Application of Chitosan and its Derivatives in Drug Carriers / 中国药师

Chitosan and its derivatives with good characteristics such as non-toxicity,good biocompatibility and degradability,mu-cosal adhesion and permeability promotion etc,have been widely researched and applied in the field of drug carriers. Based on the re-cently published papers at home and abroad,the application and action mechanism of chitosan and its derivatives as drug carriers were analyzed and discussed,and the application and research progress of chitosan and its derivatives as anti-tumor drug targeting carriers, sustained-release and controlled-release drug carriers,ophthalmic drug carriers,gene carriers and gel bases were reviewed.

Research Progress in the Chemical Modification of Chitosan and the Antioxidant Activity of Its Derivatives / 中国药师

Chitosan (CS) is a natural,non-toxic biopolymer mainly made from the deacetylation of chitin. Chitosan has good bio-compatibility with unique antioxidant and biodegradable properties. Due to the poor solubility of chitosan in neutral or alkalinized media,the application of chitosan is restricted. Thus,numerous chitosan derivatives have been developed through chemical modifica-tions to broaden the application scope and improve its value. Chitosan and its derivatives with antioxidant activity have shown superior medical value in recent years. In this paper,several modification methods of chitosan were reviewed. In addition,the research progress in chitosan and its derivatives as antioxidants was introduced.

The processing technology and pharmacological effects of Chinese medicine Rhizo-ma Cory dalis / 药学实践杂志

Rhizoma Corydalis ,a herb with analgesic effects and being able to promote blood circulation ,has been used for more than hundreds of years in China .Rhizoma Corydalis mainly comes from Zhejiang ,Jiangsu ,Hubei and Hunan prov-ince .The major effective components are alkaloids ,which have sedative ,hypnotic ,analgesic pharmacological effects .It has in-dications for chest ,rib and back pain ,dysmenorrhea ,traumatic injury ,etc .The main formulation of Rhizoma Corydalis is vinegar product .The processing technology has significant effect on the content of active components and therapeutic efficacy . It is very important to improve and optimize decoction method .This paper reviewed the processing technology and the pharma-cological effects of Rhizoma corydalis .

Optimization of Film-forming Materials for Compound Rhizoma Corydalis Plastics / 中国药师

Objective:To optimize the formula of film-forming materials for compound rhizoma corydalis plastics. Methods:Poly-vinyl alcohol 124 (PVA124) and bletilla striata gum were selected as the film-forming materials. The amounts of PVA 124, bletilla striata gum, glycerol and absolute ethanol were used as the influencing factors in an orthogonal test with the composite score of film-forming time and appearance as the indices to screen out the best composition of film-forming materials. Results:The best composition of film-forming materials was as follows:8 g PVA 124, 1 g bletilla striata gum, 2 ml glycerol and 15 ml ethanol. Conclusion:The op-timized film-forming materials can be used for the preparation of compound rhizoma corydalis plastics.

Research Progress in Pathogenesis and Traditional Chinese Medicine Treatment of Primary Dysmenorrheal / 中国药师

Primary dysmenorrheal is one of the most common diseases in gynecology,which seriously affects the physical and men-tal health of women, therefore, the effective prevention and treatment of primary dysmenorrheal is a problem in medical field. The etiol-ogy of primary dysmenorrheal is very complicated, and in recent years, there are more and more domestic and foreign scholars studying on its pathogenesis and treatment. Modern medicine has some shortcomings in the treatment of dysmenorrheal including side effects and so on. Traditional Chinese medicine has unique advantages in the treatment of primary dysmenorrheal. Combined with the recent rele-vant reporters, the article reviewed the pathogenesis of primary dysmenorrheal from both traditional Chinese medicine and modern medi-cine aspects, and the research progress in traditional Chinese medicine treatment of primary dysmenorrheal was also reviewed to provide better guidance for the treatment of primary dysmenorrheal.

Extraction Technology Optimization for Tetrahydropalmatine from Corydalis Yanhusuo by Orthogonal Ex-periment / 中国药师

Objective:To optimize the extraction technology of tetrahydropalmatine in Corydalis yanhusuo. Methods:An L9 (34 ) orthogonal experiment was performed to investigate the effects of ethanol concentration, ethanol amount, extraction temperature and ex-traction time on the extraction results with the content of tetrahydropalmatine as the evaluation index. Results:The optimum conditions were as follows:the solid-liquid ratio was 1 :10 ( g·ml-1 ) , 60% ethanol was used as the extraction solvent, the extraction tempera-ture was at 80 ° C for three-time extraction, and the extraction duration for each time was 1 h. Conclusion: The optimized extraction technology for tetrahydropalmatine from Corydalis yanhusuo is stable, reasonable, feasible and easy-operated with low energy consump-tion, which can enhance the comprehensive utilization of Corydalis yanhusuo.

Application of Polymeric Micelles in Transdermal Drug Delivery Systems / 中国药师

Objective: To review the application of polymeric micelles as the vehicles in transdermal delivery systems.Methods: Based on the recently published papers, the researches of preparation, penetration mechanism, drug release and application of polymeric micelles in transdermal delivery systems were classified and summarized.Results: Polymeric micelles were extensively applied as drug vehicles due to the ability of solubilization and transdermal absorption enhancement.Conclusion: Polymeric micelles can be used as promising vehicles in transdermal delivery systems, which show a good application prospect.

Inhibitory Effect of Rupixiao Granule on Hyperplasia of Mammary Gland in Rabbits / 中国药师

Objective:To determine the inhibitory effect of Rupixiao ( RPX) granule on mammary gland hyperplasia ( HMG) in rabbits and explore the possible mechanism to provide reference for clinical medication. Methods:Rabbit model of mammary hyperpla-sia was established by estradiol benzoate and progesterone. Xiaoyao pills and tamoxifen were used as the positive control, and the RPX granule group was respectively at low, medium and high dose (0. 525,1. 05,2. 1 g·kg-1). Each group was with intragastric adminis-tration for 30 days. The levels of E2 , PROG, FSH, LH and PRL in serum and the expression of VEGF in the homogenate tissue were determined by an Elisa method. The breast tissue of rabbits in each group was withdrawn to observe the structure changes after Hema-toxylin-eosin staining ( HE) . Results:Ovarian preservation-benzoic acid, estradiol combined with progesterone could be used to estab-lish mammary gland hyperplasia in rabbits. RPX granule could significantly decrease the serum levels of E2 and PRL (P<0. 01)and increase that of PROG (P<0. 01 or P<0. 001). The results of pathological section showed that the breast structure in RPX granule high dose group could be restored to the level of the blank control group, which showed its therapeutic effect on HMG was better than that of tamoxifen and Xiaoyao pills. The expression of VEGF in each treatment group significantly decreased compared with that in the model group by the Elisa reagent (P<0. 001). Conclusion:RPX granule has good efficacy in HMG rabbits. The inhibitory effects of RPX granule on HMG in rabbits maybe related to the inhibition of VEGF in rabbit breast tissues, and the inhibition of RPX granule was similar to that of tamoxifen and Xiaoyao pills.

Optimization of Extraction Technology of Panax Notoginseng and Scrophulariae Radix from Rupixiao Granule by Orthogonal Design / 中国药师

Objective: To optimize the extraction technology of Panax notoginseng and Scrophulariae radix from Rupixiao granule.Methods: With the dry extract rate and transfer rates of ginsenoside Rg1, ginsenoside Rb1 and harpagoside as the comprehensive index, the orthogonal design was adopted to investigate the effects of the amount and concentration of ethanol, extracting duration and times on the extraction technology.The contents of ginsenoside Rg1, ginsenoside Rb1 and harpagoside were determined by HPLC.Results: The optimal extraction technology was extracted twice with 8-fold amount of 60% ethanol with 2 h per time.The transfer rate of ginsenoside Rg1, ginsenoside Rb1 and harpagoside was (79.4%±1.56%), (42.62%±0.68%) and (44.89%±0.58%)(n=3), respectively.The dry extract rate was (20.99%±0.411%).Conclusion: The optimized extraction technology is stable and feasible, which can be used for extracting Panax notoginseng and Scrophulariae radix from Rupixiao granule.

Inhibition Effects of Rupixiao Granules on Contractility of Uterus of Mice in Vitro / 医药导报

Objective To study effects of Rupixiao granules on contraction of uterus of mice in vitro. Methods Mouse model with isolated uterine contraction was established. The mice pretreated with estradiol benzoate were sacrificed and then the uteri were taken out. The normal contractions were recorded by the biological function system. Effects of 10, 20, 30, 40, 50, 60 mg.mL-1 Rupixiao granules on spontaneous and oxytocin-induced (5 U.L-1) uterine contractions were recorded,inhibition of Rupixiao granules on mean constriction amplitude,constriction frequency and contraction activity of pitocin-pretreated uterus was observed and the inhibition rates were calculated. Results Compared with the baselines, the amplitude, frequency, activity of spontaneous uterine contraction were significantly down-regulated by Rupixiao solution at a range of 10-60 mg.mL-1 ,as well as it could inhibit oxytocin-induced spasmodic contraction of isolated uterus at 10-50 mg . mL-1 ( P<0. 01 ) . Conclusion The Rupixiao granules inhibits spontaneous contraction of isolated mouse uteri and oxytocin-induced spasm of uterine smooth muscle in vitro.

Effects of Different Extracts of Rupixiao Granules on Mouse Primary Dysmenorrhea Model / 中国药师

Objective:To research the anti-dysmenorrhea effect of different extracts of Rupixiao granules. Methods:The anti-dys-menorrhea effect of different extracts of Rupixiao granules was studied by writhing test induced by oxytocin in mice. Results:Compared with the model group, the extracts of Rupixiao granules could reduce the writhing times induced by oxytocin significantly (P0. 05). Conclusion:The water-soluble parts of Rupixiao granules have significant anti-dysmenor-rhea effect.

Application of Novel Liposomes in Transdermal Drug Delivery System / 中国药师

The stratum corneum barrier and the other issues in transdermal drug delivery system have attracted more and more at-tention, and the novel liposomes as the drug delivery vehicles effectively solve the problems. The novel liposomes can significantly im-prove transdermal drug penetration, therefore, can enhance efficacy and shows high application value and development prospects. In the paper, combined with some domestic and foreign current researches, the classification, penetration mechanisms and application of the novel liposomes were reviewed.

Study Progress in Vaginal Mucoadhesive Drug Delivery Systems / 中国药师

Objective:To review the progress in vaginal mucoadhesive drug delivery systems. Methods:Based on the recently published papers,the research on the application of vaginal mucoadhesive drug delivery systems was classified and summarized. Re-sults:Vaginal mucoadhesive drug delivery systems not only showed safety,effectiveness and strong permeability but also avoided the first pass effect,prolonged drug residence time and improved bioavailability and compliance of patients. Conclusion:Vaginal mucoad-hesive drug delivery systems are becoming research hotspots and exhibit broad application prospects to replace the traditional delivery systems.

Study Progress in Eye Irritation Test in vivo for Ophthalmic Preparations / 中国药师

Various new ophthalmic formulations have been prepared to enhance ocular bioavailability,while lots of irritant sub-stances are applied,including surfactants,polymers and other cationic materials. Therefore,safety of the preparations has been paid more and more attention besides the efficacy. Since in vitro experiments lack of associated enzymes and integral reaction of organiza-tion,the reasonability and correlation of the results extrapolated to the animal experiments still need to be further proved. The in vivo common eye irritation methods( winking,histopathological slices,Draize score and confocal microscopy test etc)were reviewed,eval-uated and analyzed in the paper.

Anti-inflammatory and Analgesic Activity of Rupixiao Granules / 中国药师

Objective:To investigate the anti-inflammatory and analgesic effects of Rupixiao granules. Methods:Activity of Rupixi-ao granules against xylene-induced ear edema in mice was measured to evaluate the anti-inflammatory effect, while the analgesic effect was evaluated by acetic acid induced writhing test and hot plate test in mice. Results:Compared with the control group, Rupixiao gran-ules groups (1. 0, 2. 0 and 4. 0 g·kg·d-1) could significantly inhibit ear swelling in mice(P<0. 05 or 0. 001), and reduce the acetic acid induced writhing times(P<0. 01 or 0. 001). Rupixiao granules at medium and high dose could significantly increase the pain thresh-old of mice in the hot plate test. Conclusion:Rupixiao granules exhibit significant anti-inflammatory and analgesic activities.

Application of Microemulsions on Transdermal Delivery Systems / 中国药师

Objective:To review the application of microemulsions as vehicles in transdermal delivery systems. Methods:Based on the recently published papers, the research on the application of microemulsions was classified and summarized. Results: Microe-mulsions is extensively applied as drug vehicles due to the ability of solubilization, drug permeation enhancement and efficacy improve-ment. Conclusion:Microemulsions as promising vehicles for transdermal delivery show a good application prospect.

Determination of Content and Encapsulation Efficiency of Genistein-loaded Eudragit Nanoparticles by HPLC / 中国药师

Objective:To establish an HPLC method for the determination of genistein in genistein-loaded Eudragit nanoparticles. Methods:The HPLC analysis was carried out on a DiamonsilTM C18(250 mm ×4.6 mm,5μm)column with the mobile phase of meth-anol-water (85∶15) at the flow rate of 1. 0 ml·min-1 . The detection wavelength was set at 261nm and the column temperature was 25℃. Results: A good separation was displayed between the drug peak and the excipient peaks. An excellent linearity range for genistein was obtained from 1.0 μg·ml-1 to 100.0 μg·ml-1(r =0.999 8). The recovery of genistein was 99.85%(RSD =0. 65%,n=9). Conclusion:The method is simple, rapid, accurate and specific, which is suitable for the determination of content and encapsulation efficiency of genistein-loaded nanoparticles.

Recognition of Mercury Ion and Copper Ion with 8-Aminoquinoline Derivatives / 分析化学

The novel 8-Aminoquinoline(8-AQ) derivatives receptor was designed and synthesized.Its struc ture was characterized by NMR and ESI-MS.It was investigated to recognize metal ions such as Cu~(2+), Hg~(2+), Pb~(2+), Zn~(2+), Ni~(2+) and Cd~(2+) via its absorption and fluorescence spectra.The recognition mechanism .and bind ing mode were discussed.The results showed that 8-AQ derivatives 1 coordinated with Cu~(2+) can induce a new absorption peak at 509 nm, which turned the solution to red from colorless.In acetonitrile Hg~(2+) and Cu~(2+) induced dramatic enhancement in the fluorescence of the derivation 1 by 368 and 192 folds.Job plot showed 1:1 stoichiometry between 8-AQ and Cu~(2+) or Hg~(2+).

Determination of Main Components in Minocycline Hydrochloride Sustained-release Tablets by HPLC / 中国药房

OBJECTIVE:To establish an HPLC method for determining the content of main components in minocycline hydrochloride sustained-release tablets.METHODS:The sample was separated on ODS-C_(18)column with the mobile phase consisted of 0.2 mol?L~(-1)ammonium oxalate-0.01 mol?L~(-1)edetate disodium-dimethylformamide-tetrahydrofuran (600:180:120:80)at a flow rate of 1.5 mL?min~(-1).The detection wavelength was set at 280 nm and the sample volume was 20?L.RESULTS:The linear range of minocycline was 0.05～0.5 mg?mL~(-1)(r=0.999 8)and the average recovery was 99.11%,RSD=0.5%.CONCLUSIONS:This method was proved to be accurate and reliable,sensitive and reproducible,and it can be used for determining the content of this tablets.

Preparation of ?-elemene solid lipid nanoparticles by film-ultrasonic wave dissolving techniques / 中草药

Objective To prepare ?-elemene solid lipid nanoparticles and investigate their particle size diameter and entrapment efficiency.Methods The ?-elemene solid lipid nanoparticles were prepared by film ultrasonic wave dissolving techniques.And the optimum formula was selected through orthogonal design test according to the entrapment efficiency.Results The optimizing technique was ?-elemene(20 ?L),stearic acid(90 mg),lecithin(90 mg),Tween80(2.5 %,5 mL) and Poloxamer 188(2.5 %,5 mL).Conclusion The technique of preparing ?-elemene by film-ultrasonic wave dissolving technique is feasible.