Agglomeration of ibuprofen with talc by novel crystallo-co-agglomeration technique

Pawar, Atmaram; Paradkar, Anant; Kadam, Shivajirao; Mahadik, Kakasaheb R.

doi:10.1208/pt050455

Cited by 41 publications

(31 citation statements)

References 24 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Mainly, recrystallization of the drug during agglomeration generates the miniscular dosage form. The miniscular dosage form of Linezolidtalc in this new study showed sustained drug release fitting the Higuchi matrix model, whereas sustained zero-order drug release was reported for ibuprofen-talc [29]. …”

Section: Fig 5: X-ray Powder Diffraction Pattern Of Pure Linezolid Amentioning

confidence: 62%

Improvement of Micromeritic, Compressibility and Solubility Characteristics of Linezolid by Crystallo-Co-Agglomeration Technique

Kadam

Patil

2017

Int J App Pharm

View full text Add to dashboard Cite

Objective: The purpose of current study was to improve physicochemical properties such as micrometric, compressibility and solubility of linezolid (LNZ) by preparing crystallo-co-agglomerates (CCA) in the presence of polymer for the enhancement of overall physicochemical performance. Methods:The process of agglomeration involves the use of dichloromethane (DCM) as a good solvent and chloroform as bridging liquid were used to prepare agglomerates. Agglomerates were characterised in the solid state using several techniques such as Scanning electronic microscopy(SEM), Fourier transformation infrared spectroscopy (FTIR), X-ray powder diffraction analysis (XRPD) The agglomerates obtained were evaluated for micrometric, mechanical, deformation, compressibility and drug release properties.Results: It was found that micrometric properties and dissolution characteristics of agglomerates were significantly improved than that of pure linezolid. Solubility was found to be increased than pure linezolid. The solubility of crystallo co-agglomerates was found an increase in 5 fold 3 fold and 3.7 fold for PVPK30 (0.5%), PVPK30 (0.25%) and PVPK30 (0.75%) respectively. The angle of repose for all batches was found between 22 ° to 30 °Carrs index was between 12.27±0.6 to 18.73±0.4 and Hausners ratio Near to 1, indicated good flow ability of agglomerates. The time required for drug release over a period of 60 min, is as LA1>LA2>LA3. LA3 shows fast drug release than LA1 and LA2, due to solubilization of drug due to more concentration of PVPK30 and less concentration of talc.Conclusion: Based on the above results, it was revealed that CCA of linezolid prepared with DCM and HPMC (Hydroxypropyl methyl cellulose)/PEG (Polyethylene glycol)/PVP (Polyvinylpyrrolidone) K30 exhibited improved micrometric properties, compressibility and in addition to improving solubility and dissolution rate.

show abstract

Section: Fig 5: X-ray Powder Diffraction Pattern Of Pure Linezolid Amentioning

confidence: 62%

Improvement of Micromeritic, Compressibility and Solubility Characteristics of Linezolid by Crystallo-Co-Agglomeration Technique

Kadam

Patil

2017

Int J App Pharm

View full text Add to dashboard Cite

show abstract

“…There was a research paper on the agglomerates formed by ibuprofen and talc [32] . The percentageprocess yield is of 95-96% w/w.…”

Section: Significance Of Crystallo Co Agglomerationmentioning

confidence: 99%

“…Blank talc agglomerates were used as an inert core or coating substrate by the aid of which drug loaded talc pellets can be prepared. This drug loaded talc pellets have better mechanical, micromeritical and compressional properties [7][8][9] . With the selection and use of appropriate polymers, it is possible to compress into tablet intermediate and or spensules, which possess all advantages, required in the design of MUPS.…”

Section: Introductionmentioning

confidence: 99%

Crystallo – Co - Agglomeration: An Innovative Technique for Size Enlargement and Improved Flow Properties of Powders

Enlargement¹

2016

Res. Rev. J Mat. Sci

View full text Add to dashboard Cite

Direct compression is the preferred method for tablet manufacturing due to the simplicity in processing and its cost effectiveness. However, for applying direct compression in tablet manufacturing, the drug used should have good flow properties and compaction characteristics. Many drugs are lacking these properties and so it is not possible to compress them directly into tablets. Crystallo co agglomeration (CCA) is an innovative technique developed with intends to provide the drugs with good micromeritic and mechanical characteristics. The process of CCA involves crystallisation followed by simultaneous agglomeration of the drug with the aid of a good solvent and /or a bridging liquid and a bad solvent. It is also possible to incorporate other drugs (to get a combination tablet), excipients (e.g. disintegrants for fast dissolving tablets) and different polymer combinations (to modify the drug release properties). In the recent years,attempts were made to produce Crystallo co agglomerates of various drugs, whichwere briefly discussed in this article. Even though large scale applications of CCA is not yet made possible, this technique gives a new line of opportunities to the tablet manufacturing process, ensuring low cost, single stepped production of particles with good micromeritic and mechanical characters which can be directly compressed.

show abstract

“…It is a modification of the spherical crystallization techniques described above, in which a drug is crystallized and agglomerated with an excipient (48,49) or with another drug (50). Similar to spherical agglomeration, a good solvent is used in this method to solubilize the drug, a poor solvent to cause drug crystallization and the bridging liquid, which is immiscible with the poor solvent, to form liquid bridges during the agglomeration process.…”

Section: Crystallo-co-agglomerationmentioning

confidence: 99%

Spherical crystallization of drugs

Kovačič¹,

Vrečer²,

Planinšek³

2012

Acta Pharmaceutica

View full text Add to dashboard Cite

The solid state properties of pharmaceutical compounds have a decisive impact on dosage form development, stability, and in vivo performance of the drug. Many pharmaceutical drugs are problematic per se due to their inappropriate physical and mechanical properties and poor aqueous solubility. The micromeritic properties of drug particles, such as shape and size, are of essential importance for the formulation of solid high--dose units (1). The particle size of poorly soluble drugs is always an issue due to its impact on dissolution properties. Micronized drug particles (smaller than 10 mm) have a large specific area and provide a way to improve the dissolution rate (2), but high energy input during the micronization process gives rise to increased free surface energy, electrostatic tendencies, and thus poor flowability and/or compressibility of powders and low bulk density (3), which makes them difficult to use in downstream processing in the pharmaceutical industry such as direct tablet-making or capsule-filling processes. In addition, micronized drug substances tend to agglomerate and the increase in surface area is not always reflected in improved dissolution (4). Spherical crystallization of drugs is the process of obtaining larger particles by agglomeration during crystallization. The most common techniques used to obtain such particles are spherical agglomeration and quasi-emulsion solvent diffusion. Ammonia diffusion systems and crystallo-co-agglomeration are extensions of these techniques. By controlling process parameters during crystallization, such as temperature, stirring rate, type and amount of solvents, or excipient selection, it is possible to control the formation of agglomerates and obtain spherical particles of the desired size, porosity, or hardness. Researchers have reported that the particles produced have improved micromeritic, physical, and mechanical properties, which make them suitable for direct compression. In some cases, when additional excipients are incorporated during spherical crystallization, biopharmaceutical parameters including the bioavailability of drugs can also be tailored.

show abstract

Agglomeration of ibuprofen with talc by novel crystallo-co-agglomeration technique

Cited by 41 publications

References 24 publications

Improvement of Micromeritic, Compressibility and Solubility Characteristics of Linezolid by Crystallo-Co-Agglomeration Technique

Improvement of Micromeritic, Compressibility and Solubility Characteristics of Linezolid by Crystallo-Co-Agglomeration Technique

Crystallo – Co - Agglomeration: An Innovative Technique for Size Enlargement and Improved Flow Properties of Powders

Spherical crystallization of drugs

Contact Info

Product

Resources

About