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Modified-release tablet of bupropion hydrochloride

Inactive Publication Date: 2005-10-27
BIOVAIL LAB INT SRL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0036] In another aspect of the invention, the moisture barrier substantially impedes or retards the absorption of moisture into the tablet, thereby increasing the stability of the bupropion hydrochloride

Problems solved by technology

The drug resembles a psycho stimulant in terms of its neurochemical and behavioral profiles in vivo, but it does not reliably produce stimulant-like effects in humans at clinically prescribed doses.
The immediate release formulation results in more than a 75% release of the bupropion into the dissolution media in about 45 minutes, and one of the major side effects of bupropion has been the incidence of seizures, which in part appears to be strongly associated with the immediate release of the bupropion into the system.
In general, patient compliance is a problem with medications that require a multiple dosing regimen and is especially problematic with depressed individuals.
The major disadvantage of matrix systems is that they generally display a first order release profile.
There is currently no approved commercially available stable once daily bupropion dosage form.
It is known that bupropion hydrochloride is highly hygroscopic and, as such, is relatively unstable and susceptible to decomposition over time especially under high humidity conditions.

Method used

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  • Modified-release tablet of bupropion hydrochloride
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  • Modified-release tablet of bupropion hydrochloride

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0098] 1. Modified Release Tablet Formulations

[0099] Three different core formulations were prepared for each of the 150 mg and 300 mg modified release bupropion hydrochloride tablets as shown in Table 1:

TABLE 1 CORE FORMULATION150 mg300 mgABCA′B′C′Ingredients(mg / %)1(mg / %)(mg / %)(mg / %)(mg / %)(mg / %)Bupropion 150 / 81.1 150 / 82.4150 / 79 300 / 79  300 / 87.6 300 / 83.5hydrochlorideBinder2 5.3 / 2.865.3 / 2.95.3 / 2.810.6 / 2.8 10.6 / 3.1 10.6 / 2.95Lubricant3 4.7 / 2.54 4.7 / 2.58 4.7 / 2.46 9.4 / 2.48 9.4 / 2.74 9.4 / 2.61Purified water4******Total dry weight  160 / 86.48  160 / 87.91  160 / 83.77  320 / 84.43  320 / 93.47  320 / 89.02of core

1The mg / % values represent the proportion of the ingredient in relation to the tablet dry weight

2Polyvinyl alcohol

3Glyceryl behenate (Compritol 888 ATO)

4Evaporated during drying

[0100] The water is first heated to 60±5° C. The binder (polyvinyl alcohol) is next dissolved in the water to homogeneity and then passed through a 0.7 mm mesh screen and allowed to cool to a temperature of no mor...

example 2

[0118] 1. The Moisture Barrier is not an Enteric Coat

[0119] The purpose of this study was to show that the modified release bupropion hydrochloride tablets of the invention are not enteric coated. The modified release formulation is based on a tablet core comprising bupropion hydrochloride, a binder and a lubricant. The tablet core is coated with a control-releasing coat, which functions to control the release of the bupropion hydrochloride. The control-releasing coated tablet cores are subsequently coated with a moisture barrier, which substantially impedse or retards absorption of moisture.

[0120] The release of the drug was measured spectrophotometrically by a two-stage dissolution procedure using USP enteric coating dissolution conditions method B (Basket at 75 rpm) to evaluate the tablet integrity. The results of the tests are shown in Tables 11 and 12:

TABLE 11 Acid Stage: % dissolvedTimeof 300 mg modified release bupropion HCl tablets(hr)V1V2V3V4V5V6MeanSD00.00.00.00.00.00....

example 3

[0130] The objective of this study was to investigate the dosage strength equivalency of the following test 150 mg and 300 mg product strengths of Bupropion HCl modified-release tablets under fasting conditions. A two-way, crossover, open-label, single-dose, fasting, dosage strength equivalency study of two strengths (150 mg and 300 mg) of bupropion HCl modified-release tablets of the invention was conducted. The modified-release tablets of the invention were administered once daily in normal healthy non-smoking male and female subjects.

[0131] The study design involved a 2-period, 2-treatment, single-dose crossover design under fasting conditions. The study periods were separated by a 3-week washout period. A total of 36 subjects (19 Male, 17 Female) enrolled for the study of which 35 of the subjects (19 Male, 16 Female) completed the study. Subjects were administered the following treatments: [0132] A) 2×150 mg q.d. modified-release bupropion hydrochloride tablets of the invention...

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Abstract

A modified-release tablet of bupropion hydrochloride comprising (i) a core comprising an effective amount of bupropion hydrochloride, a binder, a lubricant; and (ii) a control releasing coat surrounding said core; and (iii) a moisture barrier surrounding said control releasing coat, wherein the modified-release tablet is bioequivalent to Wellbutrin® or Zyban® / Wellbutrin® SR tablets.

Description

FIELD OF THE INVENTION [0001] The present invention relates to a modified-release tablet of pharmaceutically acceptable salts of bupropion, preferably bupropion hydrochloride. BACKGROUND [0002] Bupropion is an antidepressant chemically unrelated to tricyclics, tetracyclics, selective serotonin re-uptake inhibitors (SSRIs), or other known antidepressant agents. The drug resembles a psycho stimulant in terms of its neurochemical and behavioral profiles in vivo, but it does not reliably produce stimulant-like effects in humans at clinically prescribed doses. Its structure closely resembles that of diethylpropion and it is related to phenylethylamines. It is designated as (±)-1-(3-chlorophenyl)-2-[(1,1-dimethylethyl)amino]-1-propanone hydrochloride and by its generic name amfebutamone hydrochloride. Bupropion hydrochloride is commercially available as an immediate release form (Wellbutrin®) and a sustained release form (Wellbutrin® SR and Zyban®). Both Wellbutrin® SR and Zyban® are chem...

Claims

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Application Information

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IPC IPC(8): A61KA61K9/20A61K9/22A61K9/24A61K9/28A61K9/32A61K9/36
CPCA61K9/2027A61K9/284A61K9/2886A61K9/2866A61K9/2846A61P25/00A61P25/24A61P43/00A61K9/20A61K31/135
Inventor OBEREGGER, WERNERERADIRI, OKPONANABOFAZHOU, FANGMAES, PAUL
Owner BIOVAIL LAB INT SRL
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