ABSTRACT
Polymyxin B, which is a last-line antibiotic for extensively drug-resistant Gram-negative bacterial infections, became available in China in Dec. 2017. As dose adjustments are based solely on clinical experience of risk toxicity, treatment failure, and emergence of resistance, there is an urgent clinical need to perform therapeutic drug monitoring (TDM) to optimize the use of polymyxin B. It is thus necessary to standardize operating procedures to ensure the accuracy of TDM and provide evidence for their rational use. We report a consensus on TDM guidelines for polymyxin B, as endorsed by the Infection and Chemotherapy Committee of the Shanghai Medical Association and the Therapeutic Drug Monitoring Committee of the Chinese Pharmacological Society. The consensus panel was composed of clinicians, pharmacists, and microbiologists from different provinces in China and Australia who made recommendations regarding target concentrations, sample collection, reporting, and explanation of TDM results. The guidelines provide the first-ever consensus on conducting TDM of polymyxin B, and are intended to guide optimal clinical use.
Subject(s)
Humans , Anti-Bacterial Agents/therapeutic use , China , Drug Monitoring/methods , Polymyxin B , Practice Guidelines as TopicABSTRACT
To develop estradiol transdermal film-forming spray (TFS), various polymers were screened using solvent appearance, spray ability, film-forming rate and appearance as indices. The influence of polymer type, plasticizer and penetration enhancer on the transdermal flux were investigated by selecting porcine skin as model, and transdermal flux of TFS was compared with commercial patch and gel. The drug existing state in the formed film was investigated by differential scanning calorimetry (DSC). The solvent appearances, spray abilities, film-forming rates and appearances of eudragit E PO, RL PO, hydroxypropyl cellulose EF, polyvinylpyrrolidone K30, Plasdone S630 and Agrimer VA64 were suitable for the preparation of TFS. TFS prepared by Eudragit RL PO had the biggest transdermal flux of estradiol among all the polymers investigated. Triethyl citrate, the plasticizer, decreased the transdermal flux. Azone increased the transdermal flux, while oleic acid, isopropyl myristate and menthol had opposite effects. TFS had a higher transdermal rate and a higher accumulative penetrated estradiol of 24 h than commercial patch and gel. The DSC result showed that estradiol was spread as molecule in the formed film of TFS. It was indicated that TFS could be expected to be an effective transdermal drug delivery system.
ABSTRACT
<p><b>OBJECTIVE</b>To investigate the relationship of properties and drug release rate of hot melt pressure sensitive adhesive (HMPSA), and to provide a recommendation of preparing and selecting of HMPSA for transdermal use.</p><p><b>METHOD</b>HMPSA with different properties were prepared using styrene-isoprene-styrene triblock copolymer as main material, and the tacks, adhesions and cohesions were determined. Drug-in-adhesive type patches were prepared using alpha-asarone as model drug, and the drug release rates were investigated on single chamber diffusion cells using 60% ethanol solution as release media.</p><p><b>RESULT</b>The prepared HMPSAs had different tacks, adhesions and cohesions. The drug release rates of HMPSA patches were related to the cohesions. The release rate decreased when the cohesion increased.</p><p><b>CONCLUSION</b>The HMPSA with appropriate cohesion should be selected when preparing patches to balance the drug release rate and patch property.</p>
Subject(s)
Adhesives , Anisoles , Chemistry , Pharmacokinetics , Diffusion , PharmacokineticsABSTRACT
<p><b>OBJECTIVE</b>To screen the formulations of cryptotanshinone gel for treatment of topical diseases such as acne.</p><p><b>METHOD</b>Different cryptotanshinone gels incorporating various penetration enhancers at different concentrations were prepared using carbopol 934L as matrix. The steady transdermal fluxes and drug retention amounts in skin of the gels were investigated on single chamber diffusion cells using excised rat abdomen skin as model and 40% polyethylene glycol-400 saline as releasing media. The optimal formulation would be the gel which had the maximum drug retention amount/ transdermal drug flux ratio.</p><p><b>RESULT</b>The promotion effects of menthol at different concentrations were as follows: 5% > 3% > 1%, and the effects on drug retention amount in skin were followed as: 5% approximately equal 3% > 1%; The promotion effects of a zone at different concentrations were as follows: 5% approximately equal 3% > 1%, and the effects on drug retention amount in skin were as follows: 5% > 3% approximately equal 1%. Combination of enhancers showed no superior effects compared to single uses. 5% azone had the maximum retention amount/ transdermal flux ratio.</p><p><b>CONCLUSION</b>The optimal formulation was the cryptotanshinone gel containing 5% azone.</p>