To investigate the rat intestinal absorption of stearic acid-octaarginine (SA-R8) modified solid lipid nanoparticles containing paclitaxel (SA-R8-PTX-SLN), compared with the commercially available preparation of PTX (Taxol) and PTX-loaded solid lipid nanoparticles (PTX-SLN), the in situ intestinal absorption of SA-R8-PTX-SLN was investigated by means of single-pass rat intestinal perfusion technique. The absorptions of the preparations were investigated at different intestinal segments, different drug concentrations and in the presence of P-glycoprotein inhibitor (verapamil). The results showed that PTX could be absorbed at each intestinal segment and the three preparations all showed maximum absorptions at the duodenum. The cumulative absorptions of three preparations at each intestinal segment appeared SA-R8-PTX-SLN > PTX-SLN > Taxol (P < 0.05). SA-R8-PTX-SLN showed a liner absorption manner at the duodenum in the examined drug concentration range. The cumulative absorptions of Taxol and PTX-SLN were significantly promoted after the addition of P-glycoprotein inhibitor (verapamil) into the preparation (P < 0.05), but absorption of SA-R8-PTX-SLN existed no significantly difference compared with the preparation without verapamil (P > 0.05). SA-R8 and SLN might both effectively improve the oral absorption of PTX in the intestinal tract.
ATP-Binding Cassette, Sub-Family B, Member 1 ; antagonists & inhibitors ; Animals ; Antineoplastic Agents, Phytogenic ; administration & dosage ; chemistry ; pharmacokinetics ; Cell-Penetrating Peptides ; chemistry ; Drug Carriers ; Intestinal Absorption ; drug effects ; Lipids ; chemistry ; Male ; Nanoparticles ; Oligopeptides ; chemistry ; Paclitaxel ; administration & dosage ; chemistry ; pharmacokinetics ; Perfusion ; Rats ; Rats, Sprague-Dawley ; Stearic Acids ; chemistry ; Verapamil ; pharmacology

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

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 ; Cell Membrane ; Cerebral Cortex ; Diphenylhexatriene ; Lipid Bilayers ; Membrane Lipids ; Membrane Proteins ; Membranes ; Methanol ; Neurons ; Palmitic Acids ; Phospholipids ; Proteins ; Stearic Acids

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 ; Oral Health ; Probiotics ; Sorbitol ; Stearic Acids ; Weissella ; Xylitol

OBJECTIVETo investigate chemical constituents of the root bark of Tripterygium hypoglaucum.

METHODCompounds were isolated by column chromatography on silica gel and Sephadex LH-20, and their structures were identified on the basis of spectral data (MS, 1H-NMR and 13C-NMR).

RESULTTwelve compounds were isolated and identified as friedelin (1), 3-oxo-olean-9(11),12-diene (2), canophyllal (3), 3-acetoxy oleanolic acid (4), triptophenolide (5), triptonoterpene methyl ether (6), tricosanoic acid (7), beta-sitosterol (8), stearic acid (9), glut-5-en-3beta,28-diol (10), palmitic acid (11) and daucostorol (12).

CONCLUSIONCompounds 1, 2, 3, 7 and 10 were isolated from T. hypoglaucum and 7 from the genus Tripterygium for the first time.

Chromatography ; methods ; Diterpenes ; chemistry ; isolation & purification ; Fatty Acids, Unsaturated ; chemistry ; isolation & purification ; Magnetic Resonance Spectroscopy ; methods ; Mass Spectrometry ; methods ; Oleanolic Acid ; chemistry ; isolation & purification ; Organic Chemicals ; chemistry ; isolation & purification ; Palmitic Acid ; chemistry ; isolation & purification ; Plant Roots ; chemistry ; metabolism ; Sitosterols ; chemistry ; isolation & purification ; Stearic Acids ; chemistry ; isolation & purification ; Tripterygium ; chemistry ; metabolism ; Triterpenes ; analysis ; chemistry ; isolation & purification

The asialoglycoprotein receptor (ASGPR) was used to mediate drug carrier for hepatic targeted drug delivery, this article showed the enzyme-catalyzed esterification of galactose and vinyl stearate and a kind of ASGPR ligand-targeted which was used to insert the surface of liposome has been synthesized. The structure of product has been confirmed by TLC, ESI-MS and 1H NMR. The factors of types and quantity of enzyme, organic solvents, molar ratio of substrate, temperature and time of reaction have been studied. Results showed when using acetone as reaction medium, the quantity of Novozym 435 immobilized lipase was 30 mg mL(-1), molar ratio of galactose to vinyl stearate was 1:5, and reacted at 60 degrees C for 12 h, the transformation of vinyl stearate reached more than 70%. This study provides a novel and efficient route to the synthesis of ligand-targeted modifier.
Acetone ; chemistry ; Asialoglycoprotein Receptor ; chemical synthesis ; Catalysis ; Esterification ; Galactose ; chemistry ; Ligands ; Lipase ; chemistry ; Stearates ; chemistry ; Temperature ; Vinyl Compounds ; chemistry

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 ; Carbon ; Cell Membrane ; Cerebral Cortex ; Fluorescence Polarization ; Liposomes ; Membranes ; Neurons ; Palmitic Acid ; Palmitic Acids ; Phospholipids ; Stearic Acids

Anterior reconstruction with instrumentation of the thoracolumbar junction (TLJ) offers: 1) the biomechanical advantage of immediate restoration of the load-bearing anterior column and 2) the ideal biological milieu for an optimal arthrodesis. The authors describe the mini-transthoracic supradiaphragmatic (MTTS) approach to the TLJ. Its technical feasibility is compared with that of the traditional transdiaphragmatic and thoracoscopic supradiaphragmatic approaches to this area of the spine. This technique was performed in 21 patients from 2004 to 2006. There were no surgical mortalities. The MTTS approach without the use of a thoracoscope was successfully employed in this study to treat patients with various lesions located at the TLJ. The diaphragmatic opening, even at its smallest diameter, provides excellent views of the operative field and avoids the significant morbidities associated with the traditional transdiaphragmatic approach.
Arthrodesis ; Diaphragm ; Humans ; Imidazoles ; Nitro Compounds ; Spine ; Stearates ; Thoracoscopes ; Weight-Bearing

OBJECTIVETo investigate the effects of labrasol, solutol HS 15 and transcutol P on the corneal permeability of mangiferin in vitro.

METHODThe effects of three penetration enhancers on the corneal permeability of mangiferin were investigated in vitro by using isolated rabbit corneas.

RESULTThe apparent Papp enhancements were increased 1.80, 3.27, 3.41 and 4.76-folds with Lab at 1.0%, 1.5%, 2.0% and 3.0% (P < 0.01), respectively. The apparent Papp increased 1.98 and 3.07-folds with Sol at 0.2% and 0.4% (P < 0.01), respectively, but reduced with 0.010%-0.03% Trans.

CONCLUSIONThe Papp value of mangiferin is significantly enhanced by 1.0%-3.0% Lab, 0.2% and 0.4% Sol, however the Papp value of mangiferin is reduced by 0.01%-0.03% Trans.

Animals ; Cornea ; drug effects ; metabolism ; Drug Carriers ; chemistry ; Ethylene Glycols ; chemistry ; Glycerides ; In Vitro Techniques ; Organic Chemicals ; chemistry ; Permeability ; Plant Extracts ; pharmacokinetics ; Polyethylene Glycols ; chemistry ; Rabbits ; Stearic Acids ; chemistry ; Xanthones ; pharmacokinetics

OBJECTIVETo research the plasmic metabolites and metabolic pathway of Xin-blood stasis syndrome (XBSS).

METHODSPlasma metabolic products in patients of coronary heart disease (CHD) with XBSS or non-XBSS and subjects in the control group were identified by gas chromatographic mass spectrometry (GC-MS) type QP2010, the changes of their main elements in different groups were analyzed by principal components analysis (PCA) and partial least squares (PLS) analysis.

RESULTSPCA showed that as compared with that in the control group, in the CHD-XBSS group, contents of lactic acid, beta-hydroxy butanoic acid, urea, oleic acid, octadecanoic acid and arachidonic acid were higher and that of citric acid was lower. PLS analysis showed significant difference between the control group and the other two groups, and the latter two groups tend to be of a same category. The occurrence of XBSS was positively correlated with octadecanoic acid, arachidonic acid, urea, lactic acid and beta-hydroxy, butanoic acid contents, and negatively correlated with oleic acid, L-proline, glycine, and citric acid contents. According to VIP, the degree of correlation between variables with drug interven- tion, from high to low, were ranked as arachidonic acid, octadecanoic acid, lactic acid, urea, beta-hydroxy butanoic acid, linoleic acid, glucose, alanine, oleic acid and proline. Discrepancy analysis on 11 changeful metabolites showed that the contents of arachidonic acid, octadecanoic acid, lactic acid, urea, beta-hydroxy butanoic acid and oleic acid increased in CHD patients, especially in those with XBSS (P < 0.01). In CHD patients, contents of lactic acid, beta-hydroxy butanoic acid, linoleic acid and glucose in patients of XBSS pattern were higher than in non-XBSS pattern (P < 0.01); content of linoleic acid, glucose, alanine and proline decreased in non-XBSS pattern while increased in XBSS pattern. Content of glucose in CHD-XBSS patients was significantly higher than that in the healthy control (P < 0.01). Content of citric acid was lower in CHD patients, and showed significant difference between that in CHD-XBSS patients and healthy control (P < 0.01).

CONCLUSIONSThe major plasmic metabolites in CHD-XBSS patients are arachidonic acid, octadecanoic acid, lactic acid, urea, citric acid, beta-hydroxybutyric acid, oleic acid, glucose, and alanine. Analyzed from plasmic metabolite spectrum view, CHD-XBSS is related with lipid metabolism and glyco-metabolism, also with the stress induced by hypoxia and agonia.

Adult ; Aged ; Arachidonic Acid ; blood ; Coronary Disease ; blood ; diagnosis ; Diagnosis, Differential ; Female ; Gas Chromatography-Mass Spectrometry ; Humans ; Lactic Acid ; blood ; Least-Squares Analysis ; Male ; Medicine, Chinese Traditional ; Metabolome ; Metabolomics ; methods ; Middle Aged ; Principal Component Analysis ; Stearic Acids ; blood