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Solid Pharmaceutical Compositions Containing Pregabalin

a technology of pharmaceutical compositions and pregabalin, which is applied in the direction of drug compositions, antibody medical ingredients, peptide/protein ingredients, etc., can solve the problems of undesirable lactam formation of pharmaceutical composition components, and achieve the effect of widening the absorption window and promoting undesirable lactam formation

Inactive Publication Date: 2012-02-02
WARNER LAMBERT CO LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0005]The present invention provides a stable pharmaceutical composition containing pregabalin that is useful for once daily oral dosing. When administered as a solid dosage form, such as a tablet, the pharmaceutical composition is retained in the stomach for a longer period of time than an IR dosage form. While it is retained in the stomach, the pharmaceutical composition continuously releases pregabalin. Eventually, the pharmaceutical composition passes out of the stomach and into the small intestine where it may continue to release pregabalin. Extending the period of time during which pregabalin is released in the stomach effectively widens the absorption window associated with IR dosing, thereby permitting QD dosing. Furthermore, stability studies suggest that none of the components of the pharmaceutical composition promote undesirable lactam formation.

Problems solved by technology

Furthermore, stability studies suggest that none of the components of the pharmaceutical composition promote undesirable lactam formation.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

examples

[0064]The following examples are intended to be illustrative and non-limiting. Unless otherwise indicated, the following procedures are used to measure drug release (aqueous dissolution), swelling, rigidity, and stability of the drug product as a function of time.

Drug Product Dissolution

[0065]The amount of API released from drug product samples immersed in aqueous dissolution media (0.06 N HCl or 0.5 M acetate buffer) at 37° C. is measured using a USP Apparatus 2 (paddles) or Apparatus 3 (reciprocating cylinder), which are operated at 50 rpm or 5 dpm, respectively. Samples of the dissolution media (1 mL) are typically taken at 1, 2, 4, 6, 9, 12, 16, and 24 hours and are analyzed using HPLC under the following conditions: column: Zorbax SB-CN, 150 mm×4.6 mm, 5 μm particle size; column temperature: 23° C.; detector wavelength: 210 nm; flow rate 1 mL / min; injection volume: 25 μL; mobile phase composition: 0.05 M sulfonic acid / hexane and 2 mL Et3N; pH adjusted to 3.1 with orthophosphori...

examples 1 to 11

[0069]TABLES 2 and 3 show compositions of laboratory-scale batches (25 g) containing pregabalin and various excipients; TABLES 4 and 5 show results of drug release as a function of time. For each of the formulations, drug product was prepared by blending all of the tablet components except for magnesium stearate in a TURBULA® mixer for about 15 minutes. Magnesium stearate was passed through a #20 standard sieve and combined with the contents of the TURBULA® mixer using a spatula. The resulting coarse blend was subsequently mixed in the TURBULA® mixer for an additional 4 minutes to obtain a final blend. Each of the final blends was compacted in a CARVER® Press using a compression force of 3000 pounds (EXAMPLES 1 to 5) or 2000 pounds (EXAMPLES 6 to 11) and a dwell time of 0.1 min, resulting in tablets with average hardness values of about 30 kp and nominal tablet weights of 1 g and 1.125 g, respectively. For some of the formulations (EXAMPLES 1 to 5), pregabalin was coated with COMPRI...

examples 12 to 14

[0070]TABLE 6 shows compositions of laboratory-scale batches (100 g) which contain pregabalin and excipients, and TABLE 7 shows drug release as a function of time. For each of the compositions, drug product was prepared by first combining pregabalin with COMPRITOL® 888 in an extruder-granulator. With the exception of magnesium stearate, the remaining tablet components were blended with the resulting pregabalin granules in a 1-pint V-blender for about 15 minutes. Magnesium stearate was passed through a #20 standard sieve and was combined with the contents of the V-blender using a spatula. The resulting coarse blend was subsequently mixed in the V-blender for an additional 4 minutes to obtain a final blend. Each of the final blends was compressed using a simulated KORSCH® XL 400 press (i.e., PRESSTER® Compaction Simulator) employing an average compression force of about 21 kN and average dwell time of 12 msec. The tablets displayed an average hardness of about 20 kp and a nominal tabl...

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PUM

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Abstract

A solid pharmaceutical composition containing pregabalin is described. The composition includes a matrix forming agent and a swelling agent and is suitable for once daily oral administration. Exemplary matrix forming agents include mixtures of polyvinyl acetate and polyvinylpyrrolidone, and exemplary swelling agents include cross-linked polymers of polyvinylpyrrolidone.

Description

BACKGROUND OF THE INVENTION[0001]This invention relates to solid pharmaceutical compositions containing pregabalin which are suitable for once daily (QD) oral dosing.[0002]Pregabalin, or (S)-(+)-3-aminomethyl-5-methyl-hexanoic acid, binds to the alpha-2-delta (a28) subunit of a calcium channel and is related to the endogenous inhibitory neurotransmitter γ-aminobutyric acid (GABA), which is involved in the regulation of brain neuronal activity. Pregabalin exhibits anti-seizure activity, as discussed in U.S. Pat. No. 5,563,175 to R. B. Silverman et al., and is useful for treating, among other conditions, epilepsy, pain, physiological conditions associated with psychomotor stimulants, inflammation, gastrointestinal damage, alcoholism, insomnia, fibromyalgia, and various psychiatric disorders, including anxiety, depression, mania, and bipolar disorder. In the United States, pregabalin has been approved for the treatment of diabetic peripheral neuropathy, postherpetic neuralgia, and as a...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/197A61P25/08A61P25/18A61P25/22A61P25/24A61P25/00A61P29/00
CPCA61K9/0065A61K9/2027A61K47/32A61K47/34A61K31/197A61P1/00A61P1/04A61P25/00A61P25/02A61P25/04A61P25/08A61P25/18A61P25/20A61P25/22A61P25/24A61P25/32A61P25/36A61P29/00A61K9/20A61K47/30A61K9/141A61K2039/542A61K9/146A61K9/0053
Inventor BOCKBRADER, HOWARD N.CHO, YUN HYUNGDIAZ SANTIAGO, STEVENMAHJOUR, MAJIDREYNOLDS, THOMAS DANIELSHAO, PUSHPA GANAPATHISHAO, ZEZHI JESSEWAN, JIANSHENG
Owner WARNER LAMBERT CO LLC
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