Dissolution Improvement and the Mechanism of the Improvement from Cocrystallization of Poorly Water-soluble Compounds

Shiraki, Koji; Takata, Noriyuki; Takano, Ryusuke; Hayashi, Yoshiki; Terada, Katsuhide

doi:10.1007/s11095-008-9676-2

Cited by 169 publications

(116 citation statements)

References 38 publications

(44 reference statements)

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“…These are mainly studies of intrinsic dissolution rates measured in simple buffers or in biorelevant media and estimated on the basis of their individual molar extinction coefficients in the respective medium, with the use of simple set ups or compendial apparatus (i.e. USP Apparatus 2) (15)(16)(17)(18).…”

Section: Introductionmentioning

confidence: 99%

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Small-Scale Assays for Studying Dissolution of Pharmaceutical Cocrystals for Oral Administration

et al. 2015

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Abstract. The purpose of this study was to better understand the dissolution properties and precipitation behavior of pharmaceutical cocrystals of poorly soluble drugs for the potential for oral administration based on a small-scale dissolution assay. Carbamazepine and indomethacin cocrystals with saccharin and nicotinamide as coformers were prepared with the sonic slurry method. Dissolution of the poorly soluble drugs indomethacin and carbamazepine and their cocrystals was studied with a small-scale dissolution assay installed on a SiriusT3 instrument. Two methodologies were used: (i) surface dissolution of pressed tablet (3 mm) in 20 mL running for fixed times at four pH stages (pH 1.8, pH 3.9, pH 5.4, pH 7.3) and (ii) powder dissolution (2.6 mg) in 2 mL at a constant pH (pH 2). Improved dissolution and useful insights into precipitation kinetics of poorly soluble compounds from the cocrystal form can be revealed by the smallscale dissolution assay. A clear difference in dissolution/precipitation behaviour can be observed based on the characteristics of the coformer used.

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Section: Introductionmentioning

confidence: 99%

“…The relationship between the transformation rate and the dissolution rate is critical (15). The increase of the solubility of an API as a result of cocrystal formation often leads to transformation back into the pure API.…”

Section: Introductionmentioning

confidence: 99%

Small-Scale Assays for Studying Dissolution of Pharmaceutical Cocrystals for Oral Administration

et al. 2015

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“…The solubility and stability of the pharmaceutical product are both important considerations when designing new drugs based on new technology [8].…”

Section: 1structural Analysismentioning

confidence: 99%

“…MA treats loss of appetite, reduces suffering in patients with endometrial or advanced breast cancer and is also used to eradicate undernourishment associated with AIDS [8,[12][13][14][15]. The dissolution of BCS class II drugs is determined by the rate of drug absorption [3].…”

Section: 1structural Analysismentioning

confidence: 99%

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New Biopolymer Nanoparticles Improve the Solubility of Lipophilic Megestrol Acetate

et al. 2016

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As many substances are poorly soluble in water and thus possess decreased bioavailability, creating orally administered forms of these substances is a challenge. The objective of this study was to determine whether the solubility of megestrol acetate, a Biopharmaceutical Classification System (BCS) class II drug, can be improved by using a newly-synthesized surfactant (Rofam 70: a rapeseed methyl ester ethoxylate) and compare it with two references surfactants (Tween 80, Pluronic F68) at three different pH values. Spectrophotometry was used to compare the solubility profiles in the presence of three tested surfactants at pH 5.0, 7.4 and 9.0. Rapeseed methyl ester ethoxylate was found to improve the solubility of the BCS Class II drug and increase its bioavailability; It increased drug solubility more effectively than Pluronic F68. Its cytotoxicity results indicate its possible value as a surfactant in Medicine and Pharmacy.

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The Impact of Solubility and Dissolution Assessment on Formulation Strategy and Implications for Oral Drug Disposition

Alsenz¹

2012

Encyclopedia of Drug Metabolism and Interactions

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This review discusses the importance of drug solid–state properties and of solubility and dissolution measurement for the identification of appropriate formulations/formulation strategies and highlights their impact on drug disposition and candidate selection. Common elements of solubility/dissolution protocols are presented and the methods addressing equilibrium, apparent, kinetic, and intrinsic solubility, as well as powder and intrinsic dissolution are discussed. Tools for drug categorization (BCS, BDDCS) and estimation of oral drug absorption (MAD) are assessed. A detailed description of available formulation approaches is provided, including improvement of drug dissolution rate and/or apparent solubility, drug solubilization approaches, and inhibition of drug precipitation.

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Dissolution Improvement and the Mechanism of the Improvement from Cocrystallization of Poorly Water-soluble Compounds

Cited by 169 publications

References 38 publications

Small-Scale Assays for Studying Dissolution of Pharmaceutical Cocrystals for Oral Administration

Small-Scale Assays for Studying Dissolution of Pharmaceutical Cocrystals for Oral Administration

New Biopolymer Nanoparticles Improve the Solubility of Lipophilic Megestrol Acetate

The Impact of Solubility and Dissolution Assessment on Formulation Strategy and Implications for Oral Drug Disposition

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