Compositions and dosage forms for enhanced absorption of gabapentin and pregabalin
A technology of pregabalin and gabapentin, which is applied in the field of complexes of gabapentin or pregabalin and transport parts, which can solve the inconvenience to patients
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Embodiment 1
[0142] Preparation of gabapentin-transport moiety complexes and pregabalin-transport moiety complexes
[0143] Preparation of gabapentin-transport moiety complexes
[0144] 1. Prepare a solution of 0.5 mL of 36.5% hydrochloric acid (5 mmol HCl) in 25 mL of deionized water.
[0145] 2. Add 5 mmol gabapentin (0.86 g) to the solution from step 1. The mixture was stirred at room temperature for 10 minutes. Gabapentin hydrochloride is formed.
[0146] 3. Add 5 mmol sodium lauryl sulfate (1.4 g) to the aqueous solution of step 2. The mixture was stirred at room temperature for 20 minutes.
[0147] 4. Add 50 mL of dichloromethane to the solution from step 3. The mixture was stirred at room temperature for 2 hours.
[0148] 5. Transfer the mixture from step 4 to a separatory funnel and allow it to settle for 3 hours. Two phases form, a lower phase of dichloromethane and a higher phase of water.
[0149] 6. Separate the high and low phases from step 5. The lower phase dichloro...
Embodiment 2
[0158] In Vivo Colonic Absorption in a Rat Irrigated-Ligated Colon Model
[0159] An animal model commonly known as "flush-ligated colon model" or "intracolonic ligated model" is used. Fasted 0.3-0.5 kg Sprague-Dawley male rats were anesthetized and the segment closest to the colon was isolated. Flush the fecal material from the colon. Both ends of the colon segment are ligated while a catheter is placed in the lumen and removed intraperitoneally and placed on the skin for delivery of the test formulation. The contents of the colon were rinsed and the colon was returned to the animal's abdominal cavity. According to the set experiment, the test agent was added after the segment was perfused with 1 mL / kg of 20 mM sodium phosphate buffer, pH 7.4, more accurately mimicking the actual colonic environment in the clinical setting.
[0160] Rats (n=3) were allowed to equilibrate for approximately 1 hour following surgical preparation and prior to exposure to each test fo...
Embodiment 3
[0167] Absorption in the body
[0168] 28 large rats were randomly divided into 7 test groups (n=4). The gabapentin or gabapentin-lauryl sulfate complex prepared as described in Example 1A was intubated to the beginning of the duodenum of rats at doses of 5 mg / rat, 10 mg / rat and 20 mg / large, respectively. mouse. The remaining test group received 1 mg / kg gabapentin intravenously.
[0169] Blood samples from each animal were drawn after 4 hours and analyzed for gabapentin content. The results are shown in Tables D-H and Figures 6A-6C.
[0170] Gabapentin lauryl sulfate, duodenal dose 5mg / rat
[0171] Gabapentin lauryl sulfate, duodenal dose 10mg / rat
[0172] Gabapentin lauryl sulfate, duodenal dose 20mg / rat
[0173] Gabapentin, duodenal dose 5mg / rat
[0174] Gabapentin, duodenal dose 10mg / rat
[0175] Gabapentin, duodenal dose 20mg / rat
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