FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to pharmaceutical agents and concerns an delayed-release oral tablet containing: (a) 10-80 wt % 1-{[(α-isobutanoyloxyehtoxy)carbonyl]aminomethyl)-1-cyclohexane acetic acid, and (b) 1-30 wt % of a fatty compound, such as glycerine ester, lauryl alcohol, myristyl alcohol, stearyl alcohol, cetyl alcohol, cytostearyl alcohol, palmitoyl alcohol, ouricury wax, hydrated vegetable oil, candelilla wax, esparto wax, stearic acid, hard wax, beeswax, glyco wax, hydrated castor oil and carnauba wax or their combination, where the value wt % is calculated by total dry weight of the dosage form which when taken by a human patient on an empty stomach per 1-{[(α-isobutanoyloxyehtoxy)carbonyl]aminomethyl)-1-cyclohexane acetic acid 1100-1300 mg provides the plasma gabapentin concentration profile Cmax 3-6 mcg/ml at Tmax 4-7 hours and AUC 30-70 mcgh/ml; when taken by a human patient after meal per 1-{[(α-isobutanoyloxyehtoxy)carbonyl]aminomethyl)-1-cyclohexane acetic acid 1100-1300 mg provides the plasma gabapentin concentration profile Cmax 5-8 mcg/ml at Tmax 6-11 h and AUC 60-110 mcgh/ml. What is also offered is application of 1-{[(α-isobutanoyloxyehtoxy)carbonyl]aminomethyl)-1-cyclohexane acetic acid for preparing a delayed-release tablet for treating restless leg syndrome and postherpetic neuralgia.
EFFECT: tablets under the invention provide improved pharmacokinetic profile of gabapentin.
17 cl, 8 dwg, 2 tbl, 8 ex
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