Techniques to develop and characterize nanosized formulation for salbutamol sulfate
Techniques to develop and characterize nanosized formulation for salbutamol sulfate
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DOI：
10.1007/s10856-008-3483-5
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发表时间：
2009-12-01
影响因子：
3.7
通讯作者：
Bhatnagar, A.
中科院分区：
文献类型：
--
作者：
Bhavna;Ahmad, F. J.;Bhatnagar, A.
本研究涉及提高通过肺吸入施用的药物干粉制剂的给药效率。特别地，该研究涉及通过形成硫酸沙丁胺醇（SBM）的纳米级颗粒来提供干粉吸入器（DPI），以增加药物在肺中的渗透性和沉积。选择SBM，一种抗哮喘药，通过不同的技术如溶剂化、高压均质化和喷雾干燥开发成纳米尺寸的制剂，然后基于颗粒形状、颗粒尺寸和颗粒尺寸分布对其进行比较。在溶剂化方法的情况下，通过将SBM分散到非溶剂中并加入Tween-80作为表面活性剂以防止团聚来制备纳米悬浮液，其中获得的颗粒在2-10 μ m的范围内。第二次尝试是通过使SBM的悬浮液在10，000 - 15，000 psi下通过高压均化器。发现在Tween-80作为表面活性剂的存在下进行六个循环的均质化处理得到尺寸范围为50-100 nm的纳米混悬液。该技术的唯一缺点似乎是产品收率低和加工时间长（3-4 h）。为了克服该缺点，进一步探索了喷雾干燥技术;将含有Tween-80的SBM溶液在磁力搅拌器上以1，200 rpm搅拌，并最终通过使用喷雾干燥器在75 A ° C和56 A ° C的入口和出口温度下分别干燥。喷雾干燥器的进料速率保持为91 ml/h。收集样品并分析粒度分布，发现其在50-100 nm范围内。考虑到在更高的收率和更短的加工时间方面的积极结果，采用喷雾干燥技术给出优化的处方。通过透射电子显微镜（TEM）、扫描电子显微镜（SEM）和准弹性光散射（QELS）技术分别评价由此获得的纳米级颗粒的粒度、表面拓扑结构和粒度分布。纳米颗粒进行调查的变化上的粉末的物理稳定性，这种不同的分析方法被用来作为：傅里叶变换红外光谱（FT-IR），差示扫描量热法（DSC）和X射线衍射（XRD）分析，因此结果表明，有没有物理差异时，与商业SBM样品相比。
The present study relates to enhancing the dosing efficiency of pharmaceutical dry powder formulations administered by pulmonary inhalation. In particular, the study relates to the provision of dry powder inhalers (DPI) by forming nanosized particles of salbutamol sulfate (SBM) in order to augment the drug penetrability and deposition in the lungs. SBM, an antiasthmatic was selected to be developed into a nanosized formulation by different techniques like solvation, high-pressure homogenization, and spray drying, which were then compared on the basis of particle shape, particle size, and particle size distribution. In case of solvation method the nanosuspension was prepared by dispersing SBM into a nonsolvent and adding Tween-80 as a surfactant to prevent the agglomeration, the particles obtained therein were in the range of 2-10 mu. The second attempt was made by passing the suspension of SBM through high-pressure homogenizer at 10,000-15,000 psi. A treatment of six cycles of homogenization in presence of a Tween-80 as surfactant was found to give a nanosuspension within a size range 50-100 nm. The only drawback seemed with this technique was the low-product yield and high-processing time (3-4 h). In order to overcome this drawback spray-drying technique was further explored; the solution of SBM containing Tween-80 was stirred on magnetic stirrer at 1,200 rpm and finally dried by using spray dryer at an inlet and outlet temperature of 75A degrees C and 56A degrees C, respectively. The feed rate for spray dryer was kept to be 91 ml/h. The sample was collected and analyzed for particle size distribution which was found to be in the range of 50-100 nm. Keeping in view the positive outcomes in terms of higher yield and lower processing time, the spray-drying technique was taken to give the optimized formulation. Nanosized particles, thus obtained were evaluated for particle size, surface topology and particles size distribution, by Transmission Electron Microscopy (TEM), Scanning Electron Microscopy (SEM), and Quasi-elastic light scattering (QELS) technique, respectively. The nanosized particles were subjected to investigate changes on the physical stability of the powder, for this different analytical method was used as: Fourier transform infrared spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC) and X-ray diffraction (XRD) analysis and thus the result indicates that there was no physical disparity when compared with the commercial SBM sample.