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

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  • Perspectives & Review
    BAO Guanglong, WANG Honggang, ZHANG Naihua, XIANG Yangguang, ZHANG Guimin
    Chinese Journal of Pharmaceuticals. 2023, 54(11): 1535-1544. https://doi.org/10.16522/j.cnki.cjph.2023.11.001
    Tucatinib(1) is an oral inhibitor of HER2 for clinical treatment of HER2- positive breast cancers. In this paper, the synthesis methods of 1 and its key intermediate 4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-3- methylaniline(2) are reviewed, and the advantages and disadvantages of each synthetic route are discussed. This review is beneficial to the future process research of tucatinib.
  • Perspectives & Review
    YANG Jiawei, CHEN Shengwei, SU Weike, XU Wenhao
    Chinese Journal of Pharmaceuticals. 2023, 54(09): 1283-1293. https://doi.org/10.16522/j.cnki.cjph.2023.09.001
    Lignin is a kind of natural aromatic biopolymer, which is usually composed of highly cross-linked aromatic ether unit structures through random polymerization. It is a widely distributed and high-yield biomass resource, inferior to cellulose and hemicellulose. It is expected to become an important and inexpensive source of aromatics, which is crucial for the pharmaceutical field. This paper reviews the current extraction methods, degradation technologies of lignin, and summarizes the applications of lignin and its degradation and modification products in the pharmaceutical field, so as to provide some references for the full utilization and functional application of lignin resources.
  • Perspectives & Review
    LI Wanting, SU Junhui, WANG Yawen, ZHAO Xiaoqing, XU Bing
    Chinese Journal of Pharmaceuticals. 2023, 54(08): 1157-1165. https://doi.org/10.16522/j.cnki.cjph.2023.08.002
    This paper summarizes the relevant literature on tablet disintegration published at home and abroad from 2010 to 2021, and outlines the influencing factors and possible disintegration mechanisms of tablet disintegration process. The disintegration of tablets is affected by the properties of raw and auxiliary materials, formulation composition, process parameters and disintegration medium. The mechanisms of tablet disintegration mainly include swelling, shape recovery and wicking. Among the commonly used functional auxiliary materials for disintegration, starch and its derivatives, croscarmellose sodium and sodium carboxymethyl starch promote disintegration through swelling. The mechanism of polyvinylpolypyrrolidone promoting disintegration is shape recovery. Cellulose and its derivatives promote disintegration through strong wicking effect. Future research directions include: correlation modeling between critical material attributes, critical process parameters and tablet disintegration behavior in tablet technology; objective, visual and quantitative characterization of tablet disintegration process and behavior; development and application of new pharmaceutical excipients to promote tablet disintegration.
  • Perspectives & Review
    ZHOU Wei, LIN Kuaile, ZHOU Weicheng
    Chinese Journal of Pharmaceuticals. 2024, 55(1): 1-27. https://doi.org/10.16522/j.cnki.cjph.2024.01.001
    The U.S. FDA approved 53 new drugs in 2023, including 31 chemical small molecules, 21 biological products and 1 botanical drug. According to the prescription information for professionals and the related literature as well as patent information, this review describes the descriptions, indications, mechanism of action, dosage forms and strengths, adverse reactions, and one synthetic route of the chemical small molecules, and brief information about biological and botanical products.
  • Perspectives
    QIN Xu, TONG Zhenbo, REN Hongxian
    Chinese Journal of Pharmaceuticals. 2023, 54(07): 984-992. https://doi.org/10.16522/j.cnki.cjph.2023.07.001
    Inhalation therapy is the superior choice for treating respiratory diseases. Unlike traditional methods of drug administration, inhalation therapy requires the use of inhalation devices to deliver the drugs to targeted areas. Innovations in inhalation devices aim to improve the delivery efficiency, reduce the impact of respiratory flow rate on drug delivery and improve patient compliance. This paper reviews the development trends of oral inhalation devices and their progress in intelligentization. The soft mist inhaler based on innovative microfluidic nebulization technology and its nebulization mechanism and delivery characteristics are analyzed and discussed. Moreover, this paper further elaborates on the different stages of the development of intelligent inhalation devices. The impact of intelligent inhalation devices on patient compliance is also discussed, providing a reference for further research on intelligent inhalation devices.
  • Perspectives & Review
    GONG Lixiang, ZHANG Baoxi, TAO Yue, ZHOU Jian, YANG Shiying, LYU Yang
    Chinese Journal of Pharmaceuticals. 2023, 54(12): 1687-1693. https://doi.org/10.16522/j.cnki.cjph.2023.12.001
    Dynamic vapor sorption(DVS) technology is served as a crucial tool for the examination of pharmaceutical crystal forms and co-crystals. Not only can DVS technology assess moisture sorption performance of an API, but it also probes into phase transition issues, co-crystal screening, quantification of amorphous content at low levels in crystalline materials, as well as the miscellaneous. At present, many countries and regions have included DVS technology into their pharmacopoeias for the exploration of water-solid interactions. However, the Chinese pharmacopoeia has not recorded this technology. This paper provides an overview of the application and advance of DVS technology in the investigation of pharmaceutical crystal forms and co-crystals, as a reference for related research on polymorphism of drugs.
  • Perspectives
    GUO Junyan, WU Wenzhe, WANG Jian
    Chinese Journal of Pharmaceuticals. 2023, 54(07): 993-1001. https://doi.org/10.16522/j.cnki.cjph.2023.07.002
    In recent years, pulmonary infectious diseases have posed a serious threat to human health. Compared with the traditional oral and injection administration routes, inhalation administration is increasingly used to treat pulmonary infectious diseases. This route can achieve targeted delivery of drugs to the infected sites, and has the advantages of improving the pulmonary bioavailability, reducing systemic adverse reactions and drug resistance, and therefore has gained widely concern. This paper summarizes the research progress of inhalation preparations for treatment of pulmonary infectious diseases, with a view to providing references for the research and development of anti-infective drugs for pulmonary inhalation.
  • Perspectives & Review
    LIU Chuqiao, ZHANG Peng, FU Lili, TAO Qiaoyu, QIU Yunliang
    Chinese Journal of Pharmaceuticals. 2023, 54(10): 1403-1410. https://doi.org/10.16522/j.cnki.cjph.2023.10.001
    Inherited retinal diseases(IRD) are an important cause of irreversible vision loss or blindness, whose prognosis is poor, and clinically effective intervention methods are lacking. Gene therapy has created new possibilities for IRD treatment. Adeno-associated viral(AAV) is a widely used viral gene therapy vector with application prospects. This paper briefly describes the feasibility of AVV vectors in ocular application, focuses on the preclinical and clinical progress of the application of AAV delivery system for IRD treatment, evaluates the safety and efficacy based on the obtained data, and summarizes the influencing factors of gene therapy for IRD, as well as looks forward to the future research directions, providing references for the technological innovation of IRD treatment and the subsequent product development of AAV vectors.
  • Paper
    ZHANG Hanyilan, HU Yuhua, ZHANG Song, XU Weiguo, YANG Qingyun
    Chinese Journal of Pharmaceuticals. 2023, 54(07): 1104-1111. https://doi.org/10.16522/j.cnki.cjph.2023.07.017
    Bromhexine hydrochloride(1) is a commonly used expectorant, showing a polycrystalline phenomenon. Crystal transformation might affect its efficacy. Infrared spectroscopy(IR), powder X-ray diffraction(PXRD), and differential scanning calorimetry(DSC) analyses were adopted to characterize crystal patterns of 1 in its granules and dispersible tablets, and the crystal stability of 1 during the preparation and storage processes was studied. Through IR and PXRD analyses, three different crystal forms of 1 could be identified, while the characterization results of three different crystal forms by DSC were not remarkable. The results indicated that crystal form A of 1 showed good crystal stability and did not undergo crystal transformation during the preparation processes of granules and dispersible tablets or storage under high temperature, light, and high humidity conditions. This paper provided data for improving quality control levels and monitoring the production process.
  • Paper
    HAN Zhongli, WANG Hongying, BAO Guanglong, WEN Hao, ZHANG Guimin
    Chinese Journal of Pharmaceuticals. 2023, 54(07): 1065-1069. https://doi.org/10.16522/j.cnki.cjph.2023.07.011
    An improved synthetic process of roxadustat(1) was reported. Methyl 4-hydroxy-7- phenoxyisoquinoline-3-carboxylate(2) was chlorinated by 1,3-dichloro-5,5-dimethylhydantoin to obtain methyl 1-chloro- 4-hydroxy-7-phenoxyisoquinoline-3-carboxylate(3), 3 was transformed into 1-methyl-4-hydroxy-7-phenoxyisoquinoline- 3-carboxylic acid(4) through coupling reaction with methylboronic acid and hydrolysis. Then 4 was amidated with glycine methyl ester hydrochloride to generate methyl (1-methyl-4-hydroxy-7-phenoxyisoquinoline-3-carbonyl)- glycinate(5). Finally, the target compound 1 was obtained from 5 by hydrolysis reaction with a purity of 99.9% and an overall yield of 60.8%(based on 2). The optimized process was easy to operate and had been verified by pilot test, which was suitable for industrial production.
  • Perspectives & Review
    WANG Peng, ZHANG Yong, WANG Donghai, YANG Qingmin
    Chinese Journal of Pharmaceuticals. 2024, 55(3): 319-325. https://doi.org/10.16522/j.cnki.cjph.2024.03.002
    Orodispersible films are innovative single-layer or multi-layer composite drug-loading films that can be quickly wetted by the patient’s saliva and dissolved in the mouth without the need for drinking water. This review introduces the dosage form characteristics, global development, formulation compositions and process features, research content and general requirements of quality control of orodispersible films. For the quality evaluation of orodispersible films, except for the conventional inspection items of ordinary oral preparations, some special characteristics, such as physical, chemical, and mechanical properties of orodispersible films should also be evaluated based on the dosage form characteristics in order to ensure the safety and effectiveness of the products.
  • Pharmaceutical Management & Information
    LI Difang, TIAN Lijuan
    Chinese Journal of Pharmaceuticals. 2023, 54(07): 1132-1136. https://doi.org/10.16522/j.cnki.cjph.2023.07.021
    偏差管理是药品生产质量管理规范体系中的重要组成部分。文章结合文献研究和工作实践,分析目前制药企业偏差 管理的现状及存在问题,与某制药企业偏差管理存在问题基本一致。继而针对某制药企业建立了一套完整的偏差管理系 统,通过偏差调查深入挖掘偏差产生的根本原因并采取合理的纠正预防措施,以有效降低偏差事件的发生,提高某制药企 业的质量管理水平,切实保证药品质量、维护患者用药安全,期望能为国内制药企业改进偏差管理提供良好的借鉴。
  • Pharmaceutical Management & Information
    LIU Mengsi, YE Xiao
    Chinese Journal of Pharmaceuticals. 2023, 54(07): 1112-1117. https://doi.org/10.16522/j.cnki.cjph.2023.07.018
    包衣微丸制剂具有掩盖药物的不良臭味、改善药物含量均匀性、提高药物稳定性与改变药物释放特性等特点,是 当前仿制药研发及申报的热点。文章介绍了包衣微丸的结构、制剂的处方组成以及包衣工艺的特点。结合生产现场检查 中的常见问题,对仿制药申报中包衣微丸制剂的处方工艺及质量研究进行了分析和探讨。
  • Paper
    GUO Lishan, LI Xiyue, YAO Chengli, XI Quan
    Chinese Journal of Pharmaceuticals. 2023, 54(09): 1367-1373. https://doi.org/10.16522/j.cnki.cjph.2023.09.013
    Free vitamin K1(VK1) in VK1-loaded mixed micelles(VK1-MM) injection leads to security risks. The encapsulation efficiency is one of the indexes to evaluate the content of free VK1 in mixed micelles and their drug-loading performance, while the applicability of various determination methods is different. This study compared the applicability of extraction, centrifugation, and filtration methods in evaluating the encapsulation efficiency of VK1-MM. The study of the main factor affecting the accuracy of each method showed that the extractant altered the structure of VK1-MM during extraction. In addition, the free VK1 and VK1-MM could not be completely separated by centrifugation, which was related to the tiny density difference between free VK1 and water. However, filtration could effectively separate free VK1 and VK1- MM with the appropriate pore size and material of the filter membrane. The recovery of filtration was 100.40% (with RSD of 0.80%, n=3), which showed filtration was suitable for determining the encapsulation efficiency of VK1-MM. Simultaneously, the applicability of different encapsulation efficiency determination methods and the characteristics of formulations were analyzed, which provided a reference for establishing a suitable encapsulation efficiency determination method for other micellar preparations.
  • Perspectives & Review
    CAO Yang, ZHU Ranran, OU Xingjun, SONG Lixing, WU Fanhong
    Chinese Journal of Pharmaceuticals. 2023, 54(10): 1420-1428. https://doi.org/10.16522/j.cnki.cjph.2023.10.003
    Chirality is a widely existing property in pharmaceuticals. In general, the chiral enantiomers show higher activity and lower adverse reaction than their racemates. Therefore, the manufacturing of pure chiral enantiomer is of great scientific significance. Crystallization resolution method is an important technique in pharmaceutical industry to achieve the separation of enantiomers. As a novel crystallization technique, cocrystal has attracted much attention due to its broad applicability. In this paper, the history and development of chiral resolution based on cocrystallization are briefly introduced. Meanwhile, the recent progress in this field is classified and summarized according to the structural characteristics of cocrystals formed by racemic drugs. In addition, the main challenges of chiral resolution based on cocrystallization are summarized and prospected.
  • Perspectives & Review
    WANG Junzheng, WANG Dongmei, YANG Tianming
    Chinese Journal of Pharmaceuticals. 2023, 54(08): 1145-1156. https://doi.org/10.16522/j.cnki.cjph.2023.08.001
    Ozanimod hydrochloride, a new type of oral sphingosine 1-phosphate(S1P) receptor modulator, is clinically used for the treatment of relapsing multiple sclerosis. In this review, the synthetic methods of ozanimod hydrochloride and its key intermediates are summarized and evaluated based on different schemes described in the literature. The scaffold structure of ozanimod hydrochloride is (S)-1-amino-4-(1,2,4-oxadiazol-3-yl)-2,3-dihydro- 1H-indene. Starting from 4-cyano-2,3-dihydro-1H-inden-1-one(2), chiral auxiliary agents or catalysts for asymmetric hydrogenation are used to construct the chiral amino group at the 1-position of 2,3-dihydro-1H-indene. Alternatively, the 1-carbonyl group is converted to the chiral hydroxyl before constructing the chiral amino group. The oxadiazole ring at the 4-position of 2,3-dihydro-1H-indene is synthesized in situ from 4-cyano group.
  • Pharmaceutical Management & Information
    YANG Kangli, CHEN Zhen
    Chinese Journal of Pharmaceuticals. 2023, 54(10): 1521-1526. https://doi.org/10.16522/j.cnki.cjph.2023.10.018
    文章基于药学研究的特点,探讨药学研究不同阶段质量管理的要素,供药学研究机构建立和完善其质量管理体系时参考。 通过对比药学研究与非临床研究、临床试验的异同,以及药学研究与药品生产的异同,分析GLP、GCP 和GMP 对药学研究质 量管理的适用性;通过分析药学研究不同阶段质量管理的特点,探讨药学研究在非GMP、类GMP 和完整GMP 阶段的质量管 理要素。药学研究不同阶段的质量管理目标有所不同,药学研究机构应基于自身工作内容及药学研究各个阶段的质量管理目标 建立相应的质量管理体系,确保药学研究数据的可靠性以及临床试验用药品的质量。
  • Paper
    GAO Feng, DAI Jiawei, WANG Junfeng, XIA Chunnian
    Chinese Journal of Pharmaceuticals. 2023, 54(07): 1060-1064. https://doi.org/10.16522/j.cnki.cjph.2023.07.010
    Continuous flow process for the synthesis of losartan(1) was realized by microchannel reactor technology based on the synthetic routes reported in the literature. Compound 1 was obtained with an overall yield of 70.3% [based on 2-cyano-4'-methylbiphenyl(2)] via bromination, N-alkylation and tetrazolium cycloaddition reaction using 2 and 2-butyl-4-chloro-1H-imidazole-5-carboxaldehyde(3) as the starting materials. The optimized process bearing mild reaction conditions, simple operation and higher security is suitable for industrial production.
  • Paper
    SUN Zhe, XU Xiangyang, YANG Xiangping, WANG Hui, ZHANG Le
    Chinese Journal of Pharmaceuticals. 2023, 54(10): 1429-1432. https://doi.org/10.16522/j.cnki.cjph.2023.10.004
    Tiapride hydrochloride was synthesized from 2-methoxy benzoic acid with an overall yield of 46.0% by the reaction with chlorosulfonic acid, followed by sodium sulfite and dimethylsulfate to generate methyl 2-methoxy- 5-(methanesulfonyl) benzoate, the latter was reacted with N,N-diethylenediamine, and then by salt formation with hydrochloric acid.
  • Pharmaceutical Management & Information
    NA Xinzhu, ZHANG Junlin, HU Yuxi
    Chinese Journal of Pharmaceuticals. 2023, 54(08): 1265-1268. https://doi.org/10.16522/j.cnki.cjph.2023.08.018
    随着材料科学的发展和制药工业水平的进步,采用可生物降解的聚合物载体材料将化学药物制备为微球注射剂, 可解决药物半衰期短、需频繁给药的问题。但由于微球制备技术较为复杂,实现产业化较困难,目前上市的微球药物制 剂较少。并且,对基于微球的长效注射剂进行仿制也存在较高的技术壁垒,仿制产品数量更是寥寥无几。文章参考化学 药品注射剂仿制药相关技术要求,结合微球注射剂的产品特点和相关文献资料,对其处方工艺开发、质量和稳定性研究 等需要关注的内容进行讨论,以期为化学仿制药微球注射剂的药学研究提供参考。
  • Review
    MA Yueqin, LI Gang, XIAO Hanyang, YUE Pengfei, ZHANG Zengzhu
    Chinese Journal of Pharmaceuticals. 2023, 54(07): 1042-1051. https://doi.org/10.16522/j.cnki.cjph.2023.07.008
    Owing to simple preparation process, high drug loading capacity and strong adhesion, nanocrystals can effectively solve the problems of short-term retention time, slow release rate and low bioavailability of poorly watersoluble drugs. Therefore, it has become a hot research topic in pharmaceutics in recent years. In this paper, the preparation technologies of nanocrystals and their research progress of applications in mucosal drug delivery systems such as nasal, ocular, oral, skin and pulmonary delivery systems are reviewed, hoping to provide a reference basis for the development of nanocrystal-based dosage forms of poorly soluble drugs.
  • Pharmaceutical Management & Information
    SHEN Jili, GONG Qing, SUN Chunmeng, ZHANG Xinfang
    Chinese Journal of Pharmaceuticals. 2023, 54(12): 1774-1780. https://doi.org/10.16522/j.cnki.cjph.2023.12.013
    在我国仿制药一致性评价政策的推动下,随着ICH M9 等指导原则的实施,对参比制剂处方的正确解析直接决定 了是否可豁免仿制药的生物等效试验,且关系到仿制药与参比制剂生物等效试验的成败。该文全方位阐述了如何将逆向 工程法用于参比制剂解析,包括处方、生产工艺及包装等方面,并结合审评经验进行案例分析,旨在引导业界探索更多 的逆向工程技术用于开发高质量的仿制药,以期加速仿制药上市。
  • Review
    LU Linwei, DING Yuan, XU Qianzhu, LU Weiyue
    Chinese Journal of Pharmaceuticals. 2023, 54(07): 1052-1059. https://doi.org/10.16522/j.cnki.cjph.2023.07.009
    Baicalein, a flavone derived from Scutellaria baicalensis, exhibits antitumor effect by suppressing tumor cell proliferation, inducing tumor cell apoptosis, inhibiting tumor angiogenesis, and regulating the tumor microenvironment. However, its poor solubility has attenuated the bioavailability and thus restricting the efficacy. Many studies utilize nano-drug delivery systems to improve bioavailability and antitumor efficacy of baicalein. This review summarizes the recent studies concerning the antitumor mechanisms of baicalein and its nano delivery systems to provide approaches for its further basic research and clinical application.
  • Paper
    LI Panxin, WANG Chuting, YANG Ruoyun, ZHANG Zhiguang, ZHANG Yong
    Chinese Journal of Pharmaceuticals. 2023, 54(11): 1586-1592. https://doi.org/10.16522/j.cnki.cjph.2023.11.007
    To perform the quality control of arbidol hydrochloride, five potential related substances were synthesized. They were ethyl 6-bromo-4-[(dimethylamino)methyl]-5-hydroxy-1-methyl-2-[(phenylsulfinyl)- methyl]-1H-indole-3-carboxylate(related substance A), ethyl 6-bromo-4-[(dimethylamino)methyl]-5-hydroxy-1,2- dimethyl-1H-indole-3-carboxylate(related substance B), ethyl 6-bromo-5-hydroxy-1-methyl-4-[(methylamino)- methyl]-2-[(phenylthio)methyl]-1H-indole-3-carboxylate(related substance C), ethyl 4-[(dimethylamino)methyl]- 5-hydroxy-1-methyl-2-[(phenylthio)methyl]-1H-indole-3-carboxylate(related substance D) and ethyl 6,7-dibromo-4- [(dimethylamino)methyl]-5-hydroxy-1-methyl-2-[(phenylthio)methyl]-1H-indole-3-carboxylate(related substance E). Their chemical structures were confirmed by MS, 1H NMR and 13C NMR.
  • Perspectives & Review
    AN Qiuxu, HUO Daixia, LIU Yuanyuan, LYU Xiaojie
    Chinese Journal of Pharmaceuticals. 2023, 54(11): 1545-1552. https://doi.org/10.16522/j.cnki.cjph.2023.11.002
    Oral administration is the preferred method for drug delivery. However, due to the unique properties of drugs and the gastrointestinal barrier, the bioavailability of oral administration is limited. By referencing the structural characteristics of organisms in nature and adopting a biomimetic perspective, the biomimetic nanocarriers can be designed and prepared to improve the oral absorption of drugs, which hold promising development prospects. This review summarizes the application of nanocarriers designed and prepared with various biomimetic ideas in oral drug delivery,offering insights and references for the development and clinical application of oral nanocarriers.
  • Perspectives & Review
    LI Xiangmei, CHEN Kaidong, YE Yong, LUO Huafei
    Chinese Journal of Pharmaceuticals. 2023, 54(12): 1694-1703. https://doi.org/10.16522/j.cnki.cjph.2023.12.002
    Vaginal drug delivery has attracted great attention due to its advantages such as rich blood supply, large surface area of vagina and avoidance of the hepatic first-pass effect. However, there are still issues such as leakage and discomfort in application of traditional drug dosage forms for vaginal administration. At present, strategies such as bioadhesive materials, thermosensitive materials, pH responsive materials, mucosal penetration techniques and nano technologies have been proposed to improve the retention time, permeability, and release characteristics of drugs in the vagina. Based on the physiological structure and characteristics of the vagina, this review summarizes the delivery strategies and techniques of drug delivery through the vaginal mucosa, hoping to provide a reference for the development of vaginal topical medication and uterine-targeting delivery products.
  • Perspectives
    LU Wangding, CHEN Guiliang , LUO Huafei, WANG Jian, GE Yuanyuan, ZHANG Jingchen
    Chinese Journal of Pharmaceuticals. 2023, 54(07): 1034-1041. https://doi.org/10.16522/j.cnki.cjph.2023.07.007
    Drug-device combination products have become a hot spot of innovation with the rapid development of modern science and technology. Drug-device combined products integrate the functions of medicines and medical devices, so they generally have the characteristics of high risk and complex technical performance. The development of drug-device combination products in China is still in its infancy and the regulatory system needs to be gradually improved. The guidances issued by U.S. FDA describe the key role of human factors engineering in the development of drug-device combination products, as well as the importance of human factors engineering to product safety and effectiveness. The relatively mature review thinkings of U.S. FDA might have a positive role in promoting the understanding of human factors engineering and evaluation of some related indicators for drug-device combination products of regulatory authorities in China.
  • Perspectives & Review
    CHEN Fang , WANG Jian , LI Mingyan , SHANG Yue, HOU Huimin
    Chinese Journal of Pharmaceuticals. 2024, 55(3): 310-318. https://doi.org/10.16522/j.cnki.cjph.2024.03.001
    The pharmaceutical films are thin sheets formed by various methods such as casting or extrusion, which results in a dispersion of the active pharmaceutical ingredients through the film. They are subject to growing research and have received increasing interests recently due to their convenient administration and improved patient compliance. This review summarizes the marketed products of film dosage form, their quality standards, and storage requirements. Besides, the testing methods of quality inspection items including disintegration time and dissolution are discussed. Finally, brief explanations are provided for the revision of general requirements of pharmaceutical films in the general chapter of the Chinese Pharmacopoeia by comparing with the United States Pharmacopoeia, European Pharmacopoeia, and Japanese Pharmacopoeia.
  • Paper
    WANG Juxiang, ZHOU Da, SUN Yongqiang
    Chinese Journal of Pharmaceuticals. 2023, 54(09): 1354-1359. https://doi.org/10.16522/j.cnki.cjph.2023.09.011
    This study used styrene-isoprene-styrene(SIS) block copolymer as the matrix, liquid paraffin as carrier dispersant, hydrogenated petroleum resin as the tackifier, N-methyl pyrrolidone(NMP) as solubilizer, menthol as the penetration enhancer, citric acid as the acidity regulator and butylated hydroxytoluene(BHT) as the antioxidant to prepare loxoprofen sodium(1) transdermal patches. The preparation process was optimized by orthogonal design. The optimized formulation compositons of the patch were as follows: the mass fraction of SIS was 27%, liquid paraffin was 33%, hydrogenated petroleum resin was 26%, citric acid was 1.2%, menthol was 5.67%, and both NMP and BHT were 0.85%. The quality of 1 patch prepared according to the optimal formulation was stable, and the adhesive property was good. Its transdermal effect was equivalent to the reference preparation(the permeability per unit area at 24 h reached 72.69 μg).
  • Perspectives & Review
    ZHANG Cheng, YAN Dong, CHANG Gang, LIU Qianying, ZHAI Guangxi
    Chinese Journal of Pharmaceuticals. 2023, 54(09): 1294-1301. https://doi.org/10.16522/j.cnki.cjph.2023.09.002
    As a novel drug delivery system, microspheres can provide a sustained-release drug delivery lasting from weeks to months, which reduce drug administration frequency and improve patient compliance. Poly(lactide-coglycolide)( PLGA) has been widely used as a carrier material for microspheres manufacture. However, the molecular characteristics of PLGA are the key influence factors in the stage of formulation design, which are related to the pivotal behaviors of microspheres, such as drug loading, particle size and sustained-release properties. In this paper, by reviewing the recent studies on the preparation and evaluation of PLGA microspheres, five momentous molecular properties of PLGA(such as the relative molecular weight and distribution), which have significant effects on the properties of microspheres are screened out. The effects of each molecular property on the behaviors of microspheres are summarized and the reasons are explained, which provides a reference for the selection of PLGA type in the development of microspheres with expected properties.
  • Perspectives & Review
    TAO Xiaoqian, SUN Jiabin, LEI Jingwen, CHENG Lan, ZHANG Chungang
    Chinese Journal of Pharmaceuticals. 2023, 54(09): 1310-1318. https://doi.org/10.16522/j.cnki.cjph.2023.09.004
    Soft capsules may encounter a series of stability problems in the processes of production, transportation and storage, such as the adhesion, leakage and delayed disintegration, which greatly shorten the shelflives of soft capsules. High temperature, high humidity, ultraviolet radiation, γ-radiation, rapid drying and other physical conditions or exposing to aldehydes, ketones, imines and other chemical substances will cause cross-linking and aging of soft capsule shell, inducing above stability issues. Developing new types of soft capsule shell material might improve the aforementioned issues. In this review, new soft capsule shell materials are classified according to sources, the research progress of animal-, plant- and microbial-derived materials, as well as modified and synthetic shell materials are introduced, hoping to provide a reference for improving the stability of soft capsules during their shelf-lives.
  • Perspectives & Review
    HUANG Mengling, RUAN Haihua, SONG Yun
    Chinese Journal of Pharmaceuticals. 2023, 54(11): 1553-1561. https://doi.org/10.16522/j.cnki.cjph.2023.11.003
    Paclitaxel belongs to the diterpenoid compounds and has good antitumor activity against various cancers such as ovarian cancer and breast cancer. Due to its poor solubility, paclitaxel has significant adverse reactions when it was used directly, limiting its clinical application. Serum albumin nanoparticles can compensate for the inherent defects of paclitaxel, enhance the stability of the drug in the body, improve its bioavailability and targeting ability, achieve the purpose of enhancing efficacy and reducing toxicity, and to some extent solve the problem of paclitaxel. This review summarizes the preparation process of serum albumin-paclitaxel nanoparticles, the application of modified serum albumin in paclitaxel-loaded nanoparticles, in order to provide theoretical guidance for the development of serum albumin based nanodrug delivery systems that meet actual clinical applications.
  • Perspectives & Review
    GAO Dongxu, ZHAO Yuan, LU Weigen, HE Jun, HU Qingyuan
    Chinese Journal of Pharmaceuticals. 2024, 55(4): 445-455. https://doi.org/10.16522/j.cnki.cjph.2024.04.001
    In recent years, liposome products have been successively launched. However, standardized testing methods for in vitro release of liposomal products have not been incorporated in various pharmacopoeias, which poses great challenges for the development and regulation of liposomal products. In vitro release is an important technical indicator for evaluating the quality of pharmaceutical preparations, and plays an important role in product development, quality research, and product release. This review introduces the in vitro release methods and detection apparatuses of liposomal products reported both domestically and internationally, and elaborates on the selection basis of in vitro release methods suitable for approval products. It is hoped that this review will promote and improve the development of in vitro release methods for liposomes, and provide more scientific and accurate data support for the research and regulation of liposome products.
  • Paper
    CHEN Gangsheng, GUO Heng, ZHANG Fuli
    Chinese Journal of Pharmaceuticals. 2023, 54(12): 1713-1717. https://doi.org/10.16522/j.cnki.cjph.2023.12.004
    (R)-3-aminobutanol[(R)-1] was a versatile intermediate of several drugs, and it was of great significance to optimize its synthetic process. According to a patent, the final product was (S)-3-aminobutanol instead of the required (R)-product if prepared with (R)-α-phenethylamine[(R)-3] as the chiral auxiliary agent. So, with (S)-3 as the chiral auxiliary agent, compound (R)-3-[[(S)-1-phenylethyl]amino]butan-1-ol[(R)-5] and (S)-5 were prepared by the reductive amination of 4-hydroxy-2-butanone(2), and then (R)-5 and (S)-5 were transformed into the corresponding hydrochlorides. After that, compounds 5 hydrochloride was isolated by recrystallization with a mixed solvent of ethanol and ethyl acetate (volume ratio=3∶1). After alkalization, compound 5 was underwnt the de-benzylation with palladium charcoal and ammonium formate to obtain compound 1 with a total yield of 56.04%(based on 2), a purity of 98.5% and ee of 99%.
  • Pharmaceutical Management & Information
    CHEN Ye, LIU Xinyue, DING Xiaomi, DING Jinxi
    Chinese Journal of Pharmaceuticals. 2023, 54(11): 1663-1670. https://doi.org/10.16522/j.cnki.cjph.2023.11.017
    我国药品基本医疗保险目录已形成了“独家品种谈判准入、非独家品种竞价准入”的分类准入机制,有效增加了 临床用药的选择。但目前医保准入路径适用分类仅以批文数量作为唯一划分标准,导致有核心专利权的多批文药品丧失 谈判资格,只能通过竞价准入路径进入国家医保药品目录,其在医保准入中的启动决定权、价格决定权和“双通道”推 荐权被削弱。文章建议完善医保准入流程,采取“批文+专利”的分类处理模式,从而更好地保护创新药专利权,为我国 药品基本医疗保险目录的准入提供更为公平、合理的环境。
  • Paper
    GUAN Yingzhen, HE Yan, LIU Yan, MEUNIER Bernard
    Chinese Journal of Pharmaceuticals. 2023, 54(11): 1578-1585. https://doi.org/10.16522/j.cnki.cjph.2023.11.006
    Tumor is closely related to the copper disorder in human body. In order to discover new copper ion chelating antitumor compounds, five 8-hydroxyquinoline derivatives were synthesized by C-2 aldol condensation, elimination and Michael reaction with 2-methyl-8-hydroxyquinoline as the starting material. The copper ion chelating ability and selectivity were studied by ultraviolet titration. And their cytotoxicity against human melanoma cells(A375 cells and Colo829 cells), human lung cancer cells(A549 cells), human liver cancer cells(HepG2 cells), human cervical cancer cells(HeLa cells) and human immortalized keratinocytes(HaCaT cells) was determined by MTT assay. Finally, two compounds TDMQ51 and TDMQ53 showed higher safety than the positive control fluorouracil(5-FU), while the complexation constants for copper and zinc differed by 13 orders of magnitude. These two compounds could be studied intensively as lead compounds owing to the good inhibitory activity to a wide variety of tumor cells.
  • Pharmaceutical Management & Information
    XU Xiaohong , LI Fei , FU Meng, YUAN Lei , GONG Qing
    Chinese Journal of Pharmaceuticals. 2023, 54(12): 1781-1788. https://doi.org/10.16522/j.cnki.cjph.2023.12.014
    粉体的性质尤其是流动性对固体制剂的开发和制备具有重要意义。认识和掌握物料的粉体学性质,有助于处方筛 选、工艺改进、质量控制、生产等问题的解决。该文通过分析口服固体制剂研发中粉体学性质研究方面的常见问题,并 结合审评中接触到的实际案例,从审评角度提出了口服固体制剂开发中粉体学指标的控制建议,以期为口服固体制剂的 制剂研究和注册申报提供一定的参考。
  • Pharmaceutical Management & Information
    YANG Lan, MA Runyi, WANG Haixue, ZHOU Gang, LIU Yidi, YANG Zhimin
    Chinese Journal of Pharmaceuticals. 2023, 54(09): 1382-1386. https://doi.org/10.16522/j.cnki.cjph.2023.09.015
    ICH《E6(R3) :药物临床试验质量管理规范(GCP)》是涉及人类参与者的临床试验的国际性伦理和科学质量标准。 遵循GCP 开展临床试验将有助于确保试验参与者的权益、安全和健康得到保护,并且确保临床试验结果可靠。GCP 是各 国药品监管部门对药物临床试验监督管理的重要依据。同时,GCP 是ICH 的一级指导原则,充分实施该原则是认定ICH 成员资格的重要条件之一。文章旨在介绍此次修订的背景、修订进展及修订的亮点,有助于我国各界充分了解E6(R3) 原则及附件1 的修订意涵,为后续遵循和实施E6(R3) 奠定基础。
  • Paper
    ZHU Rongyue, LI Yifan, LIU Yanhua, YANG Jiayu
    Chinese Journal of Pharmaceuticals. 2023, 54(07): 1075-1081. https://doi.org/10.16522/j.cnki.cjph.2023.07.013
    Using adipic acid dihydrazide(ADH) as a linkage, the polymer hyaluronic acid(HA)-ADHartesunate( 1) was synthesized. Then, the polymeric micelles of HA-ADH-1 were prepared by ultrasonic dispersion. Their characteristics in vitro and anti-inflammatory effects in vitro and in vivo were investigated. The observation of transmission electron microscopy revealed that the HA-ADH-1 micelles was spherical, and the results of dynamic light scattering showed that the average particle size of HA-ADH-1 micelles was 170.90 nm. The cumulative release at 48 h of 1 from HA-ADH-1 micelles in the physiological environment(pH 7.4) was less than 50%, which was much lower than that of free 1, indicating that HA-ADH-1 micelles had sustained-release property and stable structure. The cytotoxicity and uptake assay results showed that HA-ADH-1 micelles could bind to CD44 receptors highly expressed on the macrophage surface, showing specific targeting to inflammatory macrophages induced by lipopolysaccharide, then enhanced the intracellular accumulation of 1. Therefore, the micelles demonstrated a better killing effect on inflammatory macrophages.
  • Paper
    SHI Hongjuan, OUYANG Xu, WANG Ruiqiang, WANG Zhongyan
    Chinese Journal of Pharmaceuticals. 2023, 54(08): 1216-1223. https://doi.org/10.16522/j.cnki.cjph.2023.08.011
    This study developed the formulation and preparation of azithromycin(1) dry suspension based on the concept of quality by design(QbD). First, 1 and trisodium phosphate were granulated to improve the taste, then 1 particles and sucrose(grinding) were granulated, followed by mixing with the added sucrose. The second-step granulation and mixing process were optimized by Box-Behnken design with granulation time, adding sucrose ratio after granulation, and mixing time as independent variables and content uniformity as the dependent variable. The optimal process was as follows: granule time was 14 min, adding sucrose ratio was 40%, and mixing time was 44 min. Three batches of process validation samples prepared according to the optimized parameters had an average content uniformity of 2.3. And the dissolution behaviors of self-made preparations(T) and reference preparations(R) were similar in media with pH values of 2.0, 4.5, and 6.0. The bioequivalence between T and R was studied through a three-cycle partially repeated crossover design in healthy volunteers. The results showed that under fasting conditions, the cmax of T and R were 114.675 and 114.917 ng/mL, the AUC0→t were 552.41 and 594.87 h·ng·mL–1; under fed conditons, the cmax of T and R were 37.755 and 32.945 ng/mL, the AUC0→t were 276.66 and 257.87 h·ng·mL–1. The statistical analysis results of reference-scaled average bioequivalence(RSABE) or average bioequivalence(ABE) showed that T and R were bioequivalent. The quality and efficacy of the 1 dry suspension prepared in this study were consistent with the reference.