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舒林酸二元体系对体外和体内释放曲线的影响：聚合物类型及其比例的评估

Effect of Sulindac Binary System on In Vitro and In Vivo Release Profiles: An Assessment of Polymer Type and Its Ratio.

作者信息

Shazly Gamal A

机构信息

Department of Pharmaceutics, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia; Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt.

出版信息

Biomed Res Int. 2016;2016:3182358. doi: 10.1155/2016/3182358. Epub 2016 Oct 20.

DOI:10.1155/2016/3182358
PMID:27840824
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5093299/
Abstract

The bioavailability of sulindac (SDC), a nonsteroidal anti-inflammatory drug, is low due to poor aqueous solubility and poor dissolution rate. For this reason it is necessary to enhance the solubility and enhance dissolution of the drug by dispersing SDC in polyethylene glycols 6000 (PEG 6000) and polyvinyl pyrrolidone 40000 (PVP 40000) matrices using the coevaporation technique. Studying the influence of SDC to polymer ratio on drug content, percent yield, particle size, and in vitro release was performed. Differential scanning calorimetry, X-ray diffraction, and scanning electron microscopy were used to characterize any change in crystal habit of SDC in the prepared formulae. The anti-inflammatory effect of SDC was studied using the hind paw edema model. It was found that incorporation of SDC in PEG 6000 and PVP 40000 matrices resulted in improving the dissolution rate, which was found to depend on the polymer and its weight ratio of the drug. It is clearly obvious that the dissolution rate was remarkably improved in drug PVP 40000 molecular dispersions when compared to drug PEG 6000 systems. Solid dispersion of SDC in PEG and PVP improved the anti-inflammatory effect of SDC and it was found that formula SDV5 exhibited a more pronounced inhibition of swelling than other formulae.

摘要

非甾体抗炎药舒林酸（SDC）的生物利用度较低，原因在于其水溶性差且溶解速率低。因此，有必要采用共蒸发技术将SDC分散于聚乙二醇6000（PEG 6000）和聚乙烯吡咯烷酮40000（PVP 40000）基质中，以提高药物的溶解度和溶出度。研究了SDC与聚合物比例对药物含量、产率、粒径和体外释放的影响。采用差示扫描量热法、X射线衍射法和扫描电子显微镜对所制备配方中SDC晶型的任何变化进行表征。利用后爪水肿模型研究了SDC的抗炎作用。结果发现，将SDC掺入PEG 6000和PVP 40000基质中可提高溶出速率，且溶出速率取决于聚合物及其与药物的重量比。显然，与药物PEG 6000体系相比，药物PVP 40000分子分散体中的溶出速率显著提高。SDC在PEG和PVP中的固体分散体提高了SDC的抗炎作用，且发现配方SDV5比其他配方对肿胀的抑制作用更明显。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2e32/5093299/c31266380836/BMRI2016-3182358.011.jpg
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1
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Int J Neurosci. 2011 Mar;121(3):142-8. doi: 10.3109/00207454.2010.537415. Epub 2010 Dec 8.
2
Solid dispersions: a review.固体分散体：综述
Pak J Pharm Sci. 2009 Apr;22(2):234-46.
3
Solid dispersions as strategy to improve oral bioavailability of poor water soluble drugs.固体分散体作为提高难溶性药物口服生物利用度的策略。
Drug Discov Today. 2007 Dec;12(23-24):1068-75. doi: 10.1016/j.drudis.2007.09.005. Epub 2007 Oct 30.
4
Sulindac induces apoptosis and inhibits tumor growth in vivo in head and neck squamous cell carcinoma.舒林酸可诱导头颈部鳞状细胞癌体内细胞凋亡并抑制肿瘤生长。
Neoplasia. 2007 Mar;9(3):192-9. doi: 10.1593/neo.06781.
5
Effect of hydrogen bonding interactions on the release mechanism of felodipine from nanodispersions with polyvinylpyrrolidone.氢键相互作用对非洛地平从与聚乙烯吡咯烷酮形成的纳米分散体中释放机制的影响。
Eur J Pharm Biopharm. 2006 Jun;63(2):103-14. doi: 10.1016/j.ejpb.2006.01.016. Epub 2006 May 3.
6
The "high solubility" definition of the current FDA Guidance on Biopharmaceutical Classification System may be too strict for acidic drugs.美国食品药品监督管理局（FDA）现行生物药剂学分类系统指南中“高溶解性”的定义对酸性药物而言可能过于严格。
Pharm Res. 2004 Feb;21(2):293-9. doi: 10.1023/b:pham.0000016242.48642.71.
7
Enhancement of dissolution rate and anti-inflammatory effects of piroxicam using solvent deposition technique.
Drug Dev Ind Pharm. 2002 Jul;28(6):681-6. doi: 10.1081/ddc-120003859.
8
The mechanisms of drug release from solid dispersions in water-soluble polymers.药物从水溶性聚合物固体分散体中的释放机制。
Int J Pharm. 2002 Jan 14;231(2):131-44. doi: 10.1016/s0378-5173(01)00891-2.
9
Interactions between carbamazepine and polyethylene glycol (PEG) 6000: characterisations of the physical, solid dispersed and eutectic mixtures.卡马西平与聚乙二醇（PEG）6000之间的相互作用：物理混合物、固体分散体和低共熔混合物的表征
Eur J Pharm Sci. 2001 Feb;12(4):395-404. doi: 10.1016/s0928-0987(00)00168-8.
10
Improving drug solubility for oral delivery using solid dispersions.使用固体分散体提高口服给药的药物溶解度。
Eur J Pharm Biopharm. 2000 Jul;50(1):47-60. doi: 10.1016/s0939-6411(00)00076-x.