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한국약제학회> 약제학회지> Effect of Additive of the Encapsulated Amounts and Solubility of Poorly Water-soluble Ibuprofen in Gelatin Microcapsules

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Effect of Additive of the Encapsulated Amounts and Solubility of Poorly Water-soluble Ibuprofen in Gelatin Microcapsules

Dong Xun Li , Jung Gil Park , Hong Hee Han , Chan Woo Yang , Jun Young Choi , Doug Hon Oh , Chul Soon Yong , Han Gon Choi
  • : 한국약제학회
  • : 약제학회지 37권5호
  • : 연속간행물
  • : 2007년 10월
  • : 269-273(5pages)
피인용수 : 24건

(자료제공: 네이버학술정보)

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Poorly water-soluble ibuprofen and ethanol can be encapsulated in gelatin microcapsule by spray drying technique. To select an optimal formula of ibuprofen-loaded gelatin microcapsule which increased the ethanol content and ibuprofen solubility with the decreased amount of gelatin in the microcapsules, in this study, the effect of gelatin, ibuprofen and sodium lauryl sulfate on the ibuprofen solubility and the amount of ethanol and ibuprofen encapsulated in the gelatin microcapsule were investigated. Ibuprofen solubility and the amount of ethanol encapsulated increased as gelatin and sodium lauryl sulfate increased, reached maximum at 4% and 0.6%, respectively and then followed a rapid decrease. Furthermore, the ibuprofen solubility and the encapsulated ibuprofen content increased as the amount of ibuprofen increased, reaching maximum at 0.5% and beyond that, there was no change in the solubility and ibuprofen content. However, the encapsulated ethanol content remained same irrespective of the amount of ibuprofen. On the basis of increased ibuprofen solubility, our results showed that the formula of ibuprofen-loaded gelatin microcapsule at the ratio of gelatin/ibuprofen sodium lauryl sulfate/water/ethanol of 4/0.5/0.6/30/70 with ibuprofen solubility of about 290㎍/mL and ethanol content of about 160㎍/mg could be a potential oral delivery system for poorly water-soluble ibuprofen.

UCI(KEPA)

I410-ECN-0102-2009-510-008658450

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  • : 의약학분야  > 약품제제
  • : KCI등재
  • : SCOPUS
  • : 격월
  • : 2093-5552
  • :
  • : 학술지
  • : 연속간행물
  • : 1971-2011
  • : 1610


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1Effect of Additive of the Encapsulated Amounts and Solubility of Poorly Water-soluble Ibuprofen in Gelatin Microcapsules

저자 : Dong Xun Li , Jung Gil Park , Hong Hee Han , Chan Woo Yang , Jun Young Choi , Doug Hon Oh , Chul Soon Yong , Han Gon Choi

발행기관 : 한국약제학회 간행물 : 약제학회지 37권 5호 발행 연도 : 2007 페이지 : pp. 269-273 (5 pages)

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Poorly water-soluble ibuprofen and ethanol can be encapsulated in gelatin microcapsule by spray drying technique. To select an optimal formula of ibuprofen-loaded gelatin microcapsule which increased the ethanol content and ibuprofen solubility with the decreased amount of gelatin in the microcapsules, in this study, the effect of gelatin, ibuprofen and sodium lauryl sulfate on the ibuprofen solubility and the amount of ethanol and ibuprofen encapsulated in the gelatin microcapsule were investigated. Ibuprofen solubility and the amount of ethanol encapsulated increased as gelatin and sodium lauryl sulfate increased, reached maximum at 4% and 0.6%, respectively and then followed a rapid decrease. Furthermore, the ibuprofen solubility and the encapsulated ibuprofen content increased as the amount of ibuprofen increased, reaching maximum at 0.5% and beyond that, there was no change in the solubility and ibuprofen content. However, the encapsulated ethanol content remained same irrespective of the amount of ibuprofen. On the basis of increased ibuprofen solubility, our results showed that the formula of ibuprofen-loaded gelatin microcapsule at the ratio of gelatin/ibuprofen sodium lauryl sulfate/water/ethanol of 4/0.5/0.6/30/70 with ibuprofen solubility of about 290㎍/mL and ethanol content of about 160㎍/mg could be a potential oral delivery system for poorly water-soluble ibuprofen.

2Disintegrating Behavior of A Rapidly Disintegrating Famotidine Tablet Formulation

저자 : Jeong Sook Park , Kwang Hyun Shin , Jong Bum Park , Si Beum Lee , Sung Joo Hwang

발행기관 : 한국약제학회 간행물 : 약제학회지 37권 5호 발행 연도 : 2007 페이지 : pp. 275-280 (6 pages)

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A rapidly disintegration famotidine tablet formulation in the oral cavity was developed using microcrystalline cellulose (MCC) and low-substituted hydroxypropyl cellulose (L-HPC), or additionally cropovidone as an internal disintegrant. Effects of disintegrants on the disintegration time in vitro and hardness were evaluated. Average wetting time of the tablets prepared in scale-up manufacturing process was less than 15 sec. Among the formulations tested, the tablet prepared with crospovidone as an internal disintegrant and Emcocel 90M® as an external disintegrant showed fastest disintegration. These results may suggest that crospovidone and Emcocel 90Mw possessed excellent wetting nature, which result in the rapid disintegration of tablet.

3Transdermal Delivery of Porcine Placenta Extracts using Linolenic Acid-based Emulsion Formulations

저자 : Dong Chan Kim , Sang Myoung Noh , Ki Tae Park , Young Bong Kim , Kwang Hyun Baek , Yu Kyoung Oh

발행기관 : 한국약제학회 간행물 : 약제학회지 37권 5호 발행 연도 : 2007 페이지 : pp. 281-286 (6 pages)

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For transdermal delivery of porcine placenta extract (PPE), various emulsion formulations were prepared and evaluated. Polysorbate surfactants were used as emulsiflers and various C-I 8 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.

4Effect of Hypoxia on the Doxorubicin Sensitivity of Human MCF-7 Breast Cancer Cells

저자 : Soo Jeng Lim , He Kyung Kang

발행기관 : 한국약제학회 간행물 : 약제학회지 37권 5호 발행 연도 : 2007 페이지 : pp. 287-290 (4 pages)

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Intrinsic or acquired resistance to chemotherapeutic drugs is one of the major obstacles to effective cancer treatment. Hypoxia is widespread in solid tumors as a consequence of decreased blood flow in the tumor-derived neovasculature. The recent finding of a link between hypoxia and chemoresistance prompted us to investigate whether hypoxia induces doxorubicin resistance in human MCF-7 breast cancer cells. Low oxygen concentration decreased the doxorubicin sensitivity in MCF-7 cells. The expression of p-glycoprotein, a major MDR-related transporter, and those of apoptosis-related proteins (anti-apoptotic Bcl-2, Bcl-XL and pro-apoptotic Bax) were not altered by hypoxia in MCF-7 cells. Intracellular uptake of doxorubicin was significantly decreased under hypoxic conditions. Decreased cellular uptake of doxorubicin under hypoxia may contribute to causing doxorubicin resistance in these cells. The use of agents that can modulate the doxorubicin uptake for adjuvant therapy may contribute to improving the therapeutic efficacy of doxorubicin in breast cancer patients.

5SMEDDS (Seif-Micro Emulsifying Drug Delivery System) As An Intraurethral Prostaglandin E1 Delivery System

저자 : Sang Kil Lee , San Gok Jeon , Jae Seen Kang , Jae Hwi Lee , Young Wook Choi

발행기관 : 한국약제학회 간행물 : 약제학회지 37권 5호 발행 연도 : 2007 페이지 : pp. 291-295 (5 pages)

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Prostaglandin E1 (PGE1) was formulated as two self-microemulsifying drug delivery systems (SMEDDS) composed of Cremophor EL® or Cremophor ELP® as a surfactant, ethanol as a cosurfactant and Labrafac CC® as an oil to develop liquid preparation for the treatment of erectile dysfunction. In pseudo-ternary phase diagram, viscous gel area and microemulsion area were defined. In the measurement of viscosity, the viscosity of two formulations increased gradually upon the addition of water and it decreased from the water contents over 40%. With excessive water, the present systems formed a microemulsion spontaneously. From these results, we could expect that the present liquid PGE, SMEDDS formulations might stay within the urethra in the viscous state when contacting the moisture of the urethra and can be easily eliminated by urination. In long-term stability study, we could select one formulation more stable at the shelf storage condition of 4°C.

6Pharmacokinetic Characteristics of Levosulpiride in Relation to the Genetic Polymorphism of MDR1: From Knockout Mouse to Human

저자 : Hea Young Cho , Yong Bok Lee

발행기관 : 한국약제학회 간행물 : 약제학회지 37권 5호 발행 연도 : 2007 페이지 : pp. 297-303 (7 pages)

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The purposes of this study were to clarify the involvement of P-glycoprotein (P-gp) in the efflux of levosulpiride in knockout mice that lack the mdrlalb gene and to evaluate the relationship between the genetic polymorphisms in MDR] gene (exon 21) and levosulpiride disposition in healthy Korean subjects. After oral administration (10 ㎍/g) of levosulpiride to mdrIa/Ib(-/-) and wild-type mice, plasma and brain samples were obtained at 45 mm. We also investigated the genotype for MDRI (exon 21) gene in humans using a polymerase chain reaction-restriction fragment length polymorphism (PCR-RFLP) method. A single oral dose of 25 mg levosulpiride was administered to 58 healthy subjects, who were based on the MDRJ genotype for the G2677T SNP. Blood samples were taken up to 36 hr after dosing. The concentrations of levosulpiride in mouse plasma and brain were statistically significant difference between the two animal groups (P<0.05). In addition, the average brain-to-plasma concentration ratio (Kp) of levosulpiride was 3.4-fold (P<0.01) higher in the mdr Ia/Ib(-/-) mice compared with the wild-type mice. We also found that the values of AUC, partial AUC (AUC0-4h) and C(max) were significantly different between homozygous 2677TT subjects and the subjects with at least one wild-type allele (GG and GT subjects, P=0.012 for AUC(0-∞)=0.008 for AUCcJ4h; P=0.038 for Cmax). The results confirm that levosulpiride is a P-gp substrate in vivo, and clearly demonstrate the effect of SNP 2677G>Tin exon 21 of the MDRI gene on levosulpiride disposition.

7Anti-proliferative Effect of Tetra-arsenic Oxide (TetraAs(R)) in Human Gastric Cancer Cells in Vitro

저자 : Won Heui Chung , Hyu Jin Koo , Hyo Jeong Kuh

발행기관 : 한국약제학회 간행물 : 약제학회지 37권 5호 발행 연도 : 2007 페이지 : pp. 305-309 (5 pages)

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Arsenic compounds have been used to treat various diseases including cancer in oriental medicine. Arsenic trioxide (As203, Trisenox®) has been used for the treatment of leukemia and its anti-solid tumor activity has also been reported recently. Tetra-arsenic oxide (As406, TetraAs®) is a newly developed arsenic compound which has shown an anticancer activity in some human cancer cell lines. The purpose of this study was to evaluate the anti-gastric cancer potential of TetraAs and to search for an agent with synergistic interaction with TetraAs against human gastric cancers. We analysed anti-proliferative effect of TetraAs when given alone and in combination with other chemotherapeutic agents such as 5-FU, paclitaxel, and cisplatin in SNU-216, a human gastric cancer cell line. The 1C50 of these 4 anti-cancer drugs ranged from 5.8㎚ to 7.5㎛ with a potency rank of order paclitaxel>TetraAs>cisplatin> 5-FU. TetraAs showed 10-fold greater potency than 5-FU and cisplatin at the same effect level of IC50. TetraAs+5-FU and TetraAs+paclitaxel showed synergistic and additive interaction, respectively. On the other hand, TetraAs with cisplatin group appeared to be strongly antagonistic. Apoptotic population was measured and compared between single and combination treatment. The apoptotic cells for the combination of TetraAs+5-FU showed significant increase compared to single TetraAs treatment. On the contrary, TetraAs+cisplatin showed less apoptotic cells compared to TetraAs or cisplatin alone treatment Overall, our results indicate that TetraAs can be effectively combined with 5-FU or paclitaxel, but not with cisplatin for synergistic anti-cancer effect, which warrants further evaluation using in vivo models.

8Buccal Transport of Paclitaxel using Ethanol and Glyceryl Monooleate

저자 : Yoon Jin Lee , Myung Joo Kang , Young Mi Park , Young Wook Choi , Jae Hwi Lee

발행기관 : 한국약제학회 간행물 : 약제학회지 37권 5호 발행 연도 : 2007 페이지 : pp. 311-314 (4 pages)

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Paclitaxel (PTX) is an antineoplastic agent approved for the treatment of ovarian and breast carcinomas. However, the use of paclitaxel as an anticancer drug is limited by its extremely poor water solubility (below 0.3㎍/㎖). Furthermore, it has very low bioavailability when administered orally because paclitaxel is a substrate of P-glycoprotein (P-gp) efflux pump. In this study, buccal delivery of PTX was investigated as one of the alternatives for FTX delivery. Ethanol and glyceryl monooleate (GMO) were selected as permeation enhancing agents to increase solubility and permeation across buccal mucosa of PTX. At the different concentrations of ethanol solution (30~70 w/w%), PTX permeation was studied, followed effects of GMO in the concentration range of 2.5~25% with ethanol vesicle. The transbuccal ability of PTX was evaluated in vitro using Franz diffusion cells mounted with rabbit buccal mucosa. As a result, incorporation of PTX into ethanol vesicle with OMO significantly enhanced the PTX permeation in rabbit buccal mucosa. Particularly, the mixtures of ethanol: water GMO at the ratio of 50:47.5 :2.5 showed the most excellent enhancing ability. The results showed a promising possibility for buccal delivery of PTX.

9Bioequivalence of Samchundang Lercanidipine Tablet 10 mg to Zanidip Tablet (Lercanidipine Hydrochloride 10 mg) by Liquid Chromatography with Tandem Mass Spectrometry

저자 : Se Mi Kim , Hwan Ho Kim , Sae Byeok Shin , Hyun Ah Kang , Hea Young Cho , Yoon Gyoon Kim , Yong Bok Lee

발행기관 : 한국약제학회 간행물 : 약제학회지 37권 5호 발행 연도 : 2007 페이지 : pp. 315-321 (7 pages)

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The purpose of the present study was to evaluate the bioequivalence of two lercanidipine hydrochloride tablets, Zanidip tablet (LG Life Sciences Ltd., Korea, reference drug) and Samchundang Lercanidipine tablet 10 mg (Sam Chun Dang Pharm. Co. Ltd., Korea, test drug), according to the guidelines of Korea Food and Drug Administration (KFDA). After adding an internal standard (amlodipine maleate) to human serum, serum samples were extracted using hexan-isoamyl alcohol (100:1, vlv). Compounds were analyzed by liquid chromatography/tandem mass spectrometry. This method showed linear response over the concentration range of 0.05-20ng/㎖ with correlation coefficient of 0.9999. The lower limit of quantitation using 0.5㎖ of serum was 0.05ng/㎖ which was sensitive enough for pharmacokinetic studies. Thirty healthy male Korean volunteers received each medicine at the lercanidipine hydrochloride dose of 20mg in a 2x2 crossover study. There was a one-week washout period between the doses. Serum concentrations of lercanidipine were monitored by an LC/MS/MS for over a period of 24 hr after the administration. AUC1 (the area under the serum concentration-time curve from time 0 to 24 hr) was calculated by the linear trapezoidal rule method. C, (the maximum serum drug concentration) and T(max) (the time to reach C(max)) were compiled from the serum concentration-time data. Analysis of variance was carried out using logarithmically transformed AUC, and C(max). No significant sequence effect was found for all of the bioavailability parameters, indicating that the crossover design was properly performed. The 90% confidence intervals of the AUC, ratio and the C(max) ratio for Samchundang Lercanidipine/Zanidip were log 0.9505-log 1.2258 and log 0.9987-log 1.2013, respectively. These values were within the acceptable bioequivalence intervals of log 0.80-log 1.25. Thus, the criteria of the KFDA guidelines for the bioequivalence was satisfied, indicating Samchundang Lercanidipine tablet 10mg and Zanidip tablet are bioequivalent.

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