Extended release suspension compositions

a suspension composition and composition technology, applied in the direction of digestive system, metabolism disorder, pharmaceutical non-active ingredients, etc., can solve the problems of inaccurate dosing and/or dose dumping, large compositions, poor patient compliance, etc., to improve patient compliance, facilitate administration, and improve dose flexibility

Inactive Publication Date: 2016-08-11
SUN PHARMA INDS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0015]The extended release suspension compositions of the present invention are easy to administer, thereby leading to enhanced patient compliance. Further, said extended release suspension compositions provide better dose flexibility depending on the age and body weight of the ...

Problems solved by technology

However, extended release solid compositions suffer from certain drawbacks such as difficulty in swallowing, particularly for certain groups of patients, e.g., pediatrics and geriatrics, resulting in poor patient compliance.
Further, high doses of active ingredient lead to large-sized compositions which aggravates this problem.
Also, there remains a tendency to divide extended release solid compositions such as tablets into small pieces in order to facilitate administration, which may ultimately lead to inaccurate dosing and/or dose dumping.
Although ...

Method used

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  • Extended release suspension compositions
  • Extended release suspension compositions
  • Extended release suspension compositions

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0112]

IngredientsQuantity (mg / mL)CoreMetformin hydrochloride100.00Microcrystalline cellulose spheres90.00Hydroxypropylmethyl cellulose5.00Purified waterq.s.Extended Release CoatingEthyl cellulose61.42Dibutyl sebacate6.82Acetoneq.s.Purified waterq.s.Total Weight of Extended Release Beads263.24 mgXylitol450.00Xanthan gum1.500Microcrystalline cellulose - sodium20.00carboxymethyl cellulose (Avicel ® CL 611)Strawberry flavor1.50VehiclePurified waterq.s. to 1 mL

Procedure:

[0113]1. Metformin hydrochloride and hydroxypropylmethyl cellulose were dissolved in purified water.[0114]2. Microcrystalline cellulose spheres were coated with the solution of step 1.[0115]3. Ethyl cellulose and dibutyl sebacate were dispersed in a mixture of acetone and purified water.[0116]4. The beads of step 2 were coated with the coating dispersion of step 3.[0117]5. Xylitol, xanthan gum, microcrystalline cellulose-sodium carboxymethyl cellulose, and strawberry flavor were mixed with the coated beads of step 4.[0118...

example 2

[0121]

IngredientsQuantity (mg / mL)CoreMetformin hydrochloride100.00Microcrystalline cellulose spheres90.00Hydroxypropylmethyl cellulose5.00Purified waterq.s.Extended Release CoatingEthyl cellulose61.42Dibutyl sebacate6.82Acetoneq.s.Purified waterq.s.Total Weight of Extended Release Beads263.24 mgXylitol450.00Xanthan gum1.50Microcrystalline cellulose - sodium20.00carboxymethyl cellulose (Avicel ® CL 611)Strawberry flavor1.50VehiclePurified waterq.s. to 1 mL

Procedure:

[0122]1. Metformin hydrochloride and hydroxypropylmethyl cellulose were dissolved in purified water.[0123]2. Microcrystalline cellulose spheres were coated with the solution of step 1.[0124]3. Ethyl cellulose and dibutyl sebacate were dispersed in a mixture of acetone and purified water.[0125]4. The beads of step 2 were coated with the coating dispersion of step 3.[0126]5. Xylitol, xanthan gum, microcrystalline cellulose-sodium carboxymethyl cellulose, and strawberry flavor were mixed with the coated beads of step 4 to obt...

example 3

[0128]

IngredientsQuantity (mg / 5 mL)CoreMetformin hydrochloride500.00Microcrystalline cellulose spheres375.00Hydroxypropylmethyl cellulose25.00Purified waterq.s.Extended Release CoatingEthyl cellulose340.20Dibutyl sebacate37.80Acetoneq.s.Purified waterq.s.Total Weight of Extended Release Beads1278.00 mgXylitol2250.00Xanthan gum7.50Microcrystalline cellulose - sodium100.00carboxymethyl cellulose (Avicel ® RC 591)Strawberry flavor7.50VehiclePurified waterq.s. to 5 mL

Procedure:

[0129]1. Metformin hydrochloride, microcrystalline cellulose, and hydroxypropylmethyl cellulose were sifted and mixed to obtain a blend.[0130]2. The blend of step 1 was mixed with purified water to obtain a wet mass.[0131]3. The wet mass of step 2 was extruded through an extruder.[0132]4. The extrudates of step 3 were spherionized through a spherionizer to obtain beads.[0133]5. The beads of step 4 were dried.[0134]6. Ethyl cellulose and dibutyl sebacate were dispersed in a mixture of acetone and purified water.[01...

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Abstract

The present invention relates to extended release suspension compositions of an active ingredient. Said extended release suspension compositions comprise multiple coated cores of the active ingredient and a suspension base, wherein the suspension base generates a hypertonic condition such that there is no substantial change in the in-vitro dissolution release profile of the extended release suspension compositions upon storage for at least seven days. The invention also relates to processes for the preparation of said extended release suspension compositions.

Description

FIELD OF THE INVENTION[0001]The present invention relates to extended release suspension compositions of an active ingredient. Said extended release suspension compositions comprise multiple coated cores of the active ingredient and a suspension base, wherein the suspension base generates a hypertonic condition such that there is no substantial change in the in-vitro dissolution release profile of the extended release suspension compositions upon storage for at least seven days. The invention also relates to processes for the preparation of said extended release suspension compositions.BACKGROUND OF THE INVENTION[0002]Extended release solid compositions are preferred dosage forms over immediate release solid compositions, especially for active ingredients showing fluctuations in the plasma concentration and for active ingredients having short half-lives. Extended release solid compositions can be in the form of tablets or capsules, wherein the release of the active ingredient is con...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K31/155A61K31/4439A61K31/165A61K31/522A61K31/43A61K9/10A61K9/00
CPCA61K9/0095A61K9/5089A61K9/5026A61K9/5042A61K9/5047A61K9/5078A61K9/5084A61K9/10A61K31/155A61K31/165A61K31/43A61K31/4439A61K31/522A61K9/501A61K9/5031A61K9/145A61K47/26A61K47/36A61K47/38A61K31/17A61P1/04A61P25/14A61P31/04A61P31/12A61P9/12A61P3/10A61K9/0053A61K9/1652A61K9/1676A61K9/5015
Inventor KUMAR, ASHISHSHEAR, RAJESH SRIKRISHANJAIN, SATISH KUMARSINGH, ROMI BARATJAIN, PARAS P.
Owner SUN PHARMA INDS
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