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Low Excipients Load Pharmaceutical Composition

Abstract: The present invention relates to optimized cost-efficient pharmaceutical composition and process of preparation thereof. The present invention provides a pharmaceutical composition with reduced excipient load comprising at-least one or more active ingredient and pharmaceutically acceptable excipient wherein the size and weight of the tablet has been reduced compared to the conventional reference drug.

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Patent Information

Application #
Filing Date
06 September 2022
Publication Number
10/2024
Publication Type
INA
Invention Field
CHEMICAL
Status
Email
Parent Application

Applicants

AKUMS DRUGS & PHARMACEUTICALS LIMITED
304, Mohan Place, LSC, Block-C, Saraswati Vihar

Inventors

1. Sanjeev Jain
Plot no. 131 to 133, Block – C, Mangolpuri Industrial Area, Phase – 1 (Adjoining CBSE Office), Delhi - 110083

Specification

DESC:1. A pharmaceutical composition with a reduced excipient load comprising

a) at least one active ingredient or combination of therapeutically compatible medicament; and
b) pharmaceutically acceptable excipient

wherein the reduced excipient load is reduced by 5 to 80% and the dosage form having a reduced size and weight for patient compliance.

2. The pharmaceutical composition as claimed in claim 1, wherein

the active ingredient or medicament can be selected from antidiabetic, analgesic, antibacterial, antifungal, antiviral, anticancer, anti-histamines, anti-depressants, anesthetics, antacids, anti-rheumatoid, anti-asthmatics, anti-allergic, antiarrhythmic, anti-convulsants, anti-emetics, anti-infective, anti-protozoals, anti-inflammatory agents, anti-nauseants, anti-hyperlipidemic drugs, anti- parkinson, anti-psychotics, antipyretics, anti-spasmodic, anti-thrombotic drugs, anticoagulants, anti-platelets, anti-tumor drugs, anti-urticaria drugs, anxiolytic agents, appetite stimulants, appetite suppressants, anti-hypertensive (diuretics, beta-blockers, ACE inhibitors, calcium channel blockers, vasodialators), chelating agents, cholecystokinin antagonists, cognition activators, cough suppressants, erythropoietic drugs, fertility agents, anti-diarrhoeals, laxatives, antiulcer agents, growth regulators, immunomodulating agents, Janus kinase (JAK) inhibitors, neuroleptics, neuromuscular agents, neuroprotective, Non-steroidal anti- inflammatory drug (NSAID), potassium channel blocker, potassium channel opener, prostaglandins, respiratory stimulants, selective aldosterone receptor blocker, sedatives & hypnotics, synthetic hormones, tachykinin nk 1 antagonist, vaso-constrictors and vertigo agents, vitamins or a combination thereof.

3. The pharmaceutical composition as claimed in claim 1, wherein pharmaceutically acceptable excipient is selected from a diluent, binder, preservative, colourant, solvent, glidant, lubricant or a combination thereof.

4. The pharmaceutical composition as claimed in claim 1, wherein the size and weight of the tablet has been reduced by 5% to 60% compared to the conventional reference drug.

5. The pharmaceutical composition as claimed in claim 1-3, wherein
a) the active ingredient is a combination of Aceclofenac 20% by weight and Paracetamol 65% by weight; and
b) pharmaceutically acceptable excipient
wherein the weight of the dosage is reduced by 15 to 30%.

6. The pharmaceutical composition as claimed in claim 1-3, wherein
a) the active ingredient is a combination of Nimesulide 20% by weight and Paracetamol 65% by weight; and
b) pharmaceutically acceptable excipient
wherein the weight of the dosage is reduced by 20 to 25%.

7. The pharmaceutical composition as claimed in claim 1-3, wherein
a) the active ingredient is a combination of Diclofenac 10% by weight and Paracetamol 67% by weight; and
b) pharmaceutically acceptable excipient
wherein the weight of the dosage is reduced by 20 to 40%.

8. The pharmaceutical composition as claimed in claim 1-3, wherein
a) the active ingredient is a combination of Dapagliflozin and Metformin; and
b) pharmaceutically acceptable excipient
wherein the weight of the dosage is reduced by 30 to 45%.

9. The pharmaceutical composition as claimed in claim 1-3, wherein
c) the active ingredient is a combination of Metformin hydrochloride and Glimepiride; and
d) pharmaceutically acceptable excipient
wherein the weight of the dosage is reduced by 10 to 20%.

10. The pharmaceutical composition as claimed in claim 1-3, wherein
e) the active ingredient is Ondansetron; and
f) pharmaceutically acceptable excipient
wherein the weight of the dosage is reduced by 30 to 45%.
11. The pharmaceutical composition as claimed in claim 1-3, wherein
a) the active ingredient is a combination of Telmisartan and Chlorthalidone; and
b) pharmaceutically acceptable excipient.

12. The pharmaceutical composition as claimed in claim 1-3, wherein
a) the active ingredient is a combination of Cilnidipine and Telmisartan; and
b) pharmaceutically acceptable excipient.

13. The pharmaceutical composition as claimed in claim 1-3, wherein
a) the active ingredient is a combination of Telmisartan, Cilnidipine and Chlorthalidone; and
b) pharmaceutically acceptable excipient.

14. The pharmaceutical composition as claimed in claim 1-3, wherein
a) the active ingredient is Telmisartan; and
b) pharmaceutically acceptable excipient.

15. The pharmaceutical composition as claimed in claim 1-3, wherein
a) the active ingredient is a combination of Teneligliptin and Metformin; and
b) pharmaceutically acceptable excipient.

16. The pharmaceutical composition as claimed in claim 1-3, wherein
a) the active ingredient is a combination of Glimepiride, Pioglitazone and Metformin ; and
b) pharmaceutically acceptable excipient.

17. The pharmaceutical composition as claimed in claim 1-3, wherein
a) the active ingredient is a combination of Telmisartan and Metoprolol; and
b) pharmaceutically acceptable excipient.

18. The pharmaceutical composition as claimed in claim 1-3, wherein
a) the active ingredient is a combination of Telmisartan, Amlodipine and Hydroclorthiazide; and
b) pharmaceutically acceptable excipient.

19. The pharmaceutical composition as claimed in claim 1-3, wherein
a) the active ingredient is a combination of Levocetirizine and Montelukast; and
b) pharmaceutically acceptable excipient.

20. A process of manufacturing a pharmaceutical composition with reduced excipient load comprising the following steps:
a) weighing and dispensing all the raw material under reverse laminar air flow;
b) after dispensing sieving with appropriate sieve at an optimum level of humidity and temperature;
c) solubilising with a solubilizer and stirring until a clear solution is formed;
d) pre heating the sifted raw materials in bowl of fluidized bed processor having optimum process parameters;
e) spraying the material with a binder solution after pre heating, wherein throughout the whole granulation process lump formation were avoided and uniform fluidization was maintained;
f) drying the granules obtained in step e in fluidized bed processor;
g) sifting the granules obtained in step f; and
h) after sifting, the sifter granules were transferred into clean rotocube Mixer/Octagonal Blender for mixing and after blending, the granules were unloaded in double polythene lined HDPE containers.
,CLAIMS:1. A pharmaceutical composition with a reduced excipient load comprising

a) at least one active ingredient or combination of therapeutically compatible medicament; and
b) pharmaceutically acceptable excipient

wherein the reduced excipient load is reduced by 5 to 80% and the dosage form having a reduced size and weight for patient compliance.

2. The pharmaceutical composition as claimed in claim 1, wherein

the active ingredient or medicament can be selected from antidiabetic, analgesic, antibacterial, antifungal, antiviral, anticancer, anti-histamines, anti-depressants, anesthetics, antacids, anti-rheumatoid, anti-asthmatics, anti-allergic, antiarrhythmic, anti-convulsants, anti-emetics, anti-infective, anti-protozoals, anti-inflammatory agents, anti-nauseants, anti-hyperlipidemic drugs, anti- parkinson, anti-psychotics, antipyretics, anti-spasmodic, anti-thrombotic drugs, anticoagulants, anti-platelets, anti-tumor drugs, anti-urticaria drugs, anxiolytic agents, appetite stimulants, appetite suppressants, anti-hypertensive (diuretics, beta-blockers, ACE inhibitors, calcium channel blockers, vasodialators), chelating agents, cholecystokinin antagonists, cognition activators, cough suppressants, erythropoietic drugs, fertility agents, anti-diarrhoeals, laxatives, antiulcer agents, growth regulators, immunomodulating agents, Janus kinase (JAK) inhibitors, neuroleptics, neuromuscular agents, neuroprotective, Non-steroidal anti- inflammatory drug (NSAID), potassium channel blocker, potassium channel opener, prostaglandins, respiratory stimulants, selective aldosterone receptor blocker, sedatives & hypnotics, synthetic hormones, tachykinin nk 1 antagonist, vaso-constrictors and vertigo agents, vitamins or a combination thereof.

3. The pharmaceutical composition as claimed in claim 1, wherein pharmaceutically acceptable excipient is selected from a diluent, binder, preservative, colourant, solvent, glidant, lubricant or a combination thereof.

4. The pharmaceutical composition as claimed in claim 1, wherein the size and weight of the tablet has been reduced by 5% to 60% compared to the conventional reference drug.

5. The pharmaceutical composition as claimed in claim 1-3, wherein
a) the active ingredient is a combination of Aceclofenac 20% by weight and Paracetamol 65% by weight; and
b) pharmaceutically acceptable excipient
wherein the weight of the dosage is reduced by 15 to 30%.

6. The pharmaceutical composition as claimed in claim 1-3, wherein
a) the active ingredient is a combination of Nimesulide 20% by weight and Paracetamol 65% by weight; and
b) pharmaceutically acceptable excipient
wherein the weight of the dosage is reduced by 20 to 25%.

7. The pharmaceutical composition as claimed in claim 1-3, wherein
a) the active ingredient is a combination of Diclofenac 10% by weight and Paracetamol 67% by weight; and
b) pharmaceutically acceptable excipient
wherein the weight of the dosage is reduced by 20 to 40%.

8. The pharmaceutical composition as claimed in claim 1-3, wherein
a) the active ingredient is a combination of Dapagliflozin and Metformin; and
b) pharmaceutically acceptable excipient
wherein the weight of the dosage is reduced by 30 to 45%.

9. The pharmaceutical composition as claimed in claim 1-3, wherein
c) the active ingredient is a combination of Metformin hydrochloride and Glimepiride; and
d) pharmaceutically acceptable excipient
wherein the weight of the dosage is reduced by 10 to 20%.

10. The pharmaceutical composition as claimed in claim 1-3, wherein
e) the active ingredient is Ondansetron; and
f) pharmaceutically acceptable excipient
wherein the weight of the dosage is reduced by 30 to 45%.
11. The pharmaceutical composition as claimed in claim 1-3, wherein
a) the active ingredient is a combination of Telmisartan and Chlorthalidone; and
b) pharmaceutically acceptable excipient.

12. The pharmaceutical composition as claimed in claim 1-3, wherein
a) the active ingredient is a combination of Cilnidipine and Telmisartan; and
b) pharmaceutically acceptable excipient.

13. The pharmaceutical composition as claimed in claim 1-3, wherein
a) the active ingredient is a combination of Telmisartan, Cilnidipine and Chlorthalidone; and
b) pharmaceutically acceptable excipient.

14. The pharmaceutical composition as claimed in claim 1-3, wherein
a) the active ingredient is Telmisartan; and
b) pharmaceutically acceptable excipient.

15. The pharmaceutical composition as claimed in claim 1-3, wherein
a) the active ingredient is a combination of Teneligliptin and Metformin; and
b) pharmaceutically acceptable excipient.

16. The pharmaceutical composition as claimed in claim 1-3, wherein
a) the active ingredient is a combination of Glimepiride, Pioglitazone and Metformin ; and
b) pharmaceutically acceptable excipient.

17. The pharmaceutical composition as claimed in claim 1-3, wherein
a) the active ingredient is a combination of Telmisartan and Metoprolol; and
b) pharmaceutically acceptable excipient.

18. The pharmaceutical composition as claimed in claim 1-3, wherein
a) the active ingredient is a combination of Telmisartan, Amlodipine and Hydroclorthiazide; and
b) pharmaceutically acceptable excipient.

19. The pharmaceutical composition as claimed in claim 1-3, wherein
a) the active ingredient is a combination of Levocetirizine and Montelukast; and
b) pharmaceutically acceptable excipient.

20. A process of manufacturing a pharmaceutical composition with reduced excipient load comprising the following steps:
a) weighing and dispensing all the raw material under reverse laminar air flow;
b) after dispensing sieving with appropriate sieve at an optimum level of humidity and temperature;
c) solubilising with a solubilizer and stirring until a clear solution is formed;
d) pre heating the sifted raw materials in bowl of fluidized bed processor having optimum process parameters;
e) spraying the material with a binder solution after pre heating, wherein throughout the whole granulation process lump formation were avoided and uniform fluidization was maintained;
f) drying the granules obtained in step e in fluidized bed processor;
g) sifting the granules obtained in step f; and
h) after sifting, the sifter granules were transferred into clean rotocube Mixer/Octagonal Blender for mixing and after blending, the granules were unloaded in double polythene lined HDPE containers.

Documents

Application Documents

# Name Date
1 202211050955-STATEMENT OF UNDERTAKING (FORM 3) [06-09-2022(online)].pdf 2022-09-06
2 202211050955-PROVISIONAL SPECIFICATION [06-09-2022(online)].pdf 2022-09-06
3 202211050955-FORM 1 [06-09-2022(online)].pdf 2022-09-06
4 202211050955-FIGURE OF ABSTRACT [06-09-2022(online)].pdf 2022-09-06
5 202211050955-DRAWINGS [06-09-2022(online)].pdf 2022-09-06
6 202211050955-POA [05-09-2023(online)].pdf 2023-09-05
7 202211050955-FORM 13 [05-09-2023(online)].pdf 2023-09-05
8 202211050955-AMENDED DOCUMENTS [05-09-2023(online)].pdf 2023-09-05
9 202211050955-CORRESPONDENCE-OTHERS [06-09-2023(online)].pdf 2023-09-06
10 202211050955-COMPLETE SPECIFICATION [06-09-2023(online)].pdf 2023-09-06
11 202211050955-Proof of Right [15-09-2023(online)].pdf 2023-09-15
12 202211050955-FORM 18 [28-03-2025(online)].pdf 2025-03-28
13 202211050955-Response to office action [04-08-2025(online)].pdf 2025-08-04