We report in this work the fabrication of a flow-through silica nanochannel membrane (SNM) for controlled drug release applications. The ultrathin SNM consists of parallel nanochannels with a uniform diameter of ∼2.3 nm and a density of 4 × 10¹² cm^-2, which provide simultaneously high permeability and size selectivity toward small molecules. The track-etched porous polyethylene terephthalate film premodified with silane on its surface was used to support the ultrathin SNM via irreversible covalent bond formation, thus offering mechanical strength, flexibility, and stability to the ultrathin SNM for continuous and long-term use. Alkylamines were subsequently grafted onto the SNM surface to modulate the "on" and "off" state of nanochannels by medium pH for controlled drug release. Thiamphenicol glycinate hydrochloride (TPG), an intestinal drug, was studied as a model to permeate through an ultrathin SNM in both simulated gastric fluid (pH = 1.2) and simulated intestinal fluid (pH = 7.5). The release in the latter case was 178 times faster than that in the former. Moreover, a nearly zero-order constant release of TPG via single-file diffusion was achieved up to 24 h, demonstrating the feasibility of sustained and continuous release of small-molecule drugs in a pH-controlled manner.

01 Sep 2014·XenobioticaQ4 · MEDICINE

Pharmacokinetics of thiamphenicol glycinate and its active metabolite by single and multiple intravenous infusions in healthy Chinese volunteers

Q4 · MEDICINE

Article

Author: Ning Li ; Bing Yang ; Xijing Chen ; Yang Lu ; Zhixia Qiu ; Pengfei Song ; Di Zhao

The aim of this study was to investigate the pharmacokinetics of thiamphenicol glycinate (TG) and thiamphenicol (TAP) after intravenous (i.v.) infusion of TG hydrochloride in healthy Chinese by evaluating the pharmacokinetic parameters, to provide clinical guidance in TG application. In this double-blinded, phase I clinical trial, 24 healthy Chinese volunteers were recruited and divided into three groups which received a single dose of 500, 1000 or 1500 mg TG hydrochloride. Subjects in 500 mg group received further administrations at the same dose every 12 h for 5 days. The pharmacokinetic parameters were fitted on the basis of bi-phasic or tri-phasic plasma concentration-time profiles of TG and TAP. Following a single dose of 500, 1000, 1500 mg TG hydrochloride, the AUC0-∞ of TG and TAP was 849.1±100.3, 1305.2±301.8, 2315.9±546.9 and 4509.0±565.9, 7506.5±1112.4, 12 613.3±2779.8 µgmL(-1 )min, respectively. The total clearance of TG was calculated as 0.58±0.07, 0.41±0.10 and 0.68±0.18 L min(-1). The transformed rate constant from TG to TAP was fitted as 0.153, 0.113 and 0.118 min(-1), respectively. TAP was mainly excreted as unchanged form with no tendency of accumulation via kidney (71.9±19.4%) with the renal clearance estimated at 0.097 L min(-1). The established modeling was applied successfully to evaluate the pharmacokinetics of TG and TAP, providing meaningful guidance in TG clinical application.

01 Mar 2011·XenobioticaQ4 · MEDICINE

Pharmacokinetics of the prodrug thiamphenicol glycinate and its active parent compound thiamphenicol in beagle dogs following intravenous administration

Q4 · MEDICINE

Article

Author: Di Zhao ; Bing Yang ; Yang Lu ; Xijing Chen ; Jianheng Zheng ; Jing Zhu ; Jiake He ; Pengfei Song

1. This study investigated the pharmacokinetics of thiamphenicol glycinate (TG) and thiamphenicol (TAP) in beagles (n = 6) after intravenous administration of 50 mg/kg TG hydrochloride. Plasma concentrations of TG and TAP were measured by a HPLC-UV method. 2. Two-compartment model was selected to describe the pharmacokinetic characteristics of TG and TAP in vivo. Main parameters were as follows: AUC(0-∞) of TAP and TG were 16,328 ± 1682 µg·min/mL and 3943 ± 546 µg·min/mL, respectively. The total plasma clearance (CL) of TG and TAP were 12.7 ± 2.0 mL/min/kg and 2.5 ± 0.3 mL/min/kg, respectively. Mean residence time (MRT) of TG and TAP were 27.5 ± 3.5 and 207.2 ± 20.2 min, respectively. The transformative rate constant (k(1M)) from TG to TAP was 0.0477 ± 0.0028 min(-1). The elimination rate constant (k(M10)) from TAP was 0.0238 ± 0.0044 min(-1). Coefficients of variation (CV) between observed values and predicted ones were 5.9% and 18.2%, respectively. The volume of distribution of the central compartment for TG (V(C)) and TAP (V(CM)) were 0.264 ± 0.022 L/kg and 0.127 ± 0.023 L/kg, respectively. 3. Pharmacokinetic parameters suggested that TG was presumably cleaved quickly by tissue esterase to release TAP for effectiveness in beagles after administration.

100 Deals associated with Thiamphenicol Glycinate Hydrochloride

External Link

KEGG	Wiki	ATC	Drug Bank
-	-	J01BA02	-

R&D Status

10 top approved records.

to view more data

Indication	Country/Location	Organization	Date
Respiratory Tract Infections	CN	Zhejiang Lepu Pharmaceutical Co., Ltd.	13 Jun 2006
Urinary Tract Infections	CN	Zhejiang Lepu Pharmaceutical Co., Ltd.	13 Jun 2006

Clinical Result

Indication

Phase

Evaluation

View All Results

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis