主办：上海医药工业研究院
　　　中国药学会
　　　中国化学制药工业协会
ISSN 1001-8255   CN 31-1243/R   ZYGZEA
Chinese Journal of Pharmaceuticals

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  • 2016 Volume 47 Issue 09
    Published: 09 September 2016
      
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  • Druggable Key Technologies for Natural Products
    ZHANG Zhirong
    2016, 47(09): 1118. https://doi.org/10.16522/j.cnki.cjph.2016.09.001
    Abstract ( ) Download PDF ( )   Knowledge map   Save
    Druggability of natural products has been the most critical scientific question in the research and development of natural product-based novel drugs. In this study, key technologies for improving the “druggability” of natural products have been reviewed. Through a extensive literature review, we summarize various strategies that have been used to improve the physicochemical properties, in vivo distribution and pharmacokinetic profiles of natural products including nanoparticles, microparticles, microcapsules, liposomes, inclusion, complex, osmotic pump, transdermal drug delivery system, targeted drug delivery system and prodrug design. These technologies are proven to be useful in enhancing the druggability of natural products.
    Key Words:
  • Thoughts on the Technology of New Compound Drug of TCM
    FENG Yi, ZHANG Jiquan, WANG Youjie, DU Ruofei, HONG Yanlong, WU Fei
    2016, 47(09): 1125. https://doi.org/10.16522/j.cnki.cjph.2016.09.002
    Abstract ( ) Download PDF ( )   Knowledge map   Save
    Because of the complex recipe composition and various clinical applications, the new compound drug of traditional Chinese medicine (TCM) should not be developed by limited fixed models. The research of Chinese classical prescriptions, clinical prescriptions and hospital preparations whose effects are conclusive, should follow the usage in clinical application. The impacts of the process on material base of extracting solution should be concerned, in order to maintain the maximum clinical effect. On the basis of drug safety, effectiveness, stability and controllability, the preparation process of the new compound drug of TCM should be designed and developed reasonably. By investigating the relationship between the properties of concentrated extract or dried extract, the follow-up process and product qualities, appropriate methods, process parameters and excipients will be optimized specifically to achieve the aim of improvement of the preparation process and quality of the drug products.
    Key Words: new drug of traditional Chinese medicine (TCM) development; preparation process design; index
    component; quality by design (QbD); review
  • Challenges and Strategic Solutions in Evaluation of Drug Delivery System for Traditional Chinese Medicine
    HE Yuanzhi1,2, QIN Wei1,2, ZHANG Guoqing1, ZHANG Liu1, YU Lin1, TANG Yan1,2, YANG Ming2*, ZHANG Jiwen1,2*
    2016, 47(09): 1130. https://doi.org/10.16522/j.cnki.cjph.2016.09.003
    Abstract ( ) Download PDF ( )   Knowledge map   Save
    The rapid development of drug delivery system (DDS) for traditional Chinese medicine (TCM) is one of the key progresses of modernization of TCM. The evaluation techniques and regulation system lag behind the development of TCM and become one of the main constraints to the advanced DDS for TCM. The difficulties and challenges in evaluation of DDS for TCM are reviewed from views of complexity for materials in TCM, the holistic integrity and synchronicity for multiple components, as well as multiple components absorption kinetics and in vitro-in vivo correlation-ship methodology. Strategic solutions are suggested to facilitate the research and development of DDS for TCM.
    Key Words: drug delivery system for traditional Chinese medicine; multicomponent; synchronization of release;
    holisticity; evaluation; review
  • Research Idea and Innovation Strategy of Traditional Chinese Medicine Research and Development Based on the Core of Clinical Application
    ZHANG Tiejun
    2016, 47(09): 1136. https://doi.org/10.16522/j.cnki.cjph.2016.09.004
    Abstract ( ) Download PDF ( )   Knowledge map   Save
    The research and development (R&D) of new traditional Chinese medicine (TCM) is a system engineering and the topic choosing, research design, implement method are the key factors concerning the success or failure of the R&D. Considering the characteristics of "from the clinical, applied to clinical" of new TCM, a R&D idea and innovation strategy of new TCM are proposed based on the core of clinical application, according to the characteristics of TCM complex system and the technical requirements of TCM R&D. The basic meaning of "with clinical as the core", the research design of new drugs for clinical and the innovative thinking and method of new TCM R&D are discussed in this paper, so as to provide useful reference for new drug R&D.
  • Preparation and Evaluation of the Solid Dispersions Loaded with Two Active Components of Yuanhu Zhitong Compound
    SHI Tingting, HONG Chao, HAN Limei, QIN Jing, LI Xi, WANG Jianxin
    2016, 47(09): 1151. https://doi.org/10.16522/j.cnki.cjph.2016.09.006
    Abstract ( ) Download PDF ( )   Knowledge map   Save
    In order to improve the oral bioavailability of tetrahydropalmatine (1) and imperatorin (2), two main active components of Yuanhu Zhitong compound, the solid dispersions were prepared by solvent evaporation method. The results of optimization showed that the product was prepared with polyvidone (PVP K30) as the carriers, and the ratio of two-component mixture (1∶2=1∶1) to carrier was 1∶1. The results of differential scanning calorimetry (DSC) and X-ray diffraction (XRD) showed that 1 and 2 were present in amorphous forms in the solid dispersions. The solubilities and dissolutions of 1 and 2 were significantly enhanced compared with their bulk drug. The result of pharmacokinetic study in rats showed that the AUC values of 1 and 2 in solid dispersion group were significant higher than those in 1 or 2 administration alone group (P<0.05). The relative bioavailability of 1 and 2 were 155％ and 187％ calculated by AUC0→t. It indicated that the solid dispersion could simultaneously improve the solubility, dissolution and oral absorption of 1 and 2.
  • Feasibility Study on Bionic Enzymatic Enteric Capsules for Improvement of Oral Bioavailability of Barrenwort Flavonoids
    LIU Congyan, GAO Xia, CHEN Yan, PENG Jing,
    2016, 47(09): 1158. https://doi.org/10.16522/j.cnki.cjph.2016.09.007
    Abstract ( ) Download PDF ( )   Knowledge map   Save
    Based on the hydrolytic and metabolic laws of barrenwort flavonoids and the intestinal absorption characteristics in pathologic conditions of osteoporosis, the bionic enzymatic enteric capsules of barrenwort flavonoids in which adding a small amount of exogenous hydrolytic enzymes (helicase) were prepared to prove the feasibility for the improvement of oral bioavailability of barrenwort flavonoids. The osteoporotic rat model was established. The extraction of barrenwort flavonoids and the above capsules were given by the intragastric route to these model rats in a dose of 500 mg/kg based on barrenwort flavonoids. The concentrations of the prototype glycosides (epimedin A, epimendin B, epimendin C and icariin) and their metabolites (sagittatoside A, sagittatoside B, 2''-O-rhamnosylicarisideⅡ, baohuoside and icaritin) in plasma were determined by HPLC. The plasma concentration-time curves of these prototype glycosides
    and metabolites in osteoporotic rats were drawn and then double peak phenomena were observed. The pharmacokinetic parameters of thess components were also calculated and integrated. The results showed that AUC0→t of the barrenwort flavonoids-loaded bionic enzymatic enteric capsules was significantly higher than that of the corresponding extraction (P<0.01), but there was no significant changes in other pharmacokinetic parameters.
    Key Words: barrenwort flavonoids; bionic enzymatic enteric capsule; helicase; prototype glycoside; metabolite; osteoporosis; pharmacokinetics; oral bioavailability
  • Preparation and Dissolution of Silymarin Nanosuspension
    LUO Kaipei, LI Xiaofang, YANG Lu, LIN Hao, LUO Jia
    2016, 47(09): 1165. https://doi.org/10.16522/j.cnki.cjph.2016.09.008
    Abstract ( ) Download PDF ( )   Knowledge map   Save
    To improve the dissolution of silymarin (1), the 1 nanosuspension (1-NS) was prepared by solvent precipitation method combined with high pressure homogenization method. The process and formulation parameters were optimized by single factor test and central composite design-response surface methodology with average particle size and polydispersion index (PDI) as the indexes. The optimal formulation was as follows: the concentrations of 1, polyvidone
    (PVP) K30 and sodium dodecylsulfate were 4, 1.3 and 0.7 g/L, respectively. Then the crude suspension was treated at homogeneous pressure of 100 MPa with 12 cycles. The results of validation test showed that the average particle size and PDI values of three batches of the optimal 1-NS were (191.4±1.35)nm and 0.135±0.003. Then the 1-NS was freezedried to further improve the stability. The type and concentration of cryoprotectants were also optimized. The results
    showed that the mannitol with the concentration of 5％ had the best protective effect among the tested cryoprotectants. The average particle size and PDI values of the reconstituted 1-NS freeze-dried powder were (243.5±2.8)nm and 0.182±0.018. The dissolution at 60 min of the freeze-dried powders of 1-NS and the physical mixture of 1 in water were 90.5％ and 48.6％, which indicating a significant increase in the rate and extent of dissolution.
  • Preparation of Compound Metronidazole and Artificial Bezoar Buccal Patches
    ZHUANG Shuo, YANG Xinxin, ZHAO Na, LI Chaoying
    2016, 47(09): 1171. https://doi.org/10.16522/j.cnki.cjph.2016.09.009
    Abstract ( ) Download PDF ( )   Knowledge map   Save
    The compound metronidazole and artificial bezoar had the effects of treatment of oral anaerobic infection, detoxification and elimination of gingival swelling. The types and amounts of fillers and bioadhesive agents of the compound metronidazole and artificial bezoar buccal patches were optimized by single factor test with in vitro adhesive force, adhesion time and release as the indexes. The results showed that the optimal buccal patches were obtained by direct compression with the lactose as the filler and the the mixture of Carbomer 934 and hypromellose (HPMC K4M) in a ratio of 1∶5 as the bioadhesive agents at the amount of 35％. The in vitro adhesive force, adhesion time and cumulative release at 4 h of the optimal product was (83.80±0.56)g/cm2, 6 h and 95.64％, respectively.
  • Pharmacokinetics of Arsenic of Liushen Pills and Realgar in Rats
    WANG Qizheng, PAHEERDING·Nuerlajiang, WANG Limin, QIN Jin, WANG Jianxin
    2016, 47(09): 1177. https://doi.org/10.16522/j.cnki.cjph.2016.09.010
    Abstract ( ) Download PDF ( )   Knowledge map   Save
    An inductively coupled plasma mass spectrometry (ICP-MS) method for the determination of total arsenic in blood and an high-performance liquid chromatography (HPLC)-ICP-MS method for the determination of arsenic speciation in blood were established. The results of methodology validation showed that both two determination methods had good linearity, accuracy, reproducibility and recovery. The concentrations of total arsenic and arsenic speciation in blood of rats after ig administration of Liushen pills or realgar at a dose of 125 mg/kg (based on realgar) were determined by ICP-MS and HPLC-ICP-MS. The main pharmacokinetic parameters were calculated by DAS 2.0 software to discuss the effect of compatibility on arsenic toxicity. The results showed that the MRT value of total arsenic
    in rat blood in Liushen pills group was 12.92 h, which was significantly higher than that of realgar group (MRT=19.54 h). It indicated that arsenic in rat blood of Liushen pills group could be cleared more easily. Moreover, the concentration of total arsenic in Liushen pills group was lower than that in realgar group. The total arsenic was primarily present in the form of dimethyl arsenic acid (DMA) with lower toxicity. While in realgar group, the form of arsenite [As(Ⅲ)] with high toxicity in blood also had a relative high concentration. It indicated that other components in Liushen pills might decrease the toxicity of arsenic and promote the transition from the high-toxicity form to the low-toxicity form.
    Key Words: Liushen pills; realgar; inductively coupled plasma mass spectrometry (ICP-MS); high-performance liquid chromatography (HPLC); arsenic speciation; pharmacokinetics; toxicity
  • Chemical Component Analysis and Pharmacodynamics of Essential Oil of Cinnamomum cassia Presl from Sichuan Province
    ZHANG Xiaofei, FENG Lingling, WU Zhenfeng, YANG Ming
    2016, 47(09): 1183. https://doi.org/10.16522/j.cnki.cjph.2016.09.011
    Abstract ( ) Download PDF ( )   Knowledge map   Save
    The essential oil of Cinnamomum cassia Presl from Sichuan province was extracted by steam distillation, and the constituents were analyzed by GC-MS method. The filtering paper method and resazurin staining method were used for determining inhibition zone diameter and minimum inhibitory concentration (MIC) of essential oil against seven tested strains. Its effect on tension of ex vivo small intestine smooth muscle of rats was also investigated. The results showed that 21 chemical components in essential oil were identified, in which cinnamaldehyde and α-pinene had relative high levels of 72.54％ and 8.19％. Cinnamon essential oil showed a high inhibitory effect against Escherichia coli and Candida albicans, a mild inhibitory effect against Penicillium, Aspergillus niger, Bacillus subtilis and Staphylococcus aureus, and a weak effect against Pseudomonas aeruginosa. In addition, cinnamon essential oil had an inhibitory effect on tension of the small intestine smooth muscle of rats.
    Key Words: cinnamon essential oil; gas chromatography-mass spectrometry (GC-MS); chemical component analysis; antibacterial activity; inhibition of intestinal smooth muscle
  • An Investigation of the Effect of Drug Compatibility of Tanreqing on Uptake and Transport of Baicalin by Caco-2 Cell Model
    ZHENG Yongfeng, HE Yuwei, PANG Liang, XIE Zhongyi, LIU Shaoyong,
    2016, 47(09): 1188. https://doi.org/10.16522/j.cnki.cjph.2016.09.012
    Abstract ( ) Download PDF ( )   Knowledge map   Save
    The effect of drug compatibility of Tanreqing on the uptake and transport of baicalin was investigated by Caco-2 cell model. The results showed that both the whole prescription and Jun-Chen-Zuo combined could increase the uptake of baicalin significantly (P<0.05). And the whole prescription could also improve the absorption (Papp AP→BL) as well as reduce the secretion (Papp BL→AP) of baicalin observably (P<0.05), therefore the efflux rate (ER) was decreased
    while the cumulative transport amount was increased. Meanwhile, the Jun-Chen-Zuo combined could reduce the secretion (transport) of baicalin markedly (P<0.01) and reduce the ER as well, illustrating that the drug compatibility of Tanreqing could promote the absorption of baicalin in Caco-2 cell model.
  • Formulation Optimization of Effervescent Tablets Loaded with Caulis Dendrobii officinalis
    Lü Yi, CHEN Guangyu, HE Qun, LI Shunxiang, CAI Guangxian
    2016, 47(09): 1194. https://doi.org/10.16522/j.cnki.cjph.2016.09.013
    Abstract ( ) Download PDF ( )   Knowledge map   Save
    The formulation of effervescent tablets loaded with micronized powder of Caulis Dendrobii officinalis was optimized by single factor experiment and Box-Behnken design combined with response surface methodology with the qualities of the damp mass, granules and tablets as indexes. The optimal formulation was as follows: micronized powder of Caulis Dendrobii officinalis 44.5％, anhydrous glucose 25％, sodium bicarbonate 15％, citric acid 15％ and magnesium stearate 0.5％. The granules were prepared after adding 95％ ethanol containing 7％ polyvidone (PVP) K30 as adhesive and dried until the moisture content was below 3％. The final product could dissolve in 2.1 min, and the pH value of the solution was 6.2.
  • Discussion on the Continuous Development of Traditional Chinese Medicine Preparations
    HOU Shixiang
    2016, 47(09): 1199. https://doi.org/10.16522/j.cnki.cjph.2016.09.014
    Abstract ( ) Download PDF ( )   Knowledge map   Save
  • Strategies and Suggestions for the Implementation of Green and Intelligent Manufacturing in Traditional Chinese Medicine
    YANG Ming1, WU Zhenfeng1, WANG Fang1, CANG Zhenzhong1, ZHONG Guangde2*
    2016, 47(09): 1205. https://doi.org/10.16522/j.cnki.cjph.2016.09.015
    Abstract ( ) Download PDF ( )   Knowledge map   Save
    With the gradual implementation of the "Made in China 2025" plan, accelerating the improvement of manufacturing innovation system in cooperation with green and smart manufacturing has become a breakthrough in the transformation and upgrading of manufacturing industry. The shortages in the traditional Chinese medicine (TCM) pharmaceutical industry such as the low level production, the extensive process, the backward production equipment and the low level of automation seriously restricted the improvement of the overall level of the pharmaceutical industry, thus affecting the quality and safety of drugs. This paper combined with the status of TCM pharmaceutical industry, has carried on the analysis to the principles, opportunities and challenges of green and intelligent manufacturing of TCM, and puts forward the corresponding strategies and suggestions, in order to provide references for the structure adjustment, transformation and upgrading of TCM pharmaceutical industry.
  • Quality by Design about Traditional Chinese Medicine Compound Preparation
    YANG Changming1, WANG Jianxin2
    2016, 47(09): 1211. https://doi.org/10.16522/j.cnki.cjph.2016.09.016
    Abstract ( ) Download PDF ( )   Knowledge map   Save
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