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含丁香酚用于治疗牙周疾病的黏膜黏附片的研制与评价

Formulation and evaluation of mucoadhesive tablets containing eugenol for the treatment of periodontal diseases.

作者信息

Jadhav Bhimrao K, Khandelwal Kishanchandra R, Ketkar Anant R, Pisal Sambhaji S

机构信息

Department of Pharmacognosy, Poona College of Pharmacy, Bharati Vidyapeeth Deemed University, Erandwane, Pune, Maharashtra State, India.

出版信息

Drug Dev Ind Pharm. 2004 Feb;30(2):195-203. doi: 10.1081/ddc-120028715.

DOI:10.1081/ddc-120028715
PMID:15089054
Abstract

Eugenol is the principle chemical constituent of clove oil and has been used to cure dental problems for ages. Eugenol is an integral part of the dentist's kit due to its analgesic, local anesthetic, anti-inflammatory, and antibacterial effects. It is used in the form of a paste or mixture as dental cement, filler, and restorative material. This study reports the development and evaluation of controlled-release mucoadhesive tablets for gingival application, containing eugenol, which are prepared by taking carbopol 934 P and Hydroxypropyl methylcellulose (HPMC) K4M in the ratio of 1:2, 1:1, and 2:1. Incorporation of eugenol (10 mg) in a mucoadhesive formulation provides controlled release for a period of 8 hours, which is advantageous over conventional use. In vitro mucoadhesion measured as detachment force in grams and the formulations show good correlation in vivo. The release study indicates that increase in carbopol increases the release rate of eugenol from the formulation whereas HPMC retards it. Increased in vitro bioadhesion is related to HPMC content of the formulation. The release kinetics of eugenol in vitro correlates with the in vivo results. This indicates the increased potential of eugenol as antibacterial, local analgesic, and anaesthetic treatment.

摘要

丁香酚是丁香油的主要化学成分,长期以来一直用于治疗牙科问题。由于其具有止痛、局部麻醉、抗炎和抗菌作用,丁香酚是牙医工具包中不可或缺的一部分。它以糊剂或混合物的形式用作牙科粘固粉、填充剂和修复材料。本研究报告了含丁香酚的牙龈用控释粘膜粘附片的研制与评价,该片剂采用卡波姆934P和羟丙基甲基纤维素(HPMC)K4M按1:2、1:1和2:1的比例制备。在粘膜粘附制剂中加入丁香酚(10毫克)可实现8小时的控释,这比传统用法更具优势。体外粘膜粘附力以克为单位的脱离力来衡量,并且这些制剂在体内显示出良好的相关性。释放研究表明,卡波姆的增加会提高丁香酚从制剂中的释放速率,而HPMC则会使其延缓。体外生物粘附性的增加与制剂中HPMC的含量有关。丁香酚的体外释放动力学与体内结果相关。这表明丁香酚作为抗菌、局部止痛和麻醉治疗的潜力有所增加。

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