1.Studies on sustained release solid dispersion of tripterine carried by HPMC-stearic acid.
Shao-Ying HU ; Zhen-Hai ZHANG ; Yan-Rong JIANG ; Qing NING ; Qi-Yuan LIU ; Xiao-Bin JIA
China Journal of Chinese Materia Medica 2012;37(20):3052-3055
OBJECTIVETo prepare the sustained release solid dispersion of tripterine, using HPMC-stearic acid with the intention of improving drug dissolution and controlling drug releases moderate, so that the drug performances lower toxicity.
METHODTripterine sustained release solid dispersions was prepared by the solvent method with different weight ratios of HPMC-stearic acid and tripterine, which were dissolved in 95% ethanol. And in vitro dissolution experiment was conducted. Differential scanning calorimetry, scanning electron microscopy and X-ray powder diffraction can prove the formation of solid dispersions.
RESULTThe ideal tripterine sustained release solid dispersions were prepared under the condition as follows, the weight ratio of tripterine and HPMC-stearic acid was 1: 10, and the release rate of drug can keep moderate and controllable. In vitro cumulative release of tripterine sustained release solid dispersion is up to more than 90% after 8 h, and the tripterine exist as amorphous in the solid dispersion.
CONCLUSIONThe sustained release solid dispersion of tripterine, carried by HPMC-stearic acid, can improve the release of tripterine effectively and controls the release rate keep moderate and controllable, and the preparation process is simple, which has potential applications.
Chemistry, Pharmaceutical ; methods ; Delayed-Action Preparations ; chemistry ; Drug Carriers ; chemistry ; Kinetics ; Stearic Acids ; chemistry ; Triterpenes ; chemistry
2.Studies on chemical constituents from the seed of Trigonella foenum-graecum.
Ming-ying SHANG ; Shao-qing CAI ; Wen-han LIN ; Min-chuan WANG ; Jong-hee PARK
China Journal of Chinese Materia Medica 2002;27(4):277-279
OBJECTIVETo study the chemical constituents from the seed of Trigonella foenum-graecum.
METHODThe compounds were isolated with silica gel chromatography and their structures were identified by physical, chemical properties and spectral analysis.
RESULTSeven compounds were isolated and identified as N,N'-dicarbazyl, glycerol monopalmitate, stearic acid, beta-sitosteryl glucopyranoside, ethyl-alpha-D-glucopyranoside, D-3-O-methyl-chiroinsitol and sucrose.
CONCLUSIONAll the compounds were obtained from this plant for the first time and N,N'-dicarbazyl is a new natural product.
Carbazoles ; chemistry ; isolation & purification ; Plants, Medicinal ; chemistry ; Seeds ; chemistry ; Stearic Acids ; chemistry ; isolation & purification ; Trigonella ; chemistry
3.Comparison of Temperature and Additives Affecting the Stability of the Probiotic Weissella cibaria
Mi Sun KANG ; Youn Shin KIM ; Hyun Chul LEE ; Hoi Soon LIM ; Jong Suk OH
Chonnam Medical Journal 2012;48(3):159-163
Daily use of probiotic chewing gum might have a beneficial effect on oral health, and it is important that the viability of the probiotics be maintained in this food product. In this study, we examined the stability of probiotic chewing gum containing Weissella cibaria. We evaluated the effects of various factors, including temperature and additives, on the survival of freeze-dried probiotic W. cibaria powder. No changes in viability were detected during storage at 4degrees C for 5 months, whereas the viability of bacteria stored at 20degrees C decreased. The stability of probiotic chewing gum decreased steadily during storage at 20degrees C for 4 weeks. The viability of the freeze-dried W. cibaria mixed with various additives, such as xylitol, sorbitol, menthol, sugar ester, magnesium stearate, and vitamin C, was determined over a 4-week storage period at 20degrees C. Most of the freeze-dried bacteria except for those mixed with menthol and vitamin C were generally stable during a 3-week storage period. Overall, our study showed that W. cibaria was more stable at 4degrees C than that at 20degrees C. In addition, menthol and vitamin C had a detrimental effect on the storage stability of W. cibaria. This is the first study to examine the effects of various chewing gum additives on the stability of W. cibaria. Further studies will be needed to improve the stability of probiotic bacteria for developing a novel probiotic W. cibaria gum.
Ascorbic Acid
;
Bacteria
;
Chewing Gum
;
Gingiva
;
Magnesium
;
Menthol
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Oral Health
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Probiotics
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Sorbitol
;
Stearic Acids
;
Weissella
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Xylitol
4.The Effect of Tetracaine.HCl on Rotational Mobility of n-(9-Anthroyloxy) Stearic Acid in Outer Monolayers of Neuronal and Model Membranes.
Hyung Jin JOO ; Jong Hyo RYU ; Chin U PARK ; Sun Il JUNG ; Yun Seok CHA ; Sang Young PARK ; Jung Un PARK ; Soon Gun KWON ; Moon Kyung BAE ; Soo Kyoung BAE ; Hye Ock JANG ; Il YUN
International Journal of Oral Biology 2010;35(4):159-167
To provide a basis for studying the pharmacological actions of tetracaine.HCl, we analyzed the membrane activities of this local anesthetic. The n-(9-anthroyloxy) stearic and palmitic acid (n-AS) probes (n = 2, 6, 9, 12 and 16) have been used previously to examine fluorescence polarization gradients. These probes can report the environment at a graded series of depths from the surface to the center of the membrane bilayer structure. In a dose-dependent manner, tetracaine.HCl decreased the anisotropies of 6-AS, 9-AS, 12-AS and 16-AP in the hydrocarbon interior of synaptosomal plasma membrane vesicles isolated from bovine cerebral cortex (SPMV), and liposomes derived from total lipids (SPMVTL) and phospholipids (SPMVPL) extracted from the SPMV. However, this compound increased the anisotropy of 2-AS at the membrane interface. The magnitude of the membrane rotational mobility reflects the carbon atom numbers of the phospholipids comprising SPMV, SPMVTL and SPMVPL and was in the order of the 16, 12, 9, 6, and 2 positions of the aliphatic chains. The sensitivity of the effects of tetracaine.HCl on the rotational mobility of the hydrocarbon interior or surface region was dependent on the carbon atom numbers in the descending order 16-AP, 12-AS, 9-AS, 6-AS and 2-AS and on whether neuronal or model membranes were involved in the descending order SPMV, SPMVPL and SPMVTL.
Anisotropy
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Carbon
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Cell Membrane
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Cerebral Cortex
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Fluorescence Polarization
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Liposomes
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Membranes
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Neurons
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Palmitic Acid
;
Palmitic Acids
;
Phospholipids
;
Stearic Acids
5.Serum Phospholipid Fatty Acids in Benign Breast Tumor and Breast Cancer.
Eugene SHIM ; Sei Hyun AHN ; You Jeong HWANG ; Yang Cha LEE-KIM
The Korean Journal of Nutrition 2009;42(3):213-220
Studies on the relationship between blood fatty acids and the risk of breast cancer have not yielded definite conclusions. The role of fatty acids in the development and progression of breast cancer is unclear. We conducted a case-control study to determine serum phospholipid fatty acid composition in benign breast tumor and breast cancer. Subjects consisted of 27 benign breast tumor and 68 breast cancer patients, and 28 matched controls. The levels of fatty acids were measured by gas chromatography. Higher arachidonic and palmitic acids were observed in breast cancer patients as compared with control and benign breast tumor patients. The percentage of total saturated fatty acids in breast cancer was higher than in control and benign breast tumor patients. The level of stearic acid was lower in benign breast tumor and breast cancer patients. Saturation index, the ratio of stearic to oleic acid, was lower in benign breast tumor and breast cancer patients compared to the control. Moreover, stearic acid was negatively and arachidonic acid was positively correlated with the cancer stage. In conclusion, our results support that serum phospholipid compositions of specific fatty acids are associated with the risk of benign breast tumor as well as breast cancer. Further studies are necessary to investigate mechanisms linked to the breast cancer etiology.
Arachidonic Acid
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Breast
;
Breast Neoplasms
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Case-Control Studies
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Chromatography, Gas
;
Fatty Acids
;
Humans
;
Oleic Acid
;
Palmitic Acid
;
Palmitic Acids
;
Stearic Acids
6.Studies on chemical constituents from rhizome of Impatiens pritzellii var. hupehensis.
Xiao-Ya ZHAO ; Han-Dong SUN ; Ji-Zhou WU
China Journal of Chinese Materia Medica 2005;30(8):584-586
OBJECTIVETo study the chemical constituents from the rhizome of Impatiens pritzellii var. hupehensis.
METHODThe rhizome were extracted with methanol, isolated and purified by column chromatography on silica gel. All the compounds were identified on the basis of spectral analysis (including IR, MS, NMR) and physico-chemical characters.
RESULTFive compounds were identified as a-spinasterol (I), alpha-spinasteryl-7, 22-dien-3-O-beta-D-glucopyranoside (II), stigmast-7, 22-dien-3-one (III), stearic acid (IV), hentriantane (V).
CONCLUSIONCompound I is isolated from this plant for the first time, Compound II, III, IV, V are isolated from genus Balsaminaceae for the first time.
Impatiens ; chemistry ; Plants, Medicinal ; chemistry ; Rhizome ; chemistry ; Stearic Acids ; chemistry ; isolation & purification ; Stigmasterol ; analogs & derivatives ; chemistry ; isolation & purification
7.The Effect of Methanol on the Structural Parameters of Neuronal Membrane Lipid Bilayers.
Hyung Jin JOO ; Shin Ho AHN ; Hang Rae LEE ; Sung Woo JUNG ; Chang Won CHOI ; Min Seok KIM ; Moon Kyoung BAE ; In Kyo CHUNG ; Soo Kyoung BAE ; Hye Ock JANG ; Il YUN
The Korean Journal of Physiology and Pharmacology 2012;16(4):255-264
The structures of the intact synaptosomal plasma membrane vesicles (SPMVs) isolated from bovine cerebral cortexs, and the outer and the inner monolayer separately, were evaluated with 1,6-diphenyl-1,3,5-hexatriene (DPH) and 1,3-di(1-pyrenyl)propane (Py-3-Py) as fluorescent reporters and trinitrophenyl groups as quenching agents. The methanol increased bulk rotational and lateral mobilities of SPMVs lipid bilayers. The methanol increased the rotational and lateral mobilities of the outer monolayers more than of the inner monolayers. n-(9-Anthroyloxy)stearic acid (n-AS) were used to evaluate the effect of the methanol on the rotational mobility at the 16, 12, 9, 6, and 2 position of aliphatic chains present in phospholipids of the SPMVs outer monolayers. The methanol decreased the anisotropy of the 16-(9-anthroyloxy)palmitic acid (16-AP), 12-(9-anthroyloxy)stearic acid (12-AS), 9-(9-anthroyloxy)stearic acid (9-AS), and 6-(9-anthroyloxy)stearic acid (6-AS) in the SPMVs outer monolayer but it increased the anisotropy of 2-(9-anthroyloxy)stearic acid (2-AS) in the monolayers. The magnitude of the increased rotational mobility by the methanol was in the order at the position of 16, 12, 9, and 6 of aliphatic chains in phospholipids of the outer monolayers. Furthermore, the methanol increased annular lipid fluidity and also caused membrane proteins to cluster. The important finding is that was far greater increase by methanol in annular lipid fluidity than increase in lateral and rotational mobilities by the methanol. Methanol alters the stereo or dynamics of the proteins in the lipid bilayers by combining with lipids, especially with the annular lipids. In conclusion, the present data suggest that methanol, in additions to its direct interaction with proteins, concurrently interacts with membrane lipids, fluidizing the membrane, and thus inducing conformational changes of proteins known to be intimately associated with membranes lipids.
Anisotropy
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Cell Membrane
;
Cerebral Cortex
;
Diphenylhexatriene
;
Lipid Bilayers
;
Membrane Lipids
;
Membrane Proteins
;
Membranes
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Methanol
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Neurons
;
Palmitic Acids
;
Phospholipids
;
Proteins
;
Stearic Acids
8.Orthogonal experiments for optimizing the formulation and preparation conditions of temozolomide solid lipid nanoparticles.
Mingjin DOU ; Guihua HUANG ; Yanwei XI ; Na ZHANG
Journal of Biomedical Engineering 2008;25(5):1141-1145
TMZ-SLN were prepared by emulsification-low temperature solidification method with stearic acid. The formulation and the preparation conditions were optimized by orthogonal experiments using entrapment efficiency as the evaluation index. The morphology was detected by transmission electron microscope. The Zeta potentials and the particle size distribution were evaluated by Laser Doppler Anemometry. The entrapment efficiencies and the drug release characteristics in vitro were assessed. The result showed that TMZ-SLN were concinnous and spherical in shape. The mean diameter (d(av) ) was 65.0 +/- 6.2 nm and the Zeta potential was -37.2 mV. The average entrapment efficiency was 58.9% +/- 1.21 %. The drug release behavior in vitro conformed to Higuchi Equation. The formation of a new material phase was testified by analysis of differential scanning calorimetry.
Antineoplastic Agents, Alkylating
;
administration & dosage
;
chemistry
;
Dacarbazine
;
administration & dosage
;
analogs & derivatives
;
chemistry
;
Drug Carriers
;
chemistry
;
Lipids
;
chemistry
;
Nanoparticles
;
chemistry
;
Particle Size
;
Stearic Acids
;
chemistry
9.Chemical study on petroleum ether portion of Sarcandra hainanensis.
Congmei CAO ; Lijia XU ; Kui CHEN ; Yong PENG ; Peigen XIAO
China Journal of Chinese Materia Medica 2009;34(8):1009-1010
OBJECTIVETo study the chemical constituents in the whole plants of Sarcandra hainanensis.
METHODThe chemical constituents were isolated by various column chromatographic methods. The structures were identified by spectral data.
RESULTNine compounds, palmitic acid (1), icosanoic acid (2), beta-sitosterol (3), octadecanoic (4), acidchrysophanol (5), emodin (6), 2', 3'-dihydroxy-4', 6'-dimethoxychalcone (7), 2'-hydroxy4', 6'-dimethoxychalcone (8), cardamonin (9) were isolated and identified.
CONCLUSIONCompounds 1-9 were obtained from this plant for the first time. Compounds 2, 5-9 were isolated from family Chloranthaceae for the first time.
Alkanes ; chemistry ; Chalcones ; chemistry ; Eicosanoids ; chemistry ; Emodin ; chemistry ; Magnetic Resonance Spectroscopy ; Magnoliopsida ; chemistry ; Palmitic Acid ; chemistry ; Sitosterols ; chemistry ; Stearic Acids ; chemistry
10.Structure identification of jujuboside E.
Yan-jing BAI ; Gong CHENG ; Jing TAO ; Bin WANG ; Yu-ying ZHAO ; Yi LIU ; Li-bin MA ; Guang-zhong TU
Acta Pharmaceutica Sinica 2003;38(12):934-937
AIMTo study the chemical constituents of the seeds of Ziziphus jujuba Mill var. spinosa (Bunge) Hu ex. H.F. Chou.
METHODSTo separate the constituents by using various kinds of chromatography methods and identify their structures on the basis of spectral analysis.
RESULTSSeven compounds were isolated. Their structures were established as jujuboside E (1), jujuboside B (2), jujuboside A (3), betulic acid (4), stearic acid (5), sucrose (6) and inosine (7).
CONCLUSIONCompound 1 is a new compound named jujuboside E. Compounds 5, 6, 7 were isolated for the first time from this plant.
Inosine ; chemistry ; isolation & purification ; Molecular Conformation ; Molecular Structure ; Plants, Medicinal ; chemistry ; Saponins ; chemistry ; isolation & purification ; Seeds ; chemistry ; Stearic Acids ; chemistry ; isolation & purification ; Sucrose ; chemistry ; isolation & purification ; Ziziphus ; chemistry