改善替米沙坦溶出的液固压剂的制备与表征。

Journal of drug delivery Pub Date : 2014-01-01 Epub Date: 2014-10-12 DOI:10.1155/2014/692793
Naveen Chella, Nataraj Narra, Tadikonda Rama Rao
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引用次数: 37

摘要

目前工作的目的是获得pH独立和改进的溶解谱为一种难溶性药物,替米沙坦使用液体固体压片。以Transcutol HP为载体,Avicel PH102为载体,Aerosil 200为涂层材料制备了液固压片。采用傅里叶变换红外光谱(FTIR)、差示扫描量热法(DSC)、x射线衍射(XRD)、静置角和各种药理学试验对处方进行了药物赋形剂相互作用、药物结晶度变化、流动特性和片剂的一般质量控制测试。体外溶出研究在三种pH条件下进行(1.2,4.5和7.4)。稳定性研究在40°C和75% RH下进行了三个月。该制剂被发现符合印度药典片剂的限制。FTIR研究证实药物和辅料之间没有相互作用。XRD和DSC研究表明药物的结晶度发生了变化/降低。根据溶解度研究选择溶出介质。优化后的处方具有pH不依赖性释放曲线,溶出度较普通药和常规上市处方有显著提高(P < 0.005)。贮存3个月后,两种药物的性质和释放情况无显著差异。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Preparation and characterization of liquisolid compacts for improved dissolution of telmisartan.

Preparation and characterization of liquisolid compacts for improved dissolution of telmisartan.

Preparation and characterization of liquisolid compacts for improved dissolution of telmisartan.

Preparation and characterization of liquisolid compacts for improved dissolution of telmisartan.

The objective of the present work was to obtain pH independent and improved dissolution profile for a poorly soluble drug, telmisartan using liquisolid compacts. Liquisolid compacts were prepared using Transcutol HP as vehicle, Avicel PH102 as carrier, and Aerosil 200 as a coating material. The formulations were evaluated for drug excipient interactions, change in crystallinity of drug, flow properties, and general quality control tests of tablets using Fourier transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), X-ray diffraction (XRD), angle of repose, and various pharmacopoeial tests. In vitro dissolution studies were performed at three pH conditions (1.2, 4.5 and 7.4). Stability studies were performed at 40°C and 75% RH for three months. The formulation was found to comply with Indian pharmacopoeial limits for tablets. FTIR studies confirmed no interaction between drug and excipients. XRD and DSC studies indicate change/reduction in crystallinity of drug. Dissolution media were selected based on the solubility studies. The optimized formulation showed pH independent release profile with significant improvement (P < 0.005) in dissolution compared to plain drug and conventional marketed formulation. No significant difference was seen in the tablet properties, and drug release profile after storage for 3 months.

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来源期刊
Journal of drug delivery
Journal of drug delivery PHARMACOLOGY & PHARMACY-
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