Dissolution Testing for Poorly Soluble Drugs: A Continuing Perspective

Kuppusamy, Gowthamarajan

doi:10.14227/dt170310p24

Cited by 73 publications

(38 citation statements)

References 34 publications

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“…The rate of drug dissolution will be slowed by the limited solubility of the drug in that medium. In the present study, the value of C s /C d is greater than 3 in potassium chloride buffer at pH 1.2, 1.5, and 1.8 (23); borate buffer at pH 8; and 0.1 N HCl. Accordingly, sink conditions exist in a small volume of these dissolution media.…”

Section: Determination Of Solubility and Sink Conditionscontrasting

confidence: 38%

“…In addition, water quality is variable depending on the source and water pH is variable depending on the API and the excipients. Water is not considered a physiologically relevant medium as it is not representative of the gastric environment (23).…”

Section: Determination Of Solubility and Sink Conditionsmentioning

confidence: 99%

“…If standard solutions are not stable in a dissolution medium for at least 24 h at ambient temperature, it should not be chosen (23). Stability study results (Table 2) reveal that the change in concentration of drug samples stored in different dissolution media (potassium chloride buffer pH 1.2, 1.5, and 1.8; borate buffer pH 8; and 0.1 N hydrochloric acid) and in light at 25 °C over 2 days was less than 3% of that of reference solutions.…”

Section: Stability Determinationmentioning

confidence: 99%

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Development and Validation of a Dissolution Method for Pioglitazone Tablets

Kulkarni¹,

Shahnawaz²,

Zaheer³

et al. 2012

Dissolution Technol.

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Dissolution testing has emerged in the pharmaceutical field as a very important tool to characterize drug product performance. Pioglitazone hydrochloride, a frequently prescribed antidiabetic, has no dissolution assay in official monographs. The aim of the study was to develop and validate a dissolution test for the quality control of pioglitazone hydrochloride (PH) tablets containing 15 mg of active pharmaceutical ingredient (API). Results from testing sink conditions and stability at 37 °C show that PH is stable in potassium chloride buffer at pH 1.2, 1.5, 1.8, and in 0.1 N hydrochloric acid. In vitro dissolution tests of PH tablets were performed using different test conditions but always under sink conditions. The effects of filtration and deaeration were evaluated. The most discriminatory test conditions, potassium chloride buffer at pH 1.5 (900 mL at 37 ± 0.5 °C) as dissolution medium, paddle method (Apparatus 2), 75 rpm, and 60 min, were satisfactory. The UV spectrophotometric method for determination of released PH was developed and validated. The method presented linearity (r 2 = 0.999) in the concentration range of 10-60 μg/mL. The recoveries were good, ranging from 96.407% to 100.24%. The intraday and interday precision results were 1.704% and 1.3869% RSD, respectively. The developed dissolution test is adequate for its purpose and can be applied for the quality control of 15-mg PH tablets.

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Section: Determination Of Solubility and Sink Conditionscontrasting

confidence: 38%

Section: Determination Of Solubility and Sink Conditionsmentioning

confidence: 99%

Section: Stability Determinationmentioning

confidence: 99%

See 1 more Smart Citation

Development and Validation of a Dissolution Method for Pioglitazone Tablets

Kulkarni¹,

Shahnawaz²,

Zaheer³

et al. 2012

Dissolution Technol.

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“…This is due to fact that there is no barrier for diffusion at dialysis membrane interface for ARM molecules and sink conditions were maintained (C s /C d ¼ 50.4) for diffusion to take place from drug solution into dissolution medium through dialysis membrane. To maintain sink conditions, C s /C d value should be greater than or equal to 3, where C s is the saturated solubility of the compound in the medium and C d is the concentration of compound in the bulk medium (Gowthamarajan & Singh, 2010). Hence, higher release was observed in case of ARM-SOL.…”

Section: In Vitro Release Studiesmentioning

confidence: 99%

Optimization of artemether-loaded NLC for intranasal delivery using central composite design

Jain¹,

Sood²,

Kuppusamy³

2014

Drug Delivery

126

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The objective of the study was to optimize artemether-loaded nanostructured lipid carriers (ARM-NLC) for intranasal delivery using central composite design. ARM-NLC was prepared by microemulsion method with optimized formulation having particle size of 123.4 nm and zeta potential of À34.4 mV. Differential scanning calorimetry and powder X-ray diffraction studies confirmed that drug existed in amorphous form in NLC formulation. In vitro cytotoxicity assay using SVG p12 cell line and nasal histopathological studies on sheep nasal mucosa indicated the developed formulations were non-toxic and safe for intranasal administration.In vitro release studies revealed that NLC showed sustained release up to 96 h. Ex vivo diffusion studies using sheep nasal mucosa revealed that ARM-NLC had significantly lower flux compared to drug solution (ARM-SOL). Pharmacokinetic and brain uptake studies in Wistar rats showed significantly higher drug concentration in brain in animals treated intranasally (i.n.) with ARM-NLC. Brain to blood ratios for ARM-NLC (i.n.), ARM-SOL (i.n.) and ARM-SOL (i.v.) were 2.619, 1.642 and 0.260, respectively, at 0.5 h indicating direct nose to brain transport of ARM. ARM-NLC showed highest drug targeting efficiency and drug transport percentage of 278.16 and 64.02, respectively, which indicates NLC had better brain targeting efficiency compared to drug solution.

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“…In vitro dissolution has been recognized as an important element in drug development, and under certain conditions, it can be used as a potential surrogate marker of bioequivalence (46,47).…”

Section: Dissolution Testmentioning

confidence: 99%

Development, Physical-Chemical Stability, and Release Studies of Four Alcohol-Free Spironolactone Suspensions for Use in Pediatrics

Bernal¹,

Calpena²,

Mallandrich³

et al. 2014

Dissolution Technol.

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Dissolution studies have become of great significance because, in most cases, drug dissolution is the rate-limiting step in the absorption process. As occurs with solid oral dosage forms, heterogeneous dispersed systems (suspensions) could also have some problems with their in vitro dissolution.The objective of this study was to evaluate the influence of excipients on the release of spironolactone from four alcohol-free suspensions (pharmaceutical compounding) of spironolactone 5 mg/mL suitable for pediatric use.In addition, the comparison of the physical and chemical stability of the suspensions stored at 4, 25, and 40 °C over a 60-day period has been studied. Rheological behavior, particle size, a prediction of long-term physical stability, pH, and assay of spironolactone by HPLC were assessed at preset times. The dissolution profile of each suspension was determined and compared with that of the commercial tablets. A microbiological study of the best formula was also performed. Chemically, the four spironolactone suspensions were stable for 60 days stored at three temperatures; Suspension IV had optimum pH values and the highest recovery percentage. In terms of physical stability, sedimentation occurred in Suspension IV, and flotation of spironolactone occurred in Suspensions I, II, and III. Suspension III had the highest viscosity and the slowest drug release. Suspension IV was also microbiologically stable for 60 days. In conclusion, Suspension IV had the best properties. The least suitable form was Suspension III, as its high viscosity made it difficult to achieve homogeneous redispersion and it had the slowest dissolution profile.

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Dissolution Testing for Poorly Soluble Drugs: A Continuing Perspective

Cited by 73 publications

References 34 publications

Development and Validation of a Dissolution Method for Pioglitazone Tablets

Development and Validation of a Dissolution Method for Pioglitazone Tablets

Optimization of artemether-loaded NLC for intranasal delivery using central composite design

Development, Physical-Chemical Stability, and Release Studies of Four Alcohol-Free Spironolactone Suspensions for Use in Pediatrics

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