• 약학회지
• /
• 제58권1호
• /
• pp.53-57
• /
• 2014

In recent, the abuse of newly-emerging psychoactive drugs, ('designer drugs') is a rapidly increasing problem in Korean society. Quantitative-structure activity relationship (QSAR) is an alternative method to predict bioactivities of new abused compounds. In this study, cathinone-related new designer drugs, 4-methylbuphedrone and 4-methoxy-N,N-dimethylcathinone were tested for prediction of the bioactivity with QSAR model. The bioactivity of 4-methylbuphedrone and 4-methoxy-N,N-dimethylcathinone was similar to those of methylone. These results suggest that the prediction with QSAR model may provide scientific evidences for regulatory decision.

• Journal of Pharmaceutical Investigation
• /
• 제16권3호
• /
• pp.89-100
• /
• 1986

Although insulin has been available for the treatment of diabetes mellitus for more than half a centry, the deficiency of conventional insulin therapy for diabetic patients have, to this date, not been satisfactorily overcome by any method. The development of potential delivery systems for insulin is highly important to prevent excessive fluctuation of plasma glucose levels, which results in long term complications in the diabetic. There are three major approaches toward development of glucose responding insulin delivery systems: A bioengineering approach is to devise mechanical components capable of releasing insulin in amounts appropriate to varying blood-glucose requirements. A biological approach relies upon cultured, living pancreatic beta cells encapsulated to constitute an insulin delivery unit. A biochemical approach is to synthesize a stable and biologically active glycosylated insulin that is complementary to the binding sites of lectin. This paper will cover several specific areas, including pancreatic transplantation(total or isolated islet cells), artificial pancreases(bioengineering or biological approach), controlled delivery system, glucose sensitive membrane systems, and a self-regulating insulin delivery system.

• Biomolecules & Therapeutics
• /
• 제22권1호
• /
• pp.41-46
• /
• 2014

Enterovirus 71 (EV71) is the predominant cause of hand, foot and mouth disease (HFMD). The antiviral activity of hederasaponin B from Hedera helix against EV71 subgenotypes C3 and C4a was evaluated in vero cells. In the current study, the antiviral activity of hederasaponin B against EV71 C3 and C4a was determined by cytopathic effect (CPE) reduction method and western blot assay. Our results demonstrated that hederasaponin B and 30% ethanol extract of Hedera helix containing hederasaponin B showed significant antiviral activity against EV71 subgenotypes C3 and C4a by reducing the formation of a visible CPE. Hederasaponin B also inhibited the viral VP2 protein expression, suggesting the inhibition of viral capsid protein synthesis.These results suggest that hederasaponin B and Hedera helix extract containing hederasaponin B can be novel drug candidates with broad-spectrum antiviral activity against various subgenotypes of EV71.

• 약학회지
• /
• 제56권4호
• /
• pp.211-216
• /
• 2012

Drug dissolution test has been used for the purpose of both quality control of solid oral dosage forms and predicting in vivo drug release profiles. In this study, the dissolution profiles of buflomedil hydrochloride tablets and ticlopidine hydrochloride tablets were investigated according to the "Guidelines on Specifications of Dissolution tests for Oral dosage forms" of Korean Pharmacopoeia (KP). The analytical method using HPLC was validated. The validation was performed in terms of specificity, linearity, accuracy, precision and limit of quantitation.

• KSBB Journal
• /
• 제26권3호
• /
• pp.217-222
• /
• 2011

Itraconazole is a triazole antifungal agent to inhibit most fungal pathogens. To improve the oral absorption and dissolution of poorly water-soluble itraconazole, microsponge system composed of $Eudragit^{(R)}$ E100 and polyvinyl alcohol(PVA) formulated by quasi-emulsion solvent diffusion method, and its physicochemical properties and pharmacokinetic parameters of itraconazole were studied. The microsponge of itraconazole were discrete free flowing micro sized particles with perforated orange peel like morphology as visualized by scanning electron microscope (SEM). Results showed that the drug loading efficiency, production yield, and particle size of itraconazole microsponge were affected by drug to polymer ratio, the volume of internal phase containing methylene chloride, stirring rate and the concentration of PVA used. Also, the results showed that the dissolution rate of itraconazole from the microsponges was affected by drug to polymer ratio. In other words, the release rate of itraconazole from microsponges was increased from at least 27.43% to 64.72% after 2 h. The kinetics of dissolution mechanism showed that the dissolution data followed Korsmeyer-Peppas model. Therefore, these results suggest that microsponge system can be useful for the oral delivery of itraconazole by manipulating the release profile.

• Journal of Microbiology and Biotechnology
• /
• 제16권4호
• /
• pp.538-542
• /
• 2006

Three new compounds were isolated from the methanol extracts of buckwheat (Fagopyrum esculentum) hull, and their structures were determined to be 6,7-dihydroxy-3,7-dimethyl-octa-2(Z),4(E)-dienoic acid (1), 6,7-dihydroxy-3,7-dimethyl-octa-2(E),4(E)-dienoic acid (2), and 4,7-dihydroxy-3,7-dimethyl-octa-2(E),5(E)-dienoic acid (3) by NMR and MS spectroscopic analyses. These compounds at $500{\mu}g$ concentration showed antimicrobial activity against Staphylococcus aureus, demonstrated by the paper disc method.

• 품질경영학회지
• /
• 제50권4호
• /
• pp.831-842
• /
• 2022

Purpose: This study carried out the Quality by Design (QbD)6σ process to verify the effectiveness and equivalence of the finished D-antigen quantitative test method, and compared the OFAT-based method validation and test result acceptance criteria with the Analytical Quality by Design (AQbD)-based method validation and test method. This is a study on how to reduce the risk of delay in permit change by increasing the reliability of permit data in the existing method by statistically analyzing the results. Methods: With the QbD6σ process, the effectiveness and equivalence of the D-antigen quantitative test method were verified with the data of the existing test method and the new test method. Results: Method validation tests are performed based on AQbD. Critical Method Parameters are identified through risk assessment, and single/combined actions are verified by designing and performing tests for Critical Method Parameters (analysis of variance, full factorial design method). Method validation can be effectively accomplished with the QbD6σ process. Conclusion: The use of QbD6σ can be used to achieve satisfactory results for both pharmaceutical companies and regulators by using appropriate statistical analytical methods for method validation as required by regulatory agencies.

• 대한약학회:학술대회논문집
• /
• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-1
• /
• pp.35-37
• /
• 2003

Efficacy and safety of drugs are evaluated in the process of drug registration along with the basis of setting test method and acceptance criteria for assuring quality of the drugs. Quality of drugs plays a key role to guarantee the efficacy and safety of drugs approved in the evaluation process at the marketing stage after approval. Most important role of pharmacopoeia is to give the basis of assuring the quality of drugs. (omitted)

• 한국환경농학회지
• /
• 제23권4호
• /
• pp.203-210
• /
• 2004

본 연구는 퇴비원료로 지정된 제약업종 부산물(공정오니) 및 화장품 제조업 폐수처리오니를 퇴비로서 활용 가능성을 판단하기 위하여 기존의 일반성분이나 중금속 성분 분석 이외 유기성. 화합물과 기타 여러 생물검정법 등을 활용하여 시용한 오니에 의한 토양 내 비료의 피해를 밝혀내고 이들의 평가방법을 확립하고자 포장시험을 수행하였다. 오니의 처리에 따른 HEM의 함량은 제약업종 오니2(PS2)와 화장품 오니(CS)처리가 각각 0.51, 1.10 mg/kg로 가장 높았고, PAHs의 함량은 제약업종 오니2(PS2) 처리에서 $3,406.8\;{\mu}g/kg$로 가장 높았다. 토양에 서식하는 미소동물의 밀도변화는 생육 중기(7월 23일) 및 수확기(10월 1일) 모두 제약오니2 및 돈분 처리구에서 가장 높았으며, 기타 처리구는 차이가 없이 아주 낮았다. 오니의 처리에 따른 세균 및 사상균의 균수는 제약업종오니2처리에서 각각 136, 909 cfu/g로 가장 많았고, 화장품오니도 각각 440, 236 cfu/g으로 다른 처리에 비해 많은 경향을 보였다. 제약오니 및 화장품오니 처리시 우점세균은 무비, 돈분처리에 비해 일정한 경향이 없었으나 3요소 처리보다 다양한 세균이 검출되었다. 오니의 처리에 따른 우점사상균은 무처리에 비해 제약업종 오니2와 화장품 오리처리에서 형태적 특징이 다른 콜로니가 검출되었으나 다른 처리는 비슷한 경향으로 종류간에 큰 차이는 보이지 않았다. Microcosm test를 통하여 오니 처리 후 3개월이 경과한 토양의 오염정도를 평가한 결과는 제약업종 오니3과 화장품 오니처리는 약간 영향을 받아서 $80{\sim}90%$ 생존하였으나, 제약업종 오니1처리는 처리 2주(14일) 이후에는 급격히 생존율이 떨어져서 4주 이후에는 10%만 생존하였다. 그러나 6개월이 경과한 토양에서는 지렁이의 생존율은 제약업종 오니1처리만 약간 영향을 받은 것으로 보였으며 다른 처리들은 전혀 영향을 받지 않았던 것으로 조사되었다. 유기성 오니의 퇴비원료로 활용은 비료관리법의 비료공정규격 중 퇴비의 비고란에 "퇴비의 원료로 사용 가능한 물질과 사용 불가능한 물질"(별표1)에서 "퇴비의 원료 중 사전 분석검토 후 사용 가능한 원료에 대한 지정요령"에는 유기물과 중금속(8성분) 함량(건물중)과 제조공정 등을 검토하여 지정하고 있으나, 지정된 원료가 과연 퇴비원료로 적합한지 잘 알 수 없으며 또한 앞으로 현재의 퇴비원료 규정을 변경할 필요가 있을 경우를 대비하여 퇴비원료의 적합성 여부를 판별할 수 있는 방법의 개발이 필요하다. 따라서 퇴비원료로 이미 지정('02. 12. 31)된 제약오니 및 화장품 오니를 과량으로 토양에 시용한 후 유해 유기화합물, 미소동물, 미생물 및 생물학적(지렁이) 유해성 검정방법의 도입 가능성을 평가하기 거하여 고추를 재배한 포장에서 비료의 피해시험을 실시한 과 유해 유기화합물과 생물학적(지렁이) 유해성 검정방법은 앞으로 연구를 통해서 보완할 경우 상당히 활용 가능성이 있는 좋은 평가방법인 것으로 생각된다.

• Archives of Pharmacal Research
• /
• 제18권6호
• /
• pp.396-401
• /
• 1995

As a part of trials to develop the antitumor agent from tannins isolated from plants, the antitumor activity of peduculagin, an ellagitannin, isolated from Alnus hirsuta var. microphylla was examined in vitro and in vivo. In vitro, the cytotoxicity was determined by 0.4% typanblue dye exclusion method. peduculagin showed the dose-dependent cytotoxicity against human chronic myelogenous leukemia (K-562), human promyelocytic leukemia (HL-60), mouse lymphoid neoplasm (P388), mouse lymphocytic leukemia (L1210) and mouse sarcoma 180(S180) cell lines. $ED_{50}\; values\; (ED_{50})$ of each cell line were 5.30, 0.92, 2.78, 9.35 and $1.38 \mug/ml$ respectively. The most sensitive cell line was HL-60. In vivo, pedunculagin was administered to ICR mouse with the doses of 50 and $100{\;}{\mu}g/ml$intraperitoneally once at 20 days before S180 inoculation. peduculagin showed the antitumor activity and its T/C ratio (%) was 120.82% in the group of both concentrations.