水合强力西环素环糊精配合物的制备及表征

IF 1.7 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY
Mukesh Pandey, Priyanka Rani, Lokesh Adhikari, Mukul Gupta, Ajay Semalty, Mona Semalty
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引用次数: 2

摘要

水合多西环素是生物制药分类系统的第一类药物(高溶解度和高渗透性),但其光稳定性较差。它属于四环素类抗生素,用于治疗各种感染,但由于其对光的敏感性和水的不稳定性,其生物利用度受到损害。本文研究了不同环糊精(α - cd、γ - cd、HPβCD和RMβCD)的包合作用对水合强力西环素光稳定性的影响。采用冷冻干燥法制备了主-客体包合物。对所制配合物进行了药物含量、扫描电镜(SEM)、XRPD、体外渗透和光稳定性等表征。XRPD显示大多数配合物呈扩散峰,而SEM显示不规则形状的颗粒。D20(药物与γ - CD摩尔比为1:20)的药物含量最高(83.72±1.2%),D1(药物与α - CD摩尔比为1:2)的药物含量最低。结果表明,络合后,该药物的光降解明显降低。对于Drug: CD配合物,发现药物/CD配合物水溶液的光稳定性依次为γCD > RMβCD > HPβCD > αCD,其中药物:γCD(1:20摩尔比)配合物的光稳定性最大。结果表明,环糊精络合可作为提高水合强力霉素光稳定性的一种替代方法。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Preparation and characterization of cyclodextrin complexes of doxycycline hyclate for improved photostability in aqueous solution

Preparation and characterization of cyclodextrin complexes of doxycycline hyclate for improved photostability in aqueous solution

Doxycycline hyclate is Biopharmaceutical Classification System, class I drug (high solubility and high permeability), but it is associated with poor photostability. It is in the class of tetracycline antibiotic, which is used to treat various infections, but its bioavailability is compromised due to its sensitivity to light and aqueous instability. In this paper, the influence of inclusion complexation with different cyclodextrins, i.e., αCD, γCD, HPβCD and RMβCD, on the photostability of doxycycline hyclate in aqueous media was investigated. Host–guest inclusion complexes were prepared by freeze- drying method. The prepared complexes were characterized for drug content, SEM, XRPD, in vitro permeation studies and photostability studies. XRPD showed diffused peaks for most of the complexes, while SEM showed irregularly shaped particles. The formulation D20 (Drug: γCD in 1:20 molar ratio) showed the highest % drug content (83.72 ± 1.2%), and the formulations D1 (Drug: αCD in 1: 2 molar ratio) showed the lowest % drug content among all the CD complexes. It was found that the photodegradation of the drug was reduced significantly upon complexation. For Drug: CD complexes, the photostability of the aqueous solution of drug/CD complexes was found to be in the order of γCD > RMβCD > HPβCD > αCD with maximum photostability shown by Drug: γCD (1:20 molar ratio) complex. The obtained results suggested that cyclodextrin complexation can be used as an alternative approach for increasing the photostability of doxycycline hyclate.

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来源期刊
Journal of Inclusion Phenomena and Macrocyclic Chemistry
Journal of Inclusion Phenomena and Macrocyclic Chemistry Agricultural and Biological Sciences-Food Science
CiteScore
4.10
自引率
8.70%
发文量
54
期刊介绍: The Journal of Inclusion Phenomena and Macrocyclic Chemistry is the premier interdisciplinary publication reporting on original research into all aspects of host-guest systems. Examples of specific areas of interest are: the preparation and characterization of new hosts and new host-guest systems, especially those involving macrocyclic ligands; crystallographic, spectroscopic, thermodynamic and theoretical studies; applications in chromatography and inclusion polymerization; enzyme modelling; molecular recognition and catalysis by inclusion compounds; intercalates in biological and non-biological systems, cyclodextrin complexes and their applications in the agriculture, flavoring, food and pharmaceutical industries; synthesis, characterization and applications of zeolites. The journal publishes primarily reports of original research and preliminary communications, provided the latter represent a significant advance in the understanding of inclusion science. Critical reviews dealing with recent advances in the field are a periodic feature of the journal.
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