Novel dosage form

a dosage form and a new type of technology, applied in the field of dosage forms, can solve the problems of high active ingredient concentration, difficult to achieve the effect of reducing the size of the dosage form, and reducing so as to achieve convenient swallowing, reduce the size of the dosage form, and effectively control the release rate of modified

Inactive Publication Date: 2006-07-13
TORRENT PHARMA LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0027] The present invention also teaches the use of dual retard technique to effectively control the release rate of modified release active ingredient by using small quantity of release controlling agents. This dual retard technique thus sufficiently reduces the size of the dosage form, which is convenient for swallowing.
[0076] The outer portion can also include a material that improves the processing of the release controlling agents. Such materials are generally referred to as “plasticisers” and include, for example, adipates, azelates, benzoates, citrates, isoebucaes, phthalates, sebacates, stearates, tartrates, polyhydric alcohols and glycols.

Problems solved by technology

There are several reasons to do this, namely, the disease itself is progressive, with deterioration of glycemic control over time; mono-therapeutic attempts to achieve and maintain glycemic control often fail in the long run; multiple defects in the disease and consequently primary drug failures (1, 2, 3).
However, because of the disparity in the duration of action (half-life), these combinations are given twice or thrice a day.
The techniques described above do not work well when the difference in the dose of active ingredients are high for example where the weight ratio of active ingredients in immediate release and modified release is from 1:10 to 1:15000 and the dose of modified release active ingredient per unit is from 500 mg to 1500 mg.
The techniques described in the prior art do not give good results when the active ingredient is highly soluble.
The weight of the dosage form becomes very high, or complicated process for manufacturing is required, or accurate dosing of low dose active ingredient is difficult when the techniques reported in the prior art are utilized to make formulation with high dose, high solubility active ingredient in the form of modified release and small dose active ingredient into immediate release form where the weight ratio of immediate release active ingredient and modified release active ingredient is from 1:10 to 1:15000 and the weight of modified release active ingredient per unit is from 500 mg to 1500 mg and also it is inconvenient to swallow due to large size.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

1) Production of Inner Portion

[0106] 11.71% w / w of pravastatin sodium is mixed with 52.62% w / w of lactose monohydrate and 22.22% w / w starch and the mixture is granulated in a binder of 2.22 v povidone in water and then dried. The granules are sieved and mixed with 1.11% w / w magnesium stearate, 9.0 g sodium starch glycolate, 0.11% w / w lake of sunset yellow. This mixture is compressed to 90 mg weight tablets having a diameter of 6.35 mm

2) Production of Outer Portion

[0107] A) Micro matrix particles—90.91% w / w of niacin is mixed with 9.09% w / w of Eudragit RSPO (Ammonio Methacrylate Copolymer type B USP) and the mixture is granulated with a solvent mixture of acetone and methylene chloride and then dried. The granules are sized.

[0108] B) Coating of Micro matrix particles—85.84% w / w of micro matrix particles is charged in fluidized bed processor. 13.61% w / w of hydrogenated castor oil is dissolved in acetone and this coating solution is sprayed to coat the micro matrix particles. The...

example 2

1) Production of Inner Portion

[0114] 38.47% w / w of lamotrigine is mixed with 2.71% w / w of crosspovidone and 0.18% w / w colloidal silicon dioxide and the mixture is granulated in a binder of 0.71% w / w povidone in water and then dried. The granules are sieved and mixed with 28.70% w / w of Mannitol (Pearlitol SD 200®), 12.31% w / w of crosspovidone, 2.31% w / w of magnesium stearate, 6.15% w / w aspartame, 2.31% w / w talc, 5.0% w / w flavour and 1.15% w / w of colloidal silicon dioxide. This mixture is compressed to 65 mg weight tablets having a diameter of 5.55 mm.

2) Production of Outer Portion

[0115] A) Micro matrix particles—90.91% w / w of sodium valproate is mixed with 9.09% w / w of Eudragit RSPO (Ammonio Methacrylate Copolymer type B USP) and the mixture is granulated with a solvent mixture of acetone and methylene chloride and then dried. The granules are sized.

[0116] B) Coating of Micro matrix particles—85.84% w / w of micro matrix particles is charged in fluidized bed processor. 13.61% w / w...

example 3

1) Production of Inner Portion

Same for Example 1

2) Production of Outer Portion

[0122] 77.76% w / w of niacin is mixed with 7.78% w / w of Eudragit RSPO (Ammonio Methacrylate Copolymer type B USP) and the mixture is granulated with a solvent mixture of acetone and methylene chloride and then dried. The granules are sized and mixed with 13.61% w / w of hydrogenated castor oil and 0.86% w / w of magnesium stearate.

2) Compression of Tablets

Tablet (A)—Same as for Example 1

Tablet (B)—Same as for Example 1

[0123] The dissolution rate of the novel dosage form was determined (Table 5 and 6)

TABLE 5Dissolution profile of tablet (A)NiacinPravastatin sodiumTime (hour)% ReleasedTime (min)% Released130.14575.9243.66080.9461.6674.1883.91092.11299.424102.6

[0124]

TABLE 6Dissolution profile of tablet (B)NiacinPravastatin sodiumTime (hour)% ReleasedTime (min)% Released129.94589.6236.36090.0452.8663.4873.51077.81284.52490.5

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Abstract

A dosage form comprising of a high dose, high solubility active ingredient as modified release and a low dose active ingredient as immediate release where the weight ratio of immediate release active ingredient and modified release active ingredient is from 1:10 to 1:15000 and the weight of modified release active ingredient per unit is from 500 mg to 1500 mg; a process for preparing the dosage form.

Description

FIELD OF INVENTION [0001] This invention relates to a dosage form comprising of a high dose, high solubility active ingredient as modified release and a low dose active ingredient as immediate release where the weight ratio of immediate release active ingredient and modified release active ingredient is from 1:10 to 1:15000 and the weight of modified release high dose high solubility active ingredient per unit is from 500 mg to 1500 mg and the weight of immediate release active ingredient is up to 50 mg; a process for preparing the formulation BACKGROUND OF THE INVENTION [0002] Combining two active ingredients in one pharmaceutical unit to improve patient compliance is known in literature. It can be either in the form of two or more active ingredients in immediate release form or a combination of immediate release and modified release form. There are various techniques by which the combination of immediate release and modified release is formulated in single dosage form. [0003] Seve...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/26A61K9/20A61K9/22A61K9/24A61K31/155A61K31/19A61K31/22A61K31/4025A61K31/455A61K31/53
CPCA61K9/2077A61K9/2081A61K9/209A61K31/155A61K31/19A61K31/22A61K31/4025A61K31/455A61K31/53
Inventor VAYA, NAVINKARAN, RAJESH SINGHNADKARNI, SUNIL SADANAQUPTA, VINOD KUMAR
Owner TORRENT PHARMA LTD
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