• 한국임상약학회지
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• 제8권1호
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• pp.1-12
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• 1998

Rheumatoid arthritis (RA) is a common systemic inflammatory disease which DMARDS have been widely used as a treatment modality both as monotherapy and combination therapy Bucillamine, one of newer DMARDS, has recently proven its efficacy as monotherapy in the treatment of RA. The objective of this study was to compare the efficacy and the safety of bucillamine monotherapy and bucillamine plus methotrexate combination therapy in the treatment of rheumatoid arthritis. Forty-nine mild RA patients were enrolled in this prospective, open-trial and were assigned to receive bucillamine 200 mg/day (n=18) or bucillamine 200 mg/day and methotrexate 7.5-15 mg/week (n=31) orally for 16 weeks. Concomitant use of NSAID and prednisolone <5 mg/day or equivalent dose of steroid were allowed. Both monotherapy group and combination therapy group have shown significant improvement in disease activities (Ritchie index, painful joints, swollen joints, morning stiffness, grip strength, ESR, RF, CRP, patient's self assessment of pain, physician's global assessment of disease activity) from the baseline. However, there was no statistically significant difference between two groups. The adverse effects were more frequently shown in combination therapy group than monotherapy group. In conclusion, in patients with mild RA monotherapy has shown to be equally efficacious as combination therapy with less side effects.

• Journal of Pharmaceutical Investigation
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• 제31권2호
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• pp.125-130
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• 2001

Bucillamine is a novel cysteine derivative with two free intramolecular sulfhydryl groups, and has a preventive and therapeutic effect on adjuvant arthritis, suggesting its antirheumatic action. With respect to the effect on the immune system, bucillamine-exerted such immunoregulating actions are to nomalize an excessive reduction or acceleration in immune reaction. It is useful not only in patients with early stage of rheumatoid arthritis (RA) but also in those with active RA retained for more than 10 years. The purpose of the present study was to evaluate the bioequivalence of two bucillamine tablets, $Rimatil^{TM}$ (Chong Kun Dang Pharmaceutical Co., Ltd.) and $Bucilin^{TM}$ (Kuhn Il Pharmaceutical Co., Ltd.), according to the guidelines of Korea Food and Drug Administration (KFDA). Eighteen normal male volunteers, $23.67{\pm}2.09$ years in age and $65.03{\pm}6.73\;kg$ in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After three tablets containing 100 mg of bucillamine per tablet were orally administered, blood was taken at predetermined time intervals and the concentrations of bucillamine in serum were determined using GC/MS with mass selective detector. Pharmacokinetic parameters such as $AUC_t$, $C_{max}\;and\;T_{max}$ were calculated and ANOVA test was utilized for the statistical analysis of the parameters. The results showed that the differences in $AUC_t$, $C_{max}\;and\;T_{max}$ between two tablets were -0.29%, -3.20% and 8.22%, respectively, when calculated against the $Rimatil^{TM}$ tablet. The powers $(1-{\beta})$ for $AUC_t\;and\;C_{max}$ were 84.31 % and 91.16%, respectively. Minimum detectable differences $({\Delta})$ at ${\alpha}=0.10$ and $1-{\beta}=0.8$ were less than 20% (e.g., 18.58% and 16.51% for $AUC_t\;and\;C_{max}$, respectively). The 90% confidence intervals were within ${\pm}20%$ (e.g.,$-12.77{\sim}12.20$ for $AUC_t$ and $-14.30{\sim}7.90$ for $C_{max}$). Two parameters met the criteria of KFDA for bioequivalence, indicating that $Bucilin^{TM}$ tablet is bioequivalent to $Rimatil^{TM}$ tablet.

• 약학회지
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• 제55권5호
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• pp.379-384
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• 2011

The aim of this study was to reduce the side effects and to develop effective drugs using bucillamine (B), lornoxicam (L), and its mixtures on the analgesic and anti-inflammatory effects. With this goal, we compared their effects on the four different mixtures with a sole treatment (B 40 mg/kg and L 1.60 mg/kg). The mixture 1, 2, 3, and 4 ratios of B to L (mg/kg) were 20 to 0.80, 40 to 1.60, 80 to 3.20, and 40 to 1.14, respectively. In terms of acetic acid-induced vascular permeability, B and L inhibited the amount of dye leakage approximately 37.8 and 66.5%, respectively. And mixture 1, 2 and 3 showed inhibition of 47.4%, 81.5%, and 84.3%. The mixture 4 inhibited approximately 49.4%. In carrageenan- induced paw edema model, mixtures of B and L effectively inhibited paw edema measured 1/2~3 hours after carrageenan injection. Especially, mixture 2 inhibited 50.7%, 52.7%, 50.9% of paw edema after 1, 2, and 3 hr, significantly. We also examined an analgesic effect using the writhing test. In terms of the acetic acid-induced writhing syndrome, the control group showed writhing syndrome 18.5 times. B and L showed 9 and 6.3 times, inhibiting 51.6% and 65.9% respectively. And aspirin, as a positive control drug, showed the 7.1 times writhing syndrome. The mixture 1, 2, 3, and 4 also significantly inhibited the writhing syndrome to 62.2%, 93.0%, 51.4%, and 77.8%, respectively. From these results, we could suggest that the range of B and L ratio of 25 : 1 to 35 : 1 may be applicable to developing analgesic and anti-inflammatory drugs.