• Journal of Pharmaceutical Investigation
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• v.25 no.3
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• pp.227-237
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• 1995

Omeprazole(OMP) complexes such as inclusion complexes of OMP with $hydroxypropyl-{\beta}-cyclodextrin$(HPCD) and ${\beta}-cyclodextrin({\beta}-CD)$, OMP-cholestyramine(CHL) and OMP-ethylenediamine(OMP-ED) were prepared, respectively. The partition coefficients in Witepsol H-15 /pH 7.4 phosphate buffer solution of OMP complexes$(OMP-HPCD;\;3.69{\pm}0.26,\;OMP-{\beta}-CD;\;4.08{\pm}0.21,\;OMP-CHL;\;4.36{\pm}0.25\;and\;omeprazole\;sodium(OMP-Na);\;3.64{\pm}0.37)$ were higher than that of OMP $(2.66{\pm}0.47)$. OMP was not completely dissolved until even 3 hrs, but all the OMP complexes studied were released about 100% in 20 min. The rectal suppositories containing OMP or each above OMP complex were prepared using Witepsol H-15 base, and their dissolution and stability were examined, and pharmacokinetic study were investigated after their rectal administrations to the rabbits. While the suppository containing OMP was released only less than 60% in 150 min, $OMP-{\beta}-CD$, OMP-CHL, OMP-Na and OMP-ED suppositories were all released about 65% in 20 min. Especially, OMP-HPCD suppository released OMP about 70% in 10 min. All the additives such as sodium laurylsulfate, eglumine, arginine and PVP increased drug release from OMP-HPCD suppository to some extent. The decomposition rate constants of OMP in the suppositories were $9.117{\times}10^{-3}\;day^{-l}$ for OMP suppository, $2.121{\times}10^{-2}$ for OMP-HPCD, $1.607{\times}10^{-2}$ for $OMP-{\beta}-CD$, $9.26{\times}10^{-3}$ for OMP-Na, $6.769{\times}10^{-3}$ for OMP-CHL and $5.58{\times}10^{-3}\;day^{-l}$ for OMP-ED suppository, respectively. Additives such as arginine, eglumine and ED had some stabilizing effect for OMP-HPCD, OMP-CHL and OMP-Na suppositories, respectively. After 6 month-storage at $30^{\circ}C$, 75% RH, OMP-CHL suppository was most stable. The values of Tmax for OMP-HPCD and OMP-Na suppositories were $11.7{\pm}2.36\;and\;11.4{\pm}2.56\;min$, respectively. The values of Cmax for OMP-HPCD and OMP-CHL suppository were $2.31\;{\mu}g/ml\;(p<0.01)\;and\;1.89\;{\mu}g/ml\;p<0.01)$, respectively. The values of AUC for OMP and $OMP-{\beta}-CD$ suppository were $61.9{\pm}25.79\;and\;68.6{\pm}29.48\;{\mu}g\;{\cdot}\;min/ml$, and the corresponding values for OMP-HPCD and OMP-CHL were $106.1{\pm}43.16\;(p<0.05)\;and\;127.3{\pm}42.52\;{\mu}g\;{\cdot}\;min/ml(p<0.01)$, respectively. The above results indicate the OMP-HPCD and OMP-CHL suppositories have the excellent bioavailabilties in vivo study.

• Journal of the Institute of Electronics Engineers of Korea SP
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• v.49 no.2
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• pp.122-129
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• 2012

As a greedy algorithm reconstructing the sparse signal from underdetermined system, orthogonal matching pursuit (OMP) algorithm has received much attention in recent years. In this paper, we present an extension of OMP for pursuing efficiency of the index selection. Our approach, referred to as generalized OMP (gOMP), is literally a generalization of the OMP in the sense that multiple (N) columns are identified per step. Using the restricted isometry property (RIP), we derive the condition for gOMP to recover the sparse signal exactly. The gOMP guarantees to reconstruct sparse signal when the sensing matrix satisfies the RIP constant ${\delta}_{NK}$ < $\frac{\sqrt{N}}{\sqrt{K}+2\sqrt{N}}$. In addition, we show recovery performance and the reduced number of iteration required to recover the sparse signal.

• Korean Journal of Microbiology
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• v.33 no.2
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• pp.118-124
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• 1997

In the previous study(6), we constructed the CheY-OmpR hybrid, Chp, which affects the expressions of ompF and om pC genes. Here we further characterize these effects and present the regulatory mechanism based on in vivo and in vitro data. Although Chp retained the sequence-specific DNA-binding ability, it was not possible to enhance transcriptional activity, suggesting that it may act as a competitive inhibitor to OmpR. The DNA-binding affinity of Chp was not modulated by phosphorylation of its Che Y portion. Chp was able to increase ompR transcription. FurthemlOre, it was found that the wild-type OmpR also exerts the same effect, which is also eOlltrolled by changes in medium osmolarity and in EnvZ activity.

• YAKHAK HOEJI
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• v.39 no.2
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• pp.175-184
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• 1995

The interaction of omeprazole(OMP) with $\gamma$-cyclodextrin($\gamma$-CyD) was investigated by solubility study and the complexation was confirmed by means of UV/VIS spectrophotometer, circular dichroism, differential scanning calorimeter, and $^{1}$H nuclear magnetic resonance spectra. The stability, dissolution rate, and partition coefficient of the complex were measured. The results present that the benzimidazole moiety and a part of pyridine ring containing sulfur atom of OMP might be included into the cavity of $\gamma$-CyD and the formation type of inclusion complex appeared to be B$_{s}$. The stoichiometric ratio of OMP to $\gamma$-CyD in the complex was found to be 1:1 and the stability constant of the complex found to be 97.1 M$^{-1}$. And the dissolution rate of OMP was markedly increased by inclusion complex formation with $\gamma$-CyD, and so it was above 90% in 5 min. from solid complex. Oil to water partition coefficient of OMP-$\gamma$-CyD complex was 60, which is significantly higher than that of OMP itself, 36.4. The degradation rate constant of OMP were greater than OMP-$\gamma$-CyD complex in aqueous solutions of various pHs, and the half lives of OMP and OMP-$\gamma$-CyD at pH 9 were 279.2 and 509.9 days, respectively, showing that the complex was more stable than OMP, therefore it was thought that OMP was stabilized by inclusion formation with $\gamma$-CyD.

• Journal of Pharmaceutical Investigation
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• v.27 no.4
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• pp.271-277
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• 1997

Because omeprazole(OMP) is very unstable in aqueous condition, $OMP-{\beta}-CD$, the inclusion complex of OMP and ${\beta}-cyclodextrin({\beta}-CD)$ was made and physicochemical properties of it were compared with those of OMP. Skin permeability of OMP and $OMP-{\beta}-CD$ in propylene glycol vehicle and the reciprocal action of ${\beta}-CD$ with various enhancers were examined through hairless mouse. Adhesive patches were prepared with polyisobutylene and the skin permeability and stability of OMP were investigated. The inclusion complex showed higher solubility and lower partition coefficient than OMP itself. DMSO, 1-methyl 2-pyrrolidone and sodium cholate had an enhancing effect. However ethanol and polysorbate 80 hardly showed the enhancing effect of OMP. When sodium lauryl sulfate and sodium cholate as enhancer were added in patch, the former case showed higher permeability of OMP.

• Microbiology and Biotechnology Letters
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• v.33 no.4
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• pp.274-280
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• 2005

Pasteurella multocida is known to cause widespread infections in husbandry. To induce homologous and heterologous immunity against the infections, outer membrane proteins (OMPs) in the envelope of P. multocida are thought to be attractive vaccine candidates. Outer membrane protein H is considered as the major component of OMPs. In this study, a gene for OmpH was isolated from pathogenic P. multocida serogroup A. The gene was composed of 1,047 nucleotides coding 348 amino acids with signal peptide of 20 amino acids. The amino acid composition showed about 80 to 98 per cent sequence homologies among other 10 strains of P. multocida serogroup A, reported so far. A recombinant ompH, from which signal peptide was truncated, was generated using pRSET A to name 'pRSET A/OmpH-F2'. The pRSET A/OmpH-F2 was well expressed in E. coli BL21(DE3). The truncated OmpH was purified using nickel-nitrilotriacetic acid (Ni-NTA) affinity column chromatography. Its molecular weight was registered to be 40 kDa on SDS-PAGE gel. In order to generate immunesera against the OmpH, 50 ug of the protein was intraperitoneally injected into mice three times. The anti-OmpH immuneserum recognized about $5{\times}10^{-2}$ng quantity of the purified OmpH. It can be used for an effective vaccine production to prevent fowl cholera caused by pathogenic P. multocida (Serogroup A).

• Journal of Microbiology and Biotechnology
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• v.16 no.10
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• pp.1529-1536
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• 2006

We cloned a gene of ompH(D:4) from pigs infected with P. multocida D:4 in Korea [16]. The gene is composed of 1,026 nucleotides coding 342 amino acids (aa) with a signal peptide of 20 aa (GenBank accession number AY603962). In this study, we analyzed the ability of the ompH(D:4) to induce protective immunity against a wild-type challenge in mice. To determine appropriate epitope(s) of the gene, one full and three different types of truncated genes of the ompH(D:4) were constructed by PCR using pET32a or pRSET B as vectors. They were named ompH(D:4)-F (1,026 bp [1-1026] encoding 342 aa), ompH(D:4)-t1 (693 bp [55-747] encoding 231 aa), ompH(D:4)-t2 (561 bp [187-747] encoding 187 aa), and ompH(D:4)-t3 (540 bp [487-1026] encoding 180 aa), respectively. The genes were successfully expressed in Escherichia coli BL21(DE3). Their gene products, polypeptides, OmpH(D:4)-F, -t1, -t2, and -t3, were purified individually using nickel-nitrilotriacetic acid (Ni-NTA) affinity column chromatography. Their $M_rs$ were determined to be 54.6, 29, 24, and 23.2 kDa, respectively, using SDS-PAGE. Antisera against the four kinds of polypeptides were generated in mice for protective immunity analyses. Some $50{\mu}g$ of the four kinds of polypeptides were individually provided intraperitoneally with mice (n=20) as immunogens. The titer of post-immunized antiserum revealed that it grew remarkably compared with pre-antiserum. The lethal dose of the wild-type pathogen was determined at $10{\mu}l$ of live P. multocida D:4 through direct intraperitoneal (IP) injection, into post-immune mice (n=5, three times). Some thirty days later, the lethal dose ($10{\mu}l$) of live pathogen was challenged into the immunized mouse groups [OmpH(D:4)-F, -t1, -t2, and -t3; n=20 each, two times] as well as positive and negative control groups. As compared within samples, the OmpH(D:4)-F-immunized groups showed lower immune ability than the OmpH(D:4)-t1, -t2, and -t3. The results show that the truncated-OmpH(D:4)-t1, -t2, and -t3 can be used for an effective vaccine candidate against swine atrophic rhinitis caused by pathogenic P. multocida (D:4) isolated in Korea.

• Journal of Microbiology
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• v.45 no.2
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• pp.179-184
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• 2007

Pasteurella multocida, a Gram-negative facultative anaerobic bacterium, is a causative animal pathogen in porcine atrophic rhinitis and avian fowl cholera. For the development of recombinant subunit vaccine against P. multocida, we cloned and analyzed the gene for outer membrane protein H (ompH) from a native strain of Pasteurella multocida in Korea. The OmpH had significant similarity in both primary and secondary structure with those of other serotypes. The full-length, and three short fragments of ompH were expressed in E. coli and the recombinant OmpH proteins were purified, respectively. The recombinant OmpH proteins were antigenic and detectable with antisera produced by either immunization of commercial vaccine for respiratory disease or formalin-killed cell. Antibodies raised against the full-length OmpH provided strong protection against P. multocida, however, three short fragments of recombinant OmpHs, respectively, showed slightly lower protection in mice challenge. The recombinant OmpH might be a useful vaccine candidate antigen for P. multocida.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1995.04a
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• pp.133-133
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• 1995

각종 OMP 복합체들은 OMP에 비해 용해도가 2.7-12.0배 증가하였으며, 모두 10분 이내에 85% 이상이 용출되어 용출규정에 적합하였고 pH 및 습도에 따른 안정성 결과도 OMP에 비해 각종 OMP 복합체가 안정성이 증가되었다. OMP-cholestyramine 수지염의 경우 온도, 습도 및 수용액 중에서의 안정성 모두 OMP에 비하여 향상되었으며, 4$0^{\circ}C$, RH 75%의 가혹조건에서도 OMP pellet에 비해 OMP-cholestyramine 수지염 pellet이 안정성과 내산성이 매우 우수하였다.

• YAKHAK HOEJI
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• v.35 no.5
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• pp.372-378
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• 1991

To increase the stability and bioavailability of Omeprazole(OMP), which is used newly as a proton-pump inhibitor, inclusion complex of OMP with $\beta$-cyclodextrin($\beta$-CD) was prepared by coprecipitation method and its characteristics were ascertained by means of solubility test, DSC, IR, and the accelerated stability analysis. The type of OMP inclusion complex is classified as Bs-type on phase solubility diagram, and the stoichiometric ratio of OMP: $\beta$-CD complex is 1:2 and formation constant is 80.82/mole. The solubility of the complex could be increased remarkably by complexation compare with OMP. Degradation process of both OMP and OMP complex followed apparent first-order kinetics, of which degradation rate constants and activation energies are k$_{25}$=8.1$\times$10$^{-4}$/day, E$_{a}$=22 Kcal/mole (OMP), and k$_{25}$=4.65$\times$10$^{-6}$/day, E$_{a}$=35 Kcal/mole (complex), respectively. These results show the increase of the stability and solubility of OMP markedly, therefore it is believed that the improvement of stabilization for OMP by inclusion complexation might be practically available.