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      Single dose pharmacokinetic equivalence study of two gabapentin preparations in healthy subjects

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          Abstract

          Background

          The current study was conducted to find out whether two oral preparations of 300 mg gabapentin (the test and reference capsules) were bioequivalent.

          Subjects and methods

          This was a randomized, single-blind, crossover study under fasting condition, with a 7-day washout period, which included 37 healthy adult male and female subjects. After an overnight fast, subjects were given, orally, one capsule of the test drug or of the reference drug. Blood samples were drawn immediately before taking the drug, then at 20 and 40 minutes, and 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 15, and 24 hours after dosing, to evaluate pharmacokinetic parameters of the single dose administration, ie, the area under the plasma concentration–time curve (AUC) from time zero to 24 hours (AUC t), AUC from time zero to infinity (AUC inf), the peak plasma concentration of the drug (C max), time needed to achieve C max (t max), and the elimination half-life (t 1/2). The plasma concentrations of gabapentin were determined using validated high-performance liquid chromatography with ultraviolet detection.

          Results

          The geometric mean ratios (90% confidence interval) of the test drug/reference drug for gabapentin were 103.15% (90.38%–117.72%) for AUC t, 103.53% (90.78%–118.07%) for AUC inf, and 108.06% (96.32%–121.24%) for C max. The differences in t max and t 1/2 values between the test and reference drug products for gabapentin were not statistically significant. Light-headedness, nausea, and headache were encountered during the study, but they were all mild and well tolerated. The 90% confidence intervals of the test/reference AUC ratio and C max ratio of gabapentin were within the acceptance range for bioequivalence.

          Conclusion

          The two preparations of gabapentin 300 mg capsule were bioequivalent, thus both can be used interchangeably in the clinical setting.

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          Most cited references 29

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          Gabapentin for the symptomatic treatment of painful neuropathy in patients with diabetes mellitus: a randomized controlled trial.

          Pain is the most disturbing symptom of diabetic peripheral neuropathy. As many as 45% of patients with diabetes mellitus develop peripheral neuropathies. To evaluate the effect of gabapentin monotherapy on pain associated with diabetic peripheral neuropathy. Randomized, double-blind, placebo-controlled, 8-week trial conducted between July 1996 and March 1997. Outpatient clinics at 20 sites. The 165 patients enrolled had a 1- to 5-year history of pain attributed to diabetic neuropathy and a minimum 40-mm pain score on the Short-Form McGill Pain Questionnaire visual analogue scale. Gabapentin (titrated from 900 to 3600 mg/d or maximum tolerated dosage) or placebo. The primary efficacy measure was daily pain severity as measured on an 11-point Likert scale (0, no pain; 10, worst possible pain). Secondary measures included sleep interference scores, the Short-Form McGill Pain Questionnaire scores, Patient Global Impression of Change and Clinical Global Impression of Change, the Short Form-36 Quality of Life Questionnaire scores, and the Profile of Mood States results. Eighty-four patients received gabapentin and 70 (83%) completed the study; 81 received placebo and 65 (80%) completed the study. By intent-to-treat analysis, gabapentin-treated patients' mean daily pain score at the study end point (baseline, 6.4; end point, 3.9; n = 82) was significantly lower (P<.001) compared with the placebo-treated patients' end-point score (baseline, 6.5; end point, 5.1; n = 80). All secondary outcome measures of pain were significantly better in the gabapentin group than in the placebo group. Additional statistically significant differences favoring gabapentin treatment were observed in measures of quality of life (Short Form-36 Quality of Life Questionnaire and Profile of Mood States). Adverse events experienced significantly more frequently in the gabapentin group were dizziness (20 [24%] in the gabapentin group vs 4 [4.9%] in the control group; P<.001) and somnolence (19 [23%] in the gabapentin group vs 5 [6%] in the control group; P = .003). Confusion was also more frequent in the gabapentin group (7 [8%] vs 1 [1.2%]; P = .06). Gabapentin monotherapy appears to be efficacious for the treatment of pain and sleep interference associated with diabetic peripheral neuropathy and exhibits positive effects on mood and quality of life.
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            Gabapentin: pharmacology and its use in pain management.

            Although its exact mode of action is not known, gabapentin appears to have a unique effect on voltage-dependent calcium ion channels at the postsynaptic dorsal horns and may, therefore, interrupt the series of events that possibly leads to the experience of a neuropathic pain sensation. Gabapentin is especially effective at relieving allodynia and hyperalgesia in animal models. It has been shown to be efficacious in numerous small clinical studies and case reports in a wide variety of pain syndromes. Gabapentin has been clearly demonstrated to be effective for the treatment of neuropathic pain in diabetic neuropathy and postherpetic neuralgia. This evidence, combined with its favourable side-effect profile in various patient groups (including the elderly) and lack of drug interactions, makes it an attractive agent. Therefore, gabapentin should be considered an important drug in the management of neuropathic pain syndromes.
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              Randomized double-blind study comparing the efficacy of gabapentin with amitriptyline on diabetic peripheral neuropathy pain.

              Reports of gabapentin use in diabetic peripheral neuropathy pain stimulate a need for controlled trials to determine its comparative efficacy to the therapeutic standard of amitriptyline hydrochloride. To determine the efficacy of gabapentin compared with amitriptyline in treating diabetic peripheral neuropathy pain. Prospective, randomized, double-blind, double-dummy, crossover study. Veterans Affairs San Diego Healthcare System, Ambulatory Care Clinic. Twenty-eight veterans were referred by their primary care providers. Two patients withdrew before randomization because of no neuropathic pain after washout; a third withdrew for unexpected surgery that required analgesics. Three patients withdrew because of adverse effects and 1 for protocol violation. Patients with stable glycemic control and neuropathic pain randomized to 6 weeks of therapy with gabapentin, 900 to 1800 mg/d, or amitriptyline hydrochloride, 25 to 75 mg/d, with a 1-week washout before crossover. Pain relief measured by pain scale with verbal descriptors and global pain score assessment at treatment end. Participants and investigators were blinded throughout. Mean dosages were of gabapentin, 1565 mg/d, and of amitriptyline hydrochloride, 59 mg/d. Sixty-five percent of patients reached maximum dose with gabapentin and 54% with amitriptyline. Mean score diary analysis showed pain relief with gabapentin and amitriptyline was not significantly different (P = .26). Global data were obtained from 21 of 25 enrolled patients who completed the study. Moderate or greater pain relief was experienced in 11 (52%) of 21 patients with gabapentin and 14 (67%) of 21 patients with amitriptyline. There were no significant period or carry-over effects (P = .35). Although both drugs provide pain relief, mean pain score and global pain score data indicate no significant difference between gabapentin and amitriptyline. Gabapentin may be an alternative for treating diabetic peripheral neuropathy pain, yet does not appear to offer considerable advantage over amitriptyline and is more expensive. Larger trials are necessary to define gabapentin's place in treating diabetic peripheral neuropathy pain.
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                Author and article information

                Journal
                Drug Des Devel Ther
                Drug Des Devel Ther
                Drug Design, Development and Therapy
                Drug Design, Development and Therapy
                Dove Medical Press
                1177-8881
                2014
                04 September 2014
                : 8
                : 1249-1255
                Affiliations
                [1 ]Dexa Laboratories of Biomolecular Sciences, Cikarang, Indonesia
                [2 ]PT Equilab International, Bioavailability and Bioequivalence Laboratory, Jakarta, Indonesia
                Author notes
                Correspondence: Raymond R Tjandrawinata, Dexa Laboratories of Biomolecular Sciences, Dexa Medica Group, Indonesia, Industri Selatan V, Block PP no 7, Kawasan Industri Jababeka II, Cikarang 17550, Indonesia, Tel +62 21 8984 1901, Fax +62 21 8984 1905, Email raymond@ 123456dexa-medica.com
                Article
                dddt-8-1249
                10.2147/DDDT.S69326
                4159312
                © 2014 Tjandrawinata et al. This work is published by Dove Medical Press Limited, and licensed under Creative Commons Attribution – Non Commercial (unported, v3.0) License

                The full terms of the License are available at http://creativecommons.org/licenses/by-nc/3.0/. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed.

                Categories
                Original Research

                Pharmacology & Pharmaceutical medicine

                bioavailability, bioequivalence, antiepilepsy

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