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体外和体内评价有序介孔硅作为一种新型的吸附剂在液固体制剂中的应用。

In vitro and in vivo evaluation of ordered mesoporous silica as a novel adsorbent in liquisolid formulation.

机构信息

School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, People's Republic of China.

出版信息

Int J Nanomedicine. 2012;7:199-209. doi: 10.2147/IJN.S26763. Epub 2012 Jan 6.

DOI:10.2147/IJN.S26763
PMID:22275835
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3263412/
Abstract

BACKGROUND

A liquisolid technique has been reported to be a new approach to improve the release of poorly water-soluble drugs for oral administration. However, an apparent limitation of this technique is the formulation of a high dose because a large amount of liquid vehicle is needed, which finally results in a low-dose liquisolid formulation. Silica as an absorbent has been used extensively in liquisolid formulations. Although nanoparticle silica can be prepared and used to improve liquid adsorption capacity, loading a high dose of drug into a liquisolid is still a challenge. With the aim of improving adsorption capacity and accordingly achieving high drug loading, ordered mesoporous silica with a high surface area and narrow pore size distribution was synthesized and used in a liquisolid formulation.

METHODS

Ordered mesoporous silica was synthesized and its particle size and morphology were tailored by controlling the concentration of cetyltrimethyl ammonium bromide. The ordered mesoporous silica synthesized was characterized by transmission electron microscopy, scanning electron microscopy, Fourier transform infrared spectroscopy, small-angle x-ray diffraction, wide angle x-ray diffraction, and nitrogen adsorption-desorption measurements. The liquid adsorption capacity of ordered mesoporous silica was subsequently compared with that of conventional silica materials using PEG400 as the model liquid. Carbamazepine was chosen as a model drug to prepare the liquisolid formulation, with ordered mesoporous silica as the adsorbent material. The preparation was evaluated and compared with commercially available fast-release carbamazepine tablets in vitro and in vivo.

RESULTS

Characterization of the ordered mesoporous silica synthesized in this study indicated a huge Brunauer-Emmett-Teller surface area (1030 m(2)/g), an ordered mesoporous structure with a pore size of 2.8 nm, and high adsorption capacity for liquid compared with conventional silica. Compared with fast-release commercial carbamazepine tablets, drug release from the liquisolid capsules was greatly improved, and the bioavailability of the liquisolid preparation was enhanced by 182.7%.

CONCLUSION

Ordered mesoporous silica is a potentially attractive adsorbent which may lead to a new approach for development of liquisolid products.

摘要

背景

液质技术已被报道为改善口服难溶性药物释放的新方法。然而，这种技术的一个明显限制是制剂的高剂量，因为需要大量的液体载体，最终导致低剂量的液质制剂。二氧化硅作为一种吸收剂已广泛应用于液质制剂中。虽然纳米二氧化硅可以制备并用于提高液体吸附能力，但将高剂量药物载入液质制剂仍然是一个挑战。为了提高吸附能力并相应地实现高药物负载，我们合成了具有高表面积和窄孔径分布的有序介孔硅，并将其用于液质制剂中。

方法

通过控制十六烷基三甲基溴化铵的浓度来合成有序介孔硅，并对其粒径和形貌进行了调整。采用透射电子显微镜、扫描电子显微镜、傅里叶变换红外光谱、小角 X 射线衍射、广角 X 射线衍射和氮气吸附-脱附测量对合成的有序介孔硅进行了表征。随后，使用 PEG400 作为模型液体，比较了有序介孔硅与常规硅材料的液体吸附能力。选择卡马西平作为模型药物，以有序介孔硅为吸附剂材料，制备液质制剂，并对其进行评价，与市售速释卡马西平片进行了体外和体内比较。

结果

本研究合成的有序介孔硅的表征表明其具有巨大的 Brunauer-Emmett-Teller 比表面积（1030 m²/g）、孔径为 2.8nm 的有序介孔结构和高液体吸附能力，与常规硅相比。与市售速释卡马西平片相比，液质胶囊中的药物释放得到了极大的改善，液质制剂的生物利用度提高了 182.7%。

结论

有序介孔硅是一种有吸引力的潜在吸附剂，可能为液质制剂的开发提供新方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e269/3263412/dc417d7c4978/ijn-7-199f9.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e269/3263412/85cebce6dcf5/ijn-7-199f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e269/3263412/06787b085525/ijn-7-199f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e269/3263412/adbc46ce1ef4/ijn-7-199f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e269/3263412/7eb29729befd/ijn-7-199f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e269/3263412/91b73c31d2e0/ijn-7-199f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e269/3263412/3b04d11ab18d/ijn-7-199f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e269/3263412/a75d9c0d43e3/ijn-7-199f7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e269/3263412/3c9ae8765b35/ijn-7-199f8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e269/3263412/dc417d7c4978/ijn-7-199f9.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e269/3263412/85cebce6dcf5/ijn-7-199f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e269/3263412/06787b085525/ijn-7-199f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e269/3263412/adbc46ce1ef4/ijn-7-199f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e269/3263412/7eb29729befd/ijn-7-199f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e269/3263412/91b73c31d2e0/ijn-7-199f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e269/3263412/3b04d11ab18d/ijn-7-199f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e269/3263412/a75d9c0d43e3/ijn-7-199f7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e269/3263412/3c9ae8765b35/ijn-7-199f8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e269/3263412/dc417d7c4978/ijn-7-199f9.jpg

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