Solubilization and dissolution of insoluble weak acid, ketoprofen: Effects of pH combined with surfactant

Sheng, Jennifer; Kasim, Nehal A.; Ramachandran, Chandrasekharan; Amidon, Gordon L.

doi:10.1016/j.ejps.2006.06.006

Cited by 114 publications

(84 citation statements)

References 28 publications

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“…Drug products with pKa values especially in the physiological range thus have dissolution rates that are affected greatly by pH. Sheng et al [14], Li et al [15] and Phaechamud and Ritthidej [16] have all showed this to happen for different types of dosage forms such as immediate and modified release. pH values for the jejunum ranging from 6.5 to 7.8 with a median value of 6.9 have been reported [20].…”

Section: Physiological Parametersmentioning

confidence: 99%

“…The reasoning behind this was attributed to the presence of both sodium and phosphate ions and their ability to greatly dehydrate more than if it was sodium ions present only [171]. It can, thus, be concluded that the ionic composition of the medium used can have an effect on the swelling and erosion behaviour of HPMC matrices, despite them being non-ionic polymers [172].…”

Section: Numerous Other In-vitromentioning

confidence: 99%

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Drug release from matrix tablets: physiological parameters and the effect of food

Nokhodchi

Asare-Addo

2014

Expert Opinion on Drug Delivery

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Introduction: As dissolution plays an important and vital role in the drug-delivery process of oral solid dosage forms, it is, therefore, essential to critically evaluate the parameters that can affect this process. Areas covered:The consumption of food as well as the physiological environment and properties of the gastrointestinal tract, such as its volume and composition of fluid, the fluid hydrodynamics, properties of the intestinal membrane, drug dose and solubility, pK a , diffusion coefficient, permeability and particle size, all affect drug dissolution and absorption rate. There are several dissolution approaches that have been developed to address the conditions as experienced in the in vivo environment, as the traditional dissolution being a quality control method is not biorelevant and as such do not always produce meaningful data. This review also describes the development of a systematic way that differentiates between robust and non-robust formulations by varying the effects of agitation and ionic strength through the use of the automated United States Pharmacopeia type III Bio-Dis apparatus. Expert opinion:With the improved understanding of the physiological parameters that can affect the oral bioperformance of dosage forms, strides have, therefore, been made in making dissolution testing methods more bio-logically based with the view of obtaining more in vitro--in vivo correlations.Keywords: agitation rate, biodissolution, drug release, effect of food, hydrophilic matrices, ionic strength Highlights -Understanding all the physiological parameters can serve as a basis for designing dissolution testing methods and systems that can more fully represent the gastrointestinal (GI) tract in humans and allow more in vitro-in vivo (IVIVC) correlations to be obtained thereby improving the oral bioperformance of dosage forms.-Simulation of GI conditions is essential to adequately predict the in vivo behaviour of drug formulations.-The choice of appropriate media for in vitro tests is crucial to their ability to correctly forecast the food effect in pharmacokinetic studies.-Several methods of dissolution testing have been conducted and are still ongoing that seek to further understand and develop media and dissolution methods to better represent the in vivo conditions and to aid in the better prediction of in vivo drug release.-Systematic change of agitation method and ionic strength evaluation may be used as additional tools in allowing for the identification of potential fed and fasted effects on drug release from hydrophilic matrices in the drive for developing dissolution methodologies that are more relevant in helping to achieve more IVIVC.

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Section: Physiological Parametersmentioning

confidence: 99%

Section: Numerous Other In-vitromentioning

confidence: 99%

Drug release from matrix tablets: physiological parameters and the effect of food

Nokhodchi

Asare-Addo

2014

Expert Opinion on Drug Delivery

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“…Figure 11. Rotating disk close-up (Korzhova, 2009) For many years the characterization of solid drugs has been performed using rotating disk intrinsic dissolution rate (IDR) apparatus, involving studies of dissolution-pH rate profiles in the presence of binding agents, various excipients/delivery vehicles, and buffers (Amidon, Lee & Topp, 2000;Jinno, Oh, Crison & Amidon., 2000;Li, Doyle, Metz, Royce & Serajuddin, 2005;Li, M. Wong, et al, 2005;McNamara & Amidon, 1986, 1988Mooney, Mintun, Himmelstein & Stella, 1981a, 1981bSerajuddin & Jarowski, 1984, 1985Sheng, Kasim, Chandrasekharan & L., 2006;Southard, Green, Stella & Himmelstein, 1992;Yu, Carlin, Amidon & Hussain, 2004).…”

Section: Rotating Disk Reactormentioning

confidence: 99%

Rotating Disk Apparatus: Types, Developments and Future Applications

Rashed¹,

Abdulbari²,

Salleh³

et al. 2016

MAS

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Power consumption reduction investigations attracted the attention of enormous numbers of researchers in the past few decades due to its high academic and economic impacts. The pumping power losses during the transportation of crude oils are considered as one of the main power consuming applications due to the turbulent mode of transportation. Investigating the possible solutions for this problem is expensive and time consuming due to the large apparatuses needed to simulate the flow in real pipelines. Rotating disk apparatus (RDA) is an instrument mainly comprising a rotating disk and an electrical motor to rotate the disk, which was implemented as an efficient and economical path to simulate what can be done in pipelines through generating a controlled degree of turbulence. This technique was also used in many other scientific applications due to its dynamic mode of operation. For example, a rotating disk electrode was used in electrodeposition processes and to characterize deposition film thickness and uniformity. The rotating disk reactor was employed to investigate the reaction rate between fluids and solid surfaces. The present work evaluates the RDA from different prospective and applications in order to introduce it as an efficient research tools for future dynamic investigations.

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“…The reviewed publications showed that different grades of water were used as media to determine the solubility of drug substance: double-distilled water (6)(7)(8); double deionized water (9), Milli-Q® purified water (10), 18.2 MΩ.cm/ 0.22 μm (11); Milli-Q®ultrapure water, conductivity less than 0.1 μS cm (12,13); ultrapure water Elix® Millipore (14); distilled water (5,15-21) deionized water (22)(23)(24)(25)(26); distilled, deionized, and filtered water (27); purified water (28)(29)(30)(31)(32)(33)(34)(35)(36); demineralized water (37). The type of water was not specified in 19 of 51 studies (37%) (38)(39)(40)(41)(42)(43)(44)(45)(46)(47)(48)(49)(50)(51)(52)(53)(54)(55)(56).…”

Section: Watermentioning

confidence: 99%

“…McIlvaine buffer solutions with a citrate/phosphate buffer system were used in the range of pH 4.0 to 6.8 (6.5%), or 3 out of 46 studies used it for the shake-flask method (5,27,48) and in 2 out of 20 studies as dissolution media (10.0%) (5,27). Maleate (32), Britton-Robinson universal (19,25,39), and glycine buffers (31) were selected, respectively, in the rate of 2.2% (1 out of 46 studies), 6.5% (3 out of 46 studies), and 2.2% (1 out of 46 studies), for the shake-flask method.…”

Section: Buffer Solutionsmentioning

confidence: 99%

Evolution of Choice of Solubility and Dissolution Media After Two Decades of Biopharmaceutical Classification System

Bou‐Chacra

Melo

Morales

et al. 2017

AAPS J

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Abstract.The introduction of the biopharmaceutics drug classification system (Biopharmaceutics Classification System (BCS)), in 1995, provided a simple way to describe the biopharmaceutics behavior of a drug. Solubility and permeability are among the major parameters, which determine the fraction dose absorbed of a drug substance and consequently its chances to be bioavailable. The purpose of this review is to summarize the evolution of the media used for determining solubility and dissolution and how this can be used in modern drug development. Over the years, physiologically adapted media and buffers were introduced with the intention to better predict the in vivo solubility and dissolution of drug substances. Water, buffer solutions, compendial media, micellar solubilization media, and biorelevant media are reviewed. At this time point, there is no universal medium available which can be used to predict every drug substance's solubility or a drug product's in vivo dissolution behavior. However, there have been many improvements and additions made to media to optimize their in vivo predictability; for example, the current phosphate concentrations in buffers seem to be too high to correlate with the carbonate buffer concentrations in vivo. Biorelevant media were updated to correlate them better with the composition of human intestinal fluids. The BCS was introduced into regulatory sciences as a scientific risk management tool to waive bioequivalence studies under certain conditions. Today's different guidance documents define the dose-solubility ratio differently. As shown for amoxicillin, this can cause more confusion than certainty for globally operating companies. Harmonization of BCS guidelines is highly desirable.

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Solubilization and dissolution of insoluble weak acid, ketoprofen: Effects of pH combined with surfactant

Cited by 114 publications

References 28 publications

Drug release from matrix tablets: physiological parameters and the effect of food

Drug release from matrix tablets: physiological parameters and the effect of food

Rotating Disk Apparatus: Types, Developments and Future Applications

Evolution of Choice of Solubility and Dissolution Media After Two Decades of Biopharmaceutical Classification System

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