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Novel parenteral carbamazepine formulation

一种卡马西平剂、卡马西平的技术，应用在绝对生物利用率的精确信息。领域

Inactive Publication Date: 2008-11-19
OVATION PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Preferably the modified cyclodextrin is sulfobutyl ether-7-beta-cyclodextrin

Method used

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  • Novel parenteral carbamazepine formulation
  • Novel parenteral carbamazepine formulation
  • Novel parenteral carbamazepine formulation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Preparation of embodiment 1-carbamazepine-cyclodextrin inclusion complex

[0051] 450 grams of hydroxypropyl-beta-cyclodextrin (HPBCD) was dissolved in 2.0 L of deionized water to produce a 22.5% w / v solution. 13 C. 15N-labeled carbamazepine (CBZ) [purchased from Cambridge Isotope Laboratories (CIL), 50 Frontage Road, Andover, Massachusetts 01810], 20 grams, was added to this solution. The resulting mixture was stirred at room temperature (20-25°C) for 24 hours. After 24 hours, the solution was sterile filtered through a sterile 0.22 micron Durapore filter into a sterile receiver. It is then filled into the previously sterilized ampoules under nitrogen flow and sealed. Filled ampoules are stored at 2-8°C. The resulting inclusion complex has a CBZ concentration of approximately 10 mg / ml.

Embodiment 2

[0052] Embodiment 2-stability test

[0053] Ampules containing 10.1 mg / ml carbamazepine-cyclodextrin inclusion complex were placed in a room temperature stability study and samples were taken every six months. CBZ was detected by HPLC at 215 nm using UV detection. The results are shown in Table 2.

[0054]

Embodiment 3

[0055] Example 3 - Pharmacokinetics of intravenous and oral carbamazepine for maintenance therapy in patients

[0056] An indwelling catheter is placed in the test subject's arm. A single 100 mg dose of stably labeled (non-radioactive) CBZ (SL-CBZ) was then infused over 10 minutes. At the end of the infusion, subjects' usual morning dose of oral CBZ, less than 100 mg, was administered. During and for one hour after the infusion, monitor blood pressure, heart rate and rhythm, and infusion site discomfort. A single blood sample was collected prior to infusion and 12 samples were collected over the subsequent 96 hours. Plasma was isolated from blood and analyzed using LC-MS analysis for CBZ and CBZ epoxides, active metabolites and inactive glucuronidated metabolites. Unbound CBZ was measured after ultrafiltration. CBZ concentration-time data were analyzed using the non-compartmental method with the pharmacokinetic software WinNONLIN.

[0057] Validated LC-MS analysis was use...

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Abstract

The present invention is directed to a carbamazepine-cyclodextrin inclusion complex useful for the parenteral administration of carbamazepine. The carbamazepine-cyclodextrin inclusion complex is prepared by the admixture of a modified cyclodextrin and carbamazepine in a physiologically acceptable fluid. Modified cyclodextrins include 2-hydroxypropyl-beta-cyclodextrin and sulfoalkyl cyclodextrins. More particularly, the sulfoalkyl cyclodextrins are those described and disclosed in U.S. Patent Nos. 5,134,127 and 5,376,645. A physiologically acceptable fluid includes sterile isotonic water, Ringer's lactate, D5W (5 % dextrose in water), physiological saline, and similar fluids suitable for parenteral administration.

Description

[0001] related application [0002] This application claims priority to US Provisional Patent Application 60 / 722,692, filed September 30,2005. Background technique [0003] Carbamazepine, or 5H-dibenzo[b,f]azepine-5-carboxamide, is a widely used antiepileptic agent. It is available in the US as Tegretol.RTM. trademark 100 mg chewable tablet, 200 mg tablet and 100 mg / 5 mL suspension for oral administration as a therapeutic agent for epilepsy or as a specific analgesic for trigeminal neuralgia. Other trade names include Equetro, Carbatrol, Tegretol XR, and Epitol. Generic versions of these oral dosage forms are also available. Dosage forms include Carbatrol, available in 100, 200, and 300 mg strengths; and Tegretol XR, available in 100, 200, and 400 mg strengths. [0004] As shown in Table 1, the recommended maintenance dose level in adults and children over 12 years of age is 800-1200 mg per day, while dose levels as high as 2400 mg per day have been used in adults. The mai...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/55
CPCC08B37/0015A61K31/724B82Y5/00A61K47/48969A61K31/55A61K47/6951A61P21/02A61P25/00A61P25/08A61P9/00A61P9/08A61K2300/00A61K9/0019A61K47/40C08B37/0012
Inventor 詹姆斯·克洛迪安格拉·伯恩鲍姆伊洛·莱皮克斯蒂芬·科林斯
Owner OVATION PHARMA
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