• Title/Summary/Keyword: chemical release

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Controlled Release of Gentamicin Sulfate from Poly(3-hydroxybu-tyrate-co-3-hydroxyvalerate) Wafers for the Treatment of Osteomyelitis

  • Gilson Khang;Park, Hak-Soo;John M. Rhee;Yoon, Sung-Chul;Cho, Jin-Cheol;Lee, Hai-Bang
    • Macromolecular Research
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    • v.8 no.6
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    • pp.253-260
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    • 2000
  • Biodegradable wafers were prepared with poly (hydroxybutyrate-co-hydroxyvalerate) (PHBV;5, 10, and 15 mole% for 3-hydroxyvalerate) by simple heat pressing method for the sustained release of antibiotic agent, gentamicin sulfate (GS) to investigate the possibility of the treatment for osteomyelitis. The effects of hydroxyvalerate (HV) content, thickness of wafers, various types of additives such as sodium dodecyl sulfate (SDS), microcrystalline cellulose, polyvinylpyrrolidone, and hydroxypropylcellulose (HPC), and different initial drug loading ratio on the release profile have been investigated. In vitro release studies showed that different release patterns and rates could be achieved by simply modifying factors in the preparation conditions. PHBV wafers with 3 mm thickness, 10% of GS initial loading, 15% of HV content and addition of 5% of SDS and HPC were free from initial burst and a near-zero-order sustained release was observed for over 30 days. It might be suggested that the mechanisms of G5 release may be more predominant simple dissolution and diffusion of GS than erosion of PHBV in our system.

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Preparation of Lacosamide Sustained-release Tablets and Their Pharmacokinetics in Beagles and Mini-pigs

  • Ahn, Jae Soon;Kim, Kang Min;Nam, Dae Sik;Kang, Kyoung Un;Choi, Peter S.;Jeong, Seo Young
    • Bulletin of the Korean Chemical Society
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    • v.35 no.2
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    • pp.557-561
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    • 2014
  • The aim of the present study was to improve dosing of lacosamide, a functionalized amino acid used as an antiepileptic agent, from twice daily to once daily for the convenience of patients. A sustained-release lacosamide tablet was developed and dissolution testing was employed to determine in vitro release behavior using water or buffer solutions at pH 1.2, 4.0, or 6.8. Lacosamide was released for 12 h from the sustainedrelease (SR) tablet, as compared to complete release within 1 h from an immediate-release $Vimpat^{(R)}$ tablet. Each formulation (100 mg) was orally administered to six beagle dogs and six mini-pigs under fasted conditions, and pharmacokinetic parameters such as the area under the concentration time curve ($AUC_t$), the maximum plasma concentration ($C_{max}$), and the time at which this occurred ($T_{max}$) were calculated. These results showed similar values for $AUC_t$, $C_{max}$, and $T_{max}$ following oral administration of immediate-release ($Vimpat^{(R)}$) and SR lacosamide tablets.

Chemical Forms and Release Potential of Heavy Metals from the Lime Treated Sediments (석회 처리에 의한 오염 퇴적물 내 중금속의 형태 변화 및 용출 가능성)

  • Park, Gil-Ok;Jun, Sang-Ho
    • Korean Journal of Ecology and Environment
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    • v.41 no.2
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    • pp.166-173
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    • 2008
  • Chemical forms and release potential of heavy metals were studied in the lime treated sediment of lake Chungcho. Chemical forms of heavy metals were analyzed using a sequential extraction method, and release potential of heavy metals was evaluated by the ratio of the content of labile forms to total metal one. Dominant form of Cd, Cu, Pb, and Zn in the untreated sediments was organic/sulfidic form that is stable in the reducing environment such as the bottom of Lake Chungcho. With liming of the sediment, the chemical forms of studied metals were greatly changed from organic/sulfidic form to adsorbed and reducible form, especially Cd and Cu to adsorbed and reducible form, but Pb and Zn to reducible form. It is believed that increase of unstable form of heavy metals in the sediments by liming was caused by the increase of pH of the pore water at the expense of organic/sulfidic form. Thus, we concluded that the liming approach currently used in the treatment of dredged sediments might cause the increase of labile form which is easily dissolved, and may increase the release of metals from the sediment into overlying water.

Effect of slow-release Nitrogen fertilizers to reduce labor(1) Effect of slow-release fertilizers on yield of radish (노동력 절감을 위한 수효성 질소질비료 효과(I))

  • 김경제
    • Korean Journal of Organic Agriculture
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    • v.5 no.1
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    • pp.79-85
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    • 1996
  • This experiment was carried out to investigate the effect of slow-release fertilizers on yield of radigh. Fertilizers were treated with CDU, MEISTER, Jobi Gohyungbok-hapbiryo, Kyungki Wonyebokbi 1ho, Kyungkibokbi Nojeok, Kyungki Jeonjakgo-hyungbokbi, Tradidtional manuring, and No maunring. Yields of radish were increased with slow-release fertilizers, CDU and MEISTER were effective to radish shoot, also. But analysis of chemical components of plants and soil were no difference. It was very effect to increase yields of radish, to reduce in number of supplementary manuring and laboring.

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Effect of slow-release Nitrogen fertilizers to reduce labor Effect of slow-release fertilizers on yield of lettuce (노동력 절감의 수효성 질소질비료 효과(II)-상치의 수량에 미치는 영향-)

  • 김경제
    • Korean Journal of Organic Agriculture
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    • v.5 no.2
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    • pp.85-91
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    • 1997
  • This experiment was carried out to investigate the effect of slow-release fertilizers on yield of lettuce. Fertilizers were treated with CDU, MEISTER, Jobi Gohyungbokhapbiryo, Kyungki Wonyebokbi 1ho, Kyungkibokbi Nojeok, Kyungki Jeonjakgohyungbokbi, Traditional manuring, and No manuring. Yields of Spinach was increased with slow-release fertilizers, also. But analysis of chemical components of plants and soil were no difference. It was very effect to increase yields of lettuce, to reduce in number of supplementary manuring and laboring.

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Release and Characterization of Multiple Coated Pellets Containing Melatonin (멜라토닌이 함유된 다층 코팅 펠렛의 방출 및 특성분석)

  • Kang, Bok-Ki;Khang, Gil-Son;Kim, Jong-Min;Jeung, Sang-Young;Lee, Hai-Bang;Cho, Sun-Hang
    • Journal of Pharmaceutical Investigation
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    • v.33 no.3
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    • pp.179-185
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    • 2003
  • Melatonin (MT) is an indole amide pineal hormone. It has not only very short half-life but also pH-sensitive property. The sustained release dosage form which delivers MT in a circadian fashion over 8 h is clinical value. The purpose of this study is to prepare sugar beads using multiple coating methods and enteric-coated in a sustained release to evaluate in vitro release characteristics in simulated gastric and intestinal fluids. The $Eudragit^{\circledR}$ as a polymer, sustained release membrane, and triethylcitrate (TEC) as a plasticzer were used. Multi-coated melatonin delivery system was composed of sugar, various excipients, $Eudragit^{\circledR}$ and enteric materials (e.g. hydroxy propyl methyl cellulose phthalate, HPMCP), and prepared by fluid bed coater. The dissolution test was carried out using the basket method at a stirring speed of 100 rpm at $37^{\circ}C$ in simulated gastric (pH 1.2) and intestinal fluid (pH 7.4). The released amount of MT was determined by High performance liquid chromatography method. The morhologies of surface and cross section of multi-coated beads were observed by scanning electron microscope. Size of multi-coated sugar beads was ranged over $1000{\sim}1300\;{\mu}m$. The release rate of MT from coated beads was limited in simulated gastric fluid (pH 1.2), but it was sustained in intestinal fluid (pH 7.4) during $3{\sim}8$ hours. The MT beads may provide small-intestine-targeted device for oral delivery. Studies on animal and relative experiment are in process.

Effects of Hydrophilic Additives on the Release Rate of Protein Drugs (단백질 약물 방출속도에 미치는 친수성 첨가제의 영향)

  • Kwon, Young-Kwan;Kim, Ji-Hyeon;Yoo, Young-Je
    • KSBB Journal
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    • v.22 no.4
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    • pp.213-217
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    • 2007
  • It has been reported that hydrophobic additives generally decrease the release rate of protein drugs from drug delivery systems (DDS) and hydrophilic additives increase the release rate. In many cases, however, the addition of hydrophilic molecule is necessary for improving the stability of protein drugs. In the present work, the effects of hydrophilic additives on the release profiles, and micelle formation of protein drug formulations were investigated to develop a novel method for protein drug delivery. For model protein drug, bovine serum albumin (BSA) was employed and several hydrophilic additives were used in the release experiments. Hydrophilic additive D-sorbitol showed the lower release rates of BSA than other hydrophobic additives due to the gel strengthening ability of the additive and the optimum concentration of D-sorbitol was 3 w/v % for the retarded release rate. In addition, it was found that the addition of D-sorbitol was very effective for obtaining homogeneous and stable DDS. The results were discussed in terms of the micelle formation and the micelle structure, i.e., the differences in gel structure and the distribution of drugs in micelles.

Preparation and Release Characterization of Osmotic Granule Nifedipine Delivery System (니페디핀 삼투성 과립 시스템의 제조와 약물 방출 특성)

  • Jeong, Sung-Chan;Cho, Young-Ho;Lee, Soo-Young;Lee, Bong;Kim, Moon-Suk;Kang, Gil-Son;Lee, Hai-Bang
    • Journal of Pharmaceutical Investigation
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    • v.36 no.1
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    • pp.11-17
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    • 2006
  • The objective of this study was to confirm the effect of the type of dissolution media and paddle speed on nifedipine (ND) release profile from osmotic granule and the storage stability. Osmotic granule was manufactured by fluidized bed coating method. At each coating step, morphology of osmotic granule was differed. The size of osmotic granule was $750\;{\mu}m$ at 3 wt% membrane thickness. ND release was changed in diverse dissolution media, paddle speed. ND release is governed by not only osmotic pressure but diffusion from osmotic granule. ND release from osmotic granule decreased as storage period increased. These may be caused by liquid excipient which has low molecular weight. Storage stability of osmotic granule could be improved by removing liquid excipient from semipermeable membrane.

Intercalation of Vitamer into LDH and Their Controlled Release Properties

  • Choy, Jin-Ho;Son, You-Hwan
    • Bulletin of the Korean Chemical Society
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    • v.25 no.1
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    • pp.122-126
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    • 2004
  • Biofunctional nanohybrids are synthesized from layered double hydroxide (LDH) and the vitamins such as ascorbic acid and topopherol acid succinate. Either ion exchange or copricipitaion leads to successful intercalation of the vitamins into gallery space of LDH that offers a new route to safe preservation of bioactivity as well as controlled release. Intercalations of vitamins are clearly reflected on the increase in the basal spacing of ZnAl-(Nitrate) LDH from 8.5 ${\AA}$ to 10.5 ${AA}$ for ascorbate, and 49.0 ${AA}$ for tocopherol acid succinate, respectively. No significant change in UV-Vis and IR absorption characteristics of the intercalated vitamins strongly supports the safe maintenance of their bioactivities without any deterioration of chemical and structural integrity. Furthermore, it is shown that the hybridized vitamins could be discharged in a controlled kinetics.

Revelation of the Susceptibility of Microcapsule by the Control of Polymer Structure (II) -Preparation of polyurethane microcapsules with different chemical structures- (고분자구조제어에 의한 microcapsule의 감성기능발현(II) -화학구조에 따른 polyurethane microcapsule의 특성-)

  • Hong, Ki-Jeong;Park, Soo-Min
    • Textile Coloration and Finishing
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    • v.9 no.5
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    • pp.63-74
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    • 1997
  • Polyurethane microcapsules were synthesized by interfacial polymerization in an aqueous poly(ethylene glycol) dispersion with ethylenediamine as chain extender of toluene diisocyanate in perfume oil using poly(vinyl alcohol) as the stabilizing agent. The effect of chemical structure on the average particle size and distributions, morphologies, and thermal properties to design microcapsules for the sustained release system was investigated. It came to be known that polyurethane microcapsules with ethylene diamine as chain extender had a rounder, more permeable and controlled release membranes. And the release test of polyurethane microcapsules with different soft segment content was done to certify the effect of long methylene chain. According to the higher molecular weight of polyether polyol, the release rate of microencapsulated disperse dye molecular was faster.

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