• Journal of Pharmaceutical Investigation
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• v.39 no.6
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• pp.401-409
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• 2009

Ketrorolac tromethamine (KT), a nonsteroidal anti-inflammatory drug (NSAID) is required repeated administration due to its short blood half-life. To avoid dose-dependent side effects of KT, sustained-release pellets containing KT were prepared by coating with Eudragit$^{(R)}$ RS 100 and Eudragit$^{(R)}$ NE 30D. The in vitro and in vivo drug release behavior of KT from Eudragit$^{(R)}$ RS 100 and NE 30D coated pellet (SR-A), Eudragit$^{(R)}$ RS 100 coated pellet (SR-B) and conventional commercial immediate-release tablet (IR) was investigated. KT from SR-A and SR-B was slowly released over several hours, whereas IR showed rapid initial release in vitro. The pharmacokinetic study in vivo was performed by oral administration in beagle dogs. 5 mg IR was administered 3 times at intervals 5 hr. Five milligrams of IR was administered 3 times at intervals of 5 hr and 15 mg of SR-A and SR-B did once. After administering IR, KT concentration in blood showed high peak- trough fluctuation and stomach ulcer were discovered. On the other hand, SR-A and SR-B sustainedly released KT and reduced the occurrence of stomach ulcer. There sustained-release pellets will be effective system to minimize dosedependent of side effect and improve patient compliance.

• Korean Journal of Clinical Pharmacy
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• v.8 no.2
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• pp.101-106
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• 1998

A bioequivalence study of the Kerola tablets (Dongkwang Pharmaceutical Co., Korea) to the Tarasyn tablets (Roche Co., Korea), formulations of ketorolac trometamine(KTR), was conducted. Sixteen healthy Korean male subjects received each formulation at the dose of 10 mg as KTR in a $2\times2$ crossover study. There was a 1-week washout period between the dose. Plasma concentrations of KTR were monitored by an HPLC method for over a period of 12 hr after each administration. AUC (area under the plasma concentration-time curve) was calculated by the linear trapezoidal method. $C_{max}$ (maximum plasma drug concentration) and $T_{max}$ (time to reach $C_{max}$) were compiled from the plasma drug concentration-time data. Analysis of variance (ANOVA) revealed that there are no differences in AUC, $C_{max}\;and\;T_{max}$ between the formulations. The apparent differences between the formulations in these parameters were all far less than $20\%$ (i.e., 2.31, 8.19 and $0\%$ for AUC, $C_{max}\;and\;T_{max}$, respectively). Minimum detectable differences $(\%)\;at\;\alpha=0.1\;and\;1-\beta=0.8$ were all less than $20\%$ difference in these parameters between the formulations were all over 0.8. The $90\%$ confidence intervals for these parameters were also within $20\%$. These results satisfy the bioequivalence criteria of the Korea Food and Drug Administration (KFDA) guidelines (No. 1998-86). Therefore, these results indicate that the 2 formulations of KTR are bioequivalent and, thus, may be prescribed interchangeably.

• Clinics in Shoulder and Elbow
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• v.24 no.1
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• pp.4-8
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• 2021

Background: As nonsteroidal anti-inflammatory drugs (NSAIDs) and steroids have similar effects, steroids can be avoided to reduce adverse effects. This study aimed to compare the differences in symptom improvement after subacromial injection of steroids or NSAIDs. Methods: Sixty patients with rotator cuff syndrome for at least 3 months were enrolled and divided into steroid and NSAID groups. The steroid group received a mixture of 1 mL of triamcinolone acetonide (40 mg/mL) and 1 mL of lidocaine hydrochloride 2%, while the NSAID group received a mixture of 1 mL of Ketorolac Tromethamine (30 mg/mL) and 1 mL of lidocaine hydrochloride 2%. The patients were assessed before and at 3, 6, and 12 weeks after the procedure. Shoulder scores from visual analog scale (VAS), American Shoulder and Elbow Surgeons (ASES), and University of California Los Angeles (UCLA) were used for evaluation. Results: Both groups showed improvements in the clinical outcomes. Overall VAS, ASES, and UCLA scores improved from 6.9, 32.7, and 16.0 before the procedure to 2.0, 1.2, and 1.1; 81.5, 87.6, and 88.5; and 29.7, 31.8, and 32.0 at weeks 3, 6, and 12 weeks after the procedure, respectively. Twenty-six patients (86.7%) in the steroid group and 28 (93.3%) in the NSAID group reported satisfactory treatment outcomes. There were no significant differences in the outcomes between the two groups (p=0.671). Conclusions: Subacromial injection of NSAIDs for rotator cuff tendinitis with shoulder pain had equivalent outcomes with those of steroid injection at the 12-week follow-up.