Lee Hyeontae
(Dept. of Pharmaceutical Sciences, College of Pharmacy, Catholic University)
,
Park Sang-Ae
(Korea Food & Drug Administration)
,
Sah Hongkee
(Dept. of Pharmaceutical Sciences, College of Pharmacy, Catholic University)
The objective of this study was to investigate the effects of sodium lauryl sulfate upon the saturation solubility of carbamazepine, its dissolution kinetics, and $T_{50\%}$ defined as the time required for dissolving $50\%$ of carbamazepine. Water, 0.1N-HCI, and phosphate buff...
The objective of this study was to investigate the effects of sodium lauryl sulfate upon the saturation solubility of carbamazepine, its dissolution kinetics, and $T_{50\%}$ defined as the time required for dissolving $50\%$ of carbamazepine. Water, 0.1N-HCI, and phosphate buffers at pH 4.0 and 6.8 containing 0.1, 0.5, 1, and $2\%$ sodium lauryl sulfate were used as dissolution media. The dissolution study was conducted by using the USP dissolution apparatus II with an agitation rate of 75 rpm. Samples of the dissolution media were taken in 7, 15, 30, 45, 60, 75, and 90 min, and the amounts of carbamazepine were determined spectrophotometrically at 285 nm. All dissolution data were fitted well into a four-parameter exponential equation: $Q\;=\;a(1\;-\;e^{-bxt})\;+\;c(1\;-\;e^{-dxt})$. In this equation Q represented $\%$ carbamazepine dissolved at a time t, and a, b, c, and d were constants. This equation led to the calculation of dissolution rates at various time points and $T_{50\%}$. It was found that the dissolution rate of carbamazepine was directly proportional to the aqueous concentration of sodium lauryl sulfate. In addition, under our experimental conditions $T_{50%}$ values ranged from 37.8 to 4.9 min. It was interesting to note that $T_{50\%}$ declined rapidly as the surfactant concentration increased from 0.1 to $0.5\%$, whereas it declined more slowly at concentrations greater than $1\%$. These results clearly demonstrated that the dissolution rate of carbamazepine and duration of its dissolution test could be tailored by optimizing the amount of sodium lauryl sulfate in a dissolution medium.
The objective of this study was to investigate the effects of sodium lauryl sulfate upon the saturation solubility of carbamazepine, its dissolution kinetics, and $T_{50\%}$ defined as the time required for dissolving $50\%$ of carbamazepine. Water, 0.1N-HCI, and phosphate buffers at pH 4.0 and 6.8 containing 0.1, 0.5, 1, and $2\%$ sodium lauryl sulfate were used as dissolution media. The dissolution study was conducted by using the USP dissolution apparatus II with an agitation rate of 75 rpm. Samples of the dissolution media were taken in 7, 15, 30, 45, 60, 75, and 90 min, and the amounts of carbamazepine were determined spectrophotometrically at 285 nm. All dissolution data were fitted well into a four-parameter exponential equation: $Q\;=\;a(1\;-\;e^{-bxt})\;+\;c(1\;-\;e^{-dxt})$. In this equation Q represented $\%$ carbamazepine dissolved at a time t, and a, b, c, and d were constants. This equation led to the calculation of dissolution rates at various time points and $T_{50\%}$. It was found that the dissolution rate of carbamazepine was directly proportional to the aqueous concentration of sodium lauryl sulfate. In addition, under our experimental conditions $T_{50%}$ values ranged from 37.8 to 4.9 min. It was interesting to note that $T_{50\%}$ declined rapidly as the surfactant concentration increased from 0.1 to $0.5\%$, whereas it declined more slowly at concentrations greater than $1\%$. These results clearly demonstrated that the dissolution rate of carbamazepine and duration of its dissolution test could be tailored by optimizing the amount of sodium lauryl sulfate in a dissolution medium.
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문제 정의
However, there is a dispute regarding what volume is really ade디니ate to approximate sink conditions. Therefore, this study is aimed at investigating the effects of SLS upon the saturation solubility of the poorly watersoluble model drug carbamazepine and its dissolution pattern. It focuses on the dissolution kinetics established to describe the dissolution pattern of carbamazepine.
제안 방법
Dependence of a dissolution rate upon the magnitude of sink conditions. Dissolution test was conducted by use of 50 mM phosphate buffer at pH 4 containing (.) 0.1, (■) 0.5, (▲) 1, and (▼) 2% SLS. Values inside the parenthesis represent the magnitude of sink conditions.
It focuses on the dissolution kinetics established to describe the dissolution pattern of carbamazepine. In addition, this study has attempted to correlate SLS effects to the dissolution rate of carbamazepine and T50% defined as the time req니ired for the release of 50% of the lab으led carbamazepine. To do so, the diss이니tion data of a carbamazepine immediate release tablet have been generated by use of a n니mber of diverse dissolution media containing 0.
Such a propensity was attributed to the effect of SLS upon carbamazepine solubility. To back up this supposition, T50% values were plotted as a function of carbamazepine solubility determined under 16 different experimental conditions (Fig. 8): a total of 4 different dissolution media were used in this study, and each medium contained 4 different levels of SLS. It was found that T50% could be correlated to carbamazepine solubility (Cs) with the following equation: T50% = 30.
데이터처리
where Q represented % carbamazepine dissolved at a specific time t, and a, b, c, and d were constants. A correlation coefficient was calculated to j니dge the degree of c니rve fitting. This equation permitted the determination of T50% defined as the time required for dissolving 50% of the labeled carbamazepine.
이론/모형
The USP dissolution apparatus II (paddle method) was used to conduct the dissolution test. The types of dissolution media used in this st나dy included water, 0.
성능/효과
The equation made it possible to substantiate the concentrationdependent SLS effects upon the dissolution pattern of carbamazepine, its dissolution rate, and T50%. The relevant results demonstrated that adjusting an SLS concentration would be very effective in tailoring the dissolution rate of carbamazepine and the curation of its dissolution test. Such information might be invaluable in developing a dissolution test as a QC tool for poorly water-soluble pharmaceuticals.
69%. The resuIts demonstrated that the requirements for content uniformity were met because the carbamazepine content in each of the 10 tablets lied within the range of 85% to 115% of the label claim and the relative standard deviation was less than 6%.
97). The results indicate that T50% declines rapidly as an SLS concentration shift옹 from 0.1 to 0.5%, but it declines more slowly at SLS concentrations greater than 1%.
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