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OBJECTIVE: To investigate the effect of natural and synthetic borneol on the transdermal absorption of emodin. METHODS: The supplying and receiving solutions containing emodin were selected from the abdominal skin of mice in vitro, and the samples were analyzed by HPLC. The cumulative permeability, permeability rate and permeability enhancement factor were used as the evaluation indexes of the permeability enhancement effect. RESULTS: The saline containing 1% Tween 80-80% ethanol and 60% ethanol could increase the solubility of emodin to 648 μg•mL -1 and obtain conditions of leaking trough. The penetration rate of emodin was 648 μg•mL - 1 > 569 μg•mL -1 > 457 μg•mL -1 in the range of concentration. The penetration enhancement effect of synthetic borneol was 2% > 4% > 1% > blank control group > 3% and 5%, and the steady-state permeation rates of 2% natural borneol (15.90 μg•cm- 2•h - 1 ) were higher than those of 2% synthetic borneol(12.44 μg•cm-2•h-1). CONCLUSION: Natural borneol and synthetic borneol can promote the transdermal penetration of emodin, which is limited by their concentration. This provides an experimental basis for the selection of emodin transdermal enhancers.
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@#AIM: To study the effect of synthetic borneol on transcorneal permeability of dexamethasone. The ocular irritation was also evaluated.<p>METHODS: The freshly excised corneas,whole corneas or de-epithelialized corneas, were immediately mounted in perfusion cells. Dexamethasone containing free-borneol or borneol was added into the deliver chamber respectively in each group. At different time point after addition of solution, 50μL of the receptor solution was removed. The concentration of dexamethasone was determined and the apparent permeability coefficient(Papp)was calculated. Hydration level of cornea was measured and irritation test was observed. <p>RESULTS: The Papp for dexamethasone in whole cornea increased by 2.40 fold in borneol group(<i>P</i><0.05). The Papp for dexamethasone in de-epithelialized cornea did not increased apparently(<i>P</i>>0.05). Synthetic borneol did not increase hydration level and irritation of cornea(<i>P</i>>0.05). <p>CONCLUSION: Synthetic borneol can improve the corneal permeation of lipophilic drug dexamethasone and do not damage corneal tissue.
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Objective To establish the determination method synthetic borneol and menthol in Keyou nanoemulsion. Methods HP-5 quartz capillary column (30 m×320 μm×0.25 μm) was used with nitrogen as the carrier gas, and FID as the detector. The temperature of the entrance of the capillary vessel column was at 230 ℃. Results Synthetic borneol and menthol in Keyou nanoemulsion were separated well. The calibration curves of synthetic borneol was obtained with good linear relationship within the range of 0.337-1.685 μg (r 2=0.998 2), the average recovery was 97.5%. The calibration curves of menthol was also obtained with a good linear relationship within the range of 0.234-1.17 μg (r 2=0.997 4), the average recovery was 97.0%. Conclusion The methord is simple and accurate. It can be used to control the quality of Keyou nanoemulsion.
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AIM: To investigate the nasal absorption of ligustrazine and promotion action of synthetic borneol. METHODS: In situ nasal recirculation method was used to study the dose effect relationship of nasal absorption of ligustrazine and the effect of synthetic borneol on nasal absorption of ligustrazine in rats. RESULTS: When the concentrations of ligustrazine were 0.25 , 0.75 ,and 1.25 g?L -1 in circulation liquid, respectively, the corresponding values of the absorption rate constant k were 0.0195 , 0.0227 , and 0.0241 min -1 . However, when the concentrations were 2.5 and 5.0 g?L -1 in circulation liquid, the absorption rate constant k lowered with the concentration being added. CONCLUSION: Ligustrazine can be absorbed through the nasal mucous and synthetic borneol can promote the absorption.
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Objective To optimize the proportion of three transdermal penetration enhancers on transdermal absorption of ligustrazine hydrochloride.Methods Permeation tests in vitro through BALB/c nude mouse skin in two compartment diffusion cells were performed to study the effect of synthetic borneol,menthol,and Azone on trandermal absorption of ligustrazine hydrochloride by changing their concentrations,and uniform design method was used to determine the penetration coefficient of ligustrazine hydrochloride and optimize the proportion of three transdermal penetration enhancers.ResultsThe optimal proportion and contents of synthetic borneol,menthol,and Azone were 1.5%∶1.5%∶1.5%(15 mg/mL∶15 mg/mL∶15 mg/mL),the real penetration coefficient of ligustrazine hydrochloride was 69.575 ?g/(h?cm2),while the theoretical penetration coefficient was 69.749 ?g/(h?cm2).Conclusion Uniform design method is an effective way to optimize the proportion of three transdermal penetration enhancers on trandermal absorption of ligustrazine hydrochloride.
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Objective&Methods The mutagenicity of natural Borneol and synthetic Borneol was studied by using Ames test.Results Natural Borneol and Synthetic Borneol in the dose range of 0.4～250.0 ?g/plate had no effect in reducing the reversion frequencies of Salmonella Typhimurium histidine auxotrophic mutant(TA97,TA98,TA100,TA102)whether if metabolic activation system(S9mix)existed or not.Moreover,the backward mutant colony had normal background.Conclusion Natural Borneol and Synthetic Borneol do not possess evident mutagenicity under experimental condition.
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AIM: To establish the determination for camphor, menthol, synthetic borneol, and methyl salicylate in four kinds of TCM adhesive plasters by GC. METHODS: The internal standard method was employed. Naphthalene, the internal standard, was added to the sample before treatment. The sample solution was prepared by distillation with essential oil collector. The GC system consisted of glass column, 10% PEG 20M as the stationary phase, nitrogen as the carrier gas, column temperature at 130℃, and FID as the detector. RESULTS: Camphor, menthol, synthetic borneol(borneol and isoborneol), and methyl salicylate in 6 lots of samples and naphthalene have been separated well under the chromatographic condition. In the methodology study on Fengshi Zhitong Adhesive Plasters, the average recovery of camphor, menthol, synthetic borneol, and methyl salicylate were 95.54%( RSD =1.6%), 96.90%( RSD =2.2%), 97.30%( RSD =1.4%), and 96.48%( RSD =2.8%), respectively. CONCLUSION: The method is sensitive, accurate and reproducible, and can be used to control the quality of the four kinds of preparations.
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Objective:To investigate the effect of synthetic borneol on penetration mechanism of ligustrazine hydrochloride. Methods: Permeation tests in vitro through rabbit skin in two compartment diffusion cells were performed to study the effect of synthetic borneol on transdermal absorption of ligustrazine hydrochloride by changing concentrations of synthetic borneol and rabbit skin condition. Results: Ligustrazine hydrochloride permeation coefficient increased linearly with incerease of concentrations of synthetic borneol, while those through strippde stratum corneum skin were not varied. Synthetic borneol enhanced the deposit functions of whole skin and stripped stratum corneum skin. Conclusions: Synthetic borneol could enhance the percutaneous absorption of ligustrazine hydrochloride, mainly through the stratum corneum, and increase the deposit function.
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AIM: To establish the simultaneous determination of camphor,menthol,synthetic borneol and methyl salicylate in Shexiang Zhuanggu Plaster(Camphor,Mentholum,Borneolum Syntheticum,etc). by GC. METHODS: The sample solution was distilled in volatile oil determination apparatus.Naphthalene was used for the internal standard.The GC system consisted of capillary column,PEG-20M as the stationary phase,nitrogen as the carrier gas,FID as the detector.The programmed temperature-GC and internal standard method was employed to determine four kinds of components in Shexiang Zhuanggu Plaster. RESULTS: Camphor,menthol,synthetic borneol(borneol and isoborneol) and methyl salicylate in Shexiang Zhuanggu Plaster and naphthalene have been separated well under the same chromatographic condition.The average recovery of camphor,menthol,synthetic borneol and methyl salicylate were 96.92%(RSD=2.42%),98.03%(RSD=1.81%),99.02%(RSD=1.47%) and 98.15%(RSD=1.59%),respectively. CONCLUSION: The method is simple,accurate and separable,and can be used to control the quality of Shexiang Zhuanggu Plaster
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AIM Protective action of TMP on hearts and brains under the condition of the acute hypoxia was studied. METHODS On the device of mice acute hypoxia ,ability of tolerancing hypoxia of mice was investigated,and superoxide dismutase(SOD) and malondialdehyde(MDA) and nitric oxide(NO) contents in hearts and brains were measured.RESULTS TMP could make the resisting hypoxia action in mice strengthen significantly,and the action had a does dependent increase. TMP made SOD contents in hearts and brains in does dependent increase;MDA contents in hearts and brains were not notable in low does ,but TMP could decreased MDA contents in hearts and brains in middle and high does ( P