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球形结晶:一种用于改善活性药物成分溶解性和流动性的技术。

Spherical crystallization: A technique use to reform solubility and flow property of active pharmaceutical ingredients.

作者信息

Chatterjee Arindam, Gupta Madan Mohan, Srivastava Birendra

机构信息

Department of Pharmaceutics, School of Pharmaceutical Sciences, Jaipur National University, Jaipur, Rajasthan, India.

Department of Pharmaceutics, School of Pharmaceutical Sciences, Jaipur National University, Jaipur, Rajasthan, India; Department of Pharmaceutics, Laboratory of Pharmaceutical Formulation Design and Development, School of Pharmacy, Faculty of Medical Sciences, The University of the West Indies, St. Augustine, Trinidad and Tobago, West Indies.

出版信息

Int J Pharm Investig. 2017 Jan-Mar;7(1):4-9. doi: 10.4103/jphi.JPHI_36_16.

Abstract

Tablets have been choice of manufacturers over the years due to their comparatively low cost of manufacturing, packaging, shipping, and ease of administration; also have better stability and can be considered virtually tamper proof. A major challenge in formulation development of the tablets extends from lower solubility of the active agent to the elaborated manufacturing procedures for obtaining a compressible granular material. Moreover, the validation and documentation increases, as the numbers of steps increases for an industrially acceptable granulation process. Spherical crystallization (SC) is a promising technique, which encompass the crystallization, agglomeration, and spheronization phenomenon in a single step. Initially, two methods, spherical agglomeration, and emulsion solvent diffusion, were suggested to get a desired result. Later on, the introduction of modified methods such as crystallo-co-agglomeration, ammonia diffusion system, and neutralization techniques overcame the limitations of the older techniques. Under controlled conditions such as solvent composition, mixing rate and temperature, spherical dense agglomerates cluster from particles. Application of the SC technique includes production of compacted spherical particles of drug having improved uniformity in shape and size of particles, good bulk density, better flow properties as well as better solubility so SC when used on commercial scale will bring down the production costs of pharmaceutical tablet and will increase revenue for the pharmaceutical industries in the competitive market. This review summarizes the technologies available for SC and also suggests the parameters for evaluation of a viable product.

摘要

多年来,片剂一直是制造商的首选,因为其制造、包装、运输成本相对较低,且易于给药;片剂还具有更好的稳定性,几乎可以认为是防篡改的。片剂配方开发中的一个主要挑战,从活性剂的低溶解度延伸到获得可压缩颗粒材料的复杂制造程序。此外,随着工业上可接受的制粒过程步骤数量的增加,验证和文件工作也会增加。球形结晶(SC)是一种很有前途的技术,它在一个步骤中涵盖了结晶、团聚和滚圆现象。最初,提出了两种方法,即球形团聚和乳液溶剂扩散,以获得理想的结果。后来,结晶共团聚、氨扩散系统和中和技术等改进方法的引入克服了旧技术的局限性。在溶剂组成、混合速率和温度等受控条件下,球形致密团聚体从颗粒中聚集形成。SC技术的应用包括生产药物的压实球形颗粒,这些颗粒在形状和尺寸上具有更好的均匀性、良好的堆密度、更好的流动性能以及更好的溶解性,因此,SC技术在商业规模上使用时,将降低药物片剂的生产成本,并在竞争激烈的市场中增加制药行业的收入。本综述总结了可用于SC的技术,并提出了评估可行产品的参数。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f6ac/5370348/ee8edd110a76/IJPI-7-4-g001.jpg

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