Al-Ghananeem Abeer M, Leung Kai P, Faraj Jabar, DeLuca Patrick P
College of Pharmacy, Department of Pharmaceutical Technology, Jordan University of Science and Technology, Irbid, 22110, Jordan.
Dental and Craniofacial Trauma Research and Tissue Regeneration Directorate, Institute of Surgical Research, 3650 Chambers Pass, Bldg 3611, JBSA Fort Sam, Houston, Texas, 78234, USA.
AAPS PharmSciTech. 2017 Aug;18(6):2240-2247. doi: 10.1208/s12249-016-0706-9. Epub 2017 Jan 9.
The objective of this paper was to design a chewing gum formulation delivery system in situations where typical dental hygiene practice is not practical. Thus, an analog of decapeptide KSL (KSL-W), known to possess antimicrobial and antiplaque activity, was incorporated into a chewing gum formulation containing cetylpyridinium chloride (CPC). The effect of the excipients, xylitol, and peppermint oil on active ingredients in vitro release was also assessed. Gum formulations were prepared with different excipient parameters, including heating xylitol and gum base at 65 or 85°C, using ground and unground xylitol, and the addition of 1.5, 3, and 7% peppermint oil, to determine the effect of these changes on the in vitro release of KSL-W and CPC using a chewing machine. The antimicrobial and antiplaque activities of solutions released from chewed gum formulation as well as prepared standard solutions with different concentrations were tested against placebo. The optimal temperature to avoid crystallization of xylitol during preparation was 65°C. Grinding xylitol to 104.5 μm improved release of active ingredients as compared to commercially unground xylitol. Peppermint oil had opposite effects on release of KSL-W and CPC. Peppermint oil at 1.5% was determined to be suitable (91 and 88% of KSL-W and CPC released, respectively, after 40 min). The gum formulation illustrated good sustained release of KSL-W and CPC with antibacterial and antiplaque activities after chewing. An effective antimicrobial and antiplaque chewing gum formulation was developed. This formulation has the potential to overcome oral hygiene issues in those unable to follow normal dental protocols.
本文的目的是设计一种在常规口腔卫生措施不可行的情况下的口香糖制剂递送系统。因此，将已知具有抗菌和抗牙菌斑活性的十肽KSL类似物（KSL-W）加入到含有十六烷基氯化吡啶（CPC）的口香糖制剂中。还评估了辅料木糖醇和薄荷油对活性成分体外释放的影响。制备了具有不同辅料参数的口香糖制剂，包括在65或85°C下加热木糖醇和胶基、使用磨碎和未磨碎的木糖醇，以及添加1.5%、3%和7%的薄荷油，以使用咀嚼机确定这些变化对KSL-W和CPC体外释放的影响。测试了从咀嚼口香糖制剂中释放的溶液以及制备的不同浓度标准溶液对安慰剂的抗菌和抗牙菌斑活性。制备过程中避免木糖醇结晶的最佳温度为65°C。与市售未磨碎的木糖醇相比，将木糖醇磨碎至104.5μm可改善活性成分的释放。薄荷油对KSL-W和CPC的释放有相反的影响。确定1.5%的薄荷油是合适的（40分钟后分别释放91%和88%的KSL-W和CPC）。该口香糖制剂在咀嚼后显示出KSL-W和CPC具有良好的缓释性以及抗菌和抗牙菌斑活性。开发了一种有效的抗菌和抗牙菌斑口香糖制剂。该制剂有可能克服那些无法遵循正常口腔护理方案的人群的口腔卫生问题。
