Résumé
@#In order to mask the bitterness of azithromycin (AZI) and individually regulate the drug release rate to reduce gastrointestinal irritation, immediate-release AZI-AmberliteTM IRP64/HPC and delayed-release AZI-AmberliteTM IRP69/RS100 were prepared by modifying with hydroxypropyl cellulose (HPC) and Eudragit RS100, respectively, and further combined to achieve controlled release.The drug loading and drug utilization rate of AZI-ion exchange resin complexes were measured; the structure of AZI-ion exchange resin complexes was characterized by differential scanning calorimetry and X-ray diffraction; and the wetting humidity, odor masking effects, in vitro dissolution and release behaviors were determined.The results showed that the formation of AZI-ion exchange resin complexes changed the original crystallization state of the drug, that the 2.5% HPC-modified AZI-AmberliteTM IRP64/HPC and the 0.5% RS100-modified AZI-AmberliteTM IRP69/RS100 demonstrated good taste masking effect, and that their combination in the drug content ratio of 13∶67 achieved the expected drug release behavior, i.e.rapid release of AZI in the first 10 min and smooth release in the later 6 h.These results indicated that the AZI-ion exchange resin complexes prepared by surface modification and their composites could mask the bitterness of AZI and realize the flexible adjustment of drug release rate, which lays the foundation for the research and development of new AZI preparations.
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@#This study sought to assess the therapeutic effect of celecoxib (CEL)-loaded polylactic acid-glycolic acid copolymer (PLGA) microspheres on rheumatoid arthritis in rats after intra-articular injection.The celecoxib-loaded microspheres (CEL-MS) were prepared by the O/W solvent volatilization method with PLGA as carrier.In order to investigate the therapeutic effect of CEL-MS on rheumatoid arthritis in rats after intra-articular injection, a rat model of adjuvant arthritis (AA) was constructed by complete Freund''s adjuvant, and the evaluation indicators of the therapeutic effect were rat paw swelling, arthritis index,spleen index and joint synovial histopathological examination. The results showed that the microspheres had a smooth spherical morphology with a particle size of (2.1 ± 0.3) μm and a drug loading efficiency of (20.8 ± 0.6)%.The results of the in vivo efficacy test showed that intra-articular injection of CEL-MS compared to the CEL suspension oral and the celecoxib suspension intra-articular injection in adjuvant arthritis rat model can significantly reduce joint swelling and arthritis index, thus effectively inhibiting synovial inflammation.The above results indicate that intra-articular injection of CEL-MS has a good therapeutic effect on rheumatoid arthritis in rats.
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@#Liquid preparations are the commonly used oral dosage forms in pediatric clinical practice.This review introduces the pediatric oral liquid dosage forms including extemporaneous preparation of oral liquid formulations, oral liquid sustained and controlled release formulations, nanosuspensions, nanoemulsions, self-nanoemulsions and milk-based liquid formulations.In addition, the efficient flavoring and taste masking technologies, using safe pharmaceutical excipients, high-demanding technical standards and verification strategies, establishing excellent workflow management systems can contribute to the development and application of pediatric oral liquid dosage forms which are safer, more effective and better compliant.This review is helpful in laying the relevant theoretical foundation for further studies on pediatric oral liquid dosage forms.
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@#To mask the bitterness of azithromycin（AZI） and improve patient compliance, an AZI-loaded microsphere (AZI-EC MS) for oral administration was prepared by O/W emulsion solvent evaporation with ethylcellulose (EC) as carrier. The release profiles and taste-masking effect of AZI-EC MS were preliminarily assessed. Its physical properties and morphology were then investigated by differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FTIR) and scanning electron microscope (SEM). The results indicated that the polymer weight of EC could influence the drug release behavior. With a drug polymer ratio of 1∶1 and mixed EC (N22/T10, 7∶3) as carrier, the cumulative release of AZI-EC MS at 0.5 h was less than 40% and reached 90% at 8 h; the drug loading efficiency of microspheres was (48.95 ± 0.86)% with smooth spherical morphology. The AZI bitterness threshold is 9.93 μg/mL with a strong bitter taste, which indicated a better taste masking effect. Therefore, AZI-EC MS prepared in this study can mask AZI bitterness and improve patient compliance, setting the stage for the research of new AZI preparations.
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@#In China, the incidence of adverse reactions of drugs in children is twice that in adults; especially in the newborns, it is four times that in adults. The main reason is that the physiological characteristics of children are changing constantly due to that they are in a constant process of growth and development; while the pediatric medicines cannot meet the clinical needs of children in different age states. Accordingly, the development of pediatric medicines, especially oral solid preparations which are convenient for administration and storage, has attracted a lot of attention. This review introduced various pediatric oral solid dosage forms such as multiparticulates, orally disintegrating tablets(ODT)and chewable tablets. In addition, the efficient taste masking technology and accurate dose control were the further research directions for development of pediatric medicines, which would provide important theoretical references for studies on pediatric oral solid dosage forms in future.
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To enhance the quality control of tebipenem pivoxil and establish its quality criteria,the synthetic route of tebipenem pivoxil was analyzed and five related substances (P1,P2,P6,P8 and P9)were synthesized and characterized by 1H NMR and MS.The purities of the related substances were over 95% via HPLC detec-tion.The target compounds can be used as the reference of the related substances in the quality control of tebi-penem pivoxil.The starting materials were cheap and easy to obtain;the reaction conditions were mild.
Résumé
As children are extremely sensitive to the bad taste of medicine,they have poor compliance with the bitter medicine.It is of great importance to develop the approaches of taste masking for the research of paediatric drug formulations.Besides,taste masking technology is one of the main barrier to develop children pharmaceutic preparation.This article provides an overview of the advance in taste masking technology of oral paediatric medicine in recent years,and introduces five types of taste masking technology in terms of drug,preparation and the bitter taste transduction,including principle and characteristics of these approaches,as well as their application in formulations,so as to provide some references for the development of paediatric medicine.