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DOI: 10.13140/RG.2.2.22858.36804
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ICCOSS XXIII, Stellenbosch, South Africa
2 – 7April, 2017
STUDY OF COMPTENCIES IN DIFFERENT SOLID FORMS TOWARDS SOLUBILITY AND DISSOLUTION
S. Sudalai Kumar
Department of Chemistry, Francis Xavier Engineering College, Tirunelveli 627 003.Tamil Nadu, [email protected]
Bioactive molecules (Cardiosulfa and its derivatives) and a few low aqueous soluble drugs were short listed
for solid form screening with the aim of addressing the solubility and stability issues associated with these
active ingredients.1Six bioactive sulphonamides 1-6, N-acetyl-L-cysteine (NAC-paracetamol overdose drug)
and Clonixin (CLX- a non-steroid analgesic drug) were identified as polymorphic solid forms
andVoriconazole (VZL-anti-fungal drug), Gliclazide (GLZ- type II diabetic second generation sulphonylurea
drug) and Clofibric acid (CLF- antihyperlipidemic drug) and Benzydamine(anti-inflammatory drug) were
successfully investigated as pharmaceutical salt and cocrystal solid forms.2The single crystal and powder X-
ray technique was used in analysing the crystal structures of different polymorphs of sulphonamides, NAC
and CLX and the structures of pharmaceutical salts such as Voriconazoledinitrate, sodium gliclazide,
piperazine salts of clonixin and clofibric acid, and benzydamine hydrochloride salt. The crystal structure
analysis was used in confirming the ion transfer from acid to base or vice versa in salt structure and
hydrogen bonding pattern in different polymorphs and cocrystals.3Higher solubility sulphonamides, such as
2 (10.5 mg/mL) and 5 (4.4 mg/mL), adopt a twisted confirmation whereas less soluble 1 (0.9 mg/mL) is
nearly planar in the crystal structues.1The highest solubility and faster dissolution rates of the ionic forms
were ascribed to stronger, attractive interactions between the solvent molecules and the zwitterionic
functional groups in Clonixin.4The metastable form II of NAC converted to stable form I in solid-state
grinding, slurry medium, and storage in ambient conditions for 3 months due to the difference in weak
strength of hydrogen bonding in form II.5The nitrate salt has ~ 3 times faster IDR compared to VZL base and
the dinitrate salt of voriconazole is about 10 times more soluble (2.5 mg/ mL) than the free base (0.26 mg/
mL) in 0.1 N HCl. The nitrate salt is the best among even cocrystals of VZL with p-hydroxybenzoic acid, p-
aminobenzoic acid (both are GRAS compounds) and m-nitrobenzoic acid coformers.GLZ drug forms salt
with sodium hydroxide base and exhibits successfully 10 times higher solubility than the GLZ whereas CLX
and CLF are successful in molecular salt formation with piperazine (PIP) and cytosine (CYT) organic bases.
In turn, CLX-PIP and CLF-PIP salt showed almost equal to 10 times higher solubility than their respective
individual components CLF and CLX (neutral and zwitterionic polymorphs) and the observed solubility of
these molecular salts is of having equal solubility advantage to GLZ-Na mineral salt. Similarly in dissolution
rate comparison, the sodium-gliclazate showed three times high solubility improvements in IDR compared to
GLZ whereas the molecular salts of CLX and CLF showed two times high dissolution rate developments
with respect to CLX and CLF drugs.6 All these pharmaceutical salts are good in solubility developments
with respect to the parent drug and other dosage forms such as polymorphs and cocrystals. Thereforeit is
recommended for salt formulations and scale up in pharma industries from our competency study on
polymorphs, cocrystals and salts.
Keywords: polymorphs, cocrystals, salts
[1] S. S. Kumar, S. Rana and A. NangiaChem. Asian J. 2013, 8, 1551.
[2] P. Sanphui, S. S. Kumar and A. Nangia Cryst. Growth Des., 2012, 12, 4588.
[3] S. S. Kumar, R. Thakuria and A. Nangia, CrystEngComm, 2014, 16, 4722.
[4] S. S. Kumar and A. Nangia Cryst. Growth Des., 2014, 14, 1865.
[5] S. S. Kumar and A. Nangia CrystEngComm., 2013, 15, 6498.
[6] S. S. Kumar Researchgate.net, 2015, DOI: 10.13140/RG.2.1.2051.7282.
12 January 2017
Dr. S. Sudalai Kumar Assistant Professor Department of Chemistry Francis Xavier Engineering College Vannarapet 103/G2 By pass road Tirunelveli Town Tirunelveli 627006 Tamil Nadu.
Acceptance letter
Dear Dr. S. Sudalai Kumar
We are pleased to invite you to participate in the 23rd International Conference on the
Chemistry of the Organic Solid State.
The conference will take place between 2 and 7 April 2017 at the Wallenberg Conference
Centre at the Stellenbosch Institute for Advanced Study in Stellenbosch, South Africa.
We are pleased to confirm that your abstract entitled STUDY OF COMPTENCIES IN
DIFFERENT SOLID FORMS TOWARDS SOLUBILITY AND DISSOLUTION” has been
reviewed by the Programme Committee and that it has been accepted for a poster
presentation.
For more information please visit the conference website: http://iccoss2017.co.za/
We look forward to welcoming you in Stellenbosch!
Sincerely yours,
Leonard J. Barbour
Professor of Chemistry and Chair of the ICCOSS-XXIII Local Organising Committee
21 December 2016 Dr. S. Sudalai Kumar Assistant Professor Department of Chemistry Francis Xavier Engineering College Vannarapet 103/G2 By pass road Tirunelveli 627003 Tamil Nadu. India.
Dear Dr Kumar
We would like to invite you to participate in the 23rd International Conference on the Chemistry of the Organic Solid State (ICCOSS XXIII) to be held in Stellenbosch, South Africa, from 2 - 7 April 2017. The Conference will start with registration and welcome function on Sunday afternoon 2 April 2017, with oral presentations and poster viewings through to Friday. You may use this invitation letter to apply for registration and travel grant from your relevant organisation. Please note that you are responsible for full payment of the indicated registration fee to be included in the programme, with either a poster or oral presentation. Be advised to make own arrangements and payment for travel and accommodation. We are looking forward to receiving you as a participant in this exciting event. Regards Retha Venter For ICCOSS XXIII
Tel: + 27 21 8554472 082 656 7088
Dr. S. Sudalai Kumar
Present Address
Department of Chemistry (S and H)
Francis Xavier Engineering College
Tirunelveli 627 003, TN (India)
Mail id: [email protected]
Academic Qualification
2015 – Present Assistant Professor of Engineering Chemistry and Environmental Science
and Engineering, Department of Science and Humanities, Francis Xavier
Engineering College (affiliated to Anna University, Chennai), Scad Group of
Institutions, Tirunelveli, Tamil Nadu, India.
2009 – 2015 Ph.D. in Supramolecular Chemistry and Crystal Engineering (Chemistry), School
of Chemistry, University of Hyderabad, Hyderabad, AP, India.
2007 – 2009 M. Sc. (Chemistry), Department of Chemistry, RKM Vivekananda College,
University of Madras, Chennai, Tamil Nadu, India.
2004 – 2007 B. Sc. (Chemistry), St. Xavier’s College, Manonmaniam Sundaranar University,
Tirunelveli, Tamil Nadu, India.
2009 CSIR-NET (59th rank) qualified for Professorship as per UGC/AICTE norms.
List of Publications
1. Neutral and Zwitterionic Polymorphs of 2-(p-Tolylamino)nicotinic Acid.
N. K. Nath, S. Sudalai Kumar and A. Nangia Cryst. Growth & Des., 2011, 11, 4594.
(IUCr best poster award in ICCOSS 2011 conference)
2. Pharmaceutical Cocrystals of Niclosamide. P. Sanphui, S. Sudalai Kumar and A. Nangia
Cryst. Growth & Des., 2012, 12, 4588.
3. Solid-state Form Screen of Cardiosulfa and Its Analogs.
S. Sudalai Kumar, S. Rana and A. Nangia Chem. Asian J. 2013, 8, 1551.
Gender : Male
DOB : 13th May, 1987
Marital Status: Single
Mobile : +91 9952885464
4. A new Conformational Polymorph of N-acetyl-L-cysteine, The role of S–H···O and C–
H···O interactions. S. Sudalai Kumar and A. Nangia CrystEngComm, 2013, 15, 6498.
5. Pharmaceutical Cocrystals and a Nitrate Salt of Voriconazole
S. Sudalai Kumar, R. Thakuria and A. Nangia CrystEngComm, 2014, 16, 4722. Special
Theme issue of CEC on India IYCr 2014 Celebration.
6. A Solubility Comparison of Neutral and Zwitterionic Polymorphs. S. Sudalai Kumar and
A. Nangia Cryst. Growth & Des., 2014, 14, 1865. Virtual special issue IYCr 2014
Celebrating the International Year of Crystallography.
7. New Pharmaceutical Salts of Gliclazide, Clonixin and Clofibric acid S. Sudalai Kumar,
Researchgate.net, 2015, DOI: 10.13140/RG.2.1.2051.7282.
8. Crystal Structure of Benzydamine Hydrochloride Salt, S. Sudalai Kumar, Researchgate.net,
2015, DOI: 10.13140/RG.2.1.1600.9128/1.
9. Crystal Structure of Ethamivan Drug, S. Sudalai Kumar, Researchgate.net, 2015, DOI:
10.13140/RG.2.1.4099.6009.
10. Structure-Solubility-Stability Relationships: Solid State Forms of Active Ingredients,
S. Sudalai Kumar, Researchgate.net, 2015, DOI: 10.13140/RG.2.1.3839.2165.
11. Solid state Acid–Base Reactions of Arylamino Nicotinic Acids: X-ray Crystal Structures of
Salts, S. Sudalai Kumar, Inter. J. Anal. Appl. Chem., 2015, 1 (2), 1.
12. Elucidation of synthetic mechanism involved in the conversion of zwitterionic clonixin to
carboxamide side product. S. Sudalai Kumar, N. Ram Kumar, D. Kodimunthiri, Int. J.
Chem. Syn. Chem. React., 2016, 2 (1), 1.
Awards and Achievements
1. Delivered a flash presentation on the topic of Structure Property Correlation of Neutral and
Zwitterionic Polymorphs in K. V. Rao Award 2014 at University of Hyderabad, India.
2. Delivered a flash presentation on the topic of Comparison of Stability and Solubility of
Neutral, Zwitterionic and Conformational Polymorphs in ChemFest 2014 at University of
Hyderabad, India.
3. Delivered a flash and poster presentation on the topic of Polymorph Screen and
Characterization of Cardiosulfa and Its Analogs in ICCOSS 2013 at University of Oxford,
Oxford, UK.
4. Poster presentation on the topic of Characterization of Isostructural Solid Forms of APIs in
MED-CHEM 2013 conference held at IIT-Madras, India.
5. Poster presentation on the topic of Characterization of Isostructural Solid Forms of APIs in
AP Science Congress Meet 2013 conference held at University of Hyderabad, India.
6. Poster presentation on the topic of Solid-state Forms of Cardiosulfa and Its Analogs in
ChemFest 2012 conference held at University of Hyderabad, India.
7. Poster presentation on the topic of Solid-state Forms of Cardiosulfa and Its Analogs in
INDO-US 2012 conference held at IIT-Delhi.
8. IUCr best poster award in the presentation on the topic of Neutral and Zwitterionic
Polymorphs of 2-(p-Tolylamino)nicotinic acid (TNA) in international conference ICCOSS
2011 held in IISc Bangalore.
9. Poster presentation and participation on the topic of Solid-state Forms of Cardiosulfa and
Its Analogs in IYC 2011 conference and Science exhibition, demonstration and participation
in IYC 2011 program at School of chemistry, University of Hyderabad, India.
10. Participation in FDP and FOP 2015 (faculty development program and orientation program
for Asst. Professors) at Scad Group of Institutions, Tirunelveli, Tamil Nadu, India.
11. Poster presentation of Pharmaceutical Salts: Crystal Structure to Solubility in National
level Symposium 2016 at Sipra labs Hyderabad India.
Research Experience
1. Antibacterial activity study of drugs in Department of Plant sciences, University of
Hyderabad, Hyderabad, India.
2. Summer Research Project May-June 2009, School of Chemistry, University of Hyderabad,
Hyderabad, India.
3. Summer Research Project 2008, Department of Organic Chemistry, University of Madras,
Chennai, India.
4. Analysis of Ground Water 2008, Institute for Water Analysis, PWD, Government of Tamil
Nadu, Chennai, India.
5. Chemist in Drug production 2007, Orchid Chemicals and Pharmaceuticals, Chennai, India.
6. Student Chemist in QC 2006, Savita Chemicals Pvt. Ltd, Mumbai, India.
Research Interests
With a sound background on preparation, crystallization and characterization of solid state
forms of model organic compounds and active pharmaceutical ingredients, I would like to carry out
further research in development of organic and inorganic materials using control of supersaturation
level, control of nucleation temperature, solvent screening, heating and sublimation of the materials,
low temperature and high temperature evaporation, rotovapor fast evaporation, seeding technology,
capillary crystallization, introduction of additives, polymer-induced hetero-nucleation, nucleation
confined in nanopores, heteronucleation on substrates such as ionic liquids and gels, laser-induced
nucleation. Further extension of my research will be in multi-component systems such as salts,
cocrystals and eutectic compositions because they were used as alternative methods to polymorphs
in addressing the physico-chemical challenges of low aqueous soluble drugs with low
bioavailability. In the same direction, Salts are well known in this field to make alternate formulation
dosage forms and recently cocrystals have been developed in research labs, but eutectic
compositions are not well explored in this regard. Therefore, I would like to take important stand in
this research field from crystal engineering strategies to their application in pharmaceutical
formulation.
Potential applications of the Research Activity
The model compounds and drugs studied in my PhD thesis work belong to the broad
category of drug classification such as sulfonamides, amphoteric compounds, amino acids,
antifungal azole drugs, sulfonylureas, fibrates and fenamates and hence there is a need to explore the
same structure-property relationship for these many numbers of drugs in each of these categories.
The idea of expanding the study of polymorph screening and crystal engineering strategies to the
other drugs in the same category using different crystallization conditions would provide interesting
directions to solve the pharmaceutical and developmental challenges in drug industries.
Instruments Handled
1. Trained in organic synthesis, separation, purification and characterization of organic
molecules using TLC and column chromatography and various spectroscopic techniques like
FT-IR, Raman, NIR, 1H-NMR,
13C-NMR.
2. Analysis of different crystal forms (polymorphs, solvates, hydrates, salts and cocrystals) by
X-ray diffraction (both single crystal XRD and Powder XRD) and Differential Scanning
Calorimetry (DSC), Thermal Gravimetric Analysis (TGA), Hot Stage Microscopy (HSM),
and FT-IR, NIR, Raman spectroscopy and ss-NMR spectroscopy.
3. Hands-on experience with SMART APEX CCD X-ray diffractometer, Xcalibur Gemini Eos
CCD X-ray diffractometer, crystal structure solution and refinement, determination, Bruker
400 MHz NMR spectrometer, Thermo Nicolet 6700 FT-IR and Raman spectrometer,
Thermo Scientific Evolution 300 UV-VIS Spectrometer, Metler Toledo DSC/TGA
instruments, Wagner Munz Hot stage microscope, Electrolab Dissolution Tester, Retsch MM
400 ball mill grinder.
4. Sound knowledge of various softwares such as Polymorph Prediction CSD (CCDC-
Cambridge Crystallographic Data Centre) for crystal structure database analysis, SAINT,
SHELX-TL, CrysAlisPro 171.33.55, Olex2-1.0, WinGX, Platon for crystal structure solution
and refinement, Mercury & XSeed for viewing and graphics, Powder Cell 2.4 for fingerprint
match and quantification of polymorphic phases and least squares refinement, Crystal
Explorer (Hirshfeld Surface Analysis) for analyzing intermolecular interactions and
polymorphism in molecular crystals, XPac to compare crystal structures of
similar/dissimilar.
Declaration
I hereby declare that whatever has been stated above is true to the best of my knowledge, correct and
nothing material has been concealed there from.
Place: Tirunelveli
Date: 23rd
November 2016 S. Sudalai Kumar
Benefits of the Event (200 words only)
The ICCOSS 2017 conference is to be held in Stellenbosch, South Africa this year and it would
be a great opportunity to present my research works and interact with global eminent scientists.
Over 200 delegates are expected to attend this meeting and share their ideas on pharmaceutical
applications and material chemistry. Participation in this meeting will beneficial to my research
projects and would enhance my research skills in independent research career. I will have a
chance to interact with some of my field experts listen about latest discoveries and
developments, techniques and methods of chemical crystallography. Several eminent solid state
chemists and experts Christer Aakeröy, Bill Jones, Jerry Atwood, Kenneth Harris, Len
MacGillivray, Piero Sozzani and outstanding scientists Pance Naumov, Jon Steed, Mike Ward,
Mike Zaworotko will be giving plenary lectures. The new techniques of crystallography and its
applications in the solid state chemistry which I will learn in the conference will help me to
apply in current research works. The new research centre is being started in our chemistry
department this year and would open the possibilities of more collaboration with the research
institutes worldwide and create platform for sharing my ideas and publishing papers with the
global researchers.
ICCOSS XXIII, Stellenbosch, South Africa
2 – 7April, 2017
We are pleased to announce that the 23rd International Conference on the Chemistry of the Organic
Solid State (ICCOSS-XXIII) will take place between 2 and 7 April 2017 at the Wallenberg
Conference Centre in Stellenbosch, South Africa. The main objective of the ICCOSS conference
series is to showcase frontier research relating to various aspects of organic solid state chemistry, as
well as to bring together both young and experienced scientists from around the world to establish
fruitful discourse. The ICCOSS International Advisory Committee decided on Stellenbosch as the
next venue because South Africa, and particularly the Western Cape region, has a strong
international reputation for research in organic solid state chemistry.
Organising an international conference is a costly undertaking. The selection of Stellenbosch as the
venue for the 23rd ICCOSS conference was made with a view to promoting the participation of
African delegates who would have a better opportunity to present their work at an international
conference on the African continent without the expense of travelling to more expensive and
faraway destinations. However, the costs of continental travel, registration, accommodation and
meals still need to be covered by participants. The expenses involved are particularly onerous for
students, and for delegates from poorer countries. Without significant sponsorship to partially cover
the costs of venue hire and catering, many African delegates may still find the event unaffordable.
Students in particular will also require assistance with registration, accommodation and travel costs.
With the above in mind we, the organisers, would be honoured if you would accept our invitation to
be an integral part of this 23rd ICCOSS meeting. We provide opportunities for sponsorship that will
enhance your visibility in the scientific community. The last ICCOSS conference was hosted in
Japan – it attracted about 120 delegates from a wide variety of countries and we anticipate that the
23rd meeting will be a repetition of this tremendous success. Due to many of the delegates being
important role players and stakeholders in solid state chemistry, exposure of your
company/organization to this diverse international audience should result in long term dividends.
We hope that you will make use of this opportunity to promote cutting-edge research on solid state
chemistry in the African region. Please see Page 2 for a list of sponsorship opportunities and then
return the completed sponsorship acceptance form as indicated.
We are looking forward to receiving you as a participant in this exciting event.
Regards
Retha Venter
For ICCOSS XXIII
Tel: + 27 21 8554472 082 656 7088
ICCOSS XXIII, Stellenbosch, South Africa
2 – 7April, 2017
STUDY OF COMPTENCIES IN DIFFERENT SOLID FORMS TOWARDS SOLUBILITY AND DISSOLUTION
S. Sudalai Kumar
Department of Chemistry, Francis Xavier Engineering College, Tirunelveli 627 003.Tamil Nadu, [email protected]
Bioactive molecules (Cardiosulfa and its derivatives) and a few low aqueous soluble drugs were short listed
for solid form screening with the aim of addressing the solubility and stability issues associated with these
active ingredients.1Six bioactive sulphonamides 1-6, N-acetyl-L-cysteine (NAC-paracetamol overdose drug)
and Clonixin (CLX- a non-steroid analgesic drug) were identified as polymorphic solid forms
andVoriconazole (VZL-anti-fungal drug), Gliclazide (GLZ- type II diabetic second generation sulphonylurea
drug) and Clofibric acid (CLF- antihyperlipidemic drug) and Benzydamine(anti-inflammatory drug) were
successfully investigated as pharmaceutical salt and cocrystal solid forms.2The single crystal and powder X-
ray technique was used in analysing the crystal structures of different polymorphs of sulphonamides, NAC
and CLX and the structures of pharmaceutical salts such as Voriconazoledinitrate, sodium gliclazide,
piperazine salts of clonixin and clofibric acid, and benzydamine hydrochloride salt. The crystal structure
analysis was used in confirming the ion transfer from acid to base or vice versa in salt structure and
hydrogen bonding pattern in different polymorphs and cocrystals.3Higher solubility sulphonamides, such as
2 (10.5 mg/mL) and 5 (4.4 mg/mL), adopt a twisted confirmation whereas less soluble 1 (0.9 mg/mL) is
nearly planar in the crystal structues.1The highest solubility and faster dissolution rates of the ionic forms
were ascribed to stronger, attractive interactions between the solvent molecules and the zwitterionic
functional groups in Clonixin.4The metastable form II of NAC converted to stable form I in solid-state
grinding, slurry medium, and storage in ambient conditions for 3 months due to the difference in weak
strength of hydrogen bonding in form II.5The nitrate salt has ~ 3 times faster IDR compared to VZL base and
the dinitrate salt of voriconazole is about 10 times more soluble (2.5 mg/ mL) than the free base (0.26 mg/
mL) in 0.1 N HCl. The nitrate salt is the best among even cocrystals of VZL with p-hydroxybenzoic acid, p-
aminobenzoic acid (both are GRAS compounds) and m-nitrobenzoic acid coformers.GLZ drug forms salt
with sodium hydroxide base and exhibits successfully 10 times higher solubility than the GLZ whereas CLX
and CLF are successful in molecular salt formation with piperazine (PIP) and cytosine (CYT) organic bases.
In turn, CLX-PIP and CLF-PIP salt showed almost equal to 10 times higher solubility than their respective
individual components CLF and CLX (neutral and zwitterionic polymorphs) and the observed solubility of
these molecular salts is of having equal solubility advantage to GLZ-Na mineral salt. Similarly in dissolution
rate comparison, the sodium-gliclazate showed three times high solubility improvements in IDR compared to
GLZ whereas the molecular salts of CLX and CLF showed two times high dissolution rate developments
with respect to CLX and CLF drugs.6 All these pharmaceutical salts are good in solubility developments
with respect to the parent drug and other dosage forms such as polymorphs and cocrystals. Thereforeit is
recommended for salt formulations and scale up in pharma industries from our competency study on
polymorphs, cocrystals and salts.
Keywords: polymorphs, cocrystals, salts
[1] S. S. Kumar, S. Rana and A. NangiaChem. Asian J. 2013, 8, 1551.
[2] P. Sanphui, S. S. Kumar and A. Nangia Cryst. Growth Des., 2012, 12, 4588.
[3] S. S. Kumar, R. Thakuria and A. Nangia, CrystEngComm, 2014, 16, 4722.
[4] S. S. Kumar and A. Nangia Cryst. Growth Des., 2014, 14, 1865.
[5] S. S. Kumar and A. Nangia CrystEngComm., 2013, 15, 6498.
[6] S. S. Kumar Researchgate.net, 2015, DOI: 10.13140/RG.2.1.2051.7282.
1/4/2017 ITS Online
http://its.serb.gov.in:8080/its/its/viewSubmitProjectDetail_fileDetailSuccess.action?id=10866# 1/3
Event Name: 23RD INTERNATIONAL CONFERENCE ON THE CHEMISTRY OF THE ORGANIC SOLID STATE
Organisers name:
LEN BARBOUR, STELLENBOSCH, (CHAIR) NIKOLETTA BATHORI, CAPE PENINSULA UNIVERSITY OFTECHNOLOGY SUSAN BOURNE, CAPE TOWN MINO CAIRA, CAPE TOWN MARIKE DU PLESSIS,STELLENBOSCH CATHARINE ESTERHUYSEN, STELLENBOSCH DELIA HAYNES, STELLENBOSCH TANYA LEROEX, STELLENBOSCH LUIGI NASSIMBENI, CAPE TOWN CLIVE OLIVER, CAPE TOWN, VINCENT SMITH,RHODES
Event Website Name: http://iccoss2017.co.za/
Event Start Date: 02-04-2017
Event End Date: 07-04-2017
City: STELLENBOSCH
Country: SOUTH AFRICA
Event Type: Conference
Presenting Paper Oral
No. of papers to be presented 6
Whether Single author / One of the authors One of the authors
Likely date of leaving India: 01-04-2017
Likely date of return to India: 09-04-2017
Dr. SUDALAI KUMAR S, Applicant
Application Status - Application Submitted to CM,MS
A. Event Country & Date
Application Submission Date: 04-01-2017
B. Purpose of Visit
Abstract(s) Paper(s) Details(In 500 words only) :
Bioactive molecules (Cardiosulfa and its derivatives) and a few low aqueous soluble drugs wereshort listed for solid form screening with the aim of addressing the solubility and stability issuesassociated with these active ingredients.1 Six bio active sulphonamides 1-6, N-acetyl-L-cysteine(NAC-paracetamol overdose drug) and Clonixin (CLX- a non-steroid analgesic drug) wereidentified as polymorphic solid forms and Voriconazole (VZL-anti-fungal drug), Gliclazide (GLZ-type II diabetic second generation sulphonylurea drug) and Clofibric acid (CLF- anti hyperlipidemicdrug) and Benzydamine (anti-inflammatory drug) were successfully investigated as pharmaceuticalsalt and cocrystal solid forms.2 The single crystal and powder X-ray technique was used inanalysing the crystal structures of different polymorphs of sulphonamides, NAC and CLX and thestructures of pharmaceutical salts such as Voriconazole dinitrate, sodium gliclazide, piperazinesalts of clonixin and clofibric acid, and benzydamine hydrochloride salt. The crystal structureanalysis is used in confirming the ion transfer from acid to base or vice versa in salt structure andhydrogen bonding pattern in different polymorphs and cocrystals.3 Higher solubilitysulphonamides, such as 2 (10.5 mg/mL) and 5 (4.4 mg/mL), adopt a twisted confirmationwhereas less soluble 1 (0.9 mg/mL) is nearly planar in the crystal structues.1 The highest solubilityand faster dissolution rates of the ionic forms were ascribed to stronger, attractive interactionsbetween the solvent molecules and the zwitterionic functional groups in Clonixin.4 The metastableform II of NAC converted to stable form I in solid-state grinding, slurry medium, and storage inambient conditions for 3 months due to the difference in weak strength of hydrogen bonding inform II.5 The nitrate salt has ~ 3 times faster IDR compared to VZL base and the dinitrate salt ofvoriconazole is about 10 times more soluble (2.5 mg/ mL) than the free base (0.26 mg/ mL) in0.1 N HCl. The nitrate salt is best among even cocrystals of VZL with p-hydroxybenzoic acid, p-aminobenzoic acid (both are GRAS compounds) and m-nitrobenzoic acid coformers. GLZ drugforms salt with sodium hydroxide base and exhibits successfully 10 times higher solubility than theGLZ whereas CLX and CLF are successful in molecular salt formation with piperazine (PIP) andcytosine (CYT) organic bases. In turn, CLX-PIP and CLF-PIP salt showed almost equal to 10 timeshigher solubility than their respective individual components CLF and CLX (neutral and zwitterionicpolymorphs) and the observed solubility of these molecular salts is of having equal solubilityadvantage to GLZ-Na mineral salt. Similarly in dissolution rate comparison, the sodium-gliclazateshowed three times high solubility improvements in IDR compared to GLZ whereas the molecularsalts of CLX and CLF showed two times high dissolution rate developments with respect to CLX
1/4/2017 ITS Online
http://its.serb.gov.in:8080/its/its/viewSubmitProjectDetail_fileDetailSuccess.action?id=10866# 2/3
Subject Category: Chemical Sciences
Name: Dr. SUDALAI KUMAR S (Young Scientist)
Application No. : ITS/1/2017-18
Email Address: [email protected]
Category: OBC
Date of Birth: 13-05-1987
Nationality: Indian
Gender: Male
Designation: Assistant Professor
Department: Chemistry
Telephone(O): 04622502157
Telephone(R):
Mobile : 9952885464
Fax:
Differently Abled: No
Passport: G0163555
Aadhar: 418757389828
Name:FRANCIS XAVIER ENGINEERINGCOLLEGE
Address: 103 G2 BYPASS ROAD
City: TIRUNELVELI
State: TAMIL NADU
Pincode: 627003
and CLF drugs.6 All these pharmaceutical salts are good in solubility developments with respect tothe parent drug and other dosage forms such as polymorphs and cocrystals. Therefore it isrecommended for salt formulations and scale up in pharma industries from our competency studyon polymorphs, cocrystals and salts.
C. Subject Category of the Event
Sub Category: Organic Chemistry
D. Applicant Details
E. Institution Details
F. Education and Training
Degree Year University/Institute Subject %Age,Grade,Division
PhD 2016 University of Hyderabad Chemistry nil
CSIR NET 2009 CSIR Chemical Sciences 59 rank
MSc 2009 Madras University Chemistry 71
BSc 2007 Manonmaniam Sundaranar University Chemistry 83
G. Significant Publications
5 significant papers relevant to the Event published by applicant during last 5 years :
Authors Title of Paper Journal Year VolPage
S. Sudalai Kumar, N.Ram Kumar, D.Kodimunthiri,
Elucidation of synthetic mechanism involved in theconversion of zwitterionic clonixin to carboxamide side
product.
Int. J. Chem.Syn. Chem.
React.,2016 2 1
S. Sudalai Kumar, M.Kannan
Solid state Acid–Base Reactions of Arylamino NicotinicAcids: X-ray Crystal Structures of Salts,
Inter. J. Anal.Appl. Chem.,
2015 1 1
S. Sudalai Kumar, R.Thakuria and A. Nangia
Pharmaceutical Cocrystals and a Nitrate Salt ofVoriconazole
CrystEngComm 2014 16 4722
S. Sudalai Kumar and A.Nangia
A Solubility Comparison of Neutral and ZwitterionicPolymorphs
Cryst. Growth &Des.,
2014 14 1865
S. Sudalai Kumar, S.Rana and A. Nangia
Solid-state Form Screen of Cardiosulfa and Its Analogs. Chem. Asian J. 2013 8 1551
S. Sudalai Kumar and A.Nangia
A new Conformational Polymorph of N-acetyl-L-cysteine, The role of S–H···O and C– H···O interactions.
CrystEngComm 2013 15 6498
P. Sanphui, S. SudalaiKumar and A. Nangia
Pharmaceutical Cocrystals of NiclosamideCryst. Growth &
Des.,2012 12 4588
N. K. Nath, S. SudalaiKumar and A. Nangia
Neutral and Zwitterionic Polymorphs of 2-(p-Tolylamino)nicotinic Acid.
Cryst. Growth &Des.,
2011 11 4594
H. Anticipated Expenses Details
Fare Type Mode of Transport Amount (In Rs.)
Fair both ways Airways 64317.0
Visa Fees 24724.61
Registration Fees 33378.23
Total 122419.84
1/4/2017 ITS Online
http://its.serb.gov.in:8080/its/its/viewSubmitProjectDetail_fileDetailSuccess.action?id=10866# 3/3
BIO DATA: BIO_DATA
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EVENT DETAIL: EVENT_DETAIL
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SELFCERTIFICATION:
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I. Financial Assistance Details from Other Sources
Agency Name Travel (In Rs.) Visa (In Rs.) Registration (In Rs.) Status
Nil Select
Total
J. Details of International events attended during last three years
Event Name From Date To Date City Country Sponsored/funded By
NA
K. Any other information which you may like to furnish in support of your application (200 words)
This conference is the only way for me to interact with global scientists about my research works. Some Indian institutes are notwilling to collaborate with rural and small level institutes like us. This will help us to find new international collaboration to publish ourresearch works and connected with current trends. May Indian researchers are continuing the collaboration with foreign scientistsafter their post doctoral works. Attending conference and sharing ideas in abroad are possible solution for some Indian candidateshaving no post doctoral experience like me. This will bring even better understanding in the subject as well listening to the lecturedirectly presented by the concerned scientist. Possibly We will do the exchange of student population after discussing with thestudents.
L. Application Upload Files
Certified that I have attended the above international scientific event and the particular furnished above are correct. I also certify that I have notreceived grants from SERB under this scheme during the last three years.
Certificate from the Applicant
Full Name of the scientific event : 23rd International Conference on the Chemistry of the
Organic Solid State (ICCOSS XXIII)
Duration : 2 to 7 April 2017
Venue : Wallenberg Conference Centre at the Stellenbosch Institute
for Advanced Study, Stellenbosch
Country : South Africa
I certify that
1. I have not availed support from SERB/DST during the last three years* under the scheme.
2. In the event of getting selected, I will submit my claim bills, tour reports and other details
within 90 days from the last date of the event.
3. I agree to abide by the terms and conditions of SERB grant.
(Signature)
(Name: Dr. S. Sudalai Kumar)
Place: Tirunelveli
Date: 04-01-2017
* The duration is counted from the date of start of the event attended last and the date of start of
the event one intends to apply.
Benefits of the Event (200 words only)
The ICCOSS 2017 conference is to be held in Stellenbosch, South Africa this year and it would
be a great opportunity to present my research works and interact with global eminent scientists.
Over 200 delegates are expected to attend this meeting and share their ideas on pharmaceutical
applications and material chemistry. Participation in this meeting will beneficial to my research
projects and would enhance my research skills in independent research career. I will have a
chance to interact with some of my field experts listen about latest discoveries and
developments, techniques and methods of chemical crystallography. Several eminent solid state
chemists and experts Christer Aakeröy, Bill Jones, Jerry Atwood, Kenneth Harris, Len
MacGillivray, Piero Sozzani and outstanding scientists Pance Naumov, Jon Steed, Mike Ward,
Mike Zaworotko will be giving plenary lectures. The new techniques of crystallography and its
applications in the solid state chemistry which I will learn in the conference will help me to
apply in current research works. The new research centre is being started in our chemistry
department this year and would open the possibilities of more collaboration with the research
institutes worldwide and create platform for sharing my ideas and publishing papers with the
global researchers.
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