pH-independent release of a weakly basic drug from water-insoluble and -soluble matrix tablets

Streubel, A.; Siepmann, J.; Dashevsky, Andrei; Bodmeier, Roland

doi:10.1016/s0168-3659(00)00200-5

Cited by 160 publications

(101 citation statements)

References 8 publications

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“…The whole process is governed by drug solubility in the dissolution medium. Most of the drugs have pH-dependent solubility (1,3), exhibiting varying release rates with changing pH in the gastrointestinal tract (GIT). Penetration of GIT fluids with varying pH causes conversion of the more ionizable drug (soluble form) to a less soluble form.…”

Section: Introductionmentioning

confidence: 99%

“…Thus, the diffusion rate of the drug through the matrix is reduced. This conversion into an insoluble form depends on the pK a value of the drug and the pH of the intestinal fluids (3,4). It is desirable to achieve drug release independent of the environmental pH for making the required dose bioavailable (3,4).…”

Section: Introductionmentioning

confidence: 99%

“…This conversion into an insoluble form depends on the pK a value of the drug and the pH of the intestinal fluids (3,4). It is desirable to achieve drug release independent of the environmental pH for making the required dose bioavailable (3,4). As the pH of GIT fluids cannot be changed, an optimized pH in the dosage form can be used to modulate the release rate of drugs exhibiting pH-independent solubility and to overcome the problem of varying drug release patterns in different pH environments.…”

Section: Introductionmentioning

confidence: 99%

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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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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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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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show abstract

“…7,8 Polymers decrease the gastrointestinal side effects, toxicity of drugs, 9,10 or the dermal irritation of some skin products. 11 Polymers could be employed in target therapy of cancers, 12 masking of the unfavored taste of some drugs, avoidance of the fast elimination of drugs, production of the pH resistant formulations, [13][14][15] and formulation of the injectable form of some drugs that cannot be formulated using common methods. 16 Our past solubility studies have focused on developing mathematical equations to predict drug solubilities in aqueousorganic solvent mixtures.…”

Section: Introductionmentioning

confidence: 99%

Effects of Different Concentrations of Poly(vinyl pyrrolidone) on the Solubility of Lamotrigine and Diazepam in Ethanol + Water Mixtures at 298.2 K

2009

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The effects of poly(vinyl pyrrolidone) K30 (PVP) (1) on the solubility of lamotrigine (2) and diazepam (2) at 298.2 K are reported for ethanol (3) + water (4) mixtures at five different concentrations (0.0001, 0.0005, 0.001, 0.005 and 0.01) g · mL -1 of PVP. The general version of the Jouyban-Acree model was fitted to the solubility data of each drug in a given concentration of PVP. The largest mean relative deviation (MRD) was 14 %, that is, for diazepam in the presence of (0.0005 and 0.001) g · mL -1 of PVP, and the lowest MRD was 4 % for lamotrigine in the presence of 0.01 g · mL -1 of PVP. The overall MRD for lamotrigine and diazepam was 9 %. A modified version of the Jouyban-Acree model was used to model the simultaneous effects of the ethanol and PVP on the solubility employing experimental solubility of drugs in water and ethanol in the absence of PVP. The MRDs for diazepam and lamotrigine were 23 % and 10 %, respectively, with the overall value of 17 %.

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“…HPMC K4M is a non-ionic polymer and has been reported (Streubel et al, 2000;Tatavarti and Hoag, 2006;Tatavarti et 335 al., 2004;Gabr, 1992) to exhibit pH independent drug release as a result of pH independent swelling and erosion of the matrices when drug solubility is pH independent.…”

mentioning

confidence: 99%

Starch-free grewia gum matrices: Compaction, swelling, erosion and drug release behaviour

Nep

Asare-Addo

Ghori

et al. 2015

International Journal of Pharmaceutics

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pH-independent release of a weakly basic drug from water-insoluble and -soluble matrix tablets

Cited by 160 publications

References 8 publications

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

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

Effects of Different Concentrations of Poly(vinyl pyrrolidone) on the Solubility of Lamotrigine and Diazepam in Ethanol + Water Mixtures at 298.2 K

Starch-free grewia gum matrices: Compaction, swelling, erosion and drug release behaviour

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