An Advanced Twin-Screw Granulation Technology: The use of Non-Volatile Solvents with High Solubilizing Capacity

IF 3.4 4区医学 Q2 PHARMACOLOGY & PHARMACY AAPS PharmSciTech Pub Date : 2024-07-31 DOI:10.1208/s12249-024-02890-y

Siva Satyanarayana Kolipaka, Laura Andrade Junqueira, Steven Ross, Vivek Garg, Md Sadeque Hossein Mithu, Saumil Bhatt, Dennis Douroumis

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Abstract

Purpose

Twin-screw wet granulation (TSWG) is a manufacturing process that offers several advantages for the processing of water-insoluble active pharmaceutical ingredients (APIs) and has been used for increasing the solubility and dissolution rates. Here we introduce a novel TSWG approach with reduced downstream processing steps by using non-volatile solvents as granulating binders.

Methods

Herein, TSWG was carried out using Transcutol a non-volatile protic solvent as a granulating binder and dissolution enhancer of ibuprofen (IBU) blends with cellulose polymer grades (Pharmacoat^® 603, Affinisol™, and AQOAT^®).

Results

The physicochemical characterisation of the produced granules showed excellent powder flow and the complete transformation of IBU into the amorphous state. Dissolution studies presented immediate release rates for all IBU formulations due to the high drug-polymer miscibility and the Transcutol solubilising capacity.

Conclusions

Overall, the study demonstrated an innovative approach for the development of extruded granules by processing water-insoluble APIs with non-volatile solvents for enhanced dissolution rates at high drug loadings.

Graphical Abstract

Abstract Image

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先进的双螺杆造粒技术：使用高增溶能力的非挥发性溶剂。

目的：双螺杆湿法制粒（TSWG）是一种生产工艺，在加工水不溶性活性药物成分（API）方面具有多种优势，并已用于提高溶解度和溶出率。方法：使用 Transcutol（一种非挥发性原生溶剂）作为布洛芬（IBU）与纤维素聚合物（Pharmacoat® 603、Affinisol™ 和 AQOAT®）混合物的制粒粘合剂和溶出增强剂，进行 TSWG：结果：生产出的颗粒的理化特性显示粉末流动性极佳，IBU 完全转变为无定形状态。溶解研究表明，由于药物与聚合物的高度混溶性和 Transcutol 的增溶能力，所有 IBU 制剂都能立即释放：总之，该研究展示了一种创新的挤压颗粒剂开发方法，即用非挥发性溶剂加工水不溶性原料药，从而提高高药物负荷下的溶出率。

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来源期刊

AAPS PharmSciTech 医学-药学

CiteScore

6.80

自引率

3.00%

发文量

264

审稿时长

2.4 months

期刊介绍： AAPS PharmSciTech is a peer-reviewed, online-only journal committed to serving those pharmaceutical scientists and engineers interested in the research, development, and evaluation of pharmaceutical dosage forms and delivery systems, including drugs derived from biotechnology and the manufacturing science pertaining to the commercialization of such dosage forms. Because of its electronic nature, AAPS PharmSciTech aspires to utilize evolving electronic technology to enable faster and diverse mechanisms of information delivery to its readership. Submission of uninvited expert reviews and research articles are welcomed.