Physicochemical and Structural Studies of Triamterene

Dahl, O.; Ziedrich, K. Hans; Marek, G.J.; Paradies, Henrich H.

doi:10.1002/jps.2600780719

Cited by 13 publications

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References 15 publications

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“…1. Mixed solvate systems, such as doxycycline hydrochloride [147] which forms a mixed ethanol-water solvate (i.e., hyclate) or triamterene [148] which forms mixed solvates of dimethylformamide and water.…”

Section: Drug Solvate Screeningmentioning

confidence: 99%

“…................................................................................................TGA thermograms of triamterene crystallized from different solvents: a, original material (10 K/min); b, butanol (10 K/min); c, dimethylformamide (10 K/min) and d, ethanol (20 K/min). ...........................Dehydration TGA thermogram of ouabain octahydrate at 1K/min..................Dehydration TGA thermograms for two nitrofurantoin hydrates at 10 K/min, prepared according to ref [148]. to obtain: a.…”

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Application of solid-state kinetics to desolvation reactions

Khawam¹

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Mathematical methods have been developed to evaluate solid-state kinetics. They generally fall into two categories: model-fitting or model-free (isoconversional). Modelfitting methods determine the kinetic triplet (model, frequency factor and activation energy) whereas isoconversional (model-free) methods generate the activation energy as a function of reaction progress without modelistic assumptions.This work investigated the relationship between calculation methods and artifactual variation in activation energy. Variable activation energy, often reported by isoconversional methods, could be an artifact due to experimental errors. This can lead to erroneous mechanistic conclusions about a reaction being complex.In this work, a new approach is proposed for obtaining the kinetic triplet that combines the advantages of isoconversional and model-fitting methods. An isoconversional method was used to select the reaction model by comparing calculated activation energies to that predicted by modelistic approaches. The selected model was the one that had an activation energy closest to the isoconversional value and the frequency factor was then obtained from the selected model. This complementary approach was used to evaluate simulated and real experimental data.The desolvation kinetics of several structurally related solvates of sulfameter (5methoxysulfadiazine) were evaluated both isothermally and nonisothermally. Calculated desolvation kinetic parameters were compared and related to the crystal structure of the solvates. A relationship was observed between calculated activation energy and solvent size. The larger the solvent molecule, the higher its solvate's desolvation activation energy. The solid-state reaction models selected were rationalized on the basis of crystal structures of the solvates where the solvent molecules were in cavities in the crystal.Finally, it was found that kinetic parameters obtained isothermally and nonisothermally were not in agreement. It was concluded that kinetic results from isothermal experiments may not be extended to nonisothermal or vice versa without confirmation of their equivalence.Abstract Approved: ____________________________________ Thesis Supervisor ____________________________________

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Section: Drug Solvate Screeningmentioning

confidence: 99%

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confidence: 99%

Application of solid-state kinetics to desolvation reactions

Khawam¹

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The crystal and molecular structure of 3‐aminophthalhydrazide (Luminol)

Paradies

1992

Ber Bunsenges Phys Chem

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The crystal structure of 2‐aminophthalhydrazide (luminol) has been determined by X‐ray diffraction analysis. The space group determined was P&1macr; (No. 2) with cell constants of a = 12.714 Å, b = 14.132 Å. c = 7.1027 (Å), α = 101.24°, β = 94.84° and γ = 116.60° with six molecules per unit cell of formula molecular weight 177.16. The three luminol molecules form a hydrogen bonded trimeric unit. There is one intramolecular hydrogen bond per luminol molecule involving the NH2 group and the adjacent carbonyl group. All other hydrogen bonds are intermolecular. – Luminol crystallizes as amide‐hydroxyimunol tautomer. The protonated carbonyl group acts as hydrogen bond donor to a neightbouring unprotonated carbonyl group.

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Improvement of the diuretic effect of triamterene via solid dispersion technique with PEG 4000

Arias

Ginés

Moyano

et al. 1994

Eur. J. Drug Metab. Pharmacokinet.

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The present investigation was designed and undertaken in order to substantiate further contention concerning the universality of the utilization of PEG polymers as matrix carriers. This study could then be considered an attempt to enhance the dissolution rate of triamterene, with the subsequent enhancement in its absorption rate, via solid dispersion using PEG 4000. The approach of solid dispersions was found useful for optimizing the pharmacokinetic of triamterene in rats.

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Physicochemical and Structural Studies of Triamterene

Cited by 13 publications

References 15 publications

Application of solid-state kinetics to desolvation reactions

Application of solid-state kinetics to desolvation reactions

The crystal and molecular structure of 3‐aminophthalhydrazide (Luminol)

Improvement of the diuretic effect of triamterene via solid dispersion technique with PEG 4000

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