Pulsed release caffeine formulations and a process for preparation thereof
The present invention describes pulsed release caffeine formulations comprising caffeine particulate systems prepared by using release retarding agents and at least one or more food grade excipients. The present invention also relates to the process for preparation of caffeine formulations, wherein plurality of particulate systems combined to get the pulsed release caffeine formulation comprising release retarding agents, which provide caffeine release in pulses at different physiological conditions. The pulsed release caffeine formulation is prepared as tablets, capsules, soft gel capsules, caplets, oil suspensions or mixed with nutrient supplements for administration to the subjects. Caffeine formulations as described herein release the caffeine over entire GIT in pulses in a period of 2 to 8 hours and can be administered to subjects for boosting energy, improving concentration, cardiovascular health and for weight management.
1 . A pulsed release caffeine formulation comprising plurality of three to five particulate systems,
wherein a first particulate system comprises:
a) caffeine in the range of 63 to 68% w/w of the particulate;
b) shellac in the range of 2 to 14% w/w of the particulate;
c) release retarding agent in the range of 1 to 30% w/w of the particulate, wherein the release retarding agent comprises methacrylic acid-ethyl acrylate copolymer; and
d) food grade excipient in the range of 1 to 15% w/w of the particulate, wherein the food grade excipient comprises microcrystalline cellulose,
wherein a second particulate system comprises:
a) caffeine in the range of 63 to 68% w/w of the particulate;
b) shellac in the range of 2 to 14% w/w of the particulate;
c) release retarding agent in the range of 1 to 30% w/w of the particulate, wherein the release retarding agent comprises shellac; and
d) food grade excipient in the range of 1 to 15% w/w of the particulate, wherein the food grade excipient comprises microcrystalline cellulose, and
wherein a third particulate system comprises:
a) caffeine in the range of 63 to 68% w/w of the particulate;
b) shellac in the range of 2 to 14% w/w of the particulate;
c) release retarding agent in the range of 1 to 30% w/w of the particulate, wherein the release retarding agent comprises stearic acid; and
d) food grade excipient in the range of 1 to 15% w/w of the particulate, wherein the food grade excipient comprises microcrystalline cellulose.
2 . The pulsed release caffeine formulation of claim 1 , wherein the first, second, and third particulate systems are combined in a ratio of 0.5-1:1-2:1-2.
3 . The pulsed release caffeine formulation of claim 2 wherein the combined formulation has a dissolution release profile:
Media
Time (Hrs)
% Caffeine Release
0.1N HCl
1
31.80 ± 2
2
36.40 ± 2
pH 5.5 Phosphate
3
71.0 ± 2
Buffer
4
72.40 ± 2
pH 7.2 Phosphate
5
100.0 ± 2
Buffer
6
± 2.
4 . The pulsed release caffeine formulation of claim 2 , wherein the first particulate system has a dissolution release profile:
Media
Time (Hrs)
% Caffeine Release
0.1N HCl
1
9.6 ± 2
2
17.1 ± 2
pH 5.5 Phosphate
3
96.40 ± 2
Buffer
4
100.00 ± 2.
5 . The pulsed release caffeine formulation of claim 2 , wherein the second particulate system has a dissolution release profile:
% Caffeine
Media
Time (Hrs)
Release
0.1N HCl
1
6.1 ± 2
2
9.3 ± 2
pH 5.5 Phosphate Buffer
3
12.5 ± 2
4
15.2 ± 2
pH 7.2 Phosphate Buffer
5
99.60 ± 2
6
100.00
.
6 . The pulsed release caffeine formulation of claim 2 , wherein the third particulate system has a dissolution release profile:
% Caffeine
Media
Time (Hrs)
Release
0.1N HCl
1
5.9 ± 2
2
10.4 ± 2
pH 5.5 Phosphate
3
28.7 ± 2
Buffer
4
44.3 ± 2
5
51.1 ± 2
6
55.8 ± 2
pH 7.2 Phosphate
7
84.3 ± 2
Buffer
8
96.0 ± 2.
7 . The pulsed release caffeine formulation of claim 1 , wherein the three to five particulate systems are in the form of tablets, capsules, soft gel capsules, oil suspensions, powder mixtures or granules.