Solubility of lovastatin in a family of six alcohols: Ethanol, 1-propanol, 1-butanol, 1-pentanol, 1-hexanol, and 1-octanol

Nti-Gyabaah, Joseph; Chmielowski, Rebecca A.; Chan, Vincent; Chiew, Yee C.

doi:10.1016/j.ijpharm.2008.03.046

Cited by 48 publications

(39 citation statements)

References 34 publications

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“…In Figure 3 are plotted the coefficients in Eqn. 2 against the number of carbon atoms in the alcohol, using the coefficients in Table 2, together with those for dry 1-octanol [34] and for water [41]. The coefficients for the alcohols fall on quite smooth curves, thus showing that the coefficients are consistent between one alcohol and another.…”

Section: Resultsmentioning

confidence: 97%

“…Updated correlations for the dry linear, secondary and branched alcohols are needed. Several research groups have begun publishing solubility data for crystalline pesticides and pesticide intermediates (i.e., 2-(4-ethylbenzoyl)benzoic acid [33]) and pharmaceutical drug molecules and intermediates (such as lovastatin [34], isonicotinic acid [35], pimozide [36], 4-aminobenzenesulfonamide [37] and meloxicam [38]) dissolved in alcohol solvents. Updated correlations allow us to utilize better the recently published solubility data in solute descriptor computers.…”

Section: Introductionmentioning

confidence: 99%

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Development of Abraham model correlations for solvation characteristics of linear alcohols

Sprunger

Achi

Pointer

et al. 2009

Fluid Phase Equilibria

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Data have been compiled from the published literature on the partition coefficients of solutes and vapors into the anhydrous linear alcohols (methanol through 1-heptanol, and 1-decanol) from both water and from the gas phase. The logarithms of the water-to-alcohol partition coefficients (log P) and gas-to-alcohol partition coefficients (log K) were correlated with the Abraham solvation parameter model. The derived correlations described the observed log P and log K values to within average standard deviations of 0.14 and 0.12 log units, respectively. The predictive abilities of the each correlation were assessed by dividing databases into a separate training set and test set.

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Section: Resultsmentioning

confidence: 97%

Section: Introductionmentioning

confidence: 99%

Development of Abraham model correlations for solvation characteristics of linear alcohols

Sprunger

Achi

Pointer

et al. 2009

Fluid Phase Equilibria

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show abstract

“…Figure 9 displays the correlation between the experimental and predicted solubility values (Eqs. [7][8][9] for all drugs at all temperatures (nϭ329; r 2 ϭ0.99).…”

Section: )mentioning

confidence: 99%

Solubility Behavior and Prediction for Antihelmintics at Several Temperatures in Aqueous and Nonaqueous Mixtures

Bustamante

Muela

Escalera

et al. 2010

CHEMICAL & PHARMACEUTICAL BULLETIN

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Solubility is a fundamental physico-chemical property with important applications to biological, chemical, pharmaceutical and environmental industries. Reliable solubility data require careful experimental measurements that are tedious, time consuming and costly, and this research area needs further investigation.1) Solubility data for drugs in solvent mixtures at several temperatures are scarce, in particular in solvent mixtures.2-7) These data allow to obtain thermodynamic magnitudes that provide a better understanding of the co-solvent action and solute-solvent interactions. [2][3][4][5][6]8) Aqueous mixtures are often used to increase the solubility of drugs. Non-aqueous mixtures have application in synthesis, re-crystallization and purification of drugs and in some techniques of microencapsulation. 9,10) The solubility data also serve to construct mathematical models that help to optimize solvent composition selection in pharmaceutical technology. Many drug candidates are so hydrophobic that its bioavailability depends on techniques to enhance the aqueous solubility.11) During the earlier stages of drug development the amount available of drug is often restrictive. Therefore it is desirable to have a model for correlating and predicting drug solubility from a small amount of data being at the same time easy to apply. Solubility prediction is very difficult because it depends on a large number of factors such as chemical structure, solute-solvent interactions and temperature. The drugs usually form non-ideal solutions with the solvents of pharmaceutical interest, and semi-empirical or empirical approaches are often needed to obtain useful solubility prediction. Solubility modelling may significantly reduce the experimental work in solvent selection.Predictive methods often require a number of physicochemical parameters and relatively complicate computation, and low prediction capability has been reported for the universal functional group activity coefficient (UNIFAC) method in some compounds.1) The log-linear model of Yalkowsky is not applicable for drugs showing a solubility maximum, and a model was developed to account for deviations from linearity in ethanol-water mixtures.12) In fact, when solubility behaviour of drugs is studied within a wide polarity range, curves with one or two solubility peaks may be found. 6)Mota et al. 11) used the Non-random Two Liquid Segment Activity Coefficient (NRTL-SAC) model for predicting the solubility in pure solvents and solvent mixtures at 25-40°C. The model requires the melting data from the solid phase, T f , DH f and DC p . Limited experimental DC p values are available for drugs and this contribution is frequently ignored in solubility calculations.11) The predictions did not agree well with the experimental data of paracetamol at high ethanol-in water ratios, a fact that was attributed to the appearance of a peak in the solubility profile, as was earlier reported. 13,14) Bustamante and co-workers proposed a model to predict the solubility mole fraction ln X 2 of ...

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“…For water insoluble drugs with high permeability, drug absorption by GIT is limited by drug dissolution rate solubility/dissolution are good pointer and major contributor to drug bioavailability. [5][6][7][8][9] Nanoparticles have drawn greater attention because of their solubilisation and transport properties. Therefore, it is very important to devise effective methods to enhance the solubility and dissolution rate of drug, consequently increasing its bioavailability.…”

Section: Introductionmentioning

confidence: 99%

Enhanced Oral Bioavailability in Albino Rabbits of Lovastatin Nanoparticles

Shinde

2014

J. Drug Delivery Ther.

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Solubility of lovastatin in a family of six alcohols: Ethanol, 1-propanol, 1-butanol, 1-pentanol, 1-hexanol, and 1-octanol

Cited by 48 publications

References 34 publications

Development of Abraham model correlations for solvation characteristics of linear alcohols

Development of Abraham model correlations for solvation characteristics of linear alcohols

Solubility Behavior and Prediction for Antihelmintics at Several Temperatures in Aqueous and Nonaqueous Mixtures

Enhanced Oral Bioavailability in Albino Rabbits of Lovastatin Nanoparticles

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