Chemical & pharmaceutical bulletin最新文献_第10页

Comparison of Phosphate and Bicarbonate Buffer Solutions as Dissolution Test Media for Predicting Bioequivalence of Febuxostat Formulation. 比较磷酸盐缓冲溶液和碳酸氢盐缓冲溶液作为预测非布索坦制剂生物等效性的溶出试验介质

IF 1.5 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2024-01-01 DOI: 10.1248/cpb.c24-00526

Masaki Higashino, Kiyohiko Sugano

{"title":"Comparison of Phosphate and Bicarbonate Buffer Solutions as Dissolution Test Media for Predicting Bioequivalence of Febuxostat Formulation.","authors":"Masaki Higashino, Kiyohiko Sugano","doi":"10.1248/cpb.c24-00526","DOIUrl":"https://doi.org/10.1248/cpb.c24-00526","url":null,"abstract":"The purpose of the present study was to compare phosphate buffer (PPB) and bicarbonate buffer (BCB) solutions as dissolution test media for predicting the bioequivalence (BE) of an immediate-release (IR) formulation. Febuxostat was used as a model of free acid drugs. One reference formulation (RF) and three test formulations (TF) were employed in this study. The clinical BE studies involved 18 to 24 healthy adult volunteers. Each formulation was orally administered in the fasted state. The compendial paddle apparatus was used for the dissolution tests (500 mL, 37 °C, 25 or 50 rpm). BCB (10 mM, pH 6.8, 140 mM NaCl) and PPB (2.5 to 25 mM, pH 6.8, 140 mM NaCl) were used as dissolution media. The pH value of BCB was maintained by the floating lid method. In the clinical BE studies, two TFs were BE to RF, whereas one TF was non-BE. At a paddle speed of 50 rpm, RF and TFs showed little or no difference in the dissolution profiles in all buffer solutions. At 25 rpm, the dissolution profiles in 2.5 mM PPB and 10 mM BCB were consistent with the clinical BE results. The in vitro-in vivo correlation between Cmax ratio and dissolved% ratio at each time point was highest for 10 mM BCB at 25 rpm. These results suggest that the use of BCB increases the BE predictability of dissolution tests.","PeriodicalId":9773,"journal":{"name":"Chemical & pharmaceutical bulletin","volume":"72 11","pages":"989-995"},"PeriodicalIF":1.5,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142680905","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Visualization of the Plasmid DNA Delivery System by Complementary Fluorescence Labeling of Arginine-Rich Peptides. 通过对富精氨酸肽进行互补荧光标记实现质粒 DNA 运送系统的可视化。

IF 1.5 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2024-01-01 DOI: 10.1248/cpb.c24-00479

Ayumi Imayoshi, Hidetomo Yokoo, Masashi Kawaguchi, Kazunori Tsubaki, Makoto Oba

{"title":"Visualization of the Plasmid DNA Delivery System by Complementary Fluorescence Labeling of Arginine-Rich Peptides.","authors":"Ayumi Imayoshi, Hidetomo Yokoo, Masashi Kawaguchi, Kazunori Tsubaki, Makoto Oba","doi":"10.1248/cpb.c24-00479","DOIUrl":"https://doi.org/10.1248/cpb.c24-00479","url":null,"abstract":"Cell-penetrating peptides, such as arginine-rich peptides, encapsulate nucleic acid drugs and deliver them to intracellular compartments. Comprehensive tracking of drug delivery systems (DDSs) provides information about the behavior of the drug as well as the fate of the drug carrier after drug release, which is crucial for minimizing side effects. In this study, we labeled peptides designed to carry plasmid DNA with two types of dyes, traditional dye fluorescein and aggregation-induced emission (AIE) dye tetraphenylethylene, and subsequently tracked the DDS through the complementary ON and OFF fluorescence behaviors of the dyes. Traditional fluorescent dyes are susceptible to aggregation-caused quenching during bioimaging, a problem that is mitigated by using AIE dyes. However, by using both of these contrasting fluorescent labels, we were able to clearly visualize the DDS at different stages of its deployment, from drug transport and delivery to carrier dissociation and migration, demonstrating the feasibility of accurate DDS visualization by complementary fluorescence labeling.","PeriodicalId":9773,"journal":{"name":"Chemical & pharmaceutical bulletin","volume":"72 10","pages":"856-861"},"PeriodicalIF":1.5,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142380120","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Discovery and Structural Analysis of Metabolites of Vitamin D₃ Lactones. 维生素 D3 内酯代谢物的发现与结构分析。

IF 1.5 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2024-01-01 DOI: 10.1248/cpb.c24-00495

Kazuto Iijima, Ryota Sakamoto, Rino Tsutsumi, Naoto Nakaya, Takatsugu Hirokawa, Minami Odagi, Toshiyuki Sakaki, Kaori Yasuda, Kazuo Nagasawa

{"title":"Discovery and Structural Analysis of Metabolites of Vitamin D3 Lactones.","authors":"Kazuto Iijima, Ryota Sakamoto, Rino Tsutsumi, Naoto Nakaya, Takatsugu Hirokawa, Minami Odagi, Toshiyuki Sakaki, Kaori Yasuda, Kazuo Nagasawa","doi":"10.1248/cpb.c24-00495","DOIUrl":"10.1248/cpb.c24-00495","url":null,"abstract":"25-Hydroxyvitamin D3-23,26-lactone (1) and 1α,25-dihydroxyvitamin D3-23,26-lactone (2) have long been considered as among the end metabolites of vitamin D3. Recently, however, we found that these lactones exhibit biological activity related to the β-oxidation of fatty acids. We hypothesized that a metabolic pathway might exist to inactivate their physiological activity. Here, by means of metabolic experiments with a variety of cytochrome P450 (CYP) enzymes, we show that CYP3A4 metabolizes the lactones. The metabolites were presumed to be hydroxylated at C4 based on the previous reports showing that metabolism of 25-hydroxyvitamin D3 by CYP3A4 along with the current LC-MS analysis. To confirm this, we chemically synthesized 4α,25(OH)2D3-23,26-lactone (3), 4β,25(OH)2D3-23,26-lactone (4), 1α,4α,25(OH)3D3-23,26-lactone (5), and 1α,4β,25(OH)3D3-23,26-lactone (6). HPLC analysis using these authentic compounds as standards revealed that 1 was metabolized to 3 and 4, while 2 was metabolized exclusively to 6 by CYP3A4. Docking studies suggest that the hydroxyl group at C1 in 2 forms hydrogen bonds with Ser119 and Arg212 of CYP3A4, contributing to the fixation of C4β on heme iron in the CYP, thereby resulting in stereoselective hydroxylation at C4.","PeriodicalId":9773,"journal":{"name":"Chemical & pharmaceutical bulletin","volume":"72 10","pages":"899-908"},"PeriodicalIF":1.5,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142459116","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

In Vitro Study on Combined Effect of Drugs for Hyperphosphatemia on Phosphorus Adsorption Capacity. 治疗高磷血症的药物对磷吸附能力的联合影响体外研究

IF 1.5 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2024-01-01 DOI: 10.1248/cpb.c24-00434

Kaito Yamashiro, Kazuma Kimata, Fumihiko Ogata, Naohito Kawasaki

{"title":"In Vitro Study on Combined Effect of Drugs for Hyperphosphatemia on Phosphorus Adsorption Capacity.","authors":"Kaito Yamashiro, Kazuma Kimata, Fumihiko Ogata, Naohito Kawasaki","doi":"10.1248/cpb.c24-00434","DOIUrl":"https://doi.org/10.1248/cpb.c24-00434","url":null,"abstract":"Phosphorus binders are often used in combination to produce synergistic effects. However, the synergistic effect may be affected by the change in pH or concomitant drugs. Nonetheless, the data on the adsorption capacities of these binders when used in combination with other binders are limited. In this study, we evaluated the adsorption capacity of phosphorus binders when used in combination. Precipitated calcium carbonate (CC), ferric citrate hydrate (FC), lanthanum carbonate hydrate (LC), and sucroferric oxyhydroxide (SO) were used as phosphorus binders. SO showed high adsorption capacity in the 1st and 2nd fluid, and the adsorption capacity of SO in combination with other binders was stable. In contrast, the adsorption capacities of CC + FC and FC + LC decreased in the 1st and 2nd fluid compared with that when used alone because of the release of citrate ions that chelate calcium or lanthanum ions. These results suggest that SO is less affected by interactions with other phosphorus binders and changes in pH and may be suitable for patients receiving concomitant drugs.","PeriodicalId":9773,"journal":{"name":"Chemical & pharmaceutical bulletin","volume":"72 10","pages":"932-935"},"PeriodicalIF":1.5,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142543939","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Substitution Effects of Alkene Dipeptide Isosteres on Adjacent Peptide Bond Rotation. 烯二肽异构体对相邻肽键旋转的取代效应。

IF 1.5 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2024-01-01 DOI: 10.1248/cpb.c24-00254

Chihiro Iio, Kohei Sato, Nobuyuki Mase, Tetsuo Narumi

引用次数: 0

Systematic DOE Approach for Dry Granulation Study at Early Clinical Stage of Novel Drugs: An Industrial Case. 新型药物早期临床阶段干法制粒研究的系统 DOE 方法：一个工业案例

IF 1.5 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2024-01-01 DOI: 10.1248/cpb.c23-00801

Weiqi Chen, Xiaolei Wang, Hengli Yuan, Qixuan Guan, Chun Wang, Zhiying Dong, Shicheng Zhang, Jianping Yao, Jinyang Shen

{"title":"Systematic DOE Approach for Dry Granulation Study at Early Clinical Stage of Novel Drugs: An Industrial Case.","authors":"Weiqi Chen, Xiaolei Wang, Hengli Yuan, Qixuan Guan, Chun Wang, Zhiying Dong, Shicheng Zhang, Jianping Yao, Jinyang Shen","doi":"10.1248/cpb.c23-00801","DOIUrl":"https://doi.org/10.1248/cpb.c23-00801","url":null,"abstract":"In order to introduce a cost-effective strategy method for commercial scale dry granulation at the early clinical stage of drug product development, we developed dry granulation process using formulation without API, fitted and optimized the process parameters adopted Design of Experiment (DOE). Then, the process parameters were confirmed using one formulation containing active pharmaceutical ingredient (API). The results showed that the roller pressure had significant effect on particle ratio (retained up to #60 mesh screen), bulk density and tapped density. The roller gap had significant influence on particle ratio and specific energy. The particle ratio was significantly affected by the mill speed (second level). The tabletability of the powder decreased after dry granulation. The effect of magnesium stearate on the tabletability was significant. In the process validation study, the properties of the prepared granules met the requirements for each response studied in the DOE. The prepared tablets showed higher tensile strength, good content uniformity of filled capsules, and the dissolution profiles of which were consistent with that of clinical products. This drug product process development and research strategies could be used as a preliminary experiment for the dry granulation process in the early clinical stage.","PeriodicalId":9773,"journal":{"name":"Chemical & pharmaceutical bulletin","volume":"72 6","pages":"584-595"},"PeriodicalIF":1.5,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141466470","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Preparation of Amorphous Probucol with Fluvastatin Sodium Salt and Stability Comparison Studies of Co-amorphous Probucol with Fluvastatin Sodium Salt and Atorvastatin Calcium Trihydrate Salt.

IF 1.5 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2024-01-01 DOI: 10.1248/cpb.c24-00540

Shinji Oyama, Noriko Ogawa, Toshiya Yasunaga, Hiromitsu Yamamoto

{"title":"Preparation of Amorphous Probucol with Fluvastatin Sodium Salt and Stability Comparison Studies of Co-amorphous Probucol with Fluvastatin Sodium Salt and Atorvastatin Calcium Trihydrate Salt.","authors":"Shinji Oyama, Noriko Ogawa, Toshiya Yasunaga, Hiromitsu Yamamoto","doi":"10.1248/cpb.c24-00540","DOIUrl":"10.1248/cpb.c24-00540","url":null,"abstract":"A co-amorphous state composed of probucol (PC) and fluvastatin sodium salt (FLU) was prepared by spray-drying (SD). We have previously reported that PC and atorvastatin calcium trihydrate salt (ATO) formed a co-amorphous state when prepared by a SD method and that the solubility of PC and the amorphous stability were improved by the preparation of the co-amorphous state. In the present study, the physicochemical properties, including the amorphous stability of the prepared co-amorphous state, were characterized. Powder X-ray diffraction measurement results suggested that PC and FLU formed a co-amorphous state and that a higher percentage of PC was dissolved from the PC-FLU co-amorphous state than from the PC-ATO co-amorphous state. The results are attributed to FLU exhibiting greater solubility and wettability than ATO, which is supported by the results of solubility tests and contact-angle measurements. The stability of the amorphous state of PC is higher in the co-amorphous state with ATO than in that with FLU. This difference is attributed to differences in the molecular interaction modes between PC-FLU and PC-ATO. Therefore, the selection of high-wettability molecules as a co-former for the co-amorphous state enhances its water solubility. The present study also indicates that molecular interactions enhance the stability of the co-amorphous state.","PeriodicalId":9773,"journal":{"name":"Chemical & pharmaceutical bulletin","volume":"72 12","pages":"1073-1083"},"PeriodicalIF":1.5,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142876312","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Synthetic Studies of Javaberine A Based on Intramolecular Hydroamination of Alkenes.

IF 1.5 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2024-01-01 DOI: 10.1248/cpb.c24-00693

Yasutomo Yamamoto, Hiromi Baba, Miki Toriyama, Kiyoshi Tomioka

引用次数: 0

18-Nor-Kaurane Type Diterpenoids from the Fruits of Atemoya.

IF 1.5 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2024-01-01 DOI: 10.1248/cpb.c24-00593

Hiroyuki Miyashita, Hitoshi Yoshimitsu

引用次数: 0

Evaluating a Retro-Inverso Type Inhibitor of HTLV-1 Protease as a Competitive Inhibitor. 评估作为竞争性抑制剂的 HTLV-1 蛋白酶逆转录抑制剂。