Clindamycin의 分析에 관한 硏究

李允中,尹汝生,崔點洙 성균관대학교 약학연구소 1989 成均藥硏論文集 Vol.1 No.1

Abstract-Clindamycin is a new antibiotic produced by Streptomyces lincolensis var. lincolensis. It is produced by chlorination of lincomycin. It is active against Gram postive aerobes and especially active against both Gram positive and negative anaerobic pathogens. Various analytical method for quantitation of clindamycin were reported in the literatures. However, no analytical methods has been satisfactory for both sensitivity and reproducibility. The aim of this study was to optimize the bioassay, GLC and HPLC assay conditions for the quality control of clindamycin. Comparison of bioassay, GLC and HPLC methods demonstrated that GLC and HPLC methods were much more accurate and sensitive than the bioassay method. Of 3 methods tested in this study, HPLC method was shown to be the best for convenience and quality control of clindamycin. Statistical tests were performed to comparing the results of the accepted bioassay method with the reference method to see any significant difference between the accepted bioassay and each of the refined bioassay, GLC and HPLC.

A Formal Asymmetric Synthesis of Mugineic Acid : An Efficient Synthetic Route Through Chiral Oxazolidinone

Jung, Young Hoon,Kim, Chang Min 성균관대학교 약학연구소 1999 成均藥硏論文集 Vol.11 No.-

A formal asymmetric synthesis of Mugineic acid was accomplished from cis­­-2-butene-1,4-diol through catalytic Sharpless epoxidation oxidations and coupling reaction.

Structure-Activity Relationship Study of Asiatic Acid Derivatives Against Beta Amyloid (Aβ)-induced Neurotoxicity

Jew, Sang-sup,Yoo, Chi-hyoung,Lim, Doo-yeon,Kim, Heeman,Mook-Jung, Inhee,Jung, Min Whan,Choi, Heesung,Jung, Young-hoon,Kim, Heedoo,Park, Hyeung-geun 성균관대학교 약학연구소 1999 成均藥硏論文集 Vol.11 No.-

Abstract-8 Semi-synthetic derivatives of asiatic acid were prepared and their protective effect against Aβ-induced neurotoxicity was evaluated. Among them, asiatic acid (2), and 4, 16 showed 97, 92 and 87% of protective effect, respectively. ⓒ 2000 Elsevier Science Ltd. All rights reserved.

아펜탈정의 생물학적 동등성 평가

배준호,최경업,지상철,박은석 성균관대학교 약학연구소 1999 成均藥硏論文集 Vol.11 No.-

The bioequivalence of two aceclofenac tablets was evaluated in 14 normal volunteers (age 21∼29yrs) following oral administration. The test product was "Apental tablet" made by Asia Pharmaceutical Co. and the reference was "Airtal tablet" made by Daewoong Pharmaceutical Co.. After one tablet containing 100 mg aceclofenac was administered, blood was taken at predetermined time intervals and the concentration of the drug in plasma was quantitated with an HPLC method. AUC, C_max and T_max were calculated and statistically analyzed for the bioequivalence of the two products. The results showed that the differences in AUC, C_max and T_max between two products were 4.23%, 2.15% and 0%, respectively. The powers for AUC, C_max and T_max were >90%,>90% and 85.8%, respectively. Confidence intervals were within ±20% for three parameters. All of these parameters met the criteria of KFDA for bioequivalence, indicating that "Apental tablet" is bioequivalent to "Airtal tablet". (Kor. J. Clin. Pharm. 1999; 9(1): 44-48)

In vitro chemopreventive effects of plant polysaccharides(Aloe barbadensis Miller, Lentinus edodes, Ganoderma lucidum and Coriolus versicolor)

Kim, Hyung Sik,Kacew, Sam,Lee, Byung Mu 성균관대학교 약학연구소 1999 成均藥硏論文集 Vol.11 No.-

A plant polysaccharide, Aloe gel extract, was reported to have an inhibitory effect on benzo[α]pyrene (B[α]P)-DNA adduct formation in vitro and in vivo. Hence, chemopreventive effects of plant polysaccharides [Aloe barbadensis Miller(APS), Lentinus edodes (LPS), Ganoderma lucidum (GPS) and Coriolus versicolor (CPS)] were compared using in vitro short-term screening methods associated with both initiation and promotion processes in carcinogenesis. In B[α]P-DNA adduct formation, APS (180 ㎍/ml) was the most effective in inhibition of B[α]P binding to DNA in mouse liver cells. Oxidative DNA damage (by 8-hydroxydeoxy-guanosine) was significantly decreased by APS (180 ㎍/ml) and CPS (180 ㎍/ml). In induction of glutathione S-transferase activity, GPS was found to be the most effective among plant polysaccharides. In screening anti-tumor promoting effects, APS (180 ㎍/ml) significantly inhibited phorbol myristic acetate (PMA)-induced ornithine decarboxylase activity in Balb/3T3 cells. In addition, APS significantly inhibited PMA-induced tyrosine kinase activity in human leukemic cells. APS and CPS significantly inhibited superoxide anion formation. These results suggest that some plant polysaccharides produced both anti-geno-toxic and anti-tumor promoting activities in in vitro models and, therefore, might be considered as potential agents for cancer chemoprevention.

Stability of Albuterol in Continuous Nebulization

Hunter, Dee A.,Fox, Janet L.,Yoo, Sun D.,Michniak, Bozena B. 성균관대학교 약학연구소 1998 成均藥硏論文集 Vol.10 No.1

Due to the emergent nature of situations requiring continuous nebulization of albuterol, a premixed albuterol solution would provide faster access to the therapy when required. The purpose of this study was to evaluate the stability of albuterol solutions at a concentration (200㎍/mL) used in continuous nebulization when stored in various containers of polyvinyl chloride bags, polyolefin bags, polypropylene syringes and tubes and borosilicate glass tubes. Solutions were prepared in triplicate in 0.9% sodium chloride stored under refrigerated and room temperatures for seven days. Samples were removed and analyzed using a stability-indicating high-performance Liquid chromatography assay method. Albuterol was found to be stable (>90% of the initial concentration remaining) for at least seven days in all five types of containers under the conditions tested.

Biodegradable polyanhydride devices of cefazolin sodium, bupivacaine, and taxol for local drug delivery : preparation, and kinetics and mechanism of in vitro release

Park, Eun-Seok,Manoj Maniar,Shah, Jaymin C. 성균관대학교 약학연구소 1998 成均藥硏論文集 Vol.10 No.1

The overall objective was to design and evaluate biodegradable implants for local drug delivery in clinical conditions and/or diseases described below, which are currently treated with systemic administration of drugs. Local delivery of cefazolin is desired in conditions such as osteomyelitis, soft-tissue infection and for prevention of post-surgical infections. Similarly, implanting a biodegradable device loaded with taxol in the cavity created by tumor resection will provide high local concentrations of taxol killing the malignant cells which may have survived the surgery, thus preventing metastasis and regrowth of the tumor and also prevent the systemic side effects of taxol. Prolonged reversible nerve blockade required in a number of clinical situations involving acute or chronic pain such as post-surgical pain following herniorrhaphy and thoracotomy can be achieved with local delivery of bupivacaine. Therefore, disk-shaped implants of polyanhydride, P(FAD-SA, 50:50 w/w), loaded with 10% w/w of cefazolin sodium, taxol and bupivacaine were prepared and evaluated for content uniformity and in vitro release characteristics for the above mentioned local drug delivery applications. All of cefazolin sodium was released in 14 days while 90% bupivacaine was released in 35 days. In striking contrast, taxol was released very slowly, and only 15% taxol was released in 77 days. The overall release appeared to be following first order kinetics, and the initial linear profile was fitted to zero order kinetics to obtain release parameters. Since cefazolin is highly water soluble and bupivacaine is moderately water soluble, compared to taxol which is extremely lipophilic, the aqueous solubility of the incorporated drug appeared to influence its release characteristics. Very good correlation was observed between release parameters (A_0, K_0) and the solubility and intrinsic dissolution rate (IDR) of drugs suggesting that the hydrophilic/hydrophobic nature of the drug influences its release from polyanhydride devices. Since polyanhydrides are believed to undergo pure surface erosion, release of the incorporated drug should be independent of its physicochemical properties, however the results presented in this study suggest otherwise. Therefore, P(FAD-SA, 50:50 w/w) may not be undergoing surface erosion, and that diffusion and dissolution properties of the drug in addition to erosion characteristics of the polyanhydride appear to play a role in drug release. Implants prepared and evaluated in this study released cefazolin, bupivacaine and taxol for a prolonged duration of time; however, depending upon the desired duration of release, an appropriate polyanhydride will have to be selected. For example, taxol was released so slowly that a more hydrophilic polyanhydride may have to be selected to release all the drug in a shorter period of time to be of any therapeutic use. Cefazolin implants released the drug for a sufficient duration for osteomyelitis and soft-tissue infection but the release was more prolonged than required for prevention of post-surgical wound infection.

케토프로펜 로오숀의 약물동력학적 특성과 항염증작용

단현광,배준호,박은석,지상철 성균관대학교 약학연구소 1998 成均藥硏論文集 Vol.10 No.1

The pharmacokinetic properties and antiinflammatory activity of 3% ketoprofen lotion (ID-lotion), formulated with poloxamer 407, were evaluated using rats. For the pharmacokinetic study, the lotion, at the dose of 4.5㎎/㎏, was applied on the dorsal skin of rats and the drug concentration in plasma was determined using an HPLC method. As references, ketoprofen suspended in saline was administered orally, and E-lotion, which is a 3% ketoprofen lotion in the Japanese market, was applied transdermally. Following the transdermal application of ID-lotion and E-lotion, C_max were 316±22.3ng/㎖ and 163±12.2ng/㎖, respectively, at the same T_max of 2 hours postdose, while C_max and T_max after oral administration of the drug were 1,030±89.1ng/㎖ and 0.25 hours, respectively. The antiinflammatory activity of the two 3% ketoprofen lotions was evaluated with carrageenen-induced edema method after 50㎎ of the lotions was applied on the paw of rats. ID-lotion showed 67.6% inhibition of the edema formation, while E-lotion showed 34.7%. The calculated ED_50 after transdermal application of ID-lotion was 2.5㎎/㎏, while that after oral administration was 7.0 ㎎/㎏. Based on these results, the relative equiponderal availability of ID-lotion was 296% compared to the oral administration of ketoprofen.

High-performance liquid chromatography with a column-switching system and capillary electrophoresis for the determination of ibuprofen in plasma

Kang, Seong Ho,Chang, Si-Young,Do, Ki-Chan,Chi, Sang-Cheol,Chung, Doo Soo 성균관대학교 약학연구소 1998 成均藥硏論文集 Vol.10 No.1

Quantitative aspects of high-performance liquid chromatography with a column-switching system (CSS-HPLC) and capillary electrophoresis (CE) were investigated for the determination of ibuprofen in plasma. For CSS-HPLC, 100μl of plasma was directly injected onto the column system for the three separation steps: ⑴ deproteinization and fractionation of plasma samples with a polymer-coated mixed-function phase column. ⑵ concentration with an intermediate column and ⑶ final separation with a main column. For CE, a mixture of 50μl of plasma and 1㎖ of acetonitrile was centrifuged and the supernatant was introduced onto the capillary (66㎝×50㎛ I.D.; 62㎝ to detector) at 20℃. Run buffer was 250 mM sodium borate buffer (pH 8.5) and applied electric field was 379 V ㎝^-1. Linear dynamic ranges were 0.1-250 ㎍㎖^-1 in CSS-HPLC and 1-1000 ㎍㎖^-1 in CE. Intra-day and inter-day coefficients of variation were less than 5.6% and 6.5% for CSS-HPLC, 6.3% and 6.5% for CE, respectively. The limits of detection (S/N=3) for CSS-HPLC and CE were 25ng㎖^-1 and 300 ng㎖^-1, respectively. CSS-HPLC was superior in simplicity and sensitivity, while CE was better in efficiency, rapidity, and cost.

랫드에 대한 DWP-311의 급성피하독성시험

곽승준,김형식,천선아,임소영,박현선,한하수,홍채영,안미영,이병무 성균관대학교 약학연구소 1998 成均藥硏論文集 Vol.10 No.1

The acute toxicity of DWP-311 was investigated in Sprague-Dawley rats. DWP-311 was subcutaneously administratered at dose levels of 595, 1,070, 1,930, 3,470, and 6,250 ㎎/㎏. In this study, we daily examined numbers of deaths, clinical signs, body weights, and pathological examinations for 7 days after administration of DWP-311. The results indicate that DWP-311 did not show any toxic effect in rats and the oral LD_50 value was over 6,250 ㎎/㎏ in Sprague-Dawley rats.