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·Otolaryngology–Head and Neck SurgeryQ2 · MEDICINE

Eradicating Chronic Ear, Nose, and Throat Infections

Q2 · MEDICINE

Review

Author: Post, J. Christopher ; Buchinsky, Farrel Joel ; Smith, Angelia

ObjectiveBacteria can grow as individual, planktonic organisms or as complex biofilm communities that are more resistant to treatment. This review was designed to systematically search to identify recent laboratory studies on eradication of biofilms in otolaryngologic infections to highlight promising advances in biofilm treatment.Data SourcesA systematic electronic literature search of Medline/PubMed, CINHAL, and Web of Science was conducted for articles describing the treatment of biofilm infections in ear, nose, and throat (ENT) diseases through March 2010. English‐language articles and articles with an English abstract that focused on biofilm treatment were considered for review.Review MethodsEach included article was reviewed by one of the authors for study design, treatment intervention, and outcome. Data from in vitro and animal studies were considered separately from human studies.ResultsA total of 30 articles were identified for this review, including 5 studies that included a human treatment component. In general, antibiotics were relatively ineffective for eradicating biofilm infections. Markedly higher antibiotic dosages were required to reduce biofilm presence compared with doses that were effective in eradicating planktonic bacteria. Mupirocin irrigation, gentian violet, and thiamphenicol glycinate acetylcysteine effectively eradicated biofilms. Physical disruption, surfactants, and probiotics were also shown to be beneficial in both nonhuman and human studies.ConclusionEradicating ENT biofilms is difficult when treating single‐organism or mixed flora biofilms. Antibiotic therapy is often ineffective against biofilms, and clinical treatment may need to focus on nonantibiotic therapies that reduce, disrupt, or eradicate ENT biofilms.

100 Deals associated with Thiamphenicol Glycinate Hydrochloride

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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

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