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High-dosage extended-release formulation of gepirone

A technology of gepirone and tablets, applied in the field of high-dose delayed-release preparations of gepirone, can solve problems such as adverse side effects, unsatisfactory, and reduction

Inactive Publication Date: 2007-11-21
FABRE KRAMER HLDG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] Hitherto, it was believed to be impossible to formulate high-dose gepirone extended-release forms that would not result in 1-(2-pyrimidinyl)piperazine, the major metabolite of gepirone, which is believed to be responsible for adverse side effects, including dizziness , nausea, headache, and drowsiness) had an unsatisfactory increase in the amount or a relative decrease in efficacy

Method used

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  • High-dosage extended-release formulation of gepirone
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  • High-dosage extended-release formulation of gepirone

Examples

Experimental program
Comparison scheme
Effect test

preparation example

[0153] A tablet form of the extended release oral dosage form of gepirone was prepared following the process described above and in US Patent No. 5,478,572. Generally, this process requires (i) mixing all of gepirone hydrochloride, all of colorants, all of colloidal silicon dioxide and 20% of hydroxypropyl methylcellulose; (ii) mixing of The mixture of (i) was up to 15 minutes and then crushed using a Fitzmill #0020 plate; (iii) to the blend from (ii) was added all of the microcrystalline cellulose, 50% of magnesium stearate and the remaining 80% of Hydroxypropylmethylcellulose; (iv) blending the blend from (iii) for 28 minutes; (v) slugging the blend from (iv) using a rotary tablet press; (vi) using a Fitzmill #0093 tablet Grinding the pellets from (v); (vii) adding the remaining 50% magnesium stearate to the milled pellets from (vi); (viii) lubricating / blending the mixture from (vii) up to 7 minutes; and (ix) compressing the blend from (viii) into the final desired tablet f...

Embodiment 1

[0157] Example 1: Dissolution mode of 60mg preparation and 20mg preparation

[0158] Table 2 below lists the comparative dissolution profiles of 20 mg and 60 mg tablets in all SUPAC-MR dissolution media.

[0159] time (hours)

medium

intensity

1

2

4

8

10

12

14

16

18

20

0.01M HCl

20mg

20.2

30.4

45.1

64.7

71.8

77.8

82.8

86.9

90.5

93.4

0.01M HCl

60mg

22.0

32.8

48.2

68.6

76.0

82.0

87.1

91.2

94.5

97.3

water

20mg

19.8

29.8

44.0

63.1

70.1

76.0

80.9

85.0

88.4

91.3

water

60mg

21.9

32.7

48.2

68.6

75.8

81.7

86.6

90.5

93.7

96.2

pH=4.5

20mg

17.7

26.6

39.5

57.2

63.8

69.4

74.3

...

Embodiment 2

[0165] Example 2: Bioequivalence of the 80 mg formulation versus the 20 mg formulation

[0166] To date, efficacy and pharmacokinetic data for extended-release gepirone tablets have primarily been obtained by administering one or more 20 mg extended-release gepirone tablets (similar to those described in the preparations above). Therefore, a study was undertaken to demonstrate the bioequivalence of 40 mg (data not shown) with 80 mg extended release gepirone tablets (as described in the preparation above) and multiple 20 mg extended release gepirone tablets.

[0167] To this end, an open-label, randomized, four-way crossover, single-dose study design was employed, with a one-week washout period between treatments. During each study period, subjects were hospitalized from the afternoon until 36 hours after gepirone administration. After excretion, blood samples were collected at 48, 60 and 72 hours post-dose. Thirty-two (32) subjects were administered gepirone during the study...

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Abstract

A machine ( 1 ) for making filter bags ( 4 ) of tetrahedral shape for infusion products comprises a revolving conveyor drum ( 15 ) driven by a first drive shaft ( 16 ) to feed a web ( 5 ) of filter paper along a path (P) on which there are positioned: a station ( 25 ) for feeding the filter paper web ( 5 ); a station ( 21 ) for feeding a succession of tags ( 6 ); a station ( 22 ) for feeding tie string ( 7 ) connecting the filter bags ( 4 ) to the respective tags ( 6 ); a station ( 23 ) for arranging the tie string ( 7 ) according to a defined pattern on the path (P); and a plurality of sealers ( 24 ) facing the path (P) to attach the tie string ( 7 ) and the tags ( 6 ) to the filter paper web ( 5 ). The sealers ( 24 ) perform a defined movement between a sealing position and a waiting position, and this movement, which is performed simultaneously and synchronously by all the sealers ( 24 ), is imparted, through a transmission element ( 39 ) shared by all the sealers ( 24 ), by a second cam drive shaft ( 36 ) connected to the same source of motion ( 18 ) to which the first shaft ( 16 ) that drives the conveyor drum ( 15 ) is connected.

Description

technical field [0001] The present invention relates to a high dose extended release formulation of gepirone and a method of treating major depression by administering the formulation to a subject in need thereof. More specifically, the present invention relates to high dose extended release tablets of gepirone. The invention also relates to a method of treating depression in a mammal by administering to a subject in need thereof an effective amount of a high dose extended release formulation of gepirone according to the invention. Background technique [0002] Gepirone (Gepirone, also known as 4,4-dimethyl-1-[4-[4-(2-pyrimidinyl)-1-piperazinyl]-butyl]-2,6-piperidine Diketone hydrochloride) can be prepared by the procedure described in Example 7 of Temple, U.S. Patent 4,423,049 (hereby incorporated by reference in its entirety), and has the following structure: [0003] [0004] Gepirone and its salts are known to possess antidepressant and anxiolytic properties and are...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/48
CPCA61K31/506A61K9/2054A61P25/00A61P25/22A61P25/24
Inventor S·J·克雷默L·F·法布雷
Owner FABRE KRAMER HLDG
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