The use of solubility parameters in pharmaceutical dosage form design

Hancock, Bruno C.; York, Peter; Rowe, R.C.

doi:10.1016/s0378-5173(96)04828-4

Cited by 283 publications

(157 citation statements)

References 72 publications

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“…48,49 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 Quantification analysis for the composite systems was performed by DVS and NIR due to their enhanced sensitivity at detecting low amorphous content levels, compared to DSC and pXRD.…”

Section: Discussionmentioning

confidence: 99%

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: Discussionmentioning

confidence: 99%

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 spreading coe cient (the ability of a liquid to wet a substrate) can also be derived. For a comprehensive discussion on the measurement and theory of surface energetics, the reader is referred to reviews by Buckton (1995a, b) and Hancock et al (1997). These parameters have provided an insight into the interactions between formulation components and have been used as a basis to predict blending, granulation, compression and ® lm-coating behaviour.…”

Section: Predictions Based On the Physicochemical Properties Of Raw Mmentioning

confidence: 99%

Predictive and correlative techniques for the design, optimisation and manufacture of solid dosage forms

Hardy

Cook

2003

Journal of Pharmacy and Pharmacology

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There is much interest in predicting the properties of pharmaceutical dosage forms from the properties of the raw materials they contain. Achieving this with reasonable accuracy would aid the faster development and manufacture of dosage forms. A variety of approaches to prediction or correlation of properties are reviewed. These approaches have variable accuracy, with no single technique yet able to provide an accurate prediction of the overall properties of the dosage form. However, there have been some successes in predicting trends within a formulation series based on the physicochemical and mechanical properties of raw materials, predicting process scale-up through mechanical characterisation of materials and predicting product characteristics by process monitoring. Advances in information technology have increased predictive capability and accuracy by facilitating the analysis of complex multivariate data, mapping formulation characteristics and capturing past knowledge and experience.

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“…It affords a numerical approximation of the degree of interaction between materials. It has been found particular use in predicting solubility, selection of solvents and cosolvents for increased solubility 1 , chemical kinetics 2 , drug action, drug transport kinetics 3,4 , structure activity relationship 5 , in situ release of theophylline 6 , gas-solid chromatography 7 , selection of excipients for formulations 8 , dosage form technology and design 9 , fast prediction of basic properties of materials 10 , solvent selection for organic reactions 11 , prediction of adhesion of film coating to tablets 12 , selection of co-formers for co-crystal formation 13 . Therefore, the specific value of the solubility parameter of a drug is of concern.…”

Section: Introductionmentioning

confidence: 99%

Nabumetone in Binary Solvents: Solubility Analysis

Kharwade¹,

Subrahmanyam²,

Kharwade³

2017

Int. Res. J. Pharm.

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The solubility prediction of nabumetone was studied in different solvent system (hexane-ethyl acetate-ethanol-water). The theories such as ideal, Hildebrand-Scatchard and extended Hildebrand solubility approaches were used for finalizing the solubility behavior of nabumetone. Entropy of fusion expression was used to calculate the ideal solubility. The experimental mole fraction solubility deviated from the ideal mole fraction solubility, indicating the self association of solute or solvent or both in solution. The extended Hildebrand equation was used to reproduce solubilities of nabumetone in selected solvent blend. The solubilities of nabumetone were back calculated with an interaction energy term 'W' and rational activity coefficient term '(log10 2)/A'. These parameters were regressed against a polynomial of δ1, solubility parameter of solvent blend. Solubility parameter of the nabumetone δ2 was determined and found to be ˜ 20 MPa 1/2 .

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The use of solubility parameters in pharmaceutical dosage form design

Cited by 283 publications

References 72 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

Predictive and correlative techniques for the design, optimisation and manufacture of solid dosage forms

Nabumetone in Binary Solvents: Solubility Analysis

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