AIM:To establish a HPLC method for determinaton of sodium ferulate (SF) in Beagle dog plasma and to study the pharmacokinetics of SF tablets. METHODS: Sodium ferulate in plasma was extracted with ether,separated on a Kromasil C_ 18 column (150 mm?4.6 mm,5 ?m) and the peak height ratio of sodium ferulate to the internal standard tinidazole was measured.Plasma concentration of SF was determined using acetonitrile-water-acetic acid(20∶79.2∶0.8) as the mobile phase and the flow rate was 0.8 ml/min.SF was detected at 320 nm. RESULTS: SF and the internal standard were separated completely under the condition described above.SF was linear in the range of 0.02～50 ?g/ml(r=0.9995).The accuracy,precision and sensitivity were eligible for analyse of bio-pharmic samples. CONCLUSION:A sensitive and accurate HPLC method for the quantitative determination of SF in the plasma of Beagle dog is developed and it is applicable to the determination in plasma and pharmacokinetic study of SF.

This study is undertaken to modify the chitosan nanoparticles (CS-NPs) with wheat germ agglutinin (WGA), and investigate the conjugation between WGA-CS-NPs and N-acetylglucosamine (NAG). CS-NPs were prepared by ionotropic gelation process and then conjugated with WGA under the activation of glutaricdialdehyde. The mean diameter of the CS-NPs was approximately 113.5 nm and the poly-dispersity index (PDI) was 0.18. The binding yield of WGA to CS-NPs was comprised between 27.8% and 87.9% depending mostly on the addition of 0.3% (w/v) glutaraldehyde solution. A competitive inhibition experiment of WGA-CS-NPs to bovine submaxillary gland mucin (BSM) was taken to illuminate the binding activity of WGA-CS-NPs to the sugar of N-acetylglucosamine. After the addition of NAG, the binding rates between CS-NPs and BSM almost didn't change, while the binding rates between WGA-CS-NPs and BSM dropped down significantly, which confirmed the specific binding characteristics of WGA to NAG.

This study is to prepare scopolamine hydrobromide nanoparticles-in-microsphere system (SH-NiMS) and evaluate its drug release characteristics in vitro. SH nanoparticles were prepared by ionic crosslinking method with tripolyphosphate (TPP) as crosslinker and chitosan as carrier. Orthogonal design was used to optimize the formulation of SH nanoparticles, which took the property of encapsulation efficiency and drug loading as evaluation parameters. With HPMC as carrier, adjusted the parameters of spray drying technique and sprayed the SH nanoparticles in microspheres encaposulated by HPMC was formed and which is called nanoparticles-in-microsphere system (NiMS). SH-NiMS appearances were observed by SEM, structure was obsearved by FT-IR and the release characteristics in vitro were evaluated. The optimized formulation of SH nanoparticles was TPP/CS 1:3 (w/w), HPMC 0.3%, SH 0.2%. The solution peristaltic speed of the spray drying technique was adjusted to 15%, and the temperature of inlet was 110 degrees C. The encapsulation product yeild, drug loading and particle sizes of SH-NiMS were 94.2%, 20.4%, and 1256.5 nm, respectively. The appearances and the structure of SH-NiMS were good. The preparation method of SH-NiMS is stable and reliable to use, which provide a new way to develop new dosage form.

AIM　To prepare lung targeted tetrandrine (TET) loaded sustained-release drug delivery system by microencapsulation, decrease the toxicity and enhance the therapeutic function of anti-pulmonary hypertension of TET. METHODS　Albumin microcapsules were produced by spray drying-thermal denaturation, a new technique. Some characterization of the prepared microcapsules was evaluated. Distribution of the microcapsules and their anti-pulmonary hypertension effect in vivo were investigated. RESULTS　The spherical microcapsules showed a drug loading of 37.88%. Compared to the original drug, the rate of TET released from the positively charged microcapsules in vitro was significantly decreased and fitted well by Higuchi equation. The TET concentrations in mouse lungs of TET microcapsules were significantly higher than those of TET injection, and the mean retained time of TET in lungs was prolonged from 157.1 h to 223.6 h after microencapsulation. The in vitro - in vivo correlation was established and confirmed (P＜0.001). CONCLUSION　The new spray drying-thermal denaturation method allows the preparation of drug loaded albumin microcapsules with desired results. The prepared microcapsules were found to have the potential function of delivering TET to pulmonary artery via iv, with low toxicity and high efficacy.

The volatile oil from traditional Chinese medicine has been widely used in medicine, food, agriculture and many other fields as its significant antibacterial effect on gram positive bacteria, gram negative bacteria, anaerobic bacteria and fungus.The clinical application is still not popular due to the poor stability.Cyclodextrin is used as the inclusion material to enhance the stability of volatile oil, make the preparation of production more convenient and the bioavailability improved.The literature referred to antibacterial volatile oil and the inclusion technology were summerized in order to provide reference to intensive study, optimize the technology of inclusion and develop more preparations.

ObjectiveTo establish a quantitative analysis multi-components by single marker method （QAMS） for five main components （aucubin， geniposidic acid， chlorogenic acid， asperuloside and rutin） in Eucommiae Folium， to verify its feasibility and applicability in the determination of Eucommiae Folium， so as to provide a scientific basis for the development of quality standard of this herb. MethodHigh performance liquid chromatography was performed on a Welch Boltmatetm™ C₁₈ column （4.6 mm×100 mm， 2.7 μm） with methanol （A）-0.2% phosphoric acid aqueous solution （B） as the mobile phase for gradient elution （0-8 min， 3%A； 8-10 min， 3%-11%A； 10-26 min， 11%A； 26-27 min， 11%-25%A； 27-60 min， 25%-32%A）， the column temperature was set at 30 ℃， the flow rate was 0.6 mL·min^-1， the detection wavelengths were at 210 nm and 254 nm. Chlorogenic acid was used as an internal reference to establish the relative correction factors （f） between it and the other four components， and the contents of the five components in 14 batches of Eucommiae Folium were determined by QAMS and external standard method （ESM）， respectively. ResultThe f values of chlorogenic acid to aucubin， geniposidic acid， asperuloside and rutin were 3.13， 1.45， 2.64 and 0.56， respectively. Repeatability was good under different experimental conditions， relative standard deviation （RSD） was <5.0%. The contents of aucubin， geniposidic acid， chlorogenic acid， asperuloside and rutin in 14 batches of Eucommiae Folium were 1.340-28.975， 0.252-36.086， 10.016-27.443， 1.396-8.646， 0.533-1.766 mg·g^-1， respectively. There were no significant difference between content results of QAMS and that of ESM （RSD<5.0%）. ConclusionQAMS established with chlorogenic acid as the internal reference can be used to determine the contents of five components in Eucommiae Folium， and this method is simple and accurate. After comprehensive evaluation， the quality standard of Eucommiae Folium in subsequent editions of Chinese Pharmacopoeia is suggested that three main active components， chlorogenic acid， aucubin and geniposidic acid， are selected as quality markers， and their content limits are recommended not less than 1.5%， 1.0% and 1.0%， respectively. This quality standard draft can avoid the potential quality risk due to poor specificity and low content limit of the index component （chlorogenic acid） in the previous editions of Chinese Pharmacopoeia.

ObjectiveTo prepare matrine lipid-based cubic liquid crystalline nanoparticle （MAT-LLCN） gels and investigate its in vitro release and transdermal absorption behavior. MethodTaking entrapment efficiency as the index， the optimal formulation of MAT-LLCN was screened by extreme vertex mixture method based on the optimal ratio of glycerol monooleate （GMO） to poloxamer 407 （P407）， and its drug loading was investigated. MAT-LLCN gels was prepared by mixing MAT-LLCN with pre-swelled carbomer 940 as the gel matrix. The structure of MAT-lipid-based cubic liquid crystalline （LLC） was characterized by polarized light microscopy （PLM） and small angle X-ray scattering （SAXS）. The in vitro release and transdermal absorption properties of MAT-LLCN gels and MAT ordinary gels were compared by modified Franz diffusion cell method， skin structure changes caused by them were observed by hematoxylin-eosin （HE） staining. ResultThe optimal formulation of MAT-LLCN gels was 5.5% of GMO-P407 （9∶1）， 1%-6% of MAT， 0.6% of carbomer 940， adding water to sufficient amount. The prepared MAT-LLC was confirmed as body-centered （Im3m） LLC. The in vitro release behavior of MAT-LLCN gels was in accordance with the Weibull equation （R²=0.954 0）， and the release mechanism was the Fick diffusion. In vitro transdermal test showed that all the parameters of MAT-LLCN gels were higher than those of MAT ordinary gels （P<0.05）， including cumulative release rate， steady-state release rate and the amount of drug retention in skin. HE staining results showed that MAT-LLCN gels could loose the cellular arrangement of skin stratum corneum， and maintain the stability of the cell structure of the dermis. ConclusionThe prepared MAT-LLCN gels can accelerate the transdermal drug transport and form drug storage in the dermis by rapidly opening the skin stratum corneum barrier， suggesting that LLC has good application prospects in the field of transdermal drug delivery.