Co-spray drying of metformin hydrochloride with polymers to improve compaction behavior

Al-Zoubi, Nizar; Odeh, Faten; Nikolakakis, Ioannis

doi:10.1016/j.powtec.2016.11.027

Cited by 23 publications

(23 citation statements)

References 39 publications

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“…Among PSC or PLM/PSC products, MC% was not significantly different. The lower yield of the PSC products can be attributed to the softer polysaccharide wall and to their high MC%, since both of them promote adhesion to the drying chamber walls, resulting in a loss of material [ 36 , 37 ]. Considering the effects of starch grade, higher yield in both the PCS and PLM/PCS products was obtained from SOS1 (40.8% and 49.9%), followed by SOS3 (33.5% and 39.6%) and ADA (25.0% and 29.9%).…”

Section: Resultsmentioning

confidence: 99%

Enteric Release Essential Oil Prepared by Co-Spray Drying Methacrylate/Polysaccharides—Influence of Starch Type

et al. 2020

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Oregano essential oil (EO) enteric release powder was formulated by spray drying feed emulsions stabilized with polysaccharides (PSC) and Eudragit® L100 (PLM). Different modified starches were used in the PSC component. Spray-dried powders were evaluated for particle size and morphology, dynamic packing, flowability, chemical interactions, reconstitution, and gastric protection. Feed emulsions were stable, indicating the good emulsification ability of the PLM/PSC combination. The presence of polymer in the encapsulating wall neutralized electrostatic charges indicating physical attraction, and FTIR spectra showed peaks of both PLM and PSC without significant shifting. Furthermore, the presence of polymer influenced spray drying, resulting in the elimination of surface cavities and the improvement of powder packing and flowability, which was best when the surface-active, low-viscosity sodium octenyl succinate starch was used (angle of repose 42°). When a PLM/PSC ratio of 80/20 was used in the encapsulating wall, the spray-dried product showed negligible re-emulsification and less than 15% release in pH 1.2 medium for 2 h, confirming gastric protection, whereas at pH 6.8, it provided complete re-emulsification and release. In conclusion, (1) polymer–PSC physical interaction promoted the formation of a smoother particle surface and product with improved technological properties, which is important for further processing, and (2) the gastro protective function of Eudragit® L100 was not impaired due to the absence of significant chemical interactions.

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Section: Resultsmentioning

confidence: 99%

Enteric Release Essential Oil Prepared by Co-Spray Drying Methacrylate/Polysaccharides—Influence of Starch Type

et al. 2020

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“…They found that metformin HCl co-spray dried with 2% PVP K30 showed excellent flowability and compressibility as well. Further investigation was sought out by Al-Zoubi et al [48], who compared five hydrophilic polymers (HPMC, PVP, copovidone, sodium alginate and sodium carmellose) regarding their ability to enhance the compression behavior of metformin HCl. Co-spray drying with the polymers resulted in increased amorphous drug content associated with increased deformability and reduced ejectability.…”

Section: Direct Compression Of Co-spray Dried Apis With Excipientsmentioning

confidence: 99%

“…However, compactability and tabletability of metformin HCl were improved only by co-spray drying with the anionic sodium alginate and sodium carmellose polymers that could make ionic interactions with the positively charged ammonium of the drug. [48].…”

Section: Direct Compression Of Co-spray Dried Apis With Excipientsmentioning

confidence: 99%

Spray Drying for Direct Compression of Pharmaceuticals

et al. 2021

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Tableting by direct compression (DC) is one of the simplest and most cost-effective drug manufacturing approaches. However, most active pharmaceutical ingredients (APIs) and excipients lack the compression and flow properties required to meet the needs of high-speed industrial tablet presses. Therefore, the majority of DC APIs and excipients are modified via processing/co-processing particle engineering techniques to boost their properties. Spray drying is one of the most commonly employed techniques to prepare DC grades of APIs and excipients with prominent advantages. This review aims to present an overview of the commercially marketed and investigationally-prepared DC APIs and excipients produced by spray drying.

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“…However, the development of metformin ODT using the most economical direct compression method encounters a challenge owing to its poor compressibility, moisture sensitivity, and great tendency for capping [ 14 ]. To overcome this challenge, the formulator has to use the wet granulation process to get agglomerates of drug and excipients with adequate compression characteristics [ 15 ]. This may lead to formation of solid bridges ”necks” among metformin particles that impart mechanical strength, lack powder flow, and sticking issues through the tableting process owing to consequent moisture migration or desorption during the wet granulation process [ 16 , 17 ].…”

Section: Introductionmentioning

confidence: 99%

Design, Optimization, and Correlation of In Vitro/In Vivo Disintegration of Novel Fast Orally Disintegrating Tablet of High Dose Metformin Hydrochloride Using Moisture Activated Dry Granulation Process and Quality by Design Approach

et al. 2020

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Compression of cohesive, poorly compactable, and high-dose metformin hydrochloride into the orally disintegrating tablet (ODT) is challenging. The objective of this study was to develop metformin ODT using the moisture activated dry granulation (MADG) process. There are no reports in the literature regarding the development of ODT based on MADG technology. The feasibility of developing metformin ODT was assessed utilizing a 32 full factorial design to elucidate the influence of water amount (X1) and the amount of pregelatinized starch (PGS; X2) as independent variables on key granules and tablets’ characteristics. The prepared granules and tablets were characterized for granule size, bulk density, flow properties, tablets’ weight variation, breaking force, friability, capping tendency, in vitro and in vivo disintegration, and drug release. Regression analysis showed that X1 and X2 had a significant (p ≤ 0.05) impact on key granules and tablets’ properties with a predominant effect of the water amount. Otherwise, the amount of PGS had a pronounced effect on tablet disintegration. Optimized ODT was found to show better mechanical strength, low friability, and short disintegration time in the oral cavity. Finally, this technique is expected to provide better ODT for many kinds of high-dose drugs that can improve the quality of life of patients.

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Co-spray drying of metformin hydrochloride with polymers to improve compaction behavior

Cited by 23 publications

References 39 publications

Enteric Release Essential Oil Prepared by Co-Spray Drying Methacrylate/Polysaccharides—Influence of Starch Type

Enteric Release Essential Oil Prepared by Co-Spray Drying Methacrylate/Polysaccharides—Influence of Starch Type

Spray Drying for Direct Compression of Pharmaceuticals

Design, Optimization, and Correlation of In Vitro/In Vivo Disintegration of Novel Fast Orally Disintegrating Tablet of High Dose Metformin Hydrochloride Using Moisture Activated Dry Granulation Process and Quality by Design Approach

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