Optimization of taste-masking on ibuprofen microspheres with selected structure features
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摘要
The microsphere was a primary particulate system for taste-masking with unique structural features defined by production process. In this article, ibuprofen lipid microspheres of octadecanol and glycerin monostearate were prepared to mask the undesirable taste of ibuprofen via three kinds of spray congealing processes, namely, air-cooling, water-cooling and citric acid solution-cooling. The stereoscopic and internal structures of ibuprofen microspheres were quantitatively analyzed by synchrotron radiation X-ray micro-computed tomography(SR-μCT) to establish the relationship between the preparation process and microsphere architectures. It was found that the microstructure and morphology of the microspheres were significantly influenced by preparation processes as the primary factors to determine the release profiles and taste-masking effects. The sphericity of ibuprofen microspheres congealed in citric acid solution was higher than that of other two and its morphology was more regular than that being congealed in air or distilled water, and the contact angles between congealing media and melted ibuprofen in octadecanol and glycerin monostearate well demonstrated the structure differences among microspheres of three processes which controlled the release characteristics of the microspheres. The structure parameters like porosity, sphericity, and radius ratio from quantitative analysis were correlated well with drug release behaviors. The results demonstrated that the exterior morphology and internal structure of microspheres had considerable influences on the drug release behaviors as well as taste-masking effects.
The microsphere was a primary particulate system for taste-masking with unique structural features defined by production process. In this article, ibuprofen lipid microspheres of octadecanol and glycerin monostearate were prepared to mask the undesirable taste of ibuprofen via three kinds of spray congealing processes, namely, air-cooling, water-cooling and citric acid solution-cooling. The stereoscopic and internal structures of ibuprofen microspheres were quantitatively analyzed by synchrotron radiation X-ray micro-computed tomography(SR-μCT) to establish the relationship between the preparation process and microsphere architectures. It was found that the microstructure and morphology of the microspheres were significantly influenced by preparation processes as the primary factors to determine the release profiles and taste-masking effects. The sphericity of ibuprofen microspheres congealed in citric acid solution was higher than that of other two and its morphology was more regular than that being congealed in air or distilled water, and the contact angles between congealing media and melted ibuprofen in octadecanol and glycerin monostearate well demonstrated the structure differences among microspheres of three processes which controlled the release characteristics of the microspheres. The structure parameters like porosity, sphericity, and radius ratio from quantitative analysis were correlated well with drug release behaviors. The results demonstrated that the exterior morphology and internal structure of microspheres had considerable influences on the drug release behaviors as well as taste-masking effects.
The microsphere was a primary particulate system for taste-masking with unique structural features defined by production process. In this article, ibuprofen lipid microspheres of octadecanol and glycerin monostearate were prepared to mask the undesirable taste of ibuprofen via three kinds of spray congealing processes, namely, air-cooling, water-cooling and citric acid solution-cooling. The stereoscopic and internal structures of ibuprofen microspheres were quantitatively analyzed by synchrotron radiation X-ray micro-computed tomography(SR-μCT) to establish the relationship between the preparation process and microsphere architectures. It was found that the microstructure and morphology of the microspheres were significantly influenced by preparation processes as the primary factors to determine the release profiles and taste-masking effects. The sphericity of ibuprofen microspheres congealed in citric acid solution was higher than that of other two and its morphology was more regular than that being congealed in air or distilled water, and the contact angles between congealing media and melted ibuprofen in octadecanol and glycerin monostearate well demonstrated the structure differences among microspheres of three processes which controlled the release characteristics of the microspheres. The structure parameters like porosity, sphericity, and radius ratio from quantitative analysis were correlated well with drug release behaviors. The results demonstrated that the exterior morphology and internal structure of microspheres had considerable influences on the drug release behaviors as well as taste-masking effects.
引文
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[22]Cheewatanakornkool K,Niratisai S,Manchun S,Dass CR,Sriamornsak P.Characterization and in vitro release studies of oral microbeads containing thiolated pectin-doxorubicin conjugates for colorectal cancer treatment.Asian J Pharm Sci 2017;12(6):509-20.
[23]Taylor J,Taylor JRN,Belton PS,et al.Formation of kafirin microparticles by phase separation from an organic acid and their characterisation.J Cereal Sci 2009;50(1):99-105.
[24]Cai Z,Lei X,Lin Z,et al.Preparation and evaluation of sustained-release solid dispersions co-loading gastrodin with borneol as an oral brain-targeting enhancer.Acta Pharm Sin B 2014;4(1):86-93.
[25]Yin X,Li H,Guo Z,et al.Quantification of swelling and erosion in the controlled release of a poorly water-soluble drug using synchrotron X-ray computed microtomography.AAPS J 2013;15(4):1025-34.
[26]Li HY,Yin XZ,Ji JQ,et al.Microstructural investigation to the controlled release kinetics of monolith osmotic pump tablets via synchrotron radiation X-ray microtomography.Int JPharm 2012;427(2):270-5.
[27]Liu RH,Yin XZ,Li HY,et al.Visualization and quantitative profiling of mixing and segregation of granules using synchrotron radiation X-ray microtomography and three dimensional reconstruction.Int J Pharm2013;445(1-2):125-33.
[28]Kajihara R,Noguchi S,Iwao Y,et al.Structural changes of polymer-coated microgranules and excipients on tableting investigated by microtomography using synchrotron X-ray radiation.Int J Pharm 2015;481(1-2):132-9.
[29]Guo Z,Yin X,Liu C,et al.Microstructural investigation using synchrotron radiation X-ray microtomography reveals taste-masking mechanism of acetaminophen microspheres.Int J Pharm 2016;499(1-2):47-57.
[2]Juluri A,Popescu C,Zhou L,et al.Taste masking of griseofulvin and caffeine anhydrous using kleptose linecaps DE17 by hot melt extrusion.AAPS PharmSciTech2016;17(1):99-105.
[3]Tiwari RV,Polk AN,Patil H,et al.Rat palatability study for taste assessment of caffeine citrate formulation prepared via hot-melt extrusion technology.AAPS PharmSciTech2017;18(2):341-8.
[4]Khor CM,Ng WK,Kanaujia P,Chan KP,Dong YC.Hot-melt extrusion microencapsulation of quercetin for taste-masking.J Microencapsul 2017;34(1):29-37.
[5]Campbell GA,Charles JA,Roberts-Skilton K,et al.Evaluating the taste masking effectiveness of various flavors in a stable formulated pediatric suspension and solution using the Astree(TM)electronic tongue.Powder Technol2012;224:109-23.
[6]Wu X,Onitake H,Haraguchi T,et al.Quantitative prediction of bitterness masking effect of high-potency sweeteners using taste sensor.Sens Actuat B-Chem 2016;235:11-17.
[7]Noorjahan A,Amrita B,Kavita S.In vivo evaluation of taste masking for developed chewable and orodispersible tablets in humans and rats.Pharm Dev Technol 2014;19(3):290-5.
[8]Yuan J,Liu TT,Li HR,et al.Oral sustained-release suspension based on a novel taste-masked and mucoadhesive carrier-ion-exchange fiber.Int J Pharm 2014;472(1-2):74-81.
[9]Samprasit W,Akkaramongkolporn P,Ngawhirunpat T,et al.Fast releasing oral electrospun PVP/CD nanofiber mats of taste-masked meloxicam.Int J Pharm 2015;487(1-2):213-22.
[10]Nieddu M,Rassu G,Boatto G,et al.Improvement of thymol properties by complexation with cyclodextrins:in vitro and in vivo studies.Carbohydr Polym 2014;102:393-9.
[11]Diego-Taboada A,Maillet L,Banoub JH,et al.Protein free microcapsules obtained from plant spores as a model for drug delivery:ibuprofen encapsulation,release and taste masking.J Mater Chem B 2013;1(5):707-13.
[12]Sugiura T,Uchida S,Namiki N.Taste-masking effect of physical and organoleptic methods on peppermint-scented orally disintegrating tablet of famotidine based on suspension spray-coating method.Chem Pharm Bull2012;60(3):315-19.
[13]Liu MX,Yin DP,Fu HL,et al.Double-coated enrofloxacin microparticles with chitosan and alginate:preparation,characterization and taste-masking effect study.Carbohydr Polym 2017;170:247-53.
[14]Stange U,Fuhrling C,Gieseler H.Taste masking of naproxen sodium granules by fluid-bed coating.Pharm Dev Technol2014;19(2):137-47.
[15]Yehia SA,El-Ridi MS,Tadros MI,El-Sherif NG.Phenylalanine-free taste-masked orodispersible tablets of fexofenadine hydrochloride:development,in vitro evaluation and in vivo estimation of the drug pharmacokinetics in healthy human volunteers.Pharm Dev Technol2015;20(5):528-39.
[16]Onofre F,Macleod G,Muley V,et al.An investigation into taste masking of paracetamol using Aquacoat(R)ECDapplied via different granulation processes.Int J Pharm2016;511(2):1145-6.
[17]Rogers TL,Wallick D.Reviewing the use of ethylcellulose,methylcellulose and hypromellose in microencapsulation.Part 2:techniques used to make microcapsules.Drug Dev Ind Pharm 2011;37(11):1259-71.
[18]Mohamed-Ahmed AHA,Soto J,Ernest T,Tuleu C.Non-human tools for the evaluation of bitter taste in the design and development of medicines:a systematic review.Drug Discov Today 2016;21(7):1170-80.
[19]Bile J,Bolzinger MA,Vigne C,et al.The parameters influencing the morphology of poly(?-caprolactone)microspheres and the resulting release of encapsulated drugs.Int J Pharm 2015;494(1):152-66.
[20]Qazi F,Shoaib MH,Yousuf RI,et al.Lipids bearing extruded-spheronized pellets for extended release of poorly soluble antiemetic agent-Meclizine HCl.Lipids Health Dis2017;16:75.
[21]Morkhade DM.Evaluation of gum mastic(Pistacia lentiscus)as a microencapsulating and matrix forming material for sustained drug release.Asian J Pharm Sci 2017;12(5):424-32.
[22]Cheewatanakornkool K,Niratisai S,Manchun S,Dass CR,Sriamornsak P.Characterization and in vitro release studies of oral microbeads containing thiolated pectin-doxorubicin conjugates for colorectal cancer treatment.Asian J Pharm Sci 2017;12(6):509-20.
[23]Taylor J,Taylor JRN,Belton PS,et al.Formation of kafirin microparticles by phase separation from an organic acid and their characterisation.J Cereal Sci 2009;50(1):99-105.
[24]Cai Z,Lei X,Lin Z,et al.Preparation and evaluation of sustained-release solid dispersions co-loading gastrodin with borneol as an oral brain-targeting enhancer.Acta Pharm Sin B 2014;4(1):86-93.
[25]Yin X,Li H,Guo Z,et al.Quantification of swelling and erosion in the controlled release of a poorly water-soluble drug using synchrotron X-ray computed microtomography.AAPS J 2013;15(4):1025-34.
[26]Li HY,Yin XZ,Ji JQ,et al.Microstructural investigation to the controlled release kinetics of monolith osmotic pump tablets via synchrotron radiation X-ray microtomography.Int JPharm 2012;427(2):270-5.
[27]Liu RH,Yin XZ,Li HY,et al.Visualization and quantitative profiling of mixing and segregation of granules using synchrotron radiation X-ray microtomography and three dimensional reconstruction.Int J Pharm2013;445(1-2):125-33.
[28]Kajihara R,Noguchi S,Iwao Y,et al.Structural changes of polymer-coated microgranules and excipients on tableting investigated by microtomography using synchrotron X-ray radiation.Int J Pharm 2015;481(1-2):132-9.
[29]Guo Z,Yin X,Liu C,et al.Microstructural investigation using synchrotron radiation X-ray microtomography reveals taste-masking mechanism of acetaminophen microspheres.Int J Pharm 2016;499(1-2):47-57.