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• 2017 Volume 48 Issue 03
  Published: 10 March 2017

    

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  Preparation and Structural Confirmation of the Related Substances of Vonoprazan Fumarate

  YU Qianying1,2, LIU Yu1,2*, YAO Kai1,2, LI Jianqi1,2

  2017, 48(03): 372. https://doi.org/10.16522/j.cnki.cjph.2017.03.008

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  To perform the quality control of vonoprazan fumarate, according to the structural characteristics and synthetic process, seven related substances including: di[2-[2-(2-fluorophenyl)-2-oxoethyl]]propanedinitrile, 2-amino-5-(2-fluorophenyl)furan-3-carbonitrile, 5-(2-fluorophenyl)-1H-pyrrole-3-carboxylic acid, [5-(2-fluorophenyl)-1-(3-pyridinylsulfonyl)-1H-pyrrole-3-yl]methanol, N,N-di[[5-(2-fluorophenyl)-1-(3-pyridinylsulfonyl)-1H-pyrrole-3-yl]methyl]methanamine fumarate, [5-(2-fluorophenyl)-N-methyl-1H-pyrrole-3-yl]methanamine fumarate and N,Ndi[[5-(2-fluorophenyl)-1H-pyrrole-3-yl]methyl]methanamine fumarate, were synthesized and their structures were confirmed by 1H NMR and MS.
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  Synthesis of the Related Substances of Tofacitinib Citrate

  LIU Shuai, TANG Chao, SUI Qiang, WU Maocheng, ZHONG Jingfen

  2017, 48(03): 382. https://doi.org/10.16522/j.cnki.cjph.2017.03.010

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  To perform the quality control of tofacitinib citrate, six related substances were prepared and confirmed by 1H NMR and MS. These substances were 4-(4-chloro-pyrrolo[2,3-d]pyrimidin-7-yl)-7H-pyrrolo[2,3-d]pyrimidine, N-methyl-N-[(3R,4R)-1-benzyl-4-methylpiperidin-3-yl]-7-methyl-pyrrolo[2,3-d]pyrimidin-4-amine, 3-[(3R,4R)-4-methyl-3-[N-methyl-(7H-pyrrolo[2,3-d]-4,5-dihydropyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile, 3-[(3R,4R)-4-methyl-3-[N-methyl-(7-methyl-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile, N-methyl-N-[(3R,4R)-1,4-dimethylpiperidin-3-yl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine and N-methyl-N-[(3R,4R)-1,4-dimethylpiperidin-3-yl]-7-methyl-pyrrolo[2,3-d]pyrimidin-4-amine.
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  Investigation of Microemulsion Foam System for Transdermal Delivery of Betamethasone Dipropionate

  ZHANG Furong, WU Yubo, LUO Huafei*, BIAN Qiong, WANG Hao

  2017, 48(03): 393. https://doi.org/10.16522/j.cnki.cjph.2017.03.012

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  To evaluate the transdermal behavior of betamethasone dipropionate from the microemulsion foam for transdermal delivery, the release medium and species of excised skin were screened and a methodology validation of high performance liquid chromotogrophy (HPLC) for determination was completed. The results showed that isopropanol∶pH 5.0 phosphate buffer (20∶80) was the suitable release medium and excised pig skin was selected as the percutaneous model. The established HPLC method was specific, repeateable and accurate, which could meet the requirements of drug determination in in vitro transdermal test. According to the pseudo-ternary phase diagrams and the results of in vitro transdermal test, medium chain triglyceride (MCT) was preliminarily confirmed as the suitable oil phase of microemulsion foam.
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  Preparation and Evaluation of Macitentan Tablets

  SUN Yinyin1,2, DONG Kunhua1, WANG Tiechuang1, NI Feng1, LI Jianqi1*

  2017, 48(03): 400. https://doi.org/10.16522/j.cnki.cjph.2017.03.013

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  The formulation of macitentan tablets was optimized by single factor test and orthogonal design with the similarity between the dissolution curves of the self-made tablets and the reference listed drug (Opsumit) in pH 6.8 phosphate buffer containing 0.1％ cetyltrimethyl ammonium bromide as the main index, and the qualities of tablets, such as flowability of particles and disintegration time, as the auxiliary indexes. The optimal formulation of core tablets were as follows: the active pharmaceutical ingredient (API) should be pretreated by passing through 200-mesh sieve and its amount was 30 g; the amounts of lactose monohydrate and povidone K30 were 117 and 6.6 g; microcrystalline cellulose and sodium carboxymethyl starch were added partly prior to wet granulation (11.7 and 4.2 g) and partly after size  stabilization process (35.1 and 4.2 g); the adhesive was 0.2％ Tween-80 solution. After a thin-layer coating, three batches of self-made tablets were obtained. The similarities of dissolution curves between the self-made tablets and Opsumit in pH 1.0 hydrochloric acid, pH 4.5 acetate buffer, pH 6.8 phosphate buffer and water were evaluated, and the calculated similarity factor (f2) values were all above 65. The results of stress test showed that the product was rather stable.
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  Preparation and in vitro/in vivo Evaluation of Risperidone Orodispersible Films

  ZHANG Hua1, WANG Donghai2, WANG Bing1, YANG Qingmin2, CHEN Fang1*

  2017, 48(03): 406. https://doi.org/10.16522/j.cnki.cjph.2017.03.014

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  The dissolution profiles of the risperidone orodispersible films in foreign market and orally disintegrating tablets in domestic market in different media were investigated, and water was considered as discriminative according to the results of above tests. Then the formulation of risperidone orodispersible films was optimized with the dissolution profiles in water, together with the disintegration time and the mechanical properties as the evaluation parameters. The results showed that the dissolution of risperidone from the self-made orodispersible films was above 80％within 1 min in four dissolution media with different pH values and risperidone was completely dissolved within 2 min. The dissolution behaviors of the self-made risperidone orodispersible films were similar to those of the marketed orodispersible films. The results of differential scanning calorimetry (DSC) and X-ray diffraction (XRD) demonstrated that risperidone existed in an amorphous state in the carriers. The results of pharmacokinetics in Beagle dogs indicated that the self-made and the marketed orodispersible films exhibited similar pharmacokinetic characteristics. The relative bioavailabilities of self-made films were (109.1±9.5)％ based on risperidone and (102.0±17.3)％ based on 9-hydroxyrisperidone, the active metabolite.
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  Determination of Related Substances in Dabigatran Etexilate Methanesulfonate Bulk Drug by UPLC

  CHANG Xiaohui1, WANG Hubo1, XIE Hua2, WANG Weijia2, JIANG Huijuan1*

  2017, 48(03): 422. https://doi.org/10.16522/j.cnki.cjph.2017.03.016

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  A UPLC method was established for the determination of the related substances in dabigatran etexilate methanesulfonate bulk drug. A C18 column was used, with the mobile phase of 10 mmol/L ammonium acetate solution (adjusted to pH 5.0 with acetic acid)∶acetonitrile for gradient elution, at the detection wavelength of 280 and 310 nm. The calibration curves of dabigatran etexilate methanesulfonate and its six related substances were linear in the ranges of 0.40—30 μg/ml. The recoveries of the related substances were 94.7％—102.5％, with RSDs of 0.56％—2.74％.
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  Progress in Global Pharmaceutical R&D in September to December 2016

  LIU Lingling, WANG Ying, WU Linping, GUO Linlin

  2017, 48(03): 453. https://doi.org/10.16522/j.cnki.cjph.2017.03.021

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