Effect of environmental temperature on polymorphic solid-state transformation of indomethacin during grinding.

Otsuka, Makoto; Matsumoto, Takahiro; Kaneniwa, Nobuyoshi

doi:10.1248/cpb.34.1784

Cited by 109 publications

(63 citation statements)

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“…Several APIs including salbutamol sulphate 8 , cimetidine 9 and griseofulvin 10 were amorphised upon milling. In contrast, milling at elevated temperatures above the Tg value for mannitol 11 , sorbitol 11 and indomethacin 12 resulted in crystalline products but of a different polymorph.…”

Section: Introductionmentioning

confidence: 90%

Investigation of the Capacity of Low Glass Transition Temperature Excipients to Minimize Amorphization of Sulfadimidine on Comilling

Curtin

Amharar

et al. 2012

Mol. Pharmaceutics

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The co-processing of active pharmaceutical ingredient (API) with an excipient which has a high glass transition temperature (Tg) is a recognised strategy to stabilise the amorphous form of a drug. This work investigates whether co-processing a model API, sulfadimidine (SDM) with a series of low Tg excipients prevents or reduces amorphisation of the crystalline drug. It was hypothesised that these excipients could exert a Tg lowering effect, resulting in composite Tg values lower than that of the API alone and promote crystallisation of the drug. Milled SDM and co-milled SDM with glutaric acid (GA), adipic acid (AA), succinic acid (SA) and malic acid (MA) were characterised with respect to their thermal, X-Ray diffraction, spectroscopic and vapour sorption properties.SDM was predominantly amorphous when milled alone, with an amorphous content of 82 %.No amorphous content was detected by dynamic vapour sorption (DVS) on co-milling SDM with 50 % w/w GA, and amorphous content of the API was reduced by almost 30 %, relative to the API milled alone, on co-milling with 50 % w/w AA. In contrast, amorphisation of SDM was promoted on co-milling with 50 % w/w SA and MA, as indicated by near infrared (NIR) 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 2 spectroscopy. Results indicated that the API was completely amorphised in the SDM:MA comilled composite.The saturated solubility of GA and AA in the amorphous API was estimated by thermal methods.It was observed that the Tg of the co-melt quenched composites reached a minimum and levelled out at this solubility concentration. Maximum crystallinity of API on co-milling was reached at excipient concentrations comparable to the saturated concentration solubility of excipient in the API. Moreover, the closer the Hildebrand solubility parameter of the excipient to the API, the greater was the inhibition of API amorphisation on co-milling.The results reported here indicate that an excipient with a low Tg coupled with high solubility in the API can prevent or reduce the generation of an amorphous phase on co-milling.

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Section: Introductionmentioning

confidence: 90%

Investigation of the Capacity of Low Glass Transition Temperature Excipients to Minimize Amorphization of Sulfadimidine on Comilling

Curtin

Amharar

et al. 2012

Mol. Pharmaceutics

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“…Otsuka et al have been able to transform the crystalline polymorphs of indomethacin to amorphous states during milling which had 60% higher dissolution than the crystalline state. 20 The increased dissolution of drug from solid dispersions possibly be related to the decreased drug crystallinity or effective wetting of the reduced drug particles. [45][46][47][48] Coprocessing of ibuprofen with magnesium trisilicate for enhanced dissolution possibly be a promising approach for improvement of ibuprofen bioavailability.…”

Section: In-vitro Release Of Ibuprofenmentioning

confidence: 99%

“…15,16 Ball milling presents a greener route for many processes compared to the use of microwave and ultrasound as energy sources. Impact and attrition during ball milling can bring about changes in the crystal structure of the drug and can induce amorphization [17][18][19][20][21][22] and improve bioavailability. 23 Freeze drying is a standard process used to stabilize and store the drug products in the pharmaceutical industries.…”

Section: Introductionmentioning

confidence: 99%

Infrared spectroscopy for analysis of co-processed ibuprofen and magnesium trisilicate at milling and freeze drying

Acharya¹,

Mishra²,

Sahoo³

et al. 2017

ACSi

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Assessment of interactions of ibuprofen and magnesium trisilicate after co-processing has been carried out by infrared spectroscopy. Dry-state ball-milling and, aqueous state kneading and freeze-drying were performed. FTIR spectroscopy of co-processed materials described acid-base reaction between the carboxylic acid containing ibuprofen to a significant extent. Increased absorbance of carboxylate peak accompanied by a consistently reduced absorbance of the carbonyl acid peak was evident. Absorbance of carboxylate peak was more in freeze-dried sample compared to milled product. Intermolecular hydrogen bonding between ibuprofen and magnesium trisilicate in the co-processed material has been suggested. Inhibition of crystal morphology has been noticed in the photomicrographs of both the products. DSC report has shown absence or significantly decreased melting endotherm representing almost complete amorphization of ibuprofen. Release of drug increased greatly after co-processing in comparison to crystalline ibuprofen. Freeze-dried samples have improved drug release more significantly compared to ball-milled samples.

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“…[29,30] The molecules in the network are held together by synthons that are basic structural units formed from non-covalent interactions such as van der Waals interactions, π − π interactions and hydrogen bonds between the functional groups in the molecules. [31,32] …”

Section: World Journal Of Pharmaceutical Researchmentioning

confidence: 99%

Taste Masking by Co-Crystallization: A Review

Dhakate¹

2017

WJPR

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Acceptability of any dosage form mainly depends on its taste i.e. mouth feel. Dosage form interacts with taste receptor on the tongue to give bitter, sweet or salty taste sensation, when it dissolves in saliva. In market, there are numbers of pharmaceutical preparations available in which actives are bitter in taste. Pediatric patients frequently fail to take medications properly because of unpleasant taste of medication.Thus bitterness of preparation leads to patient incompliance. So masking of bitterness becomes essential. To overcome this problem, many technique has been developed to mask the bitter taste of drugs.Co-crystallization involves alteration in molecular assemblies and composition of pharmaceutical substance and which ultimately results in enhancing physical properties. Co-crystals contains API and pharmaceutically acceptable co-formers. Co-crystals are molecular complexes, bringing about changes in solubility, bioavailability, stability and taste masking of bitter drug in pharmaceutical designing without interacting with therapeutic utility. The main objective of this review is discuss co-crystallization as a technique for masking the bitter taste of the drug.

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Effect of environmental temperature on polymorphic solid-state transformation of indomethacin during grinding.

Cited by 109 publications

References 0 publications

Investigation of the Capacity of Low Glass Transition Temperature Excipients to Minimize Amorphization of Sulfadimidine on Comilling

Investigation of the Capacity of Low Glass Transition Temperature Excipients to Minimize Amorphization of Sulfadimidine on Comilling

Infrared spectroscopy for analysis of co-processed ibuprofen and magnesium trisilicate at milling and freeze drying

Taste Masking by Co-Crystallization: A Review

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