Title of Invention	A PROCESS AND AN APPARATUS FOR THE MANUFACTURE OF PHARMACOLOGICALLY ACTIVE GASTRO PROTECTANT SUBSTANCE FROM CELERY SEEDS
Abstract	The Invention provides a process for the manufacture of pharmacologically active gastro protectant substance from celery seeds. The process comprises the steps of loading the cetery seed followed by a solvent from the top of a vessel housing a column of vertically oscillating sieve plates, located at equidistant from each other along the height of the vessel to create agltation and Intimate contact of the solvent with the celery seeds. The solvent containing the extract is discharged and filtered using ultra filtration with a filter having a nominal molecular weight cut off of less than 5000 to obtain a concentrate of the active substance which is further concentrated by vacuum distillation to obtain pharmacologlcally active, gastro protectant substance of desired concentration. An apparatus to carry out the abovementioned process is also provided. PRICE: THIRTY RUPEES

Title of Invention

A PROCESS AND AN APPARATUS FOR THE MANUFACTURE OF PHARMACOLOGICALLY ACTIVE GASTRO PROTECTANT SUBSTANCE FROM CELERY SEEDS

Abstract

The Invention provides a process for the manufacture of pharmacologically active gastro protectant substance from celery seeds. The process comprises the steps of loading the cetery seed followed by a solvent from the top of a vessel housing a column of vertically oscillating sieve plates, located at equidistant from each other along the height of the vessel to create agltation and Intimate contact of the solvent with the celery seeds. The solvent containing the extract is discharged and filtered using ultra filtration with a filter having a nominal molecular weight cut off of less than 5000 to obtain a concentrate of the active substance which is further concentrated by vacuum distillation to obtain pharmacologlcally active, gastro protectant substance of desired concentration. An apparatus to carry out the abovementioned process is also provided. PRICE: THIRTY RUPEES

Full Text	The invention provides a process and an apparatus for the manufacture of phamnacologicaily active gastro protectant substance from celer/ seeds. Celery seed (APIUM GRAVEOLENS) has been shown to have therapeutic potential against arthritis, rheumatism and gout. Recently celer/ seed extract has also been shown to have gastro protective effect. (WO 00/40258). The process according to the invention extracts actives from celery seed efficiently and has the following advantages over conventional method using static extractors or mixers. i Higher amount of actives per gm of seeds ii Lower amount of impurities and inactive solid material tli Considerably lower extraction time iv Lesser amount of solvent: seed ratio. The invention provides a process for the manufacture of pharmacologically active gastro protectant substance from celer/ seeds, said process comprising the steps of loading the celer/ seed followed by a solvent such as herein described from the top of a vessel housing a column of vertically oscillating sieve plates, located at equidistant from each other along the height of the vessel to create agitation and intimate contact of the solvent with the celery seeds, discharging the solvent containing the extract, filtering the solvent containing the extract using ultra filtration with a filter having a nominal molecular weight cut off less than 5000 to obtain a concentrate of the active substance which is further purified by vacuum distillation at 700 to 750 mm of mercury to obtain therapeutically and pharmacologically active, gastro protectant substance. Tlie invention also provides an apparatus for the manufacture of pharmacologically active gastro protectant substance from ceiery seeds comprising a cylindrical vessel having an inlet and outlet housing a column of sieves located at equal intervals, fixed to central shaft protruding outside the vessel ana 5 capable of vertical reciprocating motion and a drive for providing the reciprocating motion to the shaft. The invention will be described in greater detail with reference to the accompanying drawing in which : Figure 1 shows an apparatus for extracting the active substance from the celery seeds. Figure 2 shows the fluid motion between two sieve plates. The apparatus comprises a cylindrical vessel (1) which houses a column of sieves (2) placed at equidistant intervals. The sieves are joined together through a central shaft (3) and the shaft (3) protrudes out of the vessel (1). The shaft (3) is provided with a drive (8) comprising, an electric geared motor with a mechanism to reciprocate the sieve plate column up and down. The vessel is provided with an inlet (4) and outlet (5). The vessel is mounted on a frame (7). The celery seeds are loaded from the top inlet (4) followed by the solvent. As the sieve column (2) reciprocates up and down at pulsed intervals the suspension of seeds and solvents also moves. However, the suspension moves through the holes in the sieve plate in a jet like motion creating a vortex flow. Due to the reciprocating motion, the sieve plate column changes direction of motion, the fluid motion of the jets and vortices also change direction as shown in fig.2. This altematlng upward and downward motion of the suspension in the Jets is part of the secondary motion. The primary motion is the axial flow of the suspension through the vessel. It is the secondary motion which is responsible for the thorough mixing. The shearing action of the flow disaggregates seed clumps and induces intimate contact between seed particles and solvent. The solvent used for extraction could be methanol, ethanol, isopropanol or other solvents such as toluene, other lower alcohols with 1 to 6 carbon atoms. The solvent extract obtained from this stage Is then concentnrted though an ultra fitter cartridge having a nominal molecular weight cut off less than 5000 to concentrate the actives and recover solvent. The concentrate is then further reduced by vacuum distillation to the desiied concentration. The major difference from tfie conventional process as compned to this process > lies In the foNowing: 1. Highly dynamic mixing and mass transfer as compared to either conventional static or agitated reactors. 2. Gentle mixing as compared to agitated turblnes resultbig in less seed breakdown and debris in extract. 3. Overall higher extraction efficiency to the extent of 20% on seed weight. 4. Iteduced solvent usage. 5. Reduced thermal degradation of actives due to "cold Concentratfon" by UF. The material produced by the process aocording to the invention has been analysed by gas chromotograph and nudear magnetic resonance to determine the profile. The material has been found to be superior in tenns of lesser number of Impurtties as well as higher concentration of actives/gm of extract The extract has also proved to be phamaocologlcafly active as shown by invivo studies in rats as reported in the paper presented by Whitehouse et al. at the htemational conference on antlflammophannaooiogy on 13 September 2000 at Sheffield U.K. EXAMPLE 1: Dried and partially ground oelely seed of 10 Kgs quantity is charged into the reactor. This is followed by 50 kgs of ethanol. The reactor is then pulse agitated for 10-12 hrs and spent seeds are filtered and discarded . The solvent is then removed by ultra filtration using a pressure differenoe of 1-1.5 Bar and a cartridge having NMWOO of 3500. The concentrate is further processed under vacuum distillation at 700 - 750 mm Hg to a final weight of 1 log. The overal extraction efficiency was found to be 18% higher than the conventional process. Gas chromatography of the product revealed 15% area increase in peals of the therapeutically active compounds as compared to the impurities. EXAMPLE 2 The Steps of exmple 1 was repeated with the following changes. Solvent used was methanol Extraction time was 24 Hrs Filter cartridge having NMWOO of 1000 was used and pressure difference of 2.5 bar was kept while filtering. Overal extraction efficiency withh methanol was 20% higher as compared to conventional. Gas chromatography of the product revealed 18% area increase In the peaks of the therapeutically active compounds as compared to the Impurities. Extracts of celery seeds can be prepared by the process according to the Invention to conserve their phytophamaoeutical content The extracts so prepared have been shown to be superior as compared to conventional extracts due to their lower impurity level, higher active ingredient content as well as reduced manufacturing costs. The analytical data revealed by gas chromatography and nuclear magnetic resonance data support the above. The extract demonstrates not only anti inflammatory activity against rheumatism, arthritis and gout but also a gastroprotectant action against alcohol induced gastropathy. WE CLAIM : 1. A process for the manufacture of pharmacologically active gastro protectant substance from celer/ seeds, said process comprising the steps of loading 'die celery seed followed by a solvent such as herein described from the top of a vessel housing a column of vertically oscillating sieve plates, located at equidistant from each other along the height of the vessel to create agitation and intimate contact of the solvent with the celer/ seeds, discharging the solvent containing the extract, filtering the solvent containing the extract using ultra filtration with a filter having a nominal molecular weight cut off of less than 5000 to obtain a concentrate of the active substance which is further purified by vacuum distillation at 700 to 750 mm of mercury to obtain therapeutically and phamnacologically active, gastro protectant substance. 2. The process as claimed in claim 1, wherein the celery seed is partially ground and dried. 3. The process as claimed in claim 1, wherein the solvent is ethanol, the ultra filtration is carried out at a pressure difference of 1 to 1.5 bar with a filter cartridge having nominal molecular weight cut off of 3500, 4. The process as claimed in claim 1, wherein the solvent is methanol, the ultra filtration is carried out at a pressure difference of 2.5 bar with a filter catridge having nominal molecular weight cut off of 1000. 5. An apparatus for the manufacture of pharmacologically active gastro protectant substance from celery seeds by the process claimed in any one of the previous claims, comprising a cylindrical vessel (1) having an inlet (4) and outlet (5) housing a column of sieves (2) located at equal intervals, fixed to central shaft (3) protruding outside the vessel (1) and is capable of vertical reciprocating motion and a drive (8) for providing the reciprocating motion to the shaft (3). 6. A process for the manufacture of pharmacologically active gastro protectant substance from celer/ seeds, substantially as hereinabove described. 7. An apparatus for the manufacture of phamnacologically active gastro protectant substance from celery seeds, substantially as hereinabove described and illustrated with reference to the accompanying drawings.

Full Text

The invention provides a process and an apparatus for the manufacture of phamnacologicaily active gastro protectant substance from celer/ seeds. Celery seed (APIUM GRAVEOLENS) has been shown to have therapeutic potential against arthritis, rheumatism and gout. Recently celer/ seed extract has also been shown to have gastro protective effect. (WO 00/40258). The process according to the invention extracts actives from celery seed efficiently and has the following advantages over conventional method using static extractors or mixers.
i Higher amount of actives per gm of seeds
ii Lower amount of impurities and inactive solid material
tli Considerably lower extraction time
iv Lesser amount of solvent: seed ratio.
The invention provides a process for the manufacture of pharmacologically active gastro protectant substance from celer/ seeds, said process comprising the steps of loading the celer/ seed followed by a solvent such as herein described from the top of a vessel housing a column of vertically oscillating sieve plates, located at equidistant from each other along the height of the vessel to create agitation and intimate contact of the solvent with the celery seeds, discharging the solvent containing the extract, filtering the solvent containing the extract using ultra filtration with a filter having a nominal molecular weight cut off less than 5000 to obtain a concentrate of the active substance which is further purified by vacuum distillation at 700 to 750 mm of mercury to obtain therapeutically and pharmacologically active, gastro protectant substance.
Tlie invention also provides an apparatus for the manufacture of pharmacologically active gastro protectant substance from ceiery seeds comprising a cylindrical vessel having an inlet and outlet housing a column of sieves located at equal intervals, fixed to central shaft protruding outside the vessel ana 5 capable of vertical reciprocating motion and a drive for providing the reciprocating motion to the shaft.

The invention will be described in greater detail with reference to the accompanying drawing in which :
Figure 1 shows an apparatus for extracting the active substance from the celery seeds.
Figure 2 shows the fluid motion between two sieve plates.
The apparatus comprises a cylindrical vessel (1) which houses a column of sieves (2) placed at equidistant intervals. The sieves are joined together through a central shaft (3) and the shaft (3) protrudes out of the vessel (1). The shaft (3) is provided with a drive (8) comprising, an electric geared motor with a mechanism to reciprocate the sieve plate column up and down. The vessel is provided with an inlet (4) and outlet (5). The vessel is mounted on a frame (7).
The celery seeds are loaded from the top inlet (4) followed by the solvent. As the sieve column (2) reciprocates up and down at pulsed intervals the suspension of seeds and solvents also moves. However, the suspension moves through the holes in the sieve plate in a jet like motion creating a vortex flow. Due to the reciprocating motion, the sieve plate column changes direction of motion, the fluid motion of the jets and vortices also change direction as shown in fig.2.
This altematlng upward and downward motion of the suspension in the Jets is part of the secondary motion. The primary motion is the axial flow of the suspension through the vessel. It is the secondary motion which is responsible for the thorough mixing. The shearing action of the flow disaggregates seed clumps and induces intimate contact between seed particles and solvent.
The solvent used for extraction could be methanol, ethanol, isopropanol or other solvents such as toluene, other lower alcohols with 1 to 6 carbon atoms.

The solvent extract obtained from this stage Is then concentnrted though an ultra fitter cartridge having a nominal molecular weight cut off less than 5000 to concentrate the actives and recover solvent.
The concentrate is then further reduced by vacuum distillation to the desiied concentration.
The major difference from tfie conventional process as compned to this process > lies In the foNowing:
1. Highly dynamic mixing and mass transfer as compared to either conventional static or agitated reactors.
2. Gentle mixing as compared to agitated turblnes resultbig in less seed breakdown and debris in extract.
3. Overall higher extraction efficiency to the extent of 20% on seed weight.
4. Iteduced solvent usage.
5. Reduced thermal degradation of actives due to "cold Concentratfon" by UF.
The material produced by the process aocording to the invention has been analysed by gas chromotograph and nudear magnetic resonance to determine the profile. The material has been found to be superior in tenns of lesser number of Impurtties as well as higher concentration of actives/gm of extract
The extract has also proved to be phamaocologlcafly active as shown by invivo studies in rats as reported in the paper presented by Whitehouse et al. at the htemational conference on antlflammophannaooiogy on 13 September 2000 at Sheffield U.K.

EXAMPLE 1:
Dried and partially ground oelely seed of 10 Kgs quantity is charged into the reactor. This is followed by 50 kgs of ethanol. The reactor is then pulse agitated for 10-12 hrs and spent seeds are filtered and discarded . The solvent is then removed by ultra filtration using a pressure differenoe of 1-1.5 Bar and a cartridge having NMWOO of 3500. The concentrate is further processed under vacuum distillation at 700 - 750 mm Hg to a final weight of 1 log. The overal extraction efficiency was found to be 18% higher than the conventional process. Gas chromatography of the product revealed 15% area increase in peals of the therapeutically active compounds as compared to the impurities.
EXAMPLE 2

The Steps of exmple 1 was repeated with the following changes. Solvent used was methanol Extraction time was 24 Hrs
Filter cartridge having NMWOO of 1000 was used and pressure difference of 2.5 bar was kept while filtering.
Overal extraction efficiency withh methanol was 20% higher as compared to conventional. Gas chromatography of the product revealed 18% area increase In the peaks of the therapeutically active compounds as compared to the Impurities.
Extracts of celery seeds can be prepared by the process according to the Invention to conserve their phytophamaoeutical content The extracts so prepared have been shown to be superior as compared to conventional extracts due to their lower impurity level, higher active ingredient content as well as reduced manufacturing costs.
The analytical data revealed by gas chromatography and nuclear magnetic resonance data support the above. The extract demonstrates not only anti inflammatory activity against rheumatism, arthritis and gout but also a gastroprotectant action against alcohol induced gastropathy.

WE CLAIM :
1. A process for the manufacture of pharmacologically active gastro protectant
substance from celer/ seeds, said process comprising the steps of loading 'die celery
seed followed by a solvent such as herein described from the top of a vessel housing a
column of vertically oscillating sieve plates, located at equidistant from each other along
the height of the vessel to create agitation and intimate contact of the solvent with the
celer/ seeds, discharging the solvent containing the extract, filtering the solvent
containing the extract using ultra filtration with a filter having a nominal molecular
weight cut off of less than 5000 to obtain a concentrate of the active substance which is
further purified by vacuum distillation at 700 to 750 mm of mercury to obtain
therapeutically and phamnacologically active, gastro protectant substance.
2. The process as claimed in claim 1, wherein the celery seed is partially ground
and dried.
3. The process as claimed in claim 1, wherein the solvent is ethanol, the ultra
filtration is carried out at a pressure difference of 1 to 1.5 bar with a filter cartridge
having nominal molecular weight cut off of 3500,
4. The process as claimed in claim 1, wherein the solvent is methanol, the ultra
filtration is carried out at a pressure difference of 2.5 bar with a filter catridge having
nominal molecular weight cut off of 1000.
5. An apparatus for the manufacture of pharmacologically active gastro protectant
substance from celery seeds by the process claimed in any one of the previous claims,
comprising a cylindrical vessel (1) having an inlet (4) and outlet (5) housing a column
of sieves (2) located at equal intervals, fixed to central shaft (3) protruding outside the
vessel (1) and is capable of vertical reciprocating motion and a drive (8) for providing
the reciprocating motion to the shaft (3).

6. A process for the manufacture of pharmacologically active gastro protectant
substance from celer/ seeds, substantially as hereinabove described.
7. An apparatus for the manufacture of phamnacologically active gastro protectant
substance from celery seeds, substantially as hereinabove described and illustrated
with reference to the accompanying drawings.

Documents:

0238-mas-2001 abstract.pdf

0238-mas-2001 claims.pdf

0238-mas-2001 correspondence others.pdf

0238-mas-2001 correspondence po.pdf

0238-mas-2001 description (complete).pdf

0238-mas-2001 drawings.pdf

0238-mas-2001 form-1.pdf

0238-mas-2001 form-26.pdf

0238-mas-2001 form-3.pdf

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Patent Number

193193

Indian Patent Application Number

238/MAS/2001

PG Journal Number

02/2006

Publication Date

13-Jan-2006

Grant Date

15-Sep-2005

Date of Filing

15-Mar-2001

Name of Patentee

DR ANSELM DE SOUZA

Applicant Address

TEXTAN HOUSE, 47 FOURTH AVENUE ASHOK NAGAR CHENNAI-600 083.

Inventors:

#	Inventor's Name	Inventor's Address
1	DR ANSELM DE SOUZA	TEXTAN HOUSE, 47 FOURTH AVENUE ASHOK NAGAR CHENNAI-600 083.
2	VERN MURDOCH	P.O. BOX 66, 360 BAYVIEW STREET, PARADISE POINT 4216, QUEENSLAND
3	VERN MURDOCH	P.O. BOX 66, 360 BAYVIEW STREET, PARADISE POINT 4216, QUEENSLAND
4	VERN MURDOCH	P.O. BOX 66, 360 BAYVIEW STREET, PARADISE POINT 4216, QUEENSLAND

PCT International Classification Number

A61K35/78

PCT International Application Number

N/A

PCT International Filing date

PCT Conventions:

#	PCT Application Number	Date of Convention	Priority Country
1			NA