Analysis of the Literature and Patents on Solid Dispersions from 1980 to 2015.

Jinglu Zhang,Lijiang Chen,Weixiang Zhang,Weijie Chen,Run Han,Weisan Pan,Yuanhui Ji,Ying Li,Xinggang Yang,Hao Pan,Defang Ouyang

doi:10.3390/molecules23071697

Abstract

Background: Solid dispersions are an effective formulation technique to improve the solubility, dissolution rate, and bioavailability of water-insoluble drugs for oral delivery. In the last 15 years, increased attention was focused on this technology. There were 23 marketed drugs prepared by solid dispersion techniques. Objective: This study aimed to report the big picture of solid dispersion research from 1980 to 2015. Method: Scientific knowledge mapping tools were used for the qualitative and the quantitative analysis of patents and literature from the time and space dimensions. Results: Western Europe and North America were the major research areas in this field with frequent international cooperation. Moreover, there was a close collaboration between universities and industries, while research collaboration in Asia mainly existed between universities. The model drugs, main excipients, preparation technologies, characterization approaches and the mechanism involved in the formulation of solid dispersions were analyzed via the keyword burst and co-citation cluster techniques. Integrated experimental, theoretical and computational tools were useful techniques for in silico formulation design of the solid dispersions. Conclusions: Our research provided the qualitative and the quantitative analysis of patents and literature of solid dispersions in the last three decades.

Highlights

With the increasing discovery of water-insoluble Active Pharmaceutical Ingredients (APIs) high throughput screening, combinatorial chemistry and computer-aided drug design were extensively applied in formulation design since 1980 [1,2,3,4,5,6], the question of how to improve their poor water solubility has drawn more attention of the researchers than ever before
Due the increased interest in solid dispersions, this paper aims to provide a big picture of the solid dispersion area from 1980 to 2015 by analyzing the patents and literature in the research field of solid dispersions
The keyword burst the andkeyword co-citation wereand alsoco-citation investigated to visualized using science bibliometric mapping

Summary

Introduction

With the increasing discovery of water-insoluble Active Pharmaceutical Ingredients (APIs) high throughput screening, combinatorial chemistry and computer-aided drug design were extensively applied in formulation design since 1980 [1,2,3,4,5,6], the question of how to improve their poor water solubility has drawn more attention of the researchers than ever before. There was a lack of qualitative and quantitative analysis of literature and patents published in this research field. Solid dispersions are an effective formulation technique to improve the solubility, dissolution rate, and bioavailability of water-insoluble drugs for oral delivery. There was a close collaboration between universities and industries, while research collaboration in Asia mainly existed between universities

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Discussion

Conclusion