhancing the in vitro dissolution rate than others. Furthermore, the incorporation of DDB and phosphatidylcholine (PC) into ${\beta}-cyclodextrin$ at ratios of 1:2:20, 1:5:20 and 1:10:20 resulted in a 4.9-, 11.2- and 19.6-fold increase in DDB dissolution after 120 min as compared with the pure drug, respectively. This might be attributed to the formation of lipid vesicles which entrapped a certain concentration of DDB during dissolution. On the other hand, the permeation of DDB through rabbit duodenal mucosa was examined using some enhancers such as SDC, sod. glycocholate (SGC) and glycyrrhizic acid ammonium salt (GAA). Only trace amounts of DDB were found to permeate through deuodenal mucosa in the absence of enhancer. SDC was found to markedly decrease the permeation flux of DDB, however, SGC and GAA (5 mM) enhanced the flux of DDB 1.6 and 2.4 times higher as compared with no additive, respectively.

• Journal of Periodontal and Implant Science
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• 제42권2호
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• pp.33-38
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• 2012

Purpose: The goal of this study was to evaluate the clinical anitplaque and antigingivitis effects of a mouthrinse containing cetylpyridinium chloride (CPC), triclosan and dipotassium glycyrrhizinate (DPZ) in patients with gingivitis and mild periodontitis. Methods: Thirty-two subjects were randomized into 2 groups. The test group used a mouthrinse containing 0.05% CPC, 0.02% triclosan and 0.02% DPZ, while the control group used a placebo mouthrinse. At baseline, 2 weeks and 4 weeks, the papillary bleeding index (PBI), Turesky-Quigley-Hein plaque index (PI) and L$\ddot{o}$e-Silness gingival index (GI) were assessed. During the experimental period, the patients used the mouthrinse for 30 seconds, 4 to 5 times/day (10 mL/time) within 30 minutes after toothbrushing. Results: No adverse effects appeared in either the experimental or the control group. Regarding PBI, PI and GI values, statistical significance was detected between values at baseline and 2 weeks for both groups (P<0.05). In the experimental group, statistically significantly lower values were detected at 4 weeks compared to at 2 weeks. However, in the control group, no statistically significant difference was detected between the values at 2 weeks and 4 weeks. Additionally, the mean value after 4 weeks for the control group was slightly higher than the mean value after 2 weeks for the control group. Conclusions: This study for 4 weeks demonstrated that mouthrinses containing CPC, triclosan and DPZ may contribute to the reduction of supragingival plaque and gingivitis.

• Genomics & Informatics
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• 제18권4호
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• pp.43.1-43.13
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• 2020

The coronavirus disease 2019 is a contagious disease and had caused havoc throughout the world by creating widespread mortality and morbidity. The unavailability of vaccines and proper antiviral drugs encourages the researchers to identify potential antiviral drugs to be used against the virus. The presence of RNA binding domain in the nucleocapsid (N) protein of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) could be a potential drug target, which serves multiple critical functions during the viral life cycle, especially the viral replication. Since vaccine development might take some time, the identification of a drug compound targeting viral replication might offer a solution for treatment. The study analyzed the phylogenetic relationship of N protein sequence divergence with other 49 coronavirus species and also identified the conserved regions according to protein families through conserved domain search. Good structural binding affinities of a few natural and/or synthetic phytocompounds or drugs against N protein were determined using the molecular docking approaches. The analyzed compounds presented the higher numbers of hydrogen bonds of selected chemicals supporting the drug-ability of these compounds. Among them, the established antiviral drug glycyrrhizic acid and the phytochemical theaflavin can be considered as possible drug compounds against target N protein of SARS-CoV-2 as they showed lower binding affinities. The findings of this study might lead to the development of a drug for the SARS-CoV-2 mediated disease and offer solution to treatment of SARS-CoV-2 infection.