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含蜂胶治疗牙周病的半固体系统:体外释放动力学、可注射性、流变学、质地和黏膜黏附特性

Semisolid systems containing propolis for the treatment of periodontal disease: in vitro release kinetics, syringeability, rheological, textural, and mucoadhesive properties.

作者信息

Bruschi Marcos L, Jones David S, Panzeri Heitor, Gremião Maria P D, de Freitas Osvaldo, Lara Elza H G

机构信息

Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Av. Zeferino Vaz, s/n, CEP 14040-903, Ribeirão Preto, SP, Brazil.

出版信息

J Pharm Sci. 2007 Aug;96(8):2074-89. doi: 10.1002/jps.20843.

Abstract

Formulations containing poloxamer 407 (P407), carbopol 934P (C934P), and propolis extract (PE) were designed for the treatment of periodontal disease. Gelation temperature, in vitro drug release, rheology, hardness, compressibility, adhesiveness, mucoadhesion, and syringeability of formulations were determined. Propolis release from formulations was controlled by the phenomenon of relaxation of polymer chains. Formulations exhibited pseudoplastic flow and low degrees of thixotropy or rheopexy. In most samples, increasing the concentration of C934P content significantly increased storage modulus (G'), loss modulus (G''), and dynamic viscosity (eta'), at 5 degrees C, G'' exceeded G'. At 25 and 37 degrees C, eta' of each formulation depended on the oscillatory frequency. Formulations showed thermoresponsive behavior, existing as a liquid at room temperature and gel at 34-37 degrees C. Increasing the C934P content or temperature significantly increased formulation hardness, compressibility, and adhesiveness. The greatest mucoadhesion was noted in the formulation containing 15% P407 (w/w) and 0.25% C934P (w/w). The work of syringeability values of all formulations were similar and very desirable with regard to ease of administration. The data obtained in these formulations indicate a potentially useful role in the treatment of periodontitis and suggest they are worthy of clinical evaluation.

摘要

设计了含有泊洛沙姆407(P407)、卡波姆934P(C934P)和蜂胶提取物(PE)的制剂用于治疗牙周疾病。测定了制剂的胶凝温度、体外药物释放、流变学、硬度、可压缩性、粘附性、粘膜粘附性和可注射性。制剂中蜂胶的释放受聚合物链松弛现象的控制。制剂表现出假塑性流动以及低程度的触变性或流凝性。在大多数样品中,增加C934P的含量会显著提高储能模量(G')、损耗模量(G'')和动态粘度(η'),在5℃时,G''超过G'。在25℃和37℃时,每种制剂的η'取决于振荡频率。制剂表现出热响应行为,在室温下为液体,在34 - 37℃时为凝胶。增加C934P的含量或温度会显著提高制剂的硬度、可压缩性和粘附性。在含有15% P407(w/w)和0.25% C934P(w/w)的制剂中观察到最大的粘膜粘附性。所有制剂的可注射性功值相似,且在给药便利性方面非常理想。在这些制剂中获得的数据表明其在治疗牙周炎方面具有潜在的有用作用,并表明它们值得进行临床评估。

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