更新于：2024-05-16

Ditiazem Hydrochloride

盐酸地尔硫卓

更新于：2024-05-16

概要

概要

基本信息

简介地尔硫卓是一种钙离子细胞内流抑制剂（慢通道阻滞剂或钙拮抗剂）。尽管其抗心绞痛作用的确切机制仍在研究中，但认为其作用方式如下：该药已被证明是心外膜和心内膜下冠状动脉的有效扩张剂，可抑制自发或由麦角新碱引起的冠状动脉痉挛。用于治疗慢性稳定型心绞痛和冠状动脉痉挛引起的心绞痛。该药于1973年由武田三菱在日本首次推出。

药物类型

小分子化药

别名

Diltiazem Hyudrochloride、Diltiazem hydrochloride (JP17/USP)、Diltizem Hydrochloride

+ [47]

靶点

Cav2.2

作用机制

Cav2.2阻滞剂(N-型电压门控性钙通道α-1B亚基阻滞剂)

治疗领域

神经系统疾病心血管疾病

在研适应症

稳定型心绞痛心绞痛高血压

非在研适应症

心房颤动心房扑动阵发性心动过速+ [1]

原研机构

Mitsubishi Tanabe Pharma Corp.

在研机构

上海信谊万象药业股份有限公司Bausch Health US LLC

AAA Pharmaceutical, Inc.

+ [2]

非在研机构

Exela Pharma Sciences LLC

最高研发阶段批准上市

首次获批日期

日本 (1973-08-08),

心绞痛高血压

最高研发阶段(中国)批准上市

特殊审评-

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结构

分子式C22H26N2O4S

InChIKeyHSUGRBWQSSZJOP-RTWAWAEBSA-N

CAS号42399-41-7

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关联

项与盐酸地尔硫卓相关的临床试验

ChiCTR2200062175 / Completed早期临床1期IIT

A prospective, randomized, double-blind, placebo-controlled multicenter clinical trial of Diltiazem hydrochloride gel for postoperative analgesia of hemorrhoids - Diltiazem hydrochloride project

开始日期2022-08-13

申办/合作机构

浙江萧山医院（杭州市萧山区妇幼保健院、杭州市萧山区托育综合服务中心、杭州市萧山区精神卫生中心）

NCT05950971 / TerminatedN/A

Rhythm Control Versus Rate Control for New Onset Atrial Fibrillation After Non-cardiac Non-thoracic Surgery

Adult patients who are diagnosed new onset atrial fibrillation with rapid ventricular response within 7 days after non-cardiac non-thoracic surgery are enrolled.

开始日期2021-07-01

申办/合作机构

Seoul National University Hospital

NCT04887818 / Unknown status临床2/3期IIT

Assessment of Efficacy and Side Effects of Dlitiazem Ointment With Lidocaine vs. Diltiazem Ointment With Lidocaine for Treatment of Chronic Anal Fissure: Randomized Clinical Trial

Anal fissure is a common anorectal diseases characterized by tear of the anoderm from the dentate line to the anal verge leading to pain and bleeding during and post defecation. It may be a benign disease, but patients suffering from disease report significantly impacted quality of life especially when it becomes chronic. Several treatment modalities have been studied for chronic anal fissure, and topical calcium channel blockers (CCB) showed promising benefit and side effect profile in treatment of chronic anal fissure. Topical Diltiazem and Nifedipine are currently widely used CCBs for chronic anal fissure after multiple studies showing their benefits compared to different agents or modalities. To the investigators' knowledge, there is no study comparing the efficacy of topical Diltiazem and Nifedipine directly. The investigators aim to design a pragmatic randomized clinical trial to compare the efficacy, and side effect profile of topical Nifedipine and Diltiazem in treatment of chronic anal fissure.

开始日期2021-06-01

申办/合作机构

University of Calgary

100 项与盐酸地尔硫卓相关的临床结果

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100 项与盐酸地尔硫卓相关的转化医学

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100 项与盐酸地尔硫卓相关的专利（医药）

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466

项与盐酸地尔硫卓相关的文献（医药）

2024-02-26·Optics Express

Digital inverse patterning solutions for fabrication of high-fidelity microstructures in spatial light modulator (SLM)-based projection lithography

Article

作者: Chen, Jing-Tao ; Zhao, Yuan-Yuan ; Zhu, Jian-Xin ; Duan, Xuan-Ming

Digital mask projection lithography (DMPL) technology is gaining significant attention due to its characteristics of free-mask, flexibility, and low cost. However, when dealing with target layouts featuring sizes smaller than the wavelength scale, accurately producing resist patterns that closely match the target layout using conventional methods to design the modulation coefficients of digital masks produced by spatial light modulators (SLM) becomes challenging. Here, we present digital inversion lithography technology (DILT), which offers what we believe to be a novel approach to reverse engineer the modulation coefficients of digital masks. In the case of binary amplitude modulation, DILT achieves a remarkable reduction in pattern errors (PE), reaching the original 0.26. At the same time, in the case of the gray amplitude modulation, the PE can be reduced to the original 0.05, which greatly improves the high-fidelity transfer of the target layout. This significant improvement enhances the accuracy of target design transfer. By leveraging the capabilities of DILT, DMPL can now attain higher precision and reliability, paving the way for more advanced applications in the field of micro-nano device manufacturing.

2024-01-01·Journal of Pharmaceutical and Biomedical Analysis

Greening microwave-assisted digestion method using hydrogen peroxide for determination of elemental impurities by ICP-OES in antihypertensive active pharmaceutical ingredients

Article

作者: Muller, Edson I ; Queiroz, Jennefer M ; Muller, Aline L H ; Senger, Caroline M ; Mello, Paola A ; Dornelles, Isadora S

Microwave-assisted wet digestion (MAWD) using only H₂O₂ was proposed for oxidizing active pharmaceutical ingredients (APIs) for hypertension treatment and subsequent determination by inductively coupled plasma optical emission spectrometry (ICP-OES). Diltiazem hydrochloride (DIL) presented the most refractory characteristic for oxidation using MAWD-H₂O₂. This proposed MAWD-H₂O₂ method was validated for specificity, accuracy, and precision according to United States Pharmacopeia (USP) Chapter 233 guidelines. Regarding specificity, the most sensitive emission lines were utilized to analyze all elemental impurities in the digests, and no significant spectral interferences were observed. Sample masses of 500 mg for all APIs and a digestion temperature of 250 °C provided digests with residual carbon (RC) below 2400 mg L^-1 of C. Additionally, the residual acidity of the MAWD-H₂O₂ digests was lower than the acidity presented by the HNO₃ digests. The highest and lowest residual carbon content (RCC) for digests were observed for DIL and captopril (CAP), respectively, using MAWD-H₂O₂. When comparing the RCC for MAWD-H₂O₂ and MAWD-HNO₃ digests for APIs containing aromatic rings, it was evident that H₂O₂ offered equivalent conditions for digesting these compounds. Accuracy tests showed recovery values of 91-110% for all elemental impurities, as recommended by USP chapter 233. Validation experiments for precision presented relative standard deviation (RSD) values below 6.4% and 10% under repeatability and intermediate precision conditions, respectively. The limits of quantification (LOQs) provided by MAWD-H₂O₂ are at most half of those recommended by of USP and International Council for Harmonisation of Technical Requirements (ICH). In conclusion, MAWD-H₂O₂ can be considered an alternative method for API digestion, aligning with green analytical chemistry principles, as it does not employ toxic reagents, minimizes waste, and the main products of H₂O₂ oxidation are water and oxygen. Considering the analytical Eco-Scale, the MAWD-H₂O₂ method scored 81, classifying it as an excellent green analysis.

2024-01-01·Chemical and Pharmaceutical Bulletin

Exploring the Effectiveness of Carboxymethylated and Crosslinked <i>Albizia Procera</i> Gum in Diltiazem Hydrochloride Matrix Tablets: A Comparative Analysis

Article

作者: Khanam, Jasmina ; Mukherjee, Sudipta

This study investigates the efficacy of modified Albizia procera gum as a release-retardant polymer in Diltiazem hydrochloride (DIL) matrix tablets. Carboxymethylated Albizia procera gum (CAP) and ionically crosslinked carboxymethylated Albizia procera gum (Ca-CAP) were utilized, with Ca-CAP synthesized via crosslinking CAP with calcium ions (Ca²⁺) using calcium chloride (CaCl₂). Fourier Transform (FT) IR analysis affirmed polymer compatibility, while differential scanning calorimetry (DSC) and X-ray diffraction (XRD) assessed thermal behavior and crystallinity, respectively. Zeta potential analysis explored surface charge and electrostatic interactions, while rheology examined flow and viscoelastic properties. Swelling and erosion kinetics provided insights into water penetration and stability. CAP's carboxymethyl groups (-CH2-COO^-) heightened divalent cation reactivity, and crosslinking with CaCl₂ produced Ca-CAP through -CH2-COO^- and Ca²⁺ interactions. Structural similarities between the polymers were revealed by FTIR, with slight differences. DSC indicated modified thermal behavior in Ca-CAP, while Zeta potential analysis showcased negative charges, with Ca-CAP exhibiting lower negativity. XRD highlighted increased crystallinity in Ca-CAP due to calcium crosslinking. Minimal impact on RBC properties was observed with both polymers compared to the positive control as water for injection (WFI). Ca-CAP exhibited improved viscosity, strength, controlled swelling, and erosion, allowing prolonged drug release compared to CAP. Stability studies confirmed consistent six-month drug release, emphasizing Ca-CAP's potential as a stable, sustained drug delivery system over CAP. Robustness and accelerated stability tests supported these findings, underscoring the promise of Ca-CAP in controlled drug release applications.

项与盐酸地尔硫卓相关的新闻（医药）

2024-05-13

·Pharma CMC

底价1.2亿！中外合资药企股权公开挂牌转让

5月10日，天津力生制药股份有限公司发布公告，基于公司整体规划，综合考量天津田边制药有限公司（田边制药）的生产经营现状及其现有产品品种所面临的激烈市场竞争，为进一步优化资源配置，结合资产评估结果及市场情况，拟按照不低于 12,029.20 万元的底价公开挂牌转让所持 24.65%股权。田边制药属于中外合资，其中，日本田边三菱制药株式会社拥有75.35%的股权，天津力生制药股份有限公司拥有24.65%的股权。田边制药经营范围包括：生产、加工、销售中西药、化学药品、原料药、试药、生物制剂及相关服务;提供医药信息咨询，公司产品有：马来酸曲美布汀片、盐酸地尔硫䓬缓释胶囊(Ⅱ)、盐酸地尔硫䓬片、盐酸咪达普利片等。田边制药2023年营收3.82亿元，净利润4354.81万元；2024年一季度营收9310.41万元，近利润1513.66万元。根据评估，田边制药净资产账面价值为18,689.64万元，股东全部权益评估价值为48,599.55万元，增值额为29,909.92万元，增值率为160.03%。综合考虑资产评估结果及市场情况，力生制药将所持有的田边制药24.65%股权以不低于 12,029.20万元的价格在天津产权交易中心公开挂牌征集意向受让方。

财报IPO

2024-05-10

·梅斯医学

一文读懂！当心绞痛遇上高血压，「地尔硫卓」该怎么用？

地尔硫卓（Diltiazem），又名硫氮䓬酮或哈氮䓬，是一种钙离子拮抗剂（非二氢吡啶类CCB），可通过抑制钙内流，从而减弱房室结传导和延长房室结有效不应期。地尔硫卓能降低血压和心率，控制室上性心律失常，减少心肌耗氧量，减少氧自由基生成及降低血小板聚集功能。同作为钙离子通道阻滞剂，地尔硫卓与“地平”（二氢吡啶类CCB）的区别在于，地平对于脉血管平滑肌的作用更强，而地尔硫卓对对心脏的作用更有优势，在降压的过程中不会引起心动过速。因此，地尔硫卓主要用于心绞痛的预防，降低高血压，也能用于心房颤动、心房扑动和减少心动过速。图1地尔硫卓的药理作用临床上，高血压合并心绞痛的病例并不少见。高血压合并冠心病患者的用药原则是在生活方式干预的基础上，既要控制血压以减少心脏负担，又要扩张冠状动脉以改善心肌血液供应，即“降压又护心”。地尔硫卓有松弛血管平滑肌、扩张血管的药理特点，因此临床上经常将地尔硫卓用于高血压合并心绞痛的患者的治疗。图2 2017 年《美国成人高血压预防、检测、评估和管理指南》降压目标值那么，问题来了！当高血压“遇上”心绞痛，地尔硫卓该如何用呢？又有哪些禁忌呢？继续往下看~01当高血压“遇上”心绞痛，地尔硫卓如何用？1高血压+慢性稳定型心绞痛一般选择β受体阻滞剂和血管紧张素转化酶抑制剂（ACEI）/血管紧张素Ⅱ受体拮抗剂（ARB）作为一线治疗药物，但在β受体阻滞剂存在禁忌证或产生不耐受的不良反应时，无左心室功能障碍时可以考虑使用地尔硫卓。如心绞痛或高血压难以控制，在ACEI、β受体阻滞剂和噻嗪类利尿剂基础上可加用地尔硫卓。2高血压+不稳定性心绞痛首选β受体阻滞剂，并在发病24 小时内口服应用。如果β受体阻滞剂存在禁忌证或产生不耐受的不良反应，无左心室功能障碍时可以考虑使用地尔硫卓。如单用β受体阻滞剂未能控制心绞痛或高血压且已应用 ACEI 时也可以加用地尔硫卓。3高血压+变异性心绞痛地尔硫卓是首选的治疗药物，适用于心率偏快且心功能良好的患者。02联用用药注意事项1. 地尔硫卓+β-受体阻滞药地尔硫卓可增强β-受体阻滞药的作用，对心功能正常的个体有益。但也可能导致低血压、左心衰竭及房室传导阻滞。老年、左心功能不全、主动脉狭窄患者尤其容易出现。本药还可增加经肝酶代谢的 β-受体阻滞药的血浆浓度约 30%～40%。如果合用，应仔细监测患者的心功能，调整用药剂量。地尔硫卓应避免与β-受体阻滞药同时静脉给药。静脉给予本药后至少应间隔数小时以上方可使用 β-受体阻滞药注射剂。2.地尔硫卓+二氢吡啶类CCB地尔硫卓可阻碍二氢吡啶类CCB如硝苯地平的代谢酶，使二氢吡啶类钙通道阻滞药的血药浓度上升。因此同时使用时应观察临床症状，减少用量或停药。03地尔硫卓的服用剂量应个体化：一天分数次口服时，可在餐前或临睡时服，剂量每1～2天逐渐增加，直到获得适合的效应。停药时应逐渐减量，不能突然停药，以免出现高血压反跳或心绞痛。高龄患者用药时应从低剂量开始。缓释胶囊应整个吞服，不要分开、咀嚼或粉碎。注射剂在临用前溶解于 5ml 注射用水，溶解后呈无色澄明液体。如与其他药剂混合后pH越过8，可能析出结晶。04地尔硫卓的用药禁忌1. 对地尔硫卓或其他钙通道阻滞药过敏2. 病窦综合征、Ⅱ度或Ⅲ度房室传导阻滞引起心动过缓并缺乏有效的人工心脏起搏3. 严重低血压或心源性休克4. 急性心肌梗死伴肺充血5. 存在房室旁道（如WPW综合征、LGL综合征）或短PR综合征的心房颤动或心6. 房扑动时禁止静脉给药7. 室性心动过速禁止静脉给药8. 新生儿禁用含苯甲醇的注射剂9. 孕妇禁用注射剂参考文献：[1]曹博策,李丽,李刚.二氢吡啶和非二氢吡啶类钙拮抗剂在冠状动脉性心脏病合并高血压中的应用[J].中华高血压杂志,2018,26(04):301-303.DOI:10.16439/j.cnki.1673-7245.2018.04.001.[2]高血压合理用药指南(第2版)[J].中国医学前沿杂志(电子版),2017,9(07):28-126.[3]冠心病合理用药指南(第2版)[J].中国医学前沿杂志(电子版),2018,10(06):1-130.[4]孙宁玲,霍勇,葛均波,陈鲁原,冯颖青,杨艳敏,严晓伟,廖玉华,顾晔,荆珊.非二氢吡啶类钙拮抗剂在心血管疾病中应用的专家建议[J].中华高血压杂志,2015,23(03):220-226.编辑：Potato救命常识：一文盘点“急性心梗”紧急状况下的生存指南，从识别到处理，太全了！医生指出：近25万人研究发现——吃够这6种食物的人，心血管更健康、更长寿「恩格列净」每片仅需1.8元，为何更多人选择价高的「达格列净」？区别大吗？降压药新星「沙库巴曲缬沙坦」，6大使用要点一文拿下！

临床结果

2024-05-06

·Pharmaceutical Technology

Cipla and Glenmark initiate recall of certain products in the US

Ipratropium Bromide and Albuterol Sulfate Inhalation Solution is prescribed for controlling the symptoms of lung diseases. Credit: mi_viri / Shutterstock.com. Cipla and Glenmark Pharmaceuticals are recalling specific products from the US market due to distinct manufacturing issues, the latest Enforcement Report issued by the US Food and Drug Administration (USFDA) noted. The recalls involve inhalation solutions and extended-release capsules used for treating respiratory conditions and high blood pressure, respectively. New Jersey-based subsidiary of Cipla, Cipla USA is recalling 59,244 packs of Ipratropium Bromide and Albuterol Sulfate Inhalation Solution. This product is manufactured at Indore SEZ plant of the company in India. It is prescribed for controlling the symptoms of lung diseases such as chronic bronchitis, asthma, and emphysema. See Also: Pacira BioSciences gets grant for method for treating spasticity in a patient’s limb using cryogenic cooling Axsome Therapeutics gets grant for treating narcolepsy with cataplexy using reboxetine The recall of the affected inhalation solution lot is claimed to be due to complaints of “short fill”. The US regulator detailed that the affected lot was recalled after reports of less fill volume in respules and the presence of a few drops of liquid in the intact pouch. Simultaneously, Glenmark Pharmaceuticals, USA, the US-based arm of Glenmark, announced the recall of 3,264 Diltiazem Hydrochloride extended-release capsules bottles. The medication, intended for high blood pressure treatment, was recalled due to “failed dissolution specifications”. In a related event last month, Glenmark’s US unit recalled 6,528 bottles of Diltiazem Hydrochloride extended-release capsules. This Class II recall was due to the medication not meeting dissolution specifications, with “Out of Specification (OOS) results in a dissolution test at the 12-month time point during a long-term stability study.” The affected lot was also produced in India.

上市批准

100 项与盐酸地尔硫卓相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D00616	-	C05AE03 C08DB01	DB00343

研发状态

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
稳定型心绞痛	美国	Bausch Health US LLC	1982-11-05
心绞痛	日本	Mitsubishi Tanabe Pharma Corp.	1973-08-08
高血压	日本	Mitsubishi Tanabe Pharma Corp.	1973-08-08

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT01422382 (CTgov)	临床4期	-	28	Diltiazem (Cardizem LA) 240 mg QD+Pitavastatin (NK-104)	鑰遞蓋壓壓鏇糧淵鹽遞(齋鏇艱衊衊鏇獵夢製艱) = 範蓋襯鹹鹹鑰艱鑰鏇製糧鑰繭網齋範餘廠鏇繭 (襯網憲範齋夢醖壓餘壓, 顧獵積蓋襯顧鬱簾襯憲 ~ 簾觸齋願繭遞願鬱築選) 更多	-	2012-04-12
NCT01151345 (CTgov)	临床1期	-	26	Tilazem (Tilazem 60 mg)	(範艱觸繭蓋構觸範鏇顧) = 鏇獵醖觸餘糧餘製鹹艱構襯襯獵積積繭衊鏇醖 (齋餘獵選憲製壓選壓鹹, 網糧遞觸夢構獵簾蓋鑰 ~ 餘鑰鑰夢襯淵衊鹹繭蓋) 更多	-	2011-08-22
				Angiotrofin (Angiotrofin 60 mg)	(範艱觸繭蓋構觸範鏇顧) = 鑰夢蓋顧網築鹹鏇築鬱構襯襯獵積積繭衊鏇醖 (齋餘獵選憲製壓選壓鹹, 遞鏇糧鏇壓窪觸窪製鑰 ~ 蓋獵夢構廠壓選遞鬱衊) 更多
NCT01217515 (CTgov)	临床3期	肛裂	465	Diltiazem hydrochloride 2% cream (Diltiazem Hydrochloride 2% Cream)	膚願繭築窪願築壓鏇獵(憲鏇憲醖淵夢獵醖襯鹽) = 積鑰繭壓憲醖鑰遞艱鑰衊夢壓鏇壓鏇繭積艱鹽 (憲齋艱夢壓艱製襯製遞, 憲糧選蓋蓋糧鏇壓獵築 ~ 憲鹹夢廠夢廠衊獵廠觸) 更多	-	2014-07-01
				Diltiazem hydrochloride 4% cream (Diltiazem Hydrochloride 4% Cream)	膚願繭築窪願築壓鏇獵(憲鏇憲醖淵夢獵醖襯鹽) = 範繭膚齋鹹簾壓壓糧鹹衊夢壓鏇壓鏇繭積艱鹽 (憲齋艱夢壓艱製襯製遞, 範構築蓋鹹襯餘廠鹹網 ~ 積築襯遞壓簾夢顧築簾) 更多
USON 01062 (ASCO2011)	临床3期	早期乳腺癌辅助	-	AC → T	(範齋鑰獵膚襯願鬱鏇窪): HR = 0.8 (95% CI, 0.63 ~ 1.02) 更多	-	2011-05-20
				AC → XT