[Translation] A randomized, open-label, single-dose, two-drug, self-crossover controlled study to evaluate the bioequivalence of tulobuterol patch in Chinese healthy subjects in the fasting state

主要目的：以海南盈达润泽药业有限公司提供的妥洛特罗贴剂为受试制剂，按生物等效性试验的有关规定，与ヴィアトリス製薬株式会社持证的妥洛特罗贴剂（商品名：Hokunalin®，参比制剂）对比在健康人体内的吸收速度及吸收程度，考察两制剂的人体生物等效性。

[Translation]

Main purpose: Taking the tuloterol patch provided by Hainan Yingda Runze Pharmaceutical Co., Ltd. as the test preparation, according to the relevant provisions of the bioequivalence test, it will be compared with the certified tuloterol patch produced by Biotech Co., Ltd. (Trade name: Hokunalin®, reference preparation) Compare the absorption speed and degree of absorption in healthy humans to examine the human bioequivalence of the two preparations.

Start Date01 Nov 2024

Sponsor / Collaborator

Hainan Yingda Runze Pharmaceutical Co., Ltd.

CTR20241848 / CompletedNot Applicable

妥洛特罗贴剂在健康受试者空腹状态下的随机、开放、单剂量、两制剂、两序列、两周期、交叉生物等效性试验

[Translation] A randomized, open-label, single-dose, two-formulation, two-sequence, two-period, crossover bioequivalence study of tulobuterol patch in healthy subjects under fasting condition

主要目的：比较空腹单次给药条件下，北京泰德制药股份有限公司提供的妥洛特罗贴剂（规格：0.5mg/贴，受试制剂）与日东电工株式会社持证生产的妥洛特罗贴剂（商品名：阿米迪®，规格：0.5mg/贴，参比制剂）在健康受试者中吸收程度和速度的差异。通过主要药代动力学参数，评价两者是否生物等效，为受试制剂的注册申请提供依据。次要目的：考察受试制剂和参比制剂在健康成人受试者体内的安全性、皮肤粘贴牢固度和皮肤刺激性。

[Translation]

Primary objective: To compare the differences in absorption degree and speed of the tulobuterol patch (specification: 0.5 mg/patch, test preparation) provided by Beijing Taide Pharmaceutical Co., Ltd. and the tulobuterol patch (trade name: Amidil®, specification: 0.5 mg/patch, reference preparation) produced by Nitto Denko Corporation under the condition of single fasting administration in healthy subjects. The main pharmacokinetic parameters were used to evaluate whether the two were bioequivalent, and to provide a basis for the registration application of the test preparation. Secondary objective: To investigate the safety, skin adhesion firmness and skin irritation of the test preparation and the reference preparation in healthy adult subjects.

Start Date15 Jun 2024

Sponsor / Collaborator

Beijing Tide Pharmaceutical Co., Ltd.

CTR20242657 / CompletedNot Applicable

妥洛特罗贴剂在健康受试者中随机、开放、单剂量、两制剂、两周期、两序列交叉空腹状态下生物等效性预试验

[Translation] A randomized, open-label, single-dose, two-formulation, two-period, two-sequence crossover bioequivalence pilot study of tulobuterol patch in healthy subjects under fasting conditions

主要目的：按照生物等效性试验的相关规定，以浙江海阁堂医药有限公司研制的妥洛特罗贴剂（1 mg/贴）为受试制剂，以日东电工株式会社生产的妥洛特罗贴剂（商品名：阿米迪®，1 mg/贴）为参比制剂，各服用1mg后根据妥洛特罗的体内经时过程，估算其药代动力学参数，初步评估两制剂是否具有生物等效性，为正式试验的方案设计提供修订依据；初步了解药物的药代动力学特性，为正式试验采血点设置提供依据；同时了解药物的浓度范围，为正式试验检测方法学的优化提供参考依据。次要目的：评价妥洛特罗贴剂在健康受试者体内的安全性、皮肤粘附性和皮肤刺激性。

[Translation]

Main purpose: According to the relevant provisions of the bioequivalence test, the tulobuterol patch (1 mg/patch) developed by Zhejiang Haigetang Pharmaceutical Co., Ltd. was used as the test preparation, and the tulobuterol patch (trade name: Amidie®, 1 mg/patch) produced by Nitto Denko Corporation was used as the reference preparation. After taking 1 mg of each, the pharmacokinetic parameters were estimated according to the in vivo time course of tulobuterol, and the two preparations were preliminarily evaluated to see whether they were bioequivalent, providing a basis for revising the design of the formal test plan; the pharmacokinetic properties of the drug were preliminarily understood, providing a basis for setting up the blood collection points for the formal test; and the concentration range of the drug was understood, providing a reference for optimizing the detection methodology of the formal test. Secondary purpose: To evaluate the safety, skin adhesion and skin irritation of the tulobuterol patch in healthy subjects.

Start Date06 Jun 2024

Sponsor / Collaborator

Zhejiang Haigetang Pharmaceutical Co., Ltd.

100 Clinical Results associated with Tulobuterol

100 Translational Medicine associated with Tulobuterol

100 Patents (Medical) associated with Tulobuterol

175

Literatures (Medical) associated with Tulobuterol

01 Sep 2024·Analytica Chimica Acta

Ultrasound probe enhanced enzymatic hydrolysis for rapid separation of β2-adrenergic agonists from animal urine and livestock wastewater: Applicability to biomonitoring investigation

Article

Author: Jin, Yinji ; Zhao, Xinxue ; Wang, Shi ; Fan, Xia ; Li, Runxian ; Fu, Yao ; Xiao, Zhiming ; Suo, Decheng ; Chen, Gang ; Cao, Ying ; Yao, Ting

BACKGROUNDAn increasing number of β₂-adrenergic agonists are illicitly used for growth promoting and lean meat increasing in animal husbandry in recent years, but the development of analytical methods has lagged behind these emerging drugs.RESULTSHere, we designed and developed an ultrasound probe enhanced enzymatic hydrolysis reactor for quick separation and simultaneously quantification of 22 β₂-adrenergic agonists in animal urine and livestock wastewater. Owing to the enhancement of the conventional enzymatic digestion through the ultrasound acoustic probe power, only 2 min was required for the comprehensively separation of β₂-adrenergic agonists from the sample matrices, making it a much more desirable alternative tool for high-throughput investigation. The swine, bovine and sheep urines (n = 287), and livestock wastewater (n = 15) samples, collected from both the north and south China, were examined to demonstrate the feasibility and capability of the proposed approach. Six kinds of β₂-adrenergic agonists (clenbuterol, salbutamol, ractopamine, terbutaline, clorprenaline and cimaterol) were found in animal urines, with concentrations ranged between 0.056 μg/L (terbutaline) and 5.79 μg/L (clenbuterol). Up to nine β₂-adrenergic agonists were detected in wastewater samples, of which four were found in swine farms and nine in cattle/sheep farms, with concentration levels from 0.069 μg/L (tulobuterol) to 2470 μg/L (clenbuterol).SIGNIFICANCEInterestingly, since β₂-adrenergic agonists are usually considered to be abused mainly in the pig farms, our data indicate that both the detection frequencies and concentrations of these agonists in the ruminant farms were higher than the pig farms. Furthermore, the findings of this work indicated that there is a widespread occurrence of β₂-adrenergic agonists in livestock farms, especially for clenbuterol and salbutamol, which may pose both food safety and potential ecological risks. We recommend that stricter controls should be adopted to prevent the illegally usage of these β₂-adrenergic agonists in agricultural animals, especially ruminants, and they should also be removed before discharging to the environment.

01 Aug 2024·Journal of Chromatography A

A universal method for surface-based binding assays by preparing immobilized β2-adrenergic receptor stationary phase using solid binding peptide as a fusion tag

Article

Author: Wang, Ge ; Ou, Yuanyuan ; Zhao, Xue ; Qu, Lejing ; Zheng, Xinxin ; Li, Qian ; Zhao, Xinfeng ; Zhu, Huiting

Protein functionalized surface has the potential to develop new assays for determining the drug-like properties of potential compounds and discovering specific partners of G protein-coupled receptors (GPCRs). However, a universal method for purifying and immobilizing functional GPCRs has remained elusive. To this end, we developed a general and rapid way to purify and immobilize β₂-adrenergic receptor (β₂AR) by silicon-specific peptide. We screened CotB1p as a tag from six silica-binding peptides (minTBP-1, CotB1p, SB₇, Car₉, and Si_4-1) by examining their affinity to macroporous silica gel. We investigated the adsorption and desorption of CotB1p-tagged β₂-adrenoceptor (β₂AR-CotB1p) under diverse conditions to propose a protocol for receptor purification and immobilization. Under optimized conditions, β₂AR immobilization were achieved by directly immersing cell lysates harboring the receptor with silica gel, and the elution of the receptor without demonstratable contaminants was realized by including l-arginine/L-lysine in the elutes. This allows purification of the receptor from Escherichia coli (E.coli) lysates with a purity of 95 %. The immobilized receptor was utilized as a stationary phase to reveal the tag impact on ligand-binding outputs by comparing the CotB1p-strategy with a typical covalent method. The K_As of salbutamol, chlorprenaline, tulobuterol, and terbutaline on β₂AR-CotB1p column were 1.26 × 10⁶, 6.59 × 10⁶, 7.90 × 10⁶, and 8.97 × 10⁵ M^-1 respectively, which were two orders of magnitude higher than those on the Halo-β₂AR column. The whole immobilization was accomplished within 30 min without the requirement of any special treatment, resulting in enhanced accuracy for determining receptor-ligand binding parameters. Taken together, CotB1p-mediated strategy is simple, rapid, and universal for purification or immobilization of unstable biomolecules like GPCRs for analytical and biological applications.

01 Jul 2024·Journal of Chromatography B

Screening for promising multi-target bioactive components from Cortex Mori Radicis for the treatment of chronic cor pulmonale based on immobilized beta1-adrenergic receptor and beta2-adrenergic receptor chromatography

Article

Author: Cun, Sidi ; Wang, Jing ; He, Yunzhi ; Fan, Junni

Cortex Morin Radicis (CMR) is the dried root bark of Morus alba. L. It has a variety of effects such as antibacterial, anti-tumour, treatment of cardiovascular diseases or upper respiratory tract disease and so on. The pursuit for drugs selected from Cortex Mori Radicis having improved therapeutic efficacy necessitates increasing research on new assays for screening bioactive compounds with multi-targets. In this work, we applied immobilized β₁-AR and β₂-AR as the stationary phase in chromatographic column to screen bioactive compounds from Cortex Morin Radicis. Specific ligands of the two receptors (e.g. esmolol, metoprolol, atenolol, salbutamol, methoxyphenamine, tulobuterol and clorprenaline) were utilized to characterize the specificity and bioactivity of the columns. We used high performance affinity chromatography coupled with ESI-MS to screen targeted compounds of Cortex Morin Radicis. By zonal elution, we identified morin as a bioactive compound simultaneously binding to β₁-AR and β₂-AR. The compound exhibited the association constants of 3.10 × 10⁴ and 2.60 × 10⁴ M^-1 on the β₁-AR and β₂-AR column. On these sites, the dissociation rate constants were calculated to be 0.131 and 0.097 s^-1. Molecular docking indicated that the binding of morin to the two receptors occurred on Asp200, Asp121, and Val122 of β₁-AR, Asn312, Thr110, Asp113, Tyr316, Gly90, Phe193, Ile309, and Trp109 of β₂-AR. Likewise, mulberroside C was identified as the bioactive compound binding to β₂-AR. The association constants and dissociation rate constants were calculated to be 1.08 × 10⁴ M^-1 and 0.900 s^-1. Molecular docking also indicated that mulberroside C could bind to β₂-AR receptor on its agonist site. Taking together, we demonstrated that the chromatographic strategy to identify bioactive natural products based on the β₁-AR and β₂-AR immobilization, has potential for screening bioactive compounds with multi-targets from complex matrices including traditional Chinese medicines.

100 Deals associated with Tulobuterol

External Link

KEGG	Wiki	ATC	Drug Bank
D02151	Tulobuterol	R03CC11 R03AC11	DB12248

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Indication	Country/Location	Organization	Date
Acute Bronchitis	KR	Abbott Laboratories	01 Sep 2004
Asthma	KR	Abbott Laboratories	01 Sep 2004
Bronchitis, Chronic	KR	Abbott Laboratories	01 Sep 2004
Pulmonary Emphysema	KR	Abbott Laboratories	01 Sep 2004
Respiratory Distress Syndrome, Adult	KR	Abbott Laboratories	01 Sep 2004

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