AIM: To evaluate the effects of nitroester drugs on human sphincter of Oddi (SO) motility and their antagonistic effects against morphine which shows excitatory effect on Oddi's sphincter motility.METHODS: The eff...AIM: To evaluate the effects of nitroester drugs on human sphincter of Oddi (SO) motility and their antagonistic effects against morphine which shows excitatory effect on Oddi's sphincter motility.METHODS: The effects of these drugs on SO were evaluated by means of choledochofiberoscopy manometry.A total of 67 patients having T-tubes after cholecystectomy and choledochotomy were involved in the study, they were randomly divided into glyceryl trinitrate (GTN) group,isosorbide dinitrate (ISDN) group, pentaerythritol tetranitrate (PTN) group, morphine associated with GTN group, morphine associated with ISDN group and morphine associated with PTN group. Basal pressure of Oddi's sphincter (BPOS), amplitude of phasic contractions (SOCA), frequency of phasic contractions (SOF), duration of phasic contractions (SOD), duodenal pressure (DP) and common bile duct pressure (CBDP) were scored and analyzed. Morphine was given intramuscularly while nitroester drugs were applied sublingually.RESULTS: BPOS and SOCA decreased significantly after administration of ISDN and GTN, BPOS reduced from 10.95±7.49 mmHg to 5.92±4.04 mmHg (P＜0.05) evidently after application of PTN. BPOS increased from 7.37±5.58mmHg to 16.60±13.87 mmHg, SOCA increased from 54.09±38.37 mmHg to 100.70±43.51 mmHg, SOF increased from 7.15±3.20 mmHg to 10.38±2.93 mmHg and CBDP increased 3.75±1.95 mmHg to 10.49±8.21 mmHg (P＜0.01)evidently after injection of morphine. After associated application of ISDN and GTN, the four indications above decreased obviously. As for application associated with PTN,SOCA and SOF decreased separately from 100.64±44.99mmHg to 66.17±35.88 mmHg and from 10.70±2.76 mmHg to 9.04±1.71 mmHg (P＜0.05) markedly.CONCLUSION: The regular dose of GTN, ISDN and PTN showed inhibitory effect on SO motility, morphine showed excitatory effect on SO while GTN, ISDN and PTN could antagonize the effect of morphine. Among the three nitroester drugs, the effect of ISDN on SO was most significant.展开更多
AIM:To examine the prophylactic effect of glyceryl trinitrate on post-endoscopic retrograde cholangiopancreatography(ERCP) pancreatitis and hyperamylasemia.METHODS:Patients scheduled for ERCP were randomly divided int...AIM:To examine the prophylactic effect of glyceryl trinitrate on post-endoscopic retrograde cholangiopancreatography(ERCP) pancreatitis and hyperamylasemia.METHODS:Patients scheduled for ERCP were randomly divided into study group and placebo group.Patients in study group and placebo group were treated with 5 mg glyceryl trinitrate and 100 mg vitamin C,respectively,5 min before endoscopic maneuvers.RESULTS:A total of 74 patients were enrolled in the final analysis.Post-ERCP pancreatitis occurred in 3 patients(7.9%) of the study group and 9 patients(25%) in the placebo group(P = 0.012).Hyperamylasemia occurred in 8 patients of the study group(21.1%) and 13 patients(36.1%) of the placebo group(P = 0.037).CONCLUSION:Glyceryl trinitrate before ERCP can effectively prevent post-ERCP and hyperamylasemia.展开更多
A chronic anal fissure is a common perianal condition.This review aims to evaluate both existing and new therapies in the treatment of chronic fissures.Pharmacological therapies such as glyceryl trinitrate(GTN),Diltia...A chronic anal fissure is a common perianal condition.This review aims to evaluate both existing and new therapies in the treatment of chronic fissures.Pharmacological therapies such as glyceryl trinitrate(GTN),Diltiazem ointment and Botulinum toxin provide a relatively non-invasive option,but with higher recurrence rates.Lateral sphincterotomy remains the gold standard for treatment.Anal dilatation has no role in treatment.New therapies include perineal support devices,Gonyautoxin injection,fissurectomy,fissurotomy,sphincterolysis,and flap procedures.Further research is required comparing these new therapies with existing established therapies.This paper recommends initial pharmacological therapy with GTN or Diltiazem ointment with Botulinum toxin as a possible second line pharmacological therapy.Perineal support may offer a new dimension in improving healing rates.Lateral sphincterotomy should be offered if pharmacological therapy fails.New therapies are not suitable as first line treatments,though they can be considered if conventional treatment fails.展开更多
Objective To investigate the effects and molecular mechanism of Zhengtian Pills （ZTP） on migraine headache. Methods All rats were randomly divided into control, positive control, migraine model, low- and high-dose Z...Objective To investigate the effects and molecular mechanism of Zhengtian Pills （ZTP） on migraine headache. Methods All rats were randomly divided into control, positive control, migraine model, low- and high-dose ZTP groups, and glyceryl trinitrate was injected to induce migraine headache. The time of ears turning red, frequency of scratching head, climbing the cage, and head-twitching were used to evaluate rat behaviors. After 10 d administration of ZTP, the expression levels of transient receptor potential vanilloid 1 （TRPV1） both in cortex and hippocampus were determined by Western blotting. Results After 2 min of glyceryl trinitrate injection, rats showed headache phenomena that parallels the clinical symptoms of migraine, which peaked in 30 min, and lasted for 60 min. Frequency of head-twitching and numbers of scratching head in glyceryl trinitrate （GTN） group were significantly increased. In contrast, after ZTP （1.08 g/kg, ig） treatment, the numbers of scratching head with fore-limb, hind-limb and the frequency of head-twitching were significantly decreased. Flunarizine （FLU） and low-dose ZTP （0.54 g/kg） also showed a trend to decrease the numbers of scratching head and head-twitching frequency, but no significant difference. Besides, ZTP significantly decreased the up-regulated TRPV1 protein expression level both in cortex and hippocampus. Conclusion The present study shows that ZTP could significantly improve the migraine symptoms of headache in rats and TRPV1 might be one of the important molecular mechanisms. This is the first report about the effect of ZTP on TRPVl protein expression level both in cortex and hippocampus of rats.展开更多
BACKGROUND Acute pancreatitis is the most common and severe complication of endoscopic retrograde cholangiopancreatography(ERCP).Recent evidence suggests that combinations based on rectal nonsteroidal anti-inflammator...BACKGROUND Acute pancreatitis is the most common and severe complication of endoscopic retrograde cholangiopancreatography(ERCP).Recent evidence suggests that combinations based on rectal nonsteroidal anti-inflammatory drugs(NSAIDs)are more beneficial in preventing post-ERCP pancreatitis(PEP).Randomized controlled trials(RCTs)have also demonstrated the efficacy of glyceryl trinitrate(GTN).We conducted a network meta-analysis to compare NSAIDs and GTN for prevention of PEP and to determine whether they are better in combination.AIM To compare NSAIDs and GTN for prevention of PEP and to determine whether they are better in combination.METHODS A systematic search was done for full-text RCTs of PEP in PubMed,Embase,Science Citation Index,and the Cochrane Controlled Trials database.Inclusion and exclusion criteria were used to screen for eligible RCTs.The major data were extracted by two independent reviewers.The frequentist model was used to conduct this network meta-analysis and obtain the pairwise OR and 95%CI.The data were then extracted and assessed on the basis of the Reference Citation RESULTS Twenty-four eligible RCTs were selected,evaluating seven preventive strategies in 9416 patients.Rectal indomethacin 100 mg plus sublingual GTN(OR:0.21,95%CI:0.09–0.50),rectal diclofenac 100 mg(0.34,0.18–0.65),sublingual GTN(0.34,0.12–0.97),and rectal indomethacin 100 mg(0.49,0.33–0.73)were all more efficacious than placebo in preventing PEP.The combination of rectal indomethacin and sublingual GTN had the highest surface under the cumulative ranking curves(SUCRA)probability of(92.2%)and was the best preventive strategy for moderate-to-severe PEP with a SUCRA probability of(89.2%).CONCLUSION Combination of rectal indomethacin 100 mg with sublingual GTN offered better prevention of PEP than when used alone and could alleviate the severity of PEP.展开更多
Objective: To identify and isolate the chemical compounds of Phaleria macrocarpa(P.macrocarpa) fruit ethanolic extract.Methods: Dried fruit of P.macrocarpa was extracted with 90% ethanol and partitioned between n-hexa...Objective: To identify and isolate the chemical compounds of Phaleria macrocarpa(P.macrocarpa) fruit ethanolic extract.Methods: Dried fruit of P.macrocarpa was extracted with 90% ethanol and partitioned between n-hexane/H_2O and ethyl acetate/H_2O.The organic layer was fractionated by various stationary phase and identified by using combined data of 1D [(proton nuclear magnetic resonance(NMR), carbon-13 NMR)], 2D-NMR(heteronuclear multiplequantum correlation and heteronuclear multiple-bond correlation), and mass spectrum.Results: Purification of n-hexane and ethyl acetate fractions from ethanolic extract of P.macrocarpa fruit resulted in isolation of nine compounds.Conclusions: A new compound was isolated and identified as glyceryl pentacosanoate.Also, two xanthones, which are 1,7-dihydroxy-3,6-dimethoxyxanthone and 1,6,7-trihydroxy-3-methoxyxanthone, are firstly reported to be isolated from P.macrocarpa.展开更多
According to the moisturizing mechanism,glyceryl glucoside,polyglycerin-10 and xylitylglucoside were compounded.The hygroscopicity and moisture-retention are rated by way of weighing.On such basis,the compound moistur...According to the moisturizing mechanism,glyceryl glucoside,polyglycerin-10 and xylitylglucoside were compounded.The hygroscopicity and moisture-retention are rated by way of weighing.On such basis,the compound moisturizing agent with better ratio is applied in the emulsion formulation.Skin moisture content and skin moisture loss test are adopted to evaluate its moisturizing performance.According to the result of experiment,glyceryl glucoside,polyglycerin-10 and xylitylglucoside humectants have synergistic effects,which can significantly increase the volume of skin moisture and enhance skin barrier function and the moisturizing capability.展开更多
A series of novel polyphosphonates containing 5-flouro- N1-furanyl-N3- glyceroalkyl-uracil and formyl groups was synthesized by the condensation of 3-(w- (1-furanyl-5-flourouracil-3-yl) alkoxy)-1, 2-dihydroxy propane ...A series of novel polyphosphonates containing 5-flouro- N1-furanyl-N3- glyceroalkyl-uracil and formyl groups was synthesized by the condensation of 3-(w- (1-furanyl-5-flourouracil-3-yl) alkoxy)-1, 2-dihydroxy propane with phosphonyl dichloride. The products were characterized by IR, 1H NMR, 31P NMR, M, and elemental analysis. The results of bioassay show that compound 8a possesses potential anticancer activity.展开更多
Four kinds of strontium borates were prepared and characterized by XRD, SEM, EDS, TG-DTA and Hammett titration method and their catalytic activities were examined in the transesterification of glyceryl tributyrate wit...Four kinds of strontium borates were prepared and characterized by XRD, SEM, EDS, TG-DTA and Hammett titration method and their catalytic activities were examined in the transesterification of glyceryl tributyrate with methanol for the first time. The separate effects of the molar ratio of methanol to oil, the reaction time, and reusability were investigated. In addition, the catalytic activities of Sr（OH）2 and SrCO3 were also examined for the comparison. The results showed that the basicity and catalytic activity of these catalysts were decreased as the following order： Sr（OH）2 〉 SrB2O4·4H2O 〉 SrB6O10·5H2O 〉 SrB2O4 〉 SrB6O10 〉 SrCO3, and the reusability decreases as the following order： anhydrous strontium borates （SrBgO4, SrB6O10） 〉 hydrated strontium borates （SrB2O4·4H2O, SrB6O10·5H2O） 〉 Sr（OH）〉 The results indicate that the SrB2O4·4H2O with regular morphology, which was obtained at low temperature by a simple preparation method, might be as one kind of good potential alkaline earth salts catalyst for transesterification. Moreover, the possible reaction mechanism is proposed and analyzed.展开更多
Glyceryl monooleate(GMO)is a polar lipid that can exist in various liquid crystalline phases in the presence of different amounts of water.It is regarded as a permeation enhancer due to its amphiphilic property.Variou...Glyceryl monooleate(GMO)is a polar lipid that can exist in various liquid crystalline phases in the presence of different amounts of water.It is regarded as a permeation enhancer due to its amphiphilic property.Various phases of GMO/solvent system containing sodium fluorescein were prepared to compare permeability using confocal laser scanning microscopy(CLSM).GMO was melted in a vial in a water bath heated to 45℃.Propylene glycol and hexanediol were homogeneously dissolved in the melted GMO.Sodium fluorescein in aqueous solution was diluted to various ratios and thoroughly mixed by an ultrasonic homogenizer.Each GMO/Solvent system with fluorescein was applied onto the epidermal side of excised pig skin and incubated overnight.CLSM was performed to observe how the GMO/solvent system in its different phases affect skin permeability.Cubic and lamellar phase formulations enhanced the fluorescein permeation through the stratum corneum.A solution system had the weakest permeability compared to the other two phases.Due to the amphiphilic nature of GMO,cubic and lamellar phases might reduce the barrier function of stratum corneum which was observed by CLSM as fluorescein accumulated in the dermis.Based on the results,the glyceryl monooleate lyotropic mixtures could be applied to enhance skin permeation in various topical and transdermal formulations.展开更多
Hydrogel materials were prepared by thermopolymerization with different content of glyceryl methacrylate and hydroxyethyl methacrylate. The different states of water in swelling hydrogels were described and studied by...Hydrogel materials were prepared by thermopolymerization with different content of glyceryl methacrylate and hydroxyethyl methacrylate. The different states of water in swelling hydrogels were described and studied by differential scanning calorimetry(DSC). It was found that the hydrophilicity of GMA was stronger than HEMA,the water content and bound water of GMA hydrogel are higher than HEMA hydrogel.With the increase of GMA content, the content of free water in hydrogel increased. When GMA content was lower than 50%, the increase of GMA content also increased the content of bound water; but when GMA content was higher than 50%, the increase of GMA content decreased the content of bound water, which was caused by the chain hydrogen bond formed on the GMA chain with hydroxyl group each other.展开更多
文摘AIM: To evaluate the effects of nitroester drugs on human sphincter of Oddi (SO) motility and their antagonistic effects against morphine which shows excitatory effect on Oddi's sphincter motility.METHODS: The effects of these drugs on SO were evaluated by means of choledochofiberoscopy manometry.A total of 67 patients having T-tubes after cholecystectomy and choledochotomy were involved in the study, they were randomly divided into glyceryl trinitrate (GTN) group,isosorbide dinitrate (ISDN) group, pentaerythritol tetranitrate (PTN) group, morphine associated with GTN group, morphine associated with ISDN group and morphine associated with PTN group. Basal pressure of Oddi's sphincter (BPOS), amplitude of phasic contractions (SOCA), frequency of phasic contractions (SOF), duration of phasic contractions (SOD), duodenal pressure (DP) and common bile duct pressure (CBDP) were scored and analyzed. Morphine was given intramuscularly while nitroester drugs were applied sublingually.RESULTS: BPOS and SOCA decreased significantly after administration of ISDN and GTN, BPOS reduced from 10.95±7.49 mmHg to 5.92±4.04 mmHg (P＜0.05) evidently after application of PTN. BPOS increased from 7.37±5.58mmHg to 16.60±13.87 mmHg, SOCA increased from 54.09±38.37 mmHg to 100.70±43.51 mmHg, SOF increased from 7.15±3.20 mmHg to 10.38±2.93 mmHg and CBDP increased 3.75±1.95 mmHg to 10.49±8.21 mmHg (P＜0.01)evidently after injection of morphine. After associated application of ISDN and GTN, the four indications above decreased obviously. As for application associated with PTN,SOCA and SOF decreased separately from 100.64±44.99mmHg to 66.17±35.88 mmHg and from 10.70±2.76 mmHg to 9.04±1.71 mmHg (P＜0.05) markedly.CONCLUSION: The regular dose of GTN, ISDN and PTN showed inhibitory effect on SO motility, morphine showed excitatory effect on SO while GTN, ISDN and PTN could antagonize the effect of morphine. Among the three nitroester drugs, the effect of ISDN on SO was most significant.
文摘AIM:To examine the prophylactic effect of glyceryl trinitrate on post-endoscopic retrograde cholangiopancreatography(ERCP) pancreatitis and hyperamylasemia.METHODS:Patients scheduled for ERCP were randomly divided into study group and placebo group.Patients in study group and placebo group were treated with 5 mg glyceryl trinitrate and 100 mg vitamin C,respectively,5 min before endoscopic maneuvers.RESULTS:A total of 74 patients were enrolled in the final analysis.Post-ERCP pancreatitis occurred in 3 patients(7.9%) of the study group and 9 patients(25%) in the placebo group(P = 0.012).Hyperamylasemia occurred in 8 patients of the study group(21.1%) and 13 patients(36.1%) of the placebo group(P = 0.037).CONCLUSION:Glyceryl trinitrate before ERCP can effectively prevent post-ERCP and hyperamylasemia.
文摘A chronic anal fissure is a common perianal condition.This review aims to evaluate both existing and new therapies in the treatment of chronic fissures.Pharmacological therapies such as glyceryl trinitrate(GTN),Diltiazem ointment and Botulinum toxin provide a relatively non-invasive option,but with higher recurrence rates.Lateral sphincterotomy remains the gold standard for treatment.Anal dilatation has no role in treatment.New therapies include perineal support devices,Gonyautoxin injection,fissurectomy,fissurotomy,sphincterolysis,and flap procedures.Further research is required comparing these new therapies with existing established therapies.This paper recommends initial pharmacological therapy with GTN or Diltiazem ointment with Botulinum toxin as a possible second line pharmacological therapy.Perineal support may offer a new dimension in improving healing rates.Lateral sphincterotomy should be offered if pharmacological therapy fails.New therapies are not suitable as first line treatments,though they can be considered if conventional treatment fails.
基金Ministry of Science and Technology(grant No.2013ZX09201022)the National Natural Science Foundation of China(grant No.81373418)
文摘Objective To investigate the effects and molecular mechanism of Zhengtian Pills （ZTP） on migraine headache. Methods All rats were randomly divided into control, positive control, migraine model, low- and high-dose ZTP groups, and glyceryl trinitrate was injected to induce migraine headache. The time of ears turning red, frequency of scratching head, climbing the cage, and head-twitching were used to evaluate rat behaviors. After 10 d administration of ZTP, the expression levels of transient receptor potential vanilloid 1 （TRPV1） both in cortex and hippocampus were determined by Western blotting. Results After 2 min of glyceryl trinitrate injection, rats showed headache phenomena that parallels the clinical symptoms of migraine, which peaked in 30 min, and lasted for 60 min. Frequency of head-twitching and numbers of scratching head in glyceryl trinitrate （GTN） group were significantly increased. In contrast, after ZTP （1.08 g/kg, ig） treatment, the numbers of scratching head with fore-limb, hind-limb and the frequency of head-twitching were significantly decreased. Flunarizine （FLU） and low-dose ZTP （0.54 g/kg） also showed a trend to decrease the numbers of scratching head and head-twitching frequency, but no significant difference. Besides, ZTP significantly decreased the up-regulated TRPV1 protein expression level both in cortex and hippocampus. Conclusion The present study shows that ZTP could significantly improve the migraine symptoms of headache in rats and TRPV1 might be one of the important molecular mechanisms. This is the first report about the effect of ZTP on TRPVl protein expression level both in cortex and hippocampus of rats.
文摘BACKGROUND Acute pancreatitis is the most common and severe complication of endoscopic retrograde cholangiopancreatography(ERCP).Recent evidence suggests that combinations based on rectal nonsteroidal anti-inflammatory drugs(NSAIDs)are more beneficial in preventing post-ERCP pancreatitis(PEP).Randomized controlled trials(RCTs)have also demonstrated the efficacy of glyceryl trinitrate(GTN).We conducted a network meta-analysis to compare NSAIDs and GTN for prevention of PEP and to determine whether they are better in combination.AIM To compare NSAIDs and GTN for prevention of PEP and to determine whether they are better in combination.METHODS A systematic search was done for full-text RCTs of PEP in PubMed,Embase,Science Citation Index,and the Cochrane Controlled Trials database.Inclusion and exclusion criteria were used to screen for eligible RCTs.The major data were extracted by two independent reviewers.The frequentist model was used to conduct this network meta-analysis and obtain the pairwise OR and 95%CI.The data were then extracted and assessed on the basis of the Reference Citation RESULTS Twenty-four eligible RCTs were selected,evaluating seven preventive strategies in 9416 patients.Rectal indomethacin 100 mg plus sublingual GTN(OR:0.21,95%CI:0.09–0.50),rectal diclofenac 100 mg(0.34,0.18–0.65),sublingual GTN(0.34,0.12–0.97),and rectal indomethacin 100 mg(0.49,0.33–0.73)were all more efficacious than placebo in preventing PEP.The combination of rectal indomethacin and sublingual GTN had the highest surface under the cumulative ranking curves(SUCRA)probability of(92.2%)and was the best preventive strategy for moderate-to-severe PEP with a SUCRA probability of(89.2%).CONCLUSION Combination of rectal indomethacin 100 mg with sublingual GTN offered better prevention of PEP than when used alone and could alleviate the severity of PEP.
基金Supported by PT Dexa Medica with grant number 120/IMC/DLBS/2014
文摘Objective: To identify and isolate the chemical compounds of Phaleria macrocarpa(P.macrocarpa) fruit ethanolic extract.Methods: Dried fruit of P.macrocarpa was extracted with 90% ethanol and partitioned between n-hexane/H_2O and ethyl acetate/H_2O.The organic layer was fractionated by various stationary phase and identified by using combined data of 1D [(proton nuclear magnetic resonance(NMR), carbon-13 NMR)], 2D-NMR(heteronuclear multiplequantum correlation and heteronuclear multiple-bond correlation), and mass spectrum.Results: Purification of n-hexane and ethyl acetate fractions from ethanolic extract of P.macrocarpa fruit resulted in isolation of nine compounds.Conclusions: A new compound was isolated and identified as glyceryl pentacosanoate.Also, two xanthones, which are 1,7-dihydroxy-3,6-dimethoxyxanthone and 1,6,7-trihydroxy-3-methoxyxanthone, are firstly reported to be isolated from P.macrocarpa.
文摘According to the moisturizing mechanism,glyceryl glucoside,polyglycerin-10 and xylitylglucoside were compounded.The hygroscopicity and moisture-retention are rated by way of weighing.On such basis,the compound moisturizing agent with better ratio is applied in the emulsion formulation.Skin moisture content and skin moisture loss test are adopted to evaluate its moisturizing performance.According to the result of experiment,glyceryl glucoside,polyglycerin-10 and xylitylglucoside humectants have synergistic effects,which can significantly increase the volume of skin moisture and enhance skin barrier function and the moisturizing capability.
基金This project was supported by the National Natural Science Foundation of China.
文摘A series of novel polyphosphonates containing 5-flouro- N1-furanyl-N3- glyceroalkyl-uracil and formyl groups was synthesized by the condensation of 3-(w- (1-furanyl-5-flourouracil-3-yl) alkoxy)-1, 2-dihydroxy propane with phosphonyl dichloride. The products were characterized by IR, 1H NMR, 31P NMR, M, and elemental analysis. The results of bioassay show that compound 8a possesses potential anticancer activity.
基金supported by the National Natural Science Foundation of China(21173143)
文摘Four kinds of strontium borates were prepared and characterized by XRD, SEM, EDS, TG-DTA and Hammett titration method and their catalytic activities were examined in the transesterification of glyceryl tributyrate with methanol for the first time. The separate effects of the molar ratio of methanol to oil, the reaction time, and reusability were investigated. In addition, the catalytic activities of Sr（OH）2 and SrCO3 were also examined for the comparison. The results showed that the basicity and catalytic activity of these catalysts were decreased as the following order： Sr（OH）2 〉 SrB2O4·4H2O 〉 SrB6O10·5H2O 〉 SrB2O4 〉 SrB6O10 〉 SrCO3, and the reusability decreases as the following order： anhydrous strontium borates （SrBgO4, SrB6O10） 〉 hydrated strontium borates （SrB2O4·4H2O, SrB6O10·5H2O） 〉 Sr（OH）〉 The results indicate that the SrB2O4·4H2O with regular morphology, which was obtained at low temperature by a simple preparation method, might be as one kind of good potential alkaline earth salts catalyst for transesterification. Moreover, the possible reaction mechanism is proposed and analyzed.
基金This study was supported by Basic Science Research Program through the National Research Foundation of Korea(NRF)funded by the Korean Ministry of Education,Science and Technology(2012002399)a grant of the Korean Healthcare Technology R&D Project,Ministry of Health and Welfare,Republic of Korea.(Grant No.:A103017).
文摘Glyceryl monooleate(GMO)is a polar lipid that can exist in various liquid crystalline phases in the presence of different amounts of water.It is regarded as a permeation enhancer due to its amphiphilic property.Various phases of GMO/solvent system containing sodium fluorescein were prepared to compare permeability using confocal laser scanning microscopy(CLSM).GMO was melted in a vial in a water bath heated to 45℃.Propylene glycol and hexanediol were homogeneously dissolved in the melted GMO.Sodium fluorescein in aqueous solution was diluted to various ratios and thoroughly mixed by an ultrasonic homogenizer.Each GMO/Solvent system with fluorescein was applied onto the epidermal side of excised pig skin and incubated overnight.CLSM was performed to observe how the GMO/solvent system in its different phases affect skin permeability.Cubic and lamellar phase formulations enhanced the fluorescein permeation through the stratum corneum.A solution system had the weakest permeability compared to the other two phases.Due to the amphiphilic nature of GMO,cubic and lamellar phases might reduce the barrier function of stratum corneum which was observed by CLSM as fluorescein accumulated in the dermis.Based on the results,the glyceryl monooleate lyotropic mixtures could be applied to enhance skin permeation in various topical and transdermal formulations.
文摘Hydrogel materials were prepared by thermopolymerization with different content of glyceryl methacrylate and hydroxyethyl methacrylate. The different states of water in swelling hydrogels were described and studied by differential scanning calorimetry(DSC). It was found that the hydrophilicity of GMA was stronger than HEMA,the water content and bound water of GMA hydrogel are higher than HEMA hydrogel.With the increase of GMA content, the content of free water in hydrogel increased. When GMA content was lower than 50%, the increase of GMA content also increased the content of bound water; but when GMA content was higher than 50%, the increase of GMA content decreased the content of bound water, which was caused by the chain hydrogen bond formed on the GMA chain with hydroxyl group each other.
