Sustained-release tramadol formulations with 24-hour efficacy
A tramadol and tablet technology, applied in the field of new oral pharmaceutical compositions, can solve the problems of inability to replace successfully
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Embodiment 1
[0108] A. Cross-linking
[0109] High amylose (30.0 kg) containing about 70% w / w amylose (Cl AmyloGel 03003) was placed in the reactor. Water (55.0 l) containing sodium hydroxide (30.0 g) and sodium sulfate (2.40 kg) was added to the reactor. The resulting slurry was heated to a temperature of 30°C. Phosphorus oxychloride (22.5 g) was added to the reaction mixture and reacted for one hour.
[0110] B. Chemical Modification, Hydroxypropylation
[0111] The crude reaction mixture from Part A was transferred to the hydroxypropylation reactor. The reaction mixture was heated to a temperature of 40° C. for 30 minutes and purged with nitrogen. After complete termination, propylene oxide (1.80 kg) was added. The reaction mixture was kept at 40°C for 20 hours. with 0.1N H 2 SO 4 (1:2 v / v) to neutralize the reaction mixture to pH 5.5. The starch slurry was washed with a basket centrifuge at 1200 rpm. The resulting starch cake was reslurried in 35 l of water and centrifuged fo...
Embodiment 2
[0118] A. Cross-linking
[0119] High amylose (30.0 kg) containing about 70% w / w amylose (Cl AmyloGel 03003) was placed in the reactor. Into the reactor was charged water (55.0 1) containing sodium hydroxide (30.0 g) and sodium sulfate (2.40 kg). The resulting slurry was heated to a temperature of 30°C. Phosphorus oxychloride (45 g) was added to the reaction mixture and reacted for one hour.
[0120] B. Chemical Modification, Hydroxypropylation
[0121] The crude reaction mixture from Part A was transferred to the hydroxypropylation reactor. The reaction mixture was heated to a temperature of 40°C for 30 minutes and quenched with nitrogen. After complete termination, propylene oxide (1.80 kg) was added. The reaction mixture was kept at 40°C for 20 hours. with 0.1N H 2 SO 4 (1:2 v / v) to neutralize the reaction mixture to pH 5.5. The starch slurry was washed with a basket centrifuge at 1200 rpm. The resulting starch cake was reslurried in 35 l of water and centrifuged ...
Embodiment 3
[0137] Formulations A, B and C shown in Table 1 were prepared according to the procedure given above.
[0138] Table 1: Formulations of tramadol hydrochloride controlled release formulations A, B and C.
[0139]
[0140]
[0141] figure 2 Dissolution profiles for Formulations A, B and C are shown.
[0142] once-daily formulation of tramadol
[0143] The present invention relates to controlled release tablet compositions which provide analgesia within 2 hours of oral administration and for at least 24 hours after administration.
[0144] A 200 mg dose of the controlled release composition of the present invention surprisingly provides rapid analgesic effect within 2 hours after oral administration, with mean blood levels ranging from 100 ng / mL to 200 ng / mL for at least 24 hours after administration of a single dose between.
[0145] Furthermore, at steady state, mean tramadol plasma concentrations range between 100 ng / mL and 350 ng / mL. The controlled release composi...
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