• Title/Summary/Keyword: drug delivery route

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Improvement of Solubility of Atorvastatin Calcium Using Self-Microemulsion Drug Delivery System(SMEDDS) (자가미세유화를 통한 아토르바스타틴 칼슘의 난용성 개선)

  • Lee, Jun-Hee;Choi, Myoung-Kyu;Kim, Yun-Tae;Kim, Myoung-Jin;Oh, Jae-Min;Park, Jung-Soo;Mo, Jong-Hyun;Kim, Moon-Suk;Khang, Gil-Son;Lee, Hai-Bang
    • Journal of Pharmaceutical Investigation
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    • v.37 no.6
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    • pp.339-347
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    • 2007
  • SMEDDS is mixture of oils, surfactants, and cosurfactants, which are emulsified in aqueous media under conditions of gentle agitation and digestive motility that would be encountered in the gastro-intestinal(GI) tract. The main purpose of this work is to prepare self-microemulsifying drug delivery system(SMEDDS) for oral bioavailability enhancement of a poorly water soluble drug, atorvastatin calcium. Solubility of atorvastatin calcium was determined in various vehicles. Pseudo-ternary phase diagrams were constructed to identity the efficient self-emulsification region and particle size distributions of the resultant micro emulsions were determined using a laser diffraction sizer. Optimized formulations for in vitro dissolution and bioavailability assessment were $Capryol^{(R)}$ 90(50%), Tetraglycol(16%), and $Cremophor^{(R)}$ EL(32%). The release rate of atorvastatin from SMEDDS was significantly higher than the conventional tablet ($Lipitor^{(R)}$), 2-fold. Our studies illustrated the potential use of SMEDDS for the delivery of hydrophobic compounds, such as atorvastatin calcium by the oral route.

The Intrathecal Drug Administration System (척수강 내 약물 주입술)

  • Nahm, Francis Sahngun;Kim, Yong Chul
    • The Korean Journal of Pain
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    • v.22 no.2
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    • pp.117-123
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    • 2009
  • The intrathecal drug administration system (ITDAS) has recently been introduced for treating chronic intractable pain patients who have failed with conservative pain treatments. The obvious advantages of its use are the direct intrathecal delivery of drugs, which yields reduced adverse effects and the increased strength of drugs, as compared to its oral or intravenous route. This article offers a review of the ITDAS with a brief review of its evidence-based effectiveness, the technical approach, and the complications.

A Study on the Types and Causes of Medication Errors and Related Drugs - by Analyzing AJNs Medication Error 73 Cases - (임상에서의 투약오류원인과 관련 의약품 분석 - AJN에 기고된 Medication Error 기사의 73사례를 중심으로 -)

  • Cho Won Sun
    • Journal of Korean Public Health Nursing
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    • v.16 no.1
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    • pp.176-189
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    • 2002
  • The purpose of this study were to illustrate the various medication error types and causes and identified to related drugs to provide basic data for preventing nurses' medication error by analysing 73 cases of AJN 'medication Error' column(1993, Oct -2000, Nov). Nurses' types of medication error were classified into 7 types. The most frequent error types are wrong medication$(21.9\%)$ and the wrong dose$(21.9\%)$ together. The others are wrong $time(4.1\%)$, $omission(2.7\%)$, mechanical $error(2.7\%)$, incorrect IV $rate(1.4\%)$. wrong route $administration(1.4\%)$ in order. Nurses' causes of medication error were 9 kinds. The most frequent type is confusing between similar drug shape, color, size, name, injection devices and patient's $name(43.9\%)$ and the others are lack of knowledge about $drugs(26.8\%),\; slips(7.3\%),\; miscalculating\;dose(4.9\%)$, incorrect adjusts $devices(4.9\%)$, difficulty to read or illegible decimal $point(4.9\%),$ $abbreviation(2.4\%)$, fatigue with $overwork(2.4\%)$ and no communication with $patient(2.4\%)$ in order. Related drugs with medication error are as follows. - dose unit(IU. minims. mcg/min. mEq) : Heparin. insulin. synthetic calcitonin, some enzymes and hormones, vitamins, some antibiotics, tuberculin injection. MgSO4 injection. nitroglycerin - similar size, color and shape drug : $0.9\%$ N/S and acetic acid $0.25\%$ for irrigation. premixed 2mg lidocaine sol. and $0.9\%$ N/S, gentamycin 20mg/2mL for children and 80mg/2mL for adult, dextroamphetamine 5mg and 10mg capsule. sedatives chloral hydrate 250mg/5mL and 500mg/5mL - similar name :Aredia(pamidronate disodium) and Adriamycin(doxorubicin), Lamictal (lamotrigine) and Lamisil 250mg. Elderpryl and enalapril, cefotaxime and cefoxitin, carboplatin and cisplatin, sumatriptan and zolmitriptan, Celebrex and Celexa, Humulin and Humalog, Percodan and Percocet, Diabeta and Diabinese, Epivir and Retrovir, Xanax(alprazolam) and Zantac(ranitidine) - decimal point : low molecular weight warfarin, methotrexate - unfamiliar drug uses of familiar drug ; methotrexate. droperidol, imipramine, propranolol - number of drug name(misleading chemical name) : 6-thioguanine, 6-mercaptopurine, 5-fluorouracil - type of administration route : Oxycodone(OxyContin). - administration time : acarbose(Precose). - injection way (Z-track method): hydroxyzine - epidural cathether : LMWHs(enoxaparin, dalteparin), - ADD Vantage self contained delivery system : ceftriaxone(Rocephin)

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Transvaginal Delivery of Luteinizing Hormone-Releasing Hormone Using Bioadhesive Hydrogel (생체막점착성 하이드로겔을 이용한 황체형성호르몬 유리호르몬의 질점막 수송)

  • Han, Kun;Park, Hee-Beom;Park, Jeong-Sook;Chung, Youn-Bok
    • Journal of Pharmaceutical Investigation
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    • v.27 no.1
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    • pp.15-22
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    • 1997
  • The mucosal route of administration(nasal, buccal, conjunctival and vaginal) has recently been considered as an alternative to parenteral delivery for many peptide drugs because enzymatic degradation of these agents may be partly avoided. The objective of these study was to establish the optimal mucosal administration dosage form of $LHRH/[D-Ala^6]LHRH$, based on presystemic metabolism. We reported previously the peptidase inhibition effect of medium chain fatty acid salts(sodium caprylate, soadium caprate and sodium laurate), EDTA and STDHF on the proteolysis of $LHRH/[D-Ala^6]LHRH$ in rabbit mucosal homgenates. We also reported that EDTA, STDHF and sodium laurate markedly increased the potency of $LHRH/[D-Ala^6]LHRH$ solution applied vaginally. In the present study, by administration of polycarbophil hydrogel containing LHRH the ovulation inducing activity was 3.3 times greater than solution. These results indicate not only peptidase inhibitor but also polycarbophil hydrogel significantly improved the absorption of this drug. The results of this study would provide the feasibility as a rational dosage form for improving bioavailability and self administration of this hydrogel by the vaginal application.

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The Role of Endoscopic Interventions in Palliative Care for the Gastrointestinal Tumors (소화기 종양에 대한 내시경적 완화치료)

  • Hye Kang Kim;Dae Young Cheung
    • Journal of Digestive Cancer Research
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    • v.2 no.1
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    • pp.1-4
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    • 2014
  • Palliative care for cancer aims to relieve the discomfort and pain from the cancer itself and associated conditions. Gastrointestinal cancers originate from the tube like structure of gastrointestinal tract and cause complications such as obstruction, bleeding, adhesion, invasion, and perforation to adjacent organ. Recent advances in interventional endoscopy enables endoscopy physicians to do safe and effective care for gastrointestinal cancer patients. Endoscopic palliation includes stent, hemostasis, nutritional support and targeted drug delivery. Self expandable metallic stent is one of the most important modalities in gastrointestinal palliation. Through the endoscopy or over the wire pre-placed by endoscopy, stents restore the gastrointestinal luminal patency and relieve the obstructive condition. Endoscopic hemostasis is another important palliation in gastrointestinal cancer patients. Epinephrine injection, argon plasma coagulation and thermal cauterization are usual modalities for hemostasis. Histoacryl glue and fibrin glue are also available. Hemostatic nanopowder spray is newly reported effective in benign disease and is supposed to be effective also in cancer bleeding. Enteral feeding tubes including gastro- or jejunostomy and nosoduodenal tubes are placed by using endoscopic guidance. Enteral feeding tubes role as the route of easily absorbable or semi-digested nutrients and effectively maintain both patients calorie requirements and gut microenvironment. Photodynamic therapy is the one of the outstanding medical employments of photo-physics. Especially for superficial cancers in esophagus, photodynamic therapy is very useful in cancer removal and maintaining organ structure. In biliary neoplasm, photodynamic therapy is well known to be effective in cancer ablation and biliary ductal patency restoration. Targeted drug delivery is the lastest issue in palliative endoscopy. Debates and questions are still on the table. In this article, the role of endoscopic interventions in palliative care for the gastrointestinal tumors will be thoroughly reviewed.

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Preparation of Lipid Nanoparticles Containing Paclitaxel and their in vitro Gastrointestinal Stability (파클리탁셀을 함유한 지질나노입자의 제조와 인공 소화액에서의 안정성 평가)

  • Kim, Eun-Hye;Lee, Jung-Eun;Lim, Deok-Hwi;Jung, Suk-Hyun;Seong, Ha-Soo;Park, Eun-Seok;Shin, Byung-Cheol
    • Journal of Pharmaceutical Investigation
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    • v.38 no.2
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    • pp.127-134
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    • 2008
  • Peroral administration is the most convenient one for the administration of pharmaceutically active compounds. Most of poorly water-soluble drugs administered via the oral route, however, remain poorly available due to their precipitation in the gastrointestinal (GI) tract and low permeability through intestinal mucosa. In this study, one of drug delivery carriers, lipid nanoparticles (LNPs) were designed in order to reduce side effects and improve solubility and stability in GI tract of the poorly water soluble drugs. However, plain LNPs are generally unstable in the GI tract and susceptible to the action of acids, bile salts and enzymes. Accordingly, the surface of LNPs was modified with polyethylene glycol (PEG) for the purpose of improving solubility and GI stability of paclitaxel (PTX) in vitro. PEG-modified LNPs containing PTX was prepared by spontaneous emulsification and solvent evaporation (SESE) method and characterized for mean particle diameter, entrapping efficiency, zeta potential value and in vitro GI stability. Mean particle diameter and zeta potential value of PEG-modified LNP containing PTX showed approximately 86.9 nm and -22.9 mV, respectively. PTX entrapping efficiency was about 70.5% determined by UV/VIS spectrophotometer. Futhermore, change of particle diameter of PTX-loaded PEG-LNPs in simulated GI fluids and bile fluid was evaluated as a criteria of GI stability. Particle diameter of PTX-loaded PEG-LNPs were preserved under 200 nm for 6 hrs in simulated GI fluids and bile fluid at $37^{\circ}C$ when DSPE-mPEG2000 was added to formulation of LNPs above 4 mole ratio. As a result, PEG-modified LNPs improved stability of plain LNPs that would aggregate in simulated GI fluids and bile solution. These results indicate that LNPs modified with biocompatible and nontoxic polymer such as PEG might be useful for enhancement of GI stability of poorly water-soluble drugs and they might affect PTX absorption affirmatively in gastrointestinal mucosa.

Direct Action of Genistein on the Hypothalamic Neuronal Circuits in Female Rats

  • Lee, Woo-Cheol;Lee, Sung-Ho
    • Development and Reproduction
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    • v.14 no.1
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    • pp.35-41
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    • 2010
  • Mammalian reproduction is regulated by a feedback circuit of the key reproductive hormones such as GnRH, gonadotropin and sex steroids on the hypothalamic-pituitary-gonadal axis. In particular, the onset of female puberty is triggered by gain of a pulsatile pattern and increment of GnRH secretion from hypothalamus. Previous studies including our own clearly demonstrated that genistein (GS), a phytoestrogenic isoflavone, altered the timing of puberty onset in female rats. However, the brain-specific actions of GS in female rats has not been explored yet. The present study was performed to examine the changes in the activities of GnRH neurons and their neural circuits by GS in female rats. Concerning the drug delivery route, intracerebroventricular (ICV) injection technique was employed to eliminate the unwanted actions on the extrabrain tissues which can be occurred if the testing drug is systemically administered. Adult female rats (PND 100, 210-230 g BW) were anaesthetized, treated with single dose of GS ($3.4{\mu}g$/animal), and sacrificed at 3 hrs post-injection. To determine the transcriptional changes of reproductive hormone-related genes in hypothalamus, total RNAs were extracted and applied to the semi-quantitative reverse transcription polymerase chain reaction (RT-PCR). ICV infusion of GS significantly raised the transcriptional activities of enhanced at puberty1 (EAP-1, p<0.05), glutamic acid decarboxylase (GAD67, p<0.01) which are known to modulate GnRH secretion in the hypothalamus. However, GS infusion could not change the mRNA level of nitric oxide synthase 2 (NOS-2). GS administration significantly increased the mRNA levels of KiSS-1 (p<0.001), GPR54 (p<0.001), and GnRH (p<0.01) in the hypothalami, but decreased the mRNA levels of LH-$\beta$ (p<0.01) and FSH-$\beta$ (p<0.05) in the pituitaries. Taken together, the present study indicated that the acute exposure to GS could directly activate the hypothalamic GnRH modulating system, suggesting the GS's disrupting effects such as the early onset of puberty in immature female rats might be derived from premature activation of key reproduction related genes in hypothalamus-pituitary neuroendocrine circuit.

Apoptosis and inhibition of human epithelial cancer cells by ZnO nanoparticles synthesized using plant extract

  • Koutu, Vaibhav;Rajawat, Shweta;Shastri, Lokesh;Malik, M.M.
    • Advances in nano research
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    • v.7 no.4
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    • pp.233-240
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    • 2019
  • The present research work reports in-vitro anti-cancer activity of biologically synthesized ZnO nanoparticles (ZnO NPs) against human carcinoma cells viz SCC-40, SK-MEL-2 and SCC-29B using Sulforhodamine-B (SRB) Assay. ZnO NPs were synthesized by a unique and novel biological route using Temperature-gradient phenomenon where the extract of combination of Catharanthus roseus (L.) G. Don (C. roseus), Azadirachta indica (A. indica), Ficus religiosa (F. religiosa) and NaOH solution were used as synthesis medium. The morphology of the ZnO NPs was characterized by Transmission Electron Microscopy (TEM). TEM images reveal that particle size of the samples reduces from 76 nm to 53 nm with the increase in reaction temperature and 68 nm to 38 nm with the increase in molar concentration of NaOH respectively. XRD study confirms the presence of elements and reduction in crystallite size with increase in reaction temperature and NaOH concentration. The diffraction peaks show broadening and a slight shift towards lower Bragg angle ($2{\theta}$) which represents the reduction in crystallite size as well as presence of uniform strain. The FTIR spectra of the extract show transmittance peak fingerprint of Zn-O bond and presence of bioactive molecules These NPs exhibit inhibition greater than 50% for SCC-40, SK-MEL-2 and SCC-29B cell lines and more than 50% cell kill for SCC-29B cells at concentrations < $80{\mu}g/ml$. Nanoparticles with smallest size have shown better anti-cancer activity and peculiar cell-selectivity. The combination of extracts of these plants with ZnO NPs can be used in targeted drug delivery as an effective anti-cancer agent, a potential application in cancer treatment.