• Title/Summary/Keyword: drug release rate

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Effects of Days Open on the Subsequent Reproductive Performance Following to CIDR-Based Estrus Synchronization in Lactating Dairy Cows

  • Kang, Hyun-Gu;Kim, Ill-Hwa
    • Journal of Embryo Transfer
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    • v.26 no.2
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    • pp.91-96
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    • 2011
  • The purpose of this study was to evaluate the effects of days open on subsequent reproductive performance following to estrus synchronization in the 114 lactating dairy cows. The animals were divided into two groups according to the time of estrus synchronization; viz, ${\leq}$ 85 days, and > 85 days postpartum, respectively. The estrus synchronization protocol consisted of insertion of a controlled internal drug release (CIDR) device containing 1.9 g progesterone with an injection of 250 ${\mu}g$ gonadorelin (Day 0), an injection of $PGF_2{\alpha}$ and removal of the device on Day 7, an injection of 250 ${\mu}g$ GnRH on Day 9, and TAI 17 h later. Pregnancy diagnosis was determined at 30 to 60 days after TAI using both ultrasonography and rectal palpation. The body condition score (BCS) gradually increased over the postpartum period. In estrus synchronized cows until 85 days, conception rate on first service, number of service per conception, interval from estrus synchronization to conception, and interval from calving to conception were not significantly different among two farms (P>0.05). In estrus synchronized cows after 85 days postpartum, conception rate on first service, number of service per conception and interval from calving to conception were significantly different ($P{\leq}0.05$) between herds A and B (26.8 vs 50.0%; $2.1{\pm}1.35$ vs $1.37{\pm}0.54$ times, $237.3{\pm}97.8$ vs $164.7{\pm}69.3$ days, respectively). In estrus synchronized cows after 85 days postpartum interval from estrus synchronization to conception was greater (P<0.01) in herd B than in herd A ($63.6{\pm}57.4$ vs $26.1{\pm}24.9$). These results indicate that the time of estrus synchronization for maximized the reproductive performance is before 85 days postpartum and feeding and management is important factor for high reproductive performance.

Tolerability, Safety and Effectiveness of Paliperidone ER in Patients with Schizophrenia : A 24-Week Interim Analysis of the 48-Week Open-Label, Prospective, Switch Study (조현병 환자에서 Paliperidone Extended Release의 효능, 안전성 및 내약성 : 48주 개방형, 전향적 연구의 24주 중간 분석)

  • Choi, You Ra;Jung, Dong Chung;Kim, Eun Young;Kim, Se Hyun;Lee, Hyun Jeong;Lee, Nam Young;Chang, Sung Man;Shim, Joo Cheol;Joo, Eun Jeong;Kim, Jae Jin;Lee, Sang Hyuk;Chung, Young Chul;Kim, Yong Sik;Ahn, Yong Min
    • Korean Journal of Biological Psychiatry
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    • v.20 no.1
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    • pp.12-20
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    • 2013
  • Objectives We investigated the tolerability, safety, and treatment response to flexible-dose paliperidone ER in patients with non-acute schizophrenia in whom previous antipsychotic drugs were ineffective. Methods This 24-week interim analysis of the 48-week multicenter, prospective, open-label study assessed effectiveness using the Positive and Negative Syndrome Scale (PANSS), Clinical Global Impression-Schizophrenia-Severity (CGI-SCH-S) Scale, Personal and Social Performance (PSP) and Drug Attitude Inventory (DAI). Safety and tolerability were assessed using the Drug-Induced Extrapyramidal Symptoms Scale (DIEPSS) and Liverpool University Neuroleptic Side Effect Rating Scale (LUNSERS). Results Effectiveness was assessed in 169 patients. Significant improvement in the PANSS total score was observed by week-1 and continued until week-24. The response rate was 33%. The CGI-SCH-S and PSP total scores significantly improved during 24 weeks ; however, no change occurred in the total DAI. Fifty-nine percent of patients reported adverse events, of which extrapyramidal symptoms were the most frequent (19.0%). The DIEPSS and LUNSERS scores were improved after 24 week. Conclusions Switching to the flexible-dose paliperidone ER from an ineffective antipsychotic drug was safe, tolerable, and showed a good treatment response in Korean patients with schizophrenia.

The Bioequivalence of Two Carbamazepine Controlled Release Formulations (카르바마제핀 서방형 제제간의 생물학적 동등성 비교)

  • Kim, Min J.;Lee, Hyun J.;Rheu, Yoon M.;Shin, Wan G.;Park, Sung H.
    • Korean Journal of Clinical Pharmacy
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    • v.6 no.2
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    • pp.19-23
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    • 1996
  • Carbamazepine is an anticonvulsant drug that has been shown to be as effective as phenytoin or phenobarbital in treatment of grand mal and complex partial seizures and is also approved as the drug of choice for treatment of the pain associated with trigerminal neuralgia. And the therapeutic or toxic effects of carbamazepine are better related to plasma concentration than to dosage, which can be attributed to interindividual variability in the pharmacokinetics. A slow rate of carbamazepine dissolution in the gastrointestinal tract is believed to be the cause of its relatively slow and erratic rate of absorption. For these reasons pharmacokinetic evaluation of newly formulated carbamazepine is neccessary. In this study, the bioequivalence in carbamazepine between the $TegretoI^{TM}$ CR tablet (Geigy Co.) and $Carmazepine^{TM}$ CR tablet (Myung In Co.) was evaluated. 12 normal volunteers (age $21\~27$ years old) was divided into two groups, and a randomized cross-over study was employed. The pharmacokinetic parameters ($C_{max},\;T_{max}$ and AUC) obtained of oral administration of each formulatim of carbamazepine 400 mg were evaluated and ANOVA was utilized for the statistical analysis of parameters. $C_{max}\;is\;8.26{\pm}3.1{\mu}g/ml\;(C.V.\;37.3\%)\;in\;TegretoI^{TM}\;and\;9.39\{pm}2.9{\mu}g/ml\;(C.V.\;30.5\%)$ in $Carmazepine^{TM},\;T_{max}\;is\;28.0{\pm}5.9\;hrs(C.V.\;21.1\%)$ in $Tegretol^{TM}\;and\;24.0{\pm}7.2\;hrs(C.V.\;30.2\%)$ in $Carmazepine^{TM}$ and AUC is $786.4{\pm}360.5{\mu}g{\cdot}hr/ml\;(C.V.\;45.8\%)$ in $TegretoI^{TM}\;and\;792.8{\pm}228.6{\mu}g{\cdot}hr/ml\;(C.V.\;28.8\%)$ in $Carmazepine^{TM}$, respectively. As the result of the data, two formulations are bioequvalent, and the lower C.V. of $Carmazepine^{TM}$ in every individual can be merit.

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Evaluation of Alginate Microspheres Prepared by Emulsion and Spray Method for Oral Vaccine Delivery System (유화법과 분무법에 의해 제조된 경구백신용 알긴산 마이크로스피어의 평가)

  • Jiang, Ge;Jee, Ung-Kil;Maeng, Pil-Jae;Hwang, Sung-Joo
    • Journal of Pharmaceutical Investigation
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    • v.31 no.4
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    • pp.241-256
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    • 2001
  • Alginate microspheres, containing fluorescein isothiocyanate-bovine serum albumin (FITC-BSA) or green fluorescent protein (GFP) were prepared and used as a model drug to develop the oral vaccine delivery system. The alginate microspheres were coated with poly-L-lysine or chitosan. Two methods, w/o-emulsion and spray, were used to prepare alginate microspheres. To optimize preparation conditions, effects of several factors on the particle size and particle morphology of microsphere, and loading efficiency of model antigen were investigated. In both preparation methods, the particle size and the loading efficiency were enhanced when the concentration of sodium alginate increased. In the w/o-emulsion preparation method, as the concentration of Span 80 was increased from 0.5% to 2%, the particle size was decreased, but the loading efficiency was increased. The higher the emulsification speed was, the smaller the particle size and loading efficiency were. The concentration of calcium chloride did not show any effect on the particle size and loading efficiency. In the spray preparation method, the particle size was increased as the nozzle pressure $(from\;1\;kgf/m^2\;to\;3\;kgf/m^2)$ and spray rate was raised. Increasing calcium chloride concentration (<7%) decreased the particle size, in contrast to no effect of calcium chloride concentration on the w/o-emulsion preparation method. Alginate microspheres prepared by two methods were different in the particle size and loading efficiency, the particle size of microspheres prepared by the spray method was about $2-6\;{\mu}m$, larger than that prepared by the w/o emulsion method $(about\;2{\mu}m)$, and the loading efficiency was also higher with spray method. Furthermore, drying process for the microspheres prepared by the spray was simpler and easier, compared with the w/o emulsion preparation. Therefore, the spray method was chosen to prepare alginate microspheres for further experiments. Release pattern of FITC-BSA in alginate microspheres was evaluated in simulated intestinal fluid and PBS (phosphate buffered saline). Dissolution rate of FITC-BSA from alginate/chitosan microsphere was lower than that from alginate microsphere and alginate/poly-L-lysine microsphere. By confocal laser scanning microscope, it was revealed that alginate/FITC-poly-L-lysine microspheres were present in close apposition epithelium of the Peyer's patches of rabbits following inoculation into lumen of intestine, which proved that microspheres could be taken up by Peyer's patch. In conclusion, it is suggested that alginate microsphere prepared by spray method, showing a particle size of & $10\;{\mu}m$ and a high loading efficiency, can be used as a model drug for the development of oral vaccine delivery system.

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Characterization of Hyaluronic Acid Membrane Cross-linked with Lactide (락타이드로 가교시킨 히아루론산 막의 특성)

  • Kwon, Ji-Young;Cheong, Seong-Ihl
    • Polymer(Korea)
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    • v.29 no.6
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    • pp.599-604
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    • 2005
  • The hyaluronic acid (HA) with excellent biocompatibility has been combined with lactide, the ester dimer of polylactide, with good biodegradability to produce biocompatible materials which can control the period of degradation in a human body. By freeze frying method, HA and lactide were crosslinked with crosslinking agent, 1-ethyl-3-(3-dimethyl aminopropyl) carbodiimide (EDC). Degree of lactide and EDC reaction was determined by the analysis of nuclear magnetic resonance spectroscopy. Both lactyl group and EDC conversion increased as the mole ratio of lactide to HA increased from 5 to 13. The membrane swelled less and became more brittle with the more addition of lactyl group resulting from the higher mole ratio of lactide to HA. Swelling ratio decreased and tensile modulus increased due to the more addition of lactyl group as the EDC concentration increased or reaction temperature decreased. Drug release experiment from various membranes with different degree of crosslinking showed that permeability decreased with increasing degree of crosslinking. The degradation became slower with the more addition of lactyl group. Mechanical property and degradation rate of the synthesized membrane were shown to be controlled through adjusting operation parameters such as mole ratio, temperature, and crosslinking agent concentration.

A Study on the Factors Affecting Entrapment Efficiency and Particle Size of Ethosomes (Ethosomes의 포집효율과 입자크기에 영향을 주는 인자에 관한 연구)

  • Jin, Byung Suk;Lee, Sang Mook;Lee, Kwang Hee
    • Applied Chemistry for Engineering
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    • v.17 no.2
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    • pp.138-143
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    • 2006
  • Ethosome is a liquid crystalline vesicle prepared by hydration of ethanol-dissolved lecithin with a solution containing hydrophilic components. Investigation of factors affecting the entrapment efficiency and particle size of ethosomes was carried out, because the high entrapment efficiency and small particle size are prerequisite in developing ethosomes as a drug delivery system. The variations of properties of ethosomes with constituent composition and preparation method were examined using a calcein as a hydrophilic marker. It was observed that the amount of ethanol and calcein solution, phosphatidyl choline content in lecithin, preparation temperature, stirring rate, and PBS addition method had a considerable effect on the properties of ethosome. Sonication treatment resulted in the reduction of entrapment efficiency of ethosome, which was due to the release of entrapped components in the vesicles by strong sonication vibration.

Preliminary Evaluation of the in vitro Efficacy of 1, 2-di (Quinazolin-4-yl) Diselane against SiHa Cervical Cancer Cells

  • Huang, Yin-Jiu;Zhang, Yu-Yuan;Liu, Gang;Tang, Jie;Hu, Jian-Guo;Feng, Zhen-Zhong;Liu, Fang;Wang, Qi-Yi;Li, Dan
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.15
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    • pp.6301-6306
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    • 2014
  • Cervical cancer is one the most common malignancies among females. In recent years, its incidence rate has shown a rising trend in some countries so that development of anticancer drugs for cervical cancer is an urgent priority. In our recent anticancer drug discovery screen, 1, 2-di (quinazolin-4-yl)diselane (LG003) was found to possess wide spectrum anticancer efficacy. In the present work, the in vitro anticancer activity of LG003 was evaluated in the SiHa cervical cancer cell line. Compared with commercial anticancer drugs 10-hydroxycamptothecin, epirubicin hydrochloride, taxol and oxaliplatin, LG003 showed better anticancer activity. Furthermore, inhibition effects were time- and dose-dependent. Morphological observation exhibited LG003 treatment results in apoptosis like shrinking and blebbing, and cell membrane damage. Lactate dehydrogenase release assay revealed that LG003 exerts such effects in SiHa cells through a physiology pathway rather than cytotoxicity, which suggests that title compound LG003 can be a potential candidate agent for cervical cancer.

Timed Artificial Insemination or Embryo Transfer using CIDR, Estradiol Benzoate and Prostaglandin $F_{2{\alpha}}$ for the Rebreeding of Korean Native Donor Cattle

  • Son, Dong-Soo;Choe, Chang-Yong;Cho, Sang-Rae;Choi, Sun-Ho;Kim, Hyun-Jong;Lee, Je-In;Kim, Ill-Hwa
    • Journal of Embryo Transfer
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    • v.23 no.2
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    • pp.81-86
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    • 2008
  • This study compared the pregnancy rates of Korean native donor cattle after either a timed artificial insemination (TAI) or embryo transfer (TET) following the synchronization of ovulation using a controlled internal drug release (CIDR) device together with estradiol benzoate (EB) and prostaglandin $F_{2{\alpha}}$ ($PGF_{2{\alpha}}$). Fifty five cows and 8 heifers which had been previously used for embryo production were assigned to two treatments: (1) Thirty-two cattle received a CIDR device and 2 mg EB (Day 0), 25 mg $PGF_{2{\alpha}}$ injection at the time of CIDR removal on Day 7, and 1 mg EB injection on Day 8. All of the cattle received a TAI 30 h (Day 9) after the second EB injection (TAI group). (2) Thirty-one cattle received the same hormonal treatments as in the TAI group. The cattle with corpus luteum (CL) received a TET on Day 16 using frozen-thawed embryos (TET group). Ultrasonographic observations demonstrated that the proportion of cattle with synchronized ovulation on Day 10 and the concomitant formation of new CL on Day 13 did not differ between groups (p>0.05); the overall mean rates were 65.1 and 73.0%, respectively. The conception and pregnancy rates did not differ (p>0.05) between the TAI (12.5% and 12.5%) and TET groups (13.0% and 9.7%), respectively. We conclude that the pregnancy rate following TAI or TET in Korean native donor cattle was poor, which might be due in part to a poor synchrony of ovulation and concomitant CL formation.

Effects of Sophorae Radix (SFR) on Allergic Inflammation related Atopy Dermatitis (고삼(苦蔘)이 알러지성 염증 반응에 미치는 영향)

  • Yu, Mao-Lun;Koo, Young-Sun;Kim, Dong-Hee
    • Journal of Haehwa Medicine
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    • v.15 no.2
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    • pp.135-148
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    • 2006
  • Sophorae Radix (SFR) is known as a therapeutic drug that has been used in Oriental traditional medicine for the treatment of skin and mucosal ulcers, gastrointestinal hemorrhage, diarrhea, inflammation and arrhythmia. In the present study, we examined the effects of the aqueous extract of SFR on anti-inflammation, anti-allergic and anti-oxidant effect in various cell lines; they include mouse lung fibroblast cells (hFCs), human mast cells (HMC-1), human monocytic cells (THP-1), and RAW 264.7 cells. Treatment with SFR extract at a concentration of 250 ${\mu}g$/ml for 24h showed no significant decrease in the survival rate of the hFCs. SFR decreased the mRNA expression of IL-8, TNF-$\alpha$, and IL-6 in HMC-1 cells. SFR extract treatment significantly inhi-bited the protein expression of IL-6 and, IL-8 induced by mite in THP-1 cells and it also did MCP-1 expression. We examined the alternation of histamine release in HMC-1 cells for investigating anti-allergic effect of SFR. Histamine secretion decreased after the treatment with SFR. In addition, SFR extract treatment at a concentration of 10 ${\mu}g$/ml, 100 ${\mu}g$ /ml, and 200 ${\mu}g$/ml lowered the $\beta$-hexosaminidase to 10.3%, 21.7%, and 50.8%, respectively. IC50 of SFR extract in RBL-2H3 cells was 196.85 ${\mu}g$/ml. Both activity of NF-$\kappa$B promoter in RBL-2H3 cells significantly diminished after the dose-dependent treatment of SFR. Therefore, our results indicate that SFR has anti-inflammatory and it may be useful for treating allergic diseases such as atopic dermatitis.

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Characterization and Preparation of the Hydrogel has Excellent Release Effect of the Active Ingredients Using a Radiation Cross-linking Technology (방사선 가교 기술을 이용한 유효성분 방출력이 우수한 하이드로겔 제조 및 특성 분석)

  • Hwang, Seung-Hyun;Ahn, Sung-Jun;Park, Jong-Seok;Jeong, Sung In;Gwon, Hui-Jeong;Lee, Dong Yun;Lim, Youn-Mook
    • Journal of Radiation Industry
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    • v.9 no.4
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    • pp.199-207
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    • 2015
  • Typical radiation cross-linked hydrogels has the characteristic that high water content, but low emission efficiency of active ingredients. Therefore, the hydrogel was prepared by the addition to collagen, which is closely related to the formation of skin wrinkles in biocompatibility and highly water-soluble carboxymethyl cellulose sodium salt (CMC) in order to preparation of hydrogels has excellent emission efficiency of active ingredients. Hydrogels were prepared by dissolving CMC and collagen each of 0.5%, 10% concentration in deionized water. Then, prepared hydrogels are performed by gamma-radiation at 1, 3, 5 kGy irradiation dose. The results showed that the gel fraction of after irradiated 3 kGy hydrogel was higher than before irradiated gelation as long as the 55.3%. The swelling rate of irradiated 3 kGy hydrogel was lower than the non-irradiated sample. The compressive strength of 3 kGy irradiated hydrogel was the highest. The visco-elastic did not show any significant differences, even after irradiation. The CMC hydrogel in this study suggested a potential use as a material for the mask pack for improved emission efficiency of the active ingredient and anti-wrinkles.