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盐酸利多卡因环糊精包合物的制备与评价，旨在开发与葡萄糖酸洗必泰联合用于泌尿生殖道的稳定凝胶。

Preparation and evaluation of lidocaine hydrochloride in cyclodextrin inclusion complexes for development of stable gel in association with chlorhexidine gluconate for urogenital use.

机构信息

Departamento de Medicamentos, Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, Brazil.

出版信息

Int J Nanomedicine. 2011;6:1143-54. doi: 10.2147/IJN.S20409. Epub 2011 Jun 3.

DOI:10.2147/IJN.S20409
PMID:21822378
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3148842/
Abstract

Inclusions of lidocaine hydrochloride in cyclodextrins were prepared to obtain stable complexes compatible for association with chlorhexidine in a new gel formulation for use in urogenital applications. Two cyclodextrins, β-cyclodextrin and methyl-β-cyclodextrin, were used for encapsulating lidocaine hydrochloride through solubilization and kneading techniques. The lidocaine-cyclodextrin complexes were characterized by ultraviolet spectroscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction. The results revealed that the techniques generated good yields of inclusion products that maintained the functional properties of lidocaine. In addition, the inclusion products obtained improved the compatibility of lidocaine hydrochloride with chlorhexidine in solution and a gel formulation. The gel formulation displayed desirable rheological and physicochemical properties. The results presented here are the first description of the inclusion of lidocaine with cyclodextrins, which improves compatibility with chlorhexidine in formulations for simultaneous delivery.

摘要

盐酸利多卡因包合于环糊精中，以获得稳定的配合物，与洗必泰在新的凝胶制剂中相容，用于泌尿生殖应用。使用β-环糊精和甲基-β-环糊精两种环糊精通过增溶和捏合技术包合盐酸利多卡因。通过紫外光谱、傅里叶变换红外光谱、差示扫描量热法和 X 射线衍射对利多卡因-环糊精配合物进行了表征。结果表明，这些技术产生了具有良好收率的包含产物，这些产物保持了利多卡因的功能特性。此外，所得包含产物提高了盐酸利多卡因与溶液和凝胶制剂中洗必泰的相容性。凝胶制剂表现出理想的流变学和物理化学性质。这里呈现的结果是首次描述了将利多卡因与环糊精包合，从而改善了与洗必泰在同时递药配方中的相容性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7491/3148842/213bc3311b42/ijn-6-1143f8.jpg
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