The roles of acidifiers in solid dispersions and physical mixtures

Tran, Thao; Tran, Phuong Ha-Lien; Choi, Han‐Gon; Han, Hyo-Kyung; Lee, Beom‐Jin

doi:10.1016/j.ijpharm.2009.09.039

Cited by 79 publications

(62 citation statements)

References 23 publications

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“…The ternary SDs can not only achieve the drug release of non pH dependence, but can maintain a high degree of drug dispersion, and prevent the recrystallization of an amorphous SD system [15] . It shows a unique advantage in drug solubilisation and promotion of dissolution [16,17] .…”

Section: Inclusion Complex Of α-Lipoic Acid Containing Alkalizer For mentioning

confidence: 99%

Inclusion Complex of alpha-Lipoic Acid Containing Alkalizer for Improving the Solubility and Stability Prepared by Co-grinding

Zheng¹,

Tang²,

Kong³

et al. 2017

pharmaceutical-sciences

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Zheng, et al.: Inclusion Complex of α-Lipoic Acid Containing AlkalizerThe inclusion complex was prepared by co-grinding α-lipoic acid with hydroxypropyl-β-cyclodextrin and alkalizer to enhance the solubility and stability of α-lipoic acid. Lipoic acid was chosen as a model drug because of its poor and pH-dependent aqueous solubility. Sodium carbonate and sodium bicarbonate were chosen as the pH regulators. Furthermore, the study investigated the proportion of alkalizer, hydroxypropyl-β-cyclodextrin and α-lipoic acid. Although the micronization has little effect on the solubility of the drug, the formation of amorphous form has an important effect of inclusion complexes. X-ray powder diffractometry and differential scanning calorimetry were used to assess the phase change of the drugs. The in vitro dissolution test indicates that the alkalizer plays a positive factor for the drug dissolution rate enhancement. The intermolecular interactions in the inclusion complexes were investigated using Fourier transform infrared spectroscopy. It was found that the drug frequency of the C=O band decreased or disappeared when the alkalizer was added. Thermal stability experiments showed that the inclusion complex have better stability after adding alkalizer. The solubility of α-lipoic acid can be increased 40 times when the ratio of α-lipoic acid and sodium carbonate is 1:1.2 in the ternary inclusion complex. It was evident that the inclusion compounds with alkalizer can improved the solubility and stability of α-lipoic acid significantly.

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Section: Inclusion Complex Of α-Lipoic Acid Containing Alkalizer For mentioning

confidence: 99%

Inclusion Complex of alpha-Lipoic Acid Containing Alkalizer for Improving the Solubility and Stability Prepared by Co-grinding

Zheng¹,

Tang²,

Kong³

et al. 2017

pharmaceutical-sciences

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show abstract

“…Another possible strategy is the incorporation of pH modifiers in the dosage form. Release of pH-dependent drug from matrix tablets can be successfully enhanced by maintaining the pH of the matrix in the desired range (8,9). The release of weakly basic drugs is expected to be improved by inclusion of weak acids and vice versa.…”

Section: Introductionmentioning

confidence: 99%

Modulation of pH-Independent Release of a Class ΙΙ Drug (Domperidone) from a Polymeric Matrix Using Acidic Excipients

Khan¹,

Iqbal²,

Khan³

et al. 2016

Dissolution Technol.

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Drug release from polymeric matrix systems is the rate-limiting step for drug bioavailability and is determined by drug solubility; most drugs show pH-dependent solubility. Polymeric matrices remain in the gastrointestinal tract for a longer period of time and are exposed to environments of varying pH, which can adversely affect drug release. In the present study, the pH-independent drug release of domperidone was achieved by modifying the microenvironmental pH of a swollen polymeric matrix using acidic excipients (citric acid and tartaric acid). Matrices were prepared by a water-based, wet-granulation technique and evaluated for various official and unofficial parameters. In vitro drug release was studied using USP dissolution apparatus and pH 6.80 phosphate buffer as dissolution medium. Release kinetics was evaluated according to various mathematical models.Results show that domperidone release can be effectively modified by inclusion of acidic excipients in the formulations. Acidic excipients modulated microenvironmental pH and avoided the effect of dissolution medium pH on drug release. The resultant formulations are easy to prepare and scale up for commercial manufacturing. Better pH-independent release, following zero-order kinetics, was achieved with tartaric acid.

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“…The SD technique produces a significant increase in surface area and surface wettability as well as solid state modification from crystalline to amorphous form. However, the SD characteristics can be influenced by several factors such as preparation method, carrier type and drug:carrier ratio and pH modifiers [7,8].…”

Section: Introductionmentioning

confidence: 99%

Development and Evaluation of Praziquantel Solid Dispersions in Sodium Starch Glycolate

Chaud¹,

Lima²,

Vila³

et al. 2013

Trop. J. Pharm Res

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The roles of acidifiers in solid dispersions and physical mixtures

Cited by 79 publications

References 23 publications

Inclusion Complex of alpha-Lipoic Acid Containing Alkalizer for Improving the Solubility and Stability Prepared by Co-grinding

Inclusion Complex of alpha-Lipoic Acid Containing Alkalizer for Improving the Solubility and Stability Prepared by Co-grinding

Modulation of pH-Independent Release of a Class ΙΙ Drug (Domperidone) from a Polymeric Matrix Using Acidic Excipients

Development and Evaluation of Praziquantel Solid Dispersions in Sodium Starch Glycolate

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