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Method of treating a disease condition susceptible to baclofen therapy

a disease condition and effective treatment technology, applied in the field of effective methods of treating a disease condition susceptible to baclofen therapy, can solve the problems of reduced bioavailability of release preparations, increased plasma concentrations, and increased blood plasma concentrations. , to achieve the effect of increasing plasma levels

Inactive Publication Date: 2011-08-18
SUN PHARMA INDS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0017]It has surprisingly been found that when controlled release drug delivery system comprising baclofen or its pharmaceutically acceptable salt or its derivative was administered to human subjects in the evening in the fed state, the maximum plasma concentration of baclofen (Cmax) achieved after administration of the system in evening was sustained over a longer duration (see FIG. 1 and FIG. 3) than compared to that after administration of the system in the morning in the fed state. Surprisingly when the system was administered in the evening, it was observed that the duration over which absorption of baclofen occurred was prolonged and higher plasma levels were maintained during the latter half of the dosing period as compared to those obtained by morning dosing. Evening dosing thus can provide an optimum maintenance of relief from the systems of the disease condition by maintaining baclofen levels at higher therapeutic effective plasma concentrations even in the latter half of the dosing period.

Problems solved by technology

Frequent administration of immediate release baclofen tablets leads to fluctuations in plasma concentration producing peaks and troughs.
Peaks in plasma concentration are associated with side effects, such as drowsiness (sedation), dizziness and muscle weakness and troughs cause inadequate control of muscle spasm.
Although a single daily administration of the full daily dose (referred to as “high dose” to signify the higher amount of baclofen in a single sustained release tablet compared to that in one immediate release tablet even though the total daily dose remains the same) would be convenient however, the problem was that when baclofen was given in single high daily doses as sustained or controlled release preparation the bioavailability was reduced.
Anything in the stomach is expected to be cleared due to these strong contractions or otherwise cause the problems of blocking of the pyloric sphincter or accumulation of the object in the stomach after it is repeatedly ingested by the human subject.
It is also not possible to use a dosage form that would resist such housekeeper waves because it will be totally unacceptable for safety reasons to allow the accumulation of the residual dosage form in the stomach.
However, this alone was not sufficient and an additional design feature in these systems was that they released a fraction of the drug in a more absorbable immediate release form that contributed to baclofen levels only for the initial duration of the 24 hr dosing nevertheless it obtained 24 hrs desired plasma levels by combining the more absorbable form with the slow release form which is criticized in the prior art as being “poorly absorbable”.

Method used

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  • Method of treating a disease condition susceptible to baclofen therapy
  • Method of treating a disease condition susceptible to baclofen therapy
  • Method of treating a disease condition susceptible to baclofen therapy

Examples

Experimental program
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example 1

[0076]This example represents an embodiment of the controlled release drug delivery system which is gastric retention drug delivery system comprising baclofen. It is prepared according to formulae given Table 1 below.

TABLE 1first region of second compositionS.Qty in% by weight of theNo.Ingredientsmgdrug delivery system1Baclofen353.252Mannitol32430.123Hydroxypropyl Cellulose -mw807.431150; apparent viscosity1500-3000 at 1% w / v4Colloidal silicon dioxide50.465Talc12.51.666Magnesium stearate12.51.167Hydrogenated Vegetable oil20.01.868Mannitol46.04.279Water soluble protective20.01.85film coating based on lowviscosity hydroxypropyl-methyl cellulose

[0077]First Region of Second Composition

[0078]Table 1 gives the formula for the preparation of the first region of the second composition. The first region is the formulation that is filled into gelatin capsules. The polymer hydroxypropylmethyl cellulose, low viscosity that does not function as a rate controlling polymer but only serve as a aid ...

example 2

[0088]A gastric retention drug delivery system comprising baclofen was prepared as mentioned in Table 8 below.

TABLE 8Composition detailsmg per weightof drug% by weight of theIngredientsdelivery systemdrug delivery systemFirst region of the second compositionBaclofen22.55.49Fumaric acid10.02.44Mannitol264.564.5Hydroxypropyl cellulose68.016.59Sodium bicarbonate30.07.32Colloidal silicon dioxide5.01.22Talc5.01.22Magnesium stearate5.01.22Second region of the second compositionAlginic acid54.35Coated to aSodium bicarbonate10.87weight gain ofSodium starch glycolate27.17about 25% byMannitol13.59weight of the corePolyvinylpyrrolidone16.30Talc3.26Polysorbate1.09Third compositionPolycarbophil4.41Coated to aSodium bicarbonate8.82weight gain ofMethacrylic acid copolymer35.29about 18% byEudragit S-1008.82weightMannitol35.29Sodium starch glycolate10.29Polysorbate0.59Polyethylene glycol1.47Talc2.35Diethyl phthalate6.62First compositionBaclofen7.5Coated to aPolyvinylpyrrolidone1.50weight gain ofTalc...

example 3

[0090]A gastric retention drug delivery system comprising baclofen was prepared as mentioned in Table 9 below.

TABLE 9Quantity(% w / w of the drugIngredients(mg / capsule)delivery systemFirst region of the second compositionBaclofen22.55.49Fumaric acid10.02.44Mannitol200.548.90Polycarbophil108.026.34Sodium bicarbonate54.013.17Colloidal silicon dioxide5.01.22Talc5.01.22Magnesium stearate5.01.22

[0091]The first region of the second composition was obtained by blending the excipients listed in Table 10 with baclofen and filling it in a hard gelatin capsule. The capsule was then coated with a second region of the second composition and third composition similar to example 2 described above.

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Abstract

The present invention discloses a method of treating a disease condition susceptible to baclofen therapy, said method comprising orally administering once-a-day in the evening a controlled release drug delivery system comprising baclofen or its pharmaceutically acceptable salt or its derivatives and pharmaceutically acceptable excipients.

Description

FIELD OF INVENTION[0001]The present invention relates to an effective method of treating a disease condition susceptible to baclofen therapy, said method comprising administering a controlled release drug delivery system of baclofen or its pharmaceutically acceptable salts or its derivatives.[0002]The present invention also relates to an effective method of treating disease conditions susceptible to baclofen therapy, said method comprising administering a controlled release drug delivery system of baclofen or its pharmaceutically acceptable salts or its derivatives and to the use of baclofen for such treatment.BACKGROUND OF THE INVENTION[0003]U.S. Pat. No. 3,471,548 disclosed 4-amino-3-(p-chlorophenyl)butyric acid). 4-amino-3-(p-chlorophenyl)butyric acid) designates the R-isomers, the S-isomer and mixtures of R and S isomers including the racemate. Baclofen is indicated in many disease conditions such as for alleviating signs and symptoms of spasticity resulting from multiple sclero...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/22A61K31/195A61K9/00A61P21/00
CPCA61K31/197A61K9/006A61K9/0065A61K9/5047A61K9/4866A61K9/4891A61K9/209A61P1/04A61P1/08A61P11/14A61P19/08A61P21/00A61P21/02A61P25/24A61P25/32A61P25/34A61P25/36A61P29/00
Inventor DHARMADHIKARI, NITIN BHALACHANDRAZALA, YASHORAJ RUPSINH
Owner SUN PHARMA INDS
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