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使用圭亚那牛乳树(桑科)标准化液体提取物制备丸剂。

Obtainment of pellets using the standardized liquid extract of Brosimum gaudichaudii Trécul (Moraceae).

作者信息

Filho Omar Paulino Silva, Oliveira Leandra Almeida Ribeiro, Martins Frederico Severino, Borges Leonardo Luiz, de Freitas Osvaldo, da Conceição Edemilson Cardoso

机构信息

Laboratory of Research, Development and Inovation on Bioproducts, Faculty of Pharmacy, Federal University of Goiás, Brazil.

Laboratory of Research, Development and Pharmacotechnical, Faculty of Pharmaceutical Science from Ribeirão Preto, University of São Paulo, Brazil.

出版信息

Pharmacogn Mag. 2015 Jan-Mar;11(41):170-5. doi: 10.4103/0973-1296.149734.

DOI:10.4103/0973-1296.149734
PMID:25709229
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4329620/
Abstract

BACKGROUND

The standardized liquid extract of Brosimum gaudichaudii Trécul is an alternative for the treatment of vitiligo. There is a shortage of solid oral dosage forms developed from standardized extracts of this plant specie.

OBJECTIVE

This study is aimed to obtain pellets with a standardized liquid extract of B. gaudichaudii.

RESULTS

The standardized liquid extract of B. gaudichaudii was obtained through maceration and percolation with a 55% ethanol-water solution (v/v). Pellets were obtained through a mixture of extract of 500 g of B. gaudichaudii standardized extract, 500 g of microcrystalline cellulose PH101 and 10 g of hydroxypropyl methylcellulose K100. The pellets obtained presented a homogeneity yield of 92%, aspect ratio of 1.16 ± 0.65, shape fator e R of 0.35 ± 0.09 and Feret diammeter of 0.87 ± 0.27. These pellets were coated with a suspension composed of titanium dioxide, aluminum red lacquer, ethyl cellulose, talc and magnesium stearate. Before the photostability test, the uncoated pellets showed psoralen content equal to 0.13 ± 0.01% and to the 5-MOP was 1.40 ± 0.27%. After exposure to one level (3 J.cm(-2)) of UVB irradiation the uncoated pellets presented a degradation of 2.16% of psoralen and 8.1% of 5-MOP. After exposure to three levels (10, 20 and 30 J.cm(-2)) of UVA irradiation the uncoated pellets exhibited photodegradation of 9.78, 17.64, 24.21% of psoralen and 18.95, 23.68, 28.48% for 5-MOP. The coated pellets where unaffected after photostability test.

CONCLUSION

Pellets were obtained with the standardized liquid extract of B. gaudichaudii and coating is a technological alternative to ensure the stability of the formula.

摘要

背景

圭亚那牛乳树标准化液体提取物是治疗白癜风的一种替代药物。目前缺乏由该植物标准化提取物开发的固体口服剂型。

目的

本研究旨在制备含有圭亚那牛乳树标准化液体提取物的微丸。

结果

通过用55%乙醇 - 水溶液(v/v)浸渍和渗漉获得圭亚那牛乳树标准化液体提取物。通过将500 g圭亚那牛乳树标准化提取物、500 g微晶纤维素PH101和10 g羟丙基甲基纤维素K100混合制备微丸。所制备的微丸均匀性收率为92%,纵横比为1.16±0.65,形状因子e R为0.35±0.09,费雷特直径为0.87±0.27。这些微丸用由二氧化钛、铝红漆、乙基纤维素、滑石粉和硬脂酸镁组成的混悬液包衣。在光稳定性试验前,未包衣微丸的补骨脂素含量为0.13±0.01%,5 - 甲氧补骨脂素含量为1.40±0.27%。在暴露于一个水平(3 J.cm(-2))的UVB照射后,未包衣微丸的补骨脂素降解2.16%,5 - 甲氧补骨脂素降解8.1%。在暴露于三个水平(10、20和30 J.cm(-2))的UVA照射后,未包衣微丸的补骨脂素光降解分别为9.78%、17.64%、24.21%,5 - 甲氧补骨脂素分别为18.95%、23.68%、28.48%。光稳定性试验后包衣微丸未受影响。

结论

成功制备了含有圭亚那牛乳树标准化液体提取物的微丸,包衣是确保制剂稳定性的一种技术手段。

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