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一种与软胶囊（Avodart）生物等效的薄膜包衣度他雄胺片的制剂：γ-环糊精和增溶剂的作用

Formulation of a film-coated dutasteride tablet bioequivalent to a soft gelatin capsule (Avodart): Effect of γ-cyclodextrin and solubilizers.

作者信息

Min Mi-Hong, Park Jin-Hyong, Choi Mi-Ran, Hur Jong-Hyun, Ahn Byung-Nak, Kim Dae-Duk

机构信息

College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul 08826, Republic of Korea.

Central Research Institute, Whanin Pharmaceutical Company, 4F, GBSA, 107 Gwanggyo-ro, Yeongtong-gu, Suwon 16229, Republic of Korea.

出版信息

Asian J Pharm Sci. 2019 May;14(3):313-320. doi: 10.1016/j.ajps.2018.08.007. Epub 2018 Oct 5.

DOI:10.1016/j.ajps.2018.08.007
PMID:32104461
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7032202/
Abstract

The aim of this study was to optimize a tablet formulation of dutasteride that is bioequivalent to a commercially available soft gelatin capsule (Avodart). The effect of cyclodextrin on enhancing the aqueous solubility of dutasteride was investigated, after which the formulation was further optimized with solubilizing polymer and surfactant. Among the cyclodextrins tested, the highest solubility was observed when dutasteride was complexed with γ-cyclodextrin. Moreover, the addition of polyvinylpyrrolidone and Gelucire/TPGS further enhanced the solubility of dutasteride. Differential scanning calorimetry (DSC) and powder X-ray diffraction (pXRD) studies demonstrated that dutasteride existed in the amorphous form in the complex. Optimized dutasteride complexes were selected after a pharmacokinetic study in rats, and film-coated tablets were prepared by the direct compression method. dissolution profiles for the tablets of dutasteride complexes were similar to those of the reference. Moreover, pharmacokinetic parameters including the and values after oral administration in beagle dogs were not significantly different from those of the reference with a relative bioavailability of 92.4%. These results suggest the feasibility of developing a tablet formulation of dutasteride using cyclodextrin complex in addition to a solubilizing polymer and surfactant.

摘要

本研究的目的是优化度他雄胺的片剂制剂，使其与市售软胶囊（阿夫唑嗪）具有生物等效性。研究了环糊精对提高度他雄胺水溶性的影响，之后用增溶聚合物和表面活性剂对制剂进行了进一步优化。在所测试的环糊精中，度他雄胺与γ-环糊精形成复合物时观察到最高溶解度。此外，添加聚乙烯吡咯烷酮和Gelucire/TPGS进一步提高了度他雄胺的溶解度。差示扫描量热法（DSC）和粉末X射线衍射（pXRD）研究表明，度他雄胺在复合物中以无定形形式存在。在大鼠体内进行药代动力学研究后，选择了优化的度他雄胺复合物，并通过直接压片法制备了薄膜包衣片。度他雄胺复合物片剂的溶出曲线与参比制剂相似。此外，在比格犬口服给药后的药代动力学参数，包括 和 值，与参比制剂无显著差异，相对生物利用度为92.4%。这些结果表明，除了增溶聚合物和表面活性剂外，使用环糊精复合物开发度他雄胺片剂制剂是可行的。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3407/7032202/085a4f474d94/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3407/7032202/ee823bfa5dc5/fx1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3407/7032202/10c81b4434d2/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3407/7032202/2e807fcb474b/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3407/7032202/120c1e3cd34f/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3407/7032202/8a0d8f92e897/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3407/7032202/085a4f474d94/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3407/7032202/ee823bfa5dc5/fx1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3407/7032202/10c81b4434d2/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3407/7032202/2e807fcb474b/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3407/7032202/120c1e3cd34f/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3407/7032202/8a0d8f92e897/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3407/7032202/085a4f474d94/gr5.jpg

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本文引用的文献

1
Cyclodextrins in pharmaceutical formulations I: structure and physicochemical properties, formation of complexes, and types of complex.药物制剂中的环糊精I：结构与物理化学性质、配合物的形成及配合物类型
Drug Discov Today. 2016 Feb;21(2):356-62. doi: 10.1016/j.drudis.2015.11.017. Epub 2015 Dec 11.
2
Cyclodextrin nanoassemblies: a promising tool for drug delivery.环糊精纳米组装体：一种有前途的药物传递工具。
Drug Discov Today. 2015 Sep;20(9):1120-6. doi: 10.1016/j.drudis.2015.05.008. Epub 2015 May 30.
3
Analytical techniques for characterization of cyclodextrin complexes in the solid state: A review.
固态环糊精配合物表征的分析技术：综述
J Pharm Biomed Anal. 2015 Sep 10;113:226-38. doi: 10.1016/j.jpba.2015.01.058. Epub 2015 Feb 9.
4
Preparation, characterization and stability study of dutasteride loaded nanoemulsion for treatment of benign prostatic hypertrophy.用于治疗良性前列腺增生的度他雄胺纳米乳剂的制备、表征及稳定性研究
Iran J Pharm Res. 2014 Fall;13(4):1125-40.
5
Improved oral absorption of dutasteride via Soluplus®-based supersaturable self-emulsifying drug delivery system (S-SEDDS).通过基于固体分散体聚合物（Soluplus®）的过饱和自乳化药物递送系统（S-SEDDS）提高度他雄胺的口服吸收。
Int J Pharm. 2015 Jan 15;478(1):341-347. doi: 10.1016/j.ijpharm.2014.11.060. Epub 2014 Nov 28.
6
Influence of hydrophilic additives on the supersaturation and bioavailability of dutasteride-loaded hydroxypropyl-β-cyclodextrin nanostructures.亲水添加剂对载度他司特羟丙基-β-环糊精纳米结构的过饱和度和生物利用度的影响。
Int J Nanomedicine. 2013;8:2029-39. doi: 10.2147/IJN.S44795. Epub 2013 May 20.
7
Cyclodextrin-water soluble polymer ternary complexes enhance the solubility and dissolution behaviour of poorly soluble drugs. Case example: itraconazole.环糊精-水溶性聚合物三元配合物提高了难溶性药物的溶解度和溶解行为。案例：伊曲康唑。
Eur J Pharm Biopharm. 2013 Apr;83(3):378-87. doi: 10.1016/j.ejpb.2012.11.003. Epub 2012 Nov 28.
8
Cyclodextrins.环糊精。
Int J Pharm. 2013 Aug 30;453(1):167-80. doi: 10.1016/j.ijpharm.2012.06.055. Epub 2012 Jul 5.
9
Soft gelatin capsules (softgels).软胶囊（软胶囊剂）。
J Pharm Sci. 2010 Oct;99(10):4107-48. doi: 10.1002/jps.22151.
10
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