Excipients and their Functionality for Enabling Technologies in Oral Dosage Forms

Thakkar, Shreya; Sharma, Kunnal; Khurana, Sakshi; Bansal, Arvind K.

doi:10.1002/9781118992432.ch3

Cited by 4 publications

(2 citation statements)

References 40 publications

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“…The typical structure of microcrystalline cellulose (labeled "a" in the figure) was observed as elongated filamentary structures with angular borders [49], while the lactose structures (labeled "b") were rather small, spherical and without angular edges. The structure of the matrix by itself, in combination with the structure of an excipient, influences the behavior of the sample; for example, the filamentous structures of the microcrystalline cellulose give greater force against abrasion, while the spherical lactose structures provide greater cohesion between the particles, allowing longer disintegration times [50][51][52].…”

Section: Scanning Electron Microscopy (Sem)mentioning

confidence: 99%

Opuntia ficus-indica L. Mill Residues—Properties and Application Possibilities in Food Supplements

et al. 2020

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Recently, industry has been focusing on the development of new products made from food by-products in order to reduce and take advantage of food wastes. The objective of this study was to evaluate tablet formulations developed by mixing two commercial excipients, microcrystalline cellulose (M) and α-lactose-monohydrate (L), added with powder from residues (mesocarp and pericarp) of green and red (G and R) cactus pear fruit (Opuntia ficus-indica L. Mill), having the following formulations: green with microcrystalline cellulose (GM), green with lactose (GL), red with microcrystalline cellulose (RM), and red with lactose (RL). The results showed lower disintegration times for the tablets with microcrystalline cellulose. The fiber functional properties presented good values for lipid and water holding capacity. There was a higher total phenolic content (TPC) in formulations with green cactus pear residue powder with microcrystalline cellulose and lactose (GM and GL, respectively), but the DPPH and ferric reducing/antioxidant power (FRAP) values were higher in the formulations with red cactus pear residues (RM and RL), while ABTS values were similar among all formulations. In conclusion, tablets made from Opuntia residues are proposed as a product of interest for the food supplement industry because of the good quality parameters and the functional and antioxidant properties that they provide.

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Section: Scanning Electron Microscopy (Sem)mentioning

confidence: 99%

Opuntia ficus-indica L. Mill Residues—Properties and Application Possibilities in Food Supplements

et al. 2020

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“…Hence, the selection of an enabling technology needs to balance bioavailability over stability and manufacturing aspects, especially in case of borderline solubility-limited drug candidates in between Biopharmaceutics Classification System BCS I and II or III and IV, respectively. Interactions between active pharmaceutical ingredients ( APIs ) and functional excipients are often employed to improve solubility and dissolution kinetics in enabling formulations ( Thakkar et al, 2016 ). However, the question remains whether excipients regarded as standard might establish similar interactions; subsequently, improvement of aqueous solubility when employed at unusual manufacturing process conditions.…”

Section: Introductionmentioning

confidence: 99%

Influence of high pressure compaction on solubility and intrinsic dissolution of ibuprofen binary mixtures employing standard excipients

Ibraheem

Wagner

2021

International Journal of Pharmaceutics: X

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Enabling formulations often depend on functional excipients. However, the question remains whether excipients regarded as standard establish similar interactions and subsequently improvement of solubility when employed at unusual manufacturing process conditions. In this study, compaction of API under high pressure in the presence of hydrophilic excipients is proposed as a technique to improve the solubility and/or dissolution rate with an acceptable preservation of the supersaturation state. Binary mixtures of ibuprofen (IBU) with hydroxypropyl cellulose, isomalt, mannitol and sorbitol were compacted applying high pressure (500 MPa) with and without a previous co-milling step. Intrinsic dissolution rate (IDR) was selected to characterize and evaluate dissolution performance. The IDR of neat IBU increased from 5 to 88 fold and the aqueous solubility in the range of 3 to 54%. Regarding the polyols isomalt showed the highest impact on solubility and dissolution, without changing the crystallinity of IBU independent of a co-milling step. Even higher impact was achieved in combination with HPC. However, only without a previous co-milling step, ibuprofen remained crystalline, while co-milling induced an amorphous IBU-content of 38%. Based on XRPD and DSC findings, higher IDR and solubility values correlated with crystal modifications as well as IBU/excipient interactions.

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Emerging role of primary heterogeneous nucleation in pharmaceutical crystallization

Thakore

Sood

Bansal

2019

Drug Development Research

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Crystallization is an important and difficult to control unit operation in the pharmaceutical industry. Crystallization can control molecular (i.e., polymorphism) and particulate (i.e., particle size and crystal habit) properties of active pharmaceutical ingredient (API). Moreover, these molecular and particulate properties govern the manufacturability, stability, and biopharmaceutical performance of the API and drug product. Nucleation is a key step and primary heterogeneous nucleation is a common mode of nucleation during crystallization. Hence, it is important to understand the parameters affecting primary heterogeneous nucleation, to achieve desirable properties in crystalline APIs. Primary heterogeneous crystallization has usually been linked to the surface characteristics like topography and functionality of the heteronucleant. The review outlines recent findings in the primary heterogeneous crystallization with specific emphasis on its pharmaceutical applications including regulatory considerations. Molecular‐level mechanisms governing heteronucleation and subsequent outcome in terms of molecular as well as particulate‐level properties of API have also been discussed. Moreover, general guidance for the selection of heteronucleant has also been included. Heterogeneous crystallization is a promising tool for efficient crystallization of API having properties for optimal pharmaceutical performance.

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Excipients and their Functionality for Enabling Technologies in Oral Dosage Forms

Cited by 4 publications

References 40 publications

Opuntia ficus-indica L. Mill Residues—Properties and Application Possibilities in Food Supplements

Opuntia ficus-indica L. Mill Residues—Properties and Application Possibilities in Food Supplements

Influence of high pressure compaction on solubility and intrinsic dissolution of ibuprofen binary mixtures employing standard excipients

Emerging role of primary heterogeneous nucleation in pharmaceutical crystallization

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