• 제목/요약/키워드: active pharmaceutical ingredients

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Ingredients of Tyrosinase and Elastase Inhibitory Activity from Calyx of Diospyros kaki Thunberg (감꼭지의 Tyrosinase와 Elastase 저해 활성 성분)

  • Cha, Bae Cheon;Lee, Eun Hee
    • Korean Journal of Pharmacognosy
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    • v.44 no.2
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    • pp.182-187
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    • 2013
  • This study was conducted to investigate glutathione S-transferase(GST) activity, tyrosinase inhibitory effect and elastase inhibitory effect in persimmon calyx(calyx of Diospyros kaki Thunberg) for screening of functional materials from natural products. As a result, EtOAc extract of persimmon calyx turned out to be having tyrosinase inhibitory effect and elastase inhibitory effect. The active constituents of tyrosinase and elastase inhibitory effect were isolated from EtOAc extract of persimmon calyx. Their structure of compounds were identified as ursolic acid and (-)-daucosterol by spectroscopic evidence, respectively.

Pharmaceutical Formulation and Evaluation of Sustained - Release Hydrophilic Matrix Tablet of Cefatrizine Propyleneglycol Using Polyethylene Oxide (폴리에틸렌옥사이드를 이용한 세파트리진프로필렌글리콜 서방성매트릭스 정제의 제조 및 평가)

  • Lee, Eon-Hyoung;Park, Sun-Young;Jee, Ung-Kil;Kim, Dong-Chool
    • Journal of Pharmaceutical Investigation
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    • v.31 no.1
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    • pp.37-41
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    • 2001
  • Various characteristics of polyethylene oxide (PEO) are useful for drug delivery systems. In this study, PEO was used as a sustained release matrix system containing cefatrizine propyleneglycol (Cefa-PG) which is a new semi-synthetic broad-spectrum and orally active cephalosporin. Five kinds of sustained release matrix tablets were formulated with various content of PEO and other ingredients. And three types of matrix tablets were formulated of which compositions were the same but the hardness was different. It was found that PEO content influenced drug release rate. Increasing PEO content, the drug release rate from matrix tablets was decreased. In addition, Avicel, one of the ingredients of matrix components, changed the drug release from the sustained release PEO matrix tablets. With increasing Avicel content, the rate of drug release was increased. For the effect of hardness of matrix tablets, the rate of drug release is decreased with increasing hardness. In comparison of bioavailability parameters after oral administration of Cefa-PG PEO matrix tablets and general Cefa-PG capsule in beagle dog, the sustained release PEO matrix tablets is more useful than a general dosage form. $AUC^{0-12}$ of the sustained release PEO matrix tablet and the general dosage form was 1.16 and 0.644 respectively.

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Integration of virtual screening and proteomics reveals potential targets and pathways for ginsenoside Rg1 against myocardial ischemia

  • Rongfang Xie;Chenlu Li;Chenhui Zhong;Zuan Lin;Shaoguang Li;Bing Chen;Youjia Wu;Fen Hu;Peiying Shi;Hong Yao
    • Journal of Ginseng Research
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    • v.48 no.4
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    • pp.395-404
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    • 2024
  • Background: Ginsenoside Rg1 (Rg1) is one of the main active components in Chinese medicines, Panax ginseng and Panax notoginseng. Research has shown that Rg1 has a protective effect on the cardiovascular system, including anti-myocardial ischemia-reperfusion injury, anti-apoptosis, and promotion of myocardial angiogenesis, suggesting it a potential cardiovascular agent. However, the protective mechanism involved is still not fully understood. Methods: Based on network pharmacology, ligand-based protein docking, proteomics, Western blot, protein recombination and spectroscopic analysis (UV-Vis and fluorescence spectra) techniques, potential targets and pathways for Rg1 against myocardial ischemia (MI) were screened and explored. Results: An important target set containing 19 proteins was constructed. Two target proteins with more favorable binding activity for Rg1 against MI were further identified by molecular docking, including mitogen-activated protein kinase 1 (MAPK1) and adenosine kinase (ADK). Meanwhile, Rg1 intervention on H9c2 cells injured by H2O2 showed an inhibitory oxidative phosphorylation (OXPHOS) pathway. The inhibition of Rg1 on MAPK1 and OXPHOS pathway was confirmed by Western blot assay. By protein recombination and spectroscopic analysis, the binding reaction between ADK and Rg1 was also evaluated. Conclusion: Rg1 can effectively alleviate cardiomyocytes oxidative stress injury via targeting MAPK1 and ADK, and inhibiting oxidative phosphorylation (OXPHOS) pathway. The present study provides scientific basis for the clinical application of the natural active ingredient, Rg1, and also gives rise to a methodological reference to the searching of action targets and pathways of other natural active ingredients.

A Study on the Vinegar Fermentation Processes of Fresh Korean Ginseng Extract Using Mix Microbial Yinkin (유익하게 인체에 작용하는 균(유인균)을 이용한 인삼발효식초 제조과정에 대한 특성연구)

  • Hwang, Se Ran;Destiani, Supeno;Kwon, Soon Hong;Chung, Sung Won;Kwon, Soon Goo;Park, Jong Min;Kim, Jong Soon;Choi, Won Sik
    • Journal of the Korean Society of Industry Convergence
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    • v.20 no.4
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    • pp.345-350
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    • 2017
  • Saponin is the most pharmaceutical active ingredients of the ginseng plant, it was called "Ginsenoside" which means the Glycoside of ginseng that composed glycosides and aglycones. The human body will absorb the saponin easily if these substrate was decomposed by active microorganism. Fermentation is the most convenient technique to decompose this active ingredients. The purpose of this research was to study the sugar content, pH and acidity development during the ginseng fermentation process. Fresh Korean ginseng and red ginseng extract was used as the main ingredient. The concentrated of pure ginseng extract was added to increase the saponin extract. Furthermore, the mix microbial powder was added as starter to increase the fermentation efficiency. The ginseng was fermented in fermentation chamber at temperature $37^{\circ}C$ during 70 days. In the end of experiment the sugar content was decreased from 24% to 7.65%, The pH was decreased from 6.5 to 3.4, and the acidity level was incresed from 0% to 1.2%.

Therapeutic Duplication Criteria Development of Respiratory System Drugs (호흡기계 작용 약물의 치료군 중복처방 평가기준 개발)

  • Choi, Kyung-Eob;Sohn, Hyun-Soon;Kim, Nam-Hyo;Shin, Hyun-Taek;Lee, Young-Sook
    • YAKHAK HOEJI
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    • v.56 no.2
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    • pp.126-135
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    • 2012
  • Purpose: To develop therapeutic duplication criteria for the drugs used for respiratory diseases. Method: Therapeutic duplication was defined as "more than 2 drug ingredient-usage in which each has the same therapeutic effect and combination therapy does not confer additional therapeutic benefit". Respiratory system drugs approved in Korea were examined for the study. The WHO's Anatomical Therapeutic Chemical Classification System was used for grouping of the corresponding drug ingredients. The principles and recommendations on combination usage or multiple drug regimens were reviewed by using the clinical practice guidelines, textbooks, product labelings, and clinical articles. Clinical expert group consultation was performed and expert opinions were incorporated into the final criteria. Results: Nine hundred sixty two drug products with Korean Food and Drug Administration classification codes of 141, 149, 222, and 229 were evaluated, of which 87 active ingredients were composed. The drug ingredients were classified into 12 groups (antihistamines, oral nasal decongestants, leukotriene receptor antagonists, inhaled anticholinergics, inhaled corticosteroids, oral ${\beta}2$-agonists, long-acting ${\beta}2$-agonists, short-acting ${\beta}2$-agonists, xanthines, antiallergics, mucolytics and cough suppressants). The use of more than 2 drug ingredients including the same group was therapeutic duplication, and thus combination should be recommended not to be used. Conclusion: Twelve drug groups were identified as therapeutic duplication criteria. Combination therapy within each group should not be used otherwise therapeutic benefits outweigh potential risks.

Improvement of Hydrolysis and Bioavailability of Coprecipitated Products of Coptidis Rhizoma and Scutellariae Radix by β-Glucuronidase (베타-글루쿠로니다제에 의한 황련.황금 공침물의 가수분해 및 생체이용률 증가)

  • Kim, Mi-Jeong;Kim, Nam-Soon;Kim, Young-Il;Kim, Dae-Keun;Yang, Jae-Heon
    • Journal of Pharmaceutical Investigation
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    • v.33 no.2
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    • pp.91-97
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    • 2003
  • During the preparation of decoction from the mixture of Coptidis Rhizoma and Scutellariae Radix, insoluble copreciptate was formed. The coprecipitated product (COP) was composed of berberine and baicalin which was the active ingredient of Coptidis Rhizoma and Scutellariae Radix, respectively. COP was slightly soluble in water and could not be well absorbed after oral administration. This poor bioavailibility might be associated with its poor aqueous solubility. With the purpose of increasing the solubility and bioavailibility of COP, hydrolysis of COP by ${\beta}-glucuronidase$ was carried out. Hydrolyzed products (HOP) of COP were identified and assayed for active ingredients. The partition coefficient study, in situ absorption test, and pharmacokinetic study after oral administration were also performed. COP was found to be consisted of berberine and baicalin with molecular ratio of 1 to 1. This compound was hydrolyzed to berberine and baicalin by ${\beta}-glucuronidase$. The rate of hydrolysis was higher at higher temperature up to $50^{\circ}C$ and higher concentration of ${\beta}-glucuronidase$ up to 2500 unit under our experimental conditions. Baicalein, which is more liphophilic than baicalin, showed greater absorption in small intestine than baicalin did. The plasma concentrations of berberine and baicalein after oral administration of HOP were significantly higer than those of COP. The possible mechanism of increased bioavailibility of berberine and baicalein could be the hydrolysis of COP by ${\beta}-glucuronidase$. On the basis of the above results, it might be said that HOP should be a suitable preparation for increasing the bioavailibility of Coptidis Rhizoma and Scutellariae Radix.

Development of Novel Cosmetic Formulations using Foams (기포를 이용한 차별화된 화장품 제형 개발)

  • Cho, Wan-Goo
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.38 no.1
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    • pp.1-13
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    • 2012
  • In this review, the use of air bubbles in the pharmaceutical and cosmetic formulations was discussed. The foam bubbles show different characteristics depending on the foaming agents and foam generating devices. The foam bubbles are generated in the form of dispersion of gas bubbles in a solvent. The assessment of stability and rheological properties of bubbles are the starting point for the formulation to be used. Pharmaceutical and cosmetic uses of bubbles are substantially growing, and the foam formulations of drugs can be used for rectal, vaginal, and dermal symptoms. The foam formulation is used in hair mousse, makeup foundation, and sunscreen cosmetics in basic cosmetics. Recently, a lot of studies and patents have been filed in stabilization of active ingredients and delivery of the active ingredient in terms of foam formulations. In the future, foam formulations are expected to be used as novel cosmeceutical formulations.

Non-clinical pharmacokinetic behavior of ginsenosides

  • Won, Hyo-Joong;Kim, Hyun Il;Park, Taejun;Kim, Hyeongmin;Jo, Kanghee;Jeon, Hyojin;Ha, Seo Jun;Hyun, Jung Min;Jeong, Aeri;Kim, Jung Sik;Park, Ye Jin;Eo, Yun Ho;Lee, Jaehwi
    • Journal of Ginseng Research
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    • v.43 no.3
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    • pp.354-360
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    • 2019
  • Ginsenosides, the major active ingredients of ginseng and other plants of the genus Panax, have been used as natural medicines in the East for a long time; in addition, their popularity in the West has increased owing to their various beneficial pharmacological effects. There is therefore a wealth of literature regarding the pharmacological effects of ginsenosides. In contrast, there are few comprehensive studies that investigate their pharmacokinetic behaviors. This is because ginseng contains the complicated mixture of herbal materials as well as thousands of constituents with complex chemical properties, and ginsenosides undergo multiple biotransformation processes after administration. This is a significant issue as pharmacokinetic studies provide crucial data regarding the efficacy and safety of compounds. Moreover, there have been many difficulties in the development of the optimal dosage regimens of ginsenosides and the evaluation of their interactions with other drugs. Therefore, this review details the pharmacokinetic properties and profiles of ginsenosides determined in various animal models administered through different routes of administration. Such information is valuable for designing specialized delivery systems and determining optimal dosing strategies for ginsenosides.

Growth Characteristics, Main Constituents and Antioxidant Activities in Local Accessions of Sophora flavescens AIT. (고삼 수집종의 생육특성, 주요성분 및 항산화 활성)

  • Kwon, A Reum;Kim, Sun Ick;Seong, Bong Jae;Jee, Moo Geun;Lee, Ka Soon;Kim, Hyun Ho;Doh, Eun Soo
    • Korean Journal of Medicinal Crop Science
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    • v.28 no.5
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    • pp.360-370
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    • 2020
  • Background: Sophora flavescens AIT root is used as a herbal medicine in Asian culture. This study was aimed at selecting the best cultivars, by comparing growth characteristics, active ingredients, and antioxidant activities. Methods and Results: A total twenty nine accessions of S. flavescens were collected from five different regions in Korea. Plant height, leaf length, peduncle length, fresh root weight, and seed weight were the growth characteristics selected. Antioxidant activity was determined by measuring the total polyphenol (TPC) and total flavonoid contents (TFC) as well as the radical scavenging activity of DPPH, ABTS and FRAP. Oxymatrine and matrine, active ingredients in S. flavescens were analyzed by HPLC. Results indicated that accession YS-11 had the highest plant height (152.5 cm) and peduncle length (54.0 cm). The fresh root weight was highest in JA-01 at 4.9 kg, while the highest total seed weight was recorded in accession BH-04 at 77.7 g. The YS-03 accession contained the highest oxymatrine and matrine total contents (0.9616% and 0.9638%, respectively). Accessions BH-02, YS-11, YS-05, and MJ-03 had the highest levels of antioxidant activity (p < 0.05). Oxymatrine showed a high correlation with TPC and FRAP. TPC showed high correlations with TFC, DPPH, ABTS and FRAP. TFC showed a high correlation with DPPH. Conclusions: The superior lines can be selected for use as standard variety breeding material by comparing the growth characteristics of the accessions.

Skin Permeation and Crosslinking with Biological Tissue of the Hydrolyzed Products of Gardeniae Fructus Extract (치자엑스 가수분해물 제제의 피부투과 및 생체 피부조직과의 교차결합에 관한 연구)

  • Yang, Jae-Heon;Lee, Nam-Hee
    • Journal of Pharmaceutical Investigation
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    • v.35 no.1
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    • pp.7-16
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    • 2005
  • Gardeniae Fructus is consisted of geniposide and it's derivatives. For the purpose of treatment of skin disease, geniposide and hydrolyzed products (HP) of Gardeniae Fructus were studied on skin permeation and cross1inking with biological tissue. The hydrolyzed products (HP) and active ingredients of Gardeniae Fructus were identified and investigated about skin permeability. Genipin has provided low cytotoxic cross1inking reagents and formed stable and biocompatible crosslinked products. The permeation enhancing effects of geniposide and genipin under the hydrolyzed products of cream and hydrogel preparations were tested using Franz type diffusion cell and the skin of hairless mouse. The remaining proportions of geniposide and genipin were measured in the hydrolyzed products of cream and hydrogel preparations. The crosslinking of epidermic and endodermic tissue with genipin under the hydrolyzed prodcuts of cream and hydrogel preparation was observed using light microscopy. Increased absorption ratio of the skin of hairless mouse about genipin was higher than that of geniposide. Loads at break, tensile strengths and skin permeation rate of the hydrolyzed products (HP) of cream and hydrogel preparations were higher than the nonhydrolyzed products (NHP). The hydrolyzed products (HP) of cream and hydrogel of Gardeniae Fructus Extracts were proper preparations and crosslinking agents to increase the transdermal absorption with epidermic and endodermic tissue.