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AAPS PharmSciTech ; 22(5): 201, 2021 Jul 06.
Artigo em Inglês | MEDLINE | ID: mdl-34231193


Particle engineering of excipients, at sub-particulate level using co-processing, can provide high functionality excipients. NanoCrySP technology has been recently explored as a novel approach for the generation of nanocrystalline solid dispersion of poorly soluble drugs, using spray drying process. The purpose of the present study was to generate co-processed mannitol and sorbitol (SD-CSM) using NanoCrySP technology having similar composition to commercial co-processed excipient (Compressol® SM, CP). The characterization of excipients was performed to evaluate their various physicomechanical properties. The sub-micron crystallite size of sorbitol in the matrix of mannitol was determined using the Williamson-Hall equation and Halder-Wagner equation. The reduction in crystallite size of sorbitol and mannitol, lower melting point, and lower heat of fusion of SD-CSM could be responsible for excellent compactibility, better tabletability, and comparable compressibility with respect to CP. This was confirmed by the compressibility-tabletability-compactibility (CTC) profile and Heckel plot analysis. Overall, SD-CSM generated using NanoCrySP technology improved functionalities of excipients over CP and would be useful for direct compression application.

Composição de Medicamentos/métodos , Manitol/química , Nanotecnologia , Sorbitol/química , Força Compressiva , Cristalização , Excipientes/química , Tamanho da Partícula , Porosidade , Comprimidos/química , Resistência à Tração , Molhabilidade
Expert Opin Drug Deliv ; 18(7): 907-928, 2021 07.
Artigo em Inglês | MEDLINE | ID: mdl-33412936


INTRODUCTION: Polymers have various applications such as binder, film coating agent, stabilizer, drug release modification, and as primary packaging materials. Recently, they have been explored in co-processing technique to improve the functionality of small molecule excipients (SMEs). Co-processing is a concept wherein two or more excipients interact at sub-particle level to provide synergy in functionality and minimize drawbacks of individual excipients. AREA COVERED: The present review highlights the application of co-processing to improve the functionality of SMEs using polymers; physicochemical and mechanical properties of polymers for co-processing; advantages of co-processed excipients for different applications; functionality enhancement of co-processed excipients; novel concepts/methods for co-processing; mechanistic insights on co-processing and commercial products available in the market. EXPERT OPINION: Most of the SMEs do not possess optimal multifunctional properties like flow, compressibility, compactibility, and disintegration ability, required to compensate for poorly compactable drugs. Some of these drawbacks can be overcome by co-processing of SMEs with polymers. For example, co-processing of a brittle SME and plastic material (polymer) can provide a synergistic effect and result in the generation of single entity multi-functional excipient. Besides, novel co-processed excipients generated using combinations of SMEs and polymers can also generate intellectual property rights.

Excipientes , Polímeros , Liberação Controlada de Fármacos , Comprimidos