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Preparation, characterization and pharmacokinetics of doxycycline hydrochloride and florfenicol polyvinylpyrroliddone microparticle entrapped with hydroxypropyl-β-cyclodextrin inclusion complexes suspension
- Source :
- Colloids and surfaces. B, Biointerfaces. 141
- Publication Year :
- 2015
-
Abstract
- In order to effectively control the bacterial pneumonia in pigs, doxycycline hydrochloride (DoxHcl) and florfenicol (FF) microparticle suspension together with inclusion complexes was prepared by using hydroxypropyl-β-cyclodextrin (HP-β-CD) as host molecules, polyvinylpyrroliddone (PVP) as polymer carriers and hydroxypropyl methyl cellulose (HPMC) as suspending agents. In vitro antibacterial activity, properties, stability and pharmacokinetics of the suspension were studied. The results demonstrated that DoxHcl and FF had a synergistic or additive antibacterial activity against Streptococcus suis, Actinobacillus pleuropneumoniae and Haemophilus parasuis. The size, polydispersity index and zeta potential of microparticles were 1.46 ± 0.06 μm, 0.30 ± 0.02 and 1.53 ± 0.04 mV, respectively. The encapsulation efficiency (EE) of DoxHcl and FF was 45.28% ± 3.30% and 89.69% ± 2.71%, respectively. The re-dispersed time and sedimentation rate of the suspension were 1 min and 1. The suspension went through the 9-gage needle smoothly with withdrawal volume of 9.12 ± 0.87 mL/min. The suspension showed good stability when stored away from light, no irritation at the injection site and sustained release in PBS buffer. After intramuscular administration to pig, DoxHcl and FF could maintain over 0.15 μg/mL for 72 h. Compared to the control injection, the suspension increased the elimination half-life (T½ke) as well as mean residence time (MRT) of DoxHcl from 5.73 to 9.77 h and from 12.02 to 18.81 h, and those of FF from 12.02 to 26.19 h and from 12.02 to 28.16 h, respectively. The suspension increased the bioavailability of DoxHcl and FF by 1.74 and 1.13-fold, respectively. These results suggest that the compound suspension is a promising formulation for pig pneumonia therapy.
- Subjects :
- Florfenicol
Male
Streptococcus suis
Metabolic Clearance Rate
Swine
Drug Compounding
Dispersity
02 engineering and technology
Microbial Sensitivity Tests
Pharmacology
010402 general chemistry
01 natural sciences
chemistry.chemical_compound
Haemophilus parasuis
Colloid and Surface Chemistry
Pharmacokinetics
Suspensions
Zeta potential
Animals
Physical and Theoretical Chemistry
Microparticle
Particle Size
Thiamphenicol
Chromatography
Chemistry
Actinobacillus pleuropneumoniae
beta-Cyclodextrins
Povidone
Surfaces and Interfaces
General Medicine
021001 nanoscience & nanotechnology
0104 chemical sciences
Bioavailability
2-Hydroxypropyl-beta-cyclodextrin
Anti-Bacterial Agents
Drug Liberation
Methyl cellulose
Area Under Curve
Doxycycline
Microscopy, Electron, Scanning
Female
0210 nano-technology
Antibacterial activity
Biotechnology
Subjects
Details
- ISSN :
- 18734367
- Volume :
- 141
- Database :
- OpenAIRE
- Journal :
- Colloids and surfaces. B, Biointerfaces
- Accession number :
- edsair.doi.dedup.....956ba793abb2c8f423eb939ad26b2fae