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通过基于多糖壳聚糖的粉末颗粒工程的逐步变化来定制药物释放特性。

Tailoring Drug Release Properties by Gradual Changes in the Particle Engineering of Polysaccharide Chitosan Based Powders.

作者信息

Do Nascimento Ednaldo G, De Caland Lilia B, De Medeiros Arthur S A, Fernandes-Pedrosa Matheus F, Soares-Sobrinho José L, Dos Santos Kátia S C R, Da Silva-Júnior Arnóbio Antonio

机构信息

Laboratory of Pharmaceutical Technology and Biotechnology, Department of Pharmacy, Federal University of Rio Grande do Norte, UFRN, Gal. Gustavo Cordeiro de Farias, Petropolis, Natal 59072-570, RN, Brazil.

Department of Pharmacy, Center of Health Sciences, Federal University of Pernambuco, Professor Moraes Rego 1235, Recife 50670-901, PE, Brazil.

出版信息

Polymers (Basel). 2017 Jun 29;9(7):253. doi: 10.3390/polym9070253.

Abstract

Chitosan is a natural copolymer generally available in pharmaceutical and food powders associated with drugs, vitamins, and nutraceuticals. This study focused on monitoring the effect of the morphology and structural features of the chitosan particles for controlling the release profile of the active pharmaceutical ingredient (API) propranolol hydrochloride. Chitosan with distinct molecular mass (low and medium) were used in the formulations as crystalline and irregular particles from commercial raw material, or as spherical, uniform, and amorphous spray-dried particles. The API⁻copolymer interactions were assessed when adding the drug before (drug-loaded particles) or after the spray drying (only mixed with blank particles). The formulations were further compared with physical mixtures of the API with chitin and microcrystalline cellulose. The scanning electron microscopy (SEM) images, surface area, particle size measurements, X-ray diffraction (XRD) analysis and drug loading have supported the drug release behavior. The statistical analysis of experimental data demonstrated that it was possible to control the drug release behavior (immediate or slow drug release) from chitosan powders using different types of particles.

摘要

壳聚糖是一种天然共聚物,通常存在于与药物、维生素和营养保健品相关的药用和食品粉末中。本研究重点监测壳聚糖颗粒的形态和结构特征对活性药物成分(API)盐酸普萘洛尔释放曲线的控制作用。具有不同分子量(低和中)的壳聚糖以商业原料的结晶和不规则颗粒形式,或作为球形、均匀且无定形的喷雾干燥颗粒用于制剂中。在喷雾干燥之前(载药颗粒)或之后(仅与空白颗粒混合)加入药物时,评估了API与共聚物的相互作用。将这些制剂进一步与API与几丁质和微晶纤维素的物理混合物进行比较。扫描电子显微镜(SEM)图像、表面积、粒度测量、X射线衍射(XRD)分析和载药量均支持了药物释放行为。实验数据的统计分析表明,使用不同类型的颗粒可以控制壳聚糖粉末的药物释放行为(速释或缓释)。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5ca4/6431873/e5d16f288d34/polymers-09-00253-g001.jpg

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