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The feasibility of coating by cooling crystallization on ibuprofen naked tablets

Fatima Mameri, Ouahiba Koutchoukali, Mohamed Bouhelassa, Anne Hartwig, Leila Nemdili, Joachim Ulrich

《化学科学与工程前沿（英文）》 2017年 第11卷 第2期   页码 211-219 doi: 10.1007/s11705-017-1619-1

摘要： Sugar spray coating is a frequently used process in the pharmaceutical industry. However, this process presents the disadvantage to form an amorphous coating around the active ingredient. A crystalline coating formed on the surface of a tablet is highly desirable. Recently, a new process of coating by cooling crystallization has been developed and applied on bisacodyl pastilles obtained by melt crystallization. In this work, we investigated the feasibility of coating by cooling crystallization on ibuprofen “naked tablets” manufactured by compression. In the first part of this work, the solubility and the metastable zone width have been determined experimentally for the coating solution because they are essential factors for any crystallization process. In the second part, the coating process is investigated on the operating conditions that affect the surface morphology and the crystal growth rate. These experimental conditions include concentration of the coating solution, degree of sub-cooling, agitation speed, retention time, and surface properties of the naked ibuprofen tablets. The results show that naked tablet coating by cooling crystallization is feasible and can be applied in the pharmaceutical industry.

关键词： coating     solution crystallization     ibuprofen tablets     sucrose    

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Improved dissolution and anti-inflammatory effect of ibuprofen by solid dispersion

null

《医学前沿（英文）》 2012年 第6卷 第2期   页码 195-203 doi: 10.1007/s11684-012-0189-3

摘要：

The purpose of this study was to improve the dissolution rate and anti-inflammatory effect of ibuprofen by a solid dispersion (SD) method. Initial screening was developed based on drug solubility in carriers in the liquid state to select a suitable water-soluble carrier system for the preparation of SDs. The dissolution of ibuprofen in urea was higher than in PEG4000 or mannitol. Thus, urea was selected as the carrier for the preparation of SDs. SDs were characterized in terms of dissolution, differential scanning calorimetry (DSC), X-ray diffraction (XRD), scanning electron microscopy (SEM), and Fourier transform infrared (FTIR) spectroscopy. Solid dispersion-based (SDBT) and conventional (CT) tablets were prepared by the wet granulation method. The anti-inflammatory effect of SDBT was evaluated using the mouse ear edema test with xylene. In vitro release results indicated that the ibuprofen dissolution rate was improved by the SD. SD characterization results suggested that ibuprofen partly precipitates in crystalline and amorphous forms after SD preparation and that ibuprofen and urea do not interact. SDBT displayed more significant anti-inflammatory effects than CT. The dissolution rate and anti-inflammatory effect of ibuprofen were significantly enhanced by the ibuprofen-urea SD.

关键词： ibuprofen     solid dispersion     physical mixture     dissolution     anti-inflammatory effect    

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Isolation and application of an ibuprofen-degrading bacterium to a biological aerated filter for the

Bingjie Xu, Gang Xue, Xing Yang

《环境科学与工程前沿（英文）》 2018年 第12卷 第5期 doi: 10.1007/s11783-018-1080-5

摘要：

• An ibuprofen-degrading strain, Serratia marcescens BL1, was isolated and identified.

• The effects of various factors on ibuprofen degradation by BL1 were evaluated.

• Strain BL1 was applied to a laboratory-scale biological aerated filter system.

• Strain BL1 was stable in both static tests and in the biological aerated filter system.

关键词： Ibuprofen     Biological aerated filter     Degrading bacterium     Serratia marcescens    

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Preparation of ibuprofen/lipid composite microparticles by supercritical fluid technique

WANG Xia, CHEN Hui, GUO Yanni, SU Yuzhong, WANG Hongtao, LI Jun

《化学科学与工程前沿（英文）》 2008年 第2卷 第4期   页码 361-367 doi: 10.1007/s11705-008-0066-4

摘要： Using the CO- and N-assisted atomization processes, the production of ibuprofen/lipid composite microparticles is investigated, in which the lipid includes myristic acid and tripalmitin. The produced composite particles show similar morphology to that of the pure lipids obtained by the same process. In the case of the N-assisted process, the average size of composite particles is slightly larger than that of the pure lipid particles due to the difficulty of solidification when using N. In the case of the CO-assisted process, the average size of composite particles is slightly smaller than that of the pure myristic acid particles, but slightly larger than that of the pure tripalmitin particles. The dissolution study reveals that the drug release from the ibuprofen/myristic acid particles is enhanced in comparison with that of the unprocessed ibuprofen. For the particles produced by the N-assisted process, the X-ray diffraction (XRD) patterns clearly indicate the encapsulation of ibuprofen into myristic acid. The obtained ibuprofen/tripalmitin composite particles with 5% or 20% of ibuprofen (in mass) evidently show the controlled drug release: only about 20% of the drug is released in 500 min from the ibuprofen/tripalmitin composite particles consisting of 20% ibuprofen prepared by the CO-assisted process, and the same release is obtained from the ibuprofen/tripalmitin composite particles containing 5% ibuprofen prepared by the N-assisted process.
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屈螺酮炔雌醇片预防稽留流产清宫术后宫腔粘连初步研究

赵现立,刘朝阳,谭宏伟,张恩娣

《中国工程科学》 2015年 第17卷 第6期   页码 13-15

摘要：

目的：观察稽留流产清宫术后服用屈螺酮炔雌醇片对减轻宫腔粘连发生的效果。方法：选择2013年6月至2014年6月在西北妇女儿童医院（陕西省妇幼保健院）诊断为稽留流产并实施清宫术的患者220例，随机分成观察组和对照组，每组110例。两组患者均在清宫术前服用米非司酮片150 mg和米索前列醇片600 μg治疗，术后常规应用抗生素3天。观察组：清宫术后给予屈螺酮炔雌醇片，每天服用一片，连续3个周期，对照组：患者实施清宫术后不给予屈螺酮炔雌醇片治疗。观察手术时间、胚胎绒毛大小、患者阴道流血持续时间、月经复潮时间、术后2周超声检查子宫内膜以及宫腔镜检查宫腔粘连情况。结果：观察组术后阴道流血天数（（4.98±0.80）天）及月经复潮时间（（28.41±1.61）天）显著少于对照组（P＜0.05）。观察组患者术后子宫内膜厚度（（9.12±1.12） mm）明显高于对照组子宫内膜厚度（（6.23±1.16）mm），两组比较差异有统计学意义（P＜0.05）。观察组的宫腔粘连率显著低于对照组（x2=4.67，P=0.031）。结论：清宫术后口服屈螺酮炔雌醇片是减少稽留流产术后发生宫腔粘连的一种安全有效的方法。

关键词： 稽留流产     宫腔粘连     屈螺酮炔雌醇片    

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Utilizing melt crystallization fundamentals in the development of a new tabletting technology

Ahmed ABOUZEID,Sandra PETERSEN,Joachim ULRICH

《化学科学与工程前沿（英文）》 2014年 第8卷 第3期   页码 346-352 doi: 10.1007/s11705-014-1443-9

摘要： Increasing production effeciency and lowering costs are some of the many advantages melt crystallization technology offers over the conventional methodology of tabletting. A normal tablet consists of a pure shell or a coat and a separate core constituting the pharmaceutical active ingredient. Great emphasis is put on the purity of the shell since its purpose is to solely protect and deliver the active ingredient to its target. Melt crystallization is a purification (separation) process. It is discussed here for its ability to produce coated tablets, by separating the “coating” material from the “to be coated” material coming from one molten mixture. Molten drops of lutrol-ibuprofen mixture are produced using the drop forming technique. The subsequent analysis involves proving and quantifying the phase separation (coat purity). The mechanism of a crystallizing drop is shown as direct evidence of the ongoing process. Moreover, solidified tablet batches are analyzed for the purity of their coating by measuring the ibuprofen concentration. This optimization process is carried out through multiple stages of development and condition enhancements in order to produce the most pure tablet coating. As a result, a trial showing an almost purely coated tablet is presented here.

关键词： phase separation     melt crystallization     tablets     process optimization    

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标题 作者 时间 类型 操作

The feasibility of coating by cooling crystallization on ibuprofen naked tablets

Fatima Mameri, Ouahiba Koutchoukali, Mohamed Bouhelassa, Anne Hartwig, Leila Nemdili, Joachim Ulrich

期刊论文

Improved dissolution and anti-inflammatory effect of ibuprofen by solid dispersion

null

期刊论文

Isolation and application of an ibuprofen-degrading bacterium to a biological aerated filter for the

Bingjie Xu, Gang Xue, Xing Yang

期刊论文

Preparation of ibuprofen/lipid composite microparticles by supercritical fluid technique

WANG Xia, CHEN Hui, GUO Yanni, SU Yuzhong, WANG Hongtao, LI Jun

期刊论文

屈螺酮炔雌醇片预防稽留流产清宫术后宫腔粘连初步研究

赵现立,刘朝阳,谭宏伟,张恩娣

期刊论文

Utilizing melt crystallization fundamentals in the development of a new tabletting technology

Ahmed ABOUZEID,Sandra PETERSEN,Joachim ULRICH

期刊论文