Scientific Program

Conference Series Ltd invites all the participants across the globe to attend 14th International Conference and Exhibition on Pharmaceutical Formulations Brussels, Belgium.

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Scientific Program Day 1
Scientific Program Day 2

Day 2 :

Keynote Forum

Gabriele Sadowski

TU Dortmund University, Germany

Keynote: Physical stability and drug crystallization kinetics in amorphous solid dispersions

Time : 11:15-11:45

Conference Series Formulations 2017 International Conference Keynote Speaker Gabriele Sadowski photo
Biography:

Gabriele Sadowski is Full Professor for Thermodynamics at TU Dortmund University. She is member of the Academy of Science and Arts North Rhine-Westphalia and of the German Academy of Engineering Sciences. She is the Chair of the German working party Thermodynamics and the German Representative in the European working party Thermodynamics and Transport Properties. She is author of about 200 scientific publications in high-reputation journals in the field of chemical, biochemical and pharmaceutical engineering. The main focus of her research is studying thermodynamic properties of complex systems with particular emphasis but not restricted to those containing biological and pharmaceutical molecules. To model the thermodynamic stability of those systems, her group developed the currently worldwide most-used thermodynamic model PC-SAFT which was published in 2001. She received numerous awards for her work, the most-prestigious one being the Gottfried Wilhelm Leibniz Award of the German Science Foundation in 2011.

Abstract:

High-impact pharmaceutical drugs are constantly identified by (bio)medical research, with a high potential for the treatment of severe civilization diseases. However, such drugs often exhibit a very low solubility in water (and thus in biorelevant media). As they tend to crystallize during storage or after administration, they cannot be used for the development of the future-generation pharmaceuticals. Therefore, about 80% of the promising drugs currently under development never make it into a medicine. Several approaches exist to increase the bioavailability of drugs. Most of them aim at formulating the drug in a less-stable but better-soluble modification which is intended to be stabilized with the help of excipients, e.g. polymers. However, finding the right excipient for a given drug is quite difficult and today usually established by a “trialand- error” approach assisted by expensive high-throughput screening techniques. This results in tremendous costs for the development of advanced formulations and – when no appropriate formulation is found - even prevents a huge number of very promising drugs from being applied in a medicine at all. As pharmaceutical formulations usually have to be stored between manufacturing and use, it has moreover to be guaranteed, that their properties do not change during this period. This is best ensured when they are thermodynamically stable, i.e. at drug concentrations being lower than the drug solubility in the formulation. The latter is to a great extend influenced by the kind of drug and excipients, by temperature, and by relative humidity. It will be shown that the influence of humidity on the drug solubility in ASDs as well as on their kinetic stability can be predicted using thermodynamic models (1-3, 5). This provides the information whether an ASD will crystallize (destabilize) at humid conditions or not. However, the investigation of crystallization kinetics is usually performed by timeconsuming long-term experiments with recurring investigations of crystallinity, e.g. by X-ray diffraction. In this work it will therefore also be demonstrated that the kinetics of drug crystallization in ASDs can be determined only based on simple water-sorption measurements combined with a state-of-the-art thermodynamic modeling of the drug solubility in polymers at humid conditions. The latter allows accounting for the mutual influence of water sorption and drug crystallization in the ASD and thus for simultaneously predicting the amount of absorbed water and crystallized drug. Knowing the experimental water sorption as function of time thus directly provides the ASD crystallinity without the need of additional X-ray measurements.

Keynote Forum

Nagatoshi Nishiwaki

Kochi University, Japan

Keynote: Synthesis of versatile aza-heterocyclic compounds by three component ring transformation

Time : dgg

Conference Series Formulations 2017 International Conference Keynote Speaker Nagatoshi Nishiwaki photo
Biography:

Nagatoshi Nishiwaki received his PhD from Osaka University in 1991. He worked at Osaka Kyoiku University (1991–2008). From 2000 to 2001, he joined Karl Anker
Jørgensen’s group at Aarhus University, Denmark. Between 2008 and 2009, he worked at Anan National College of Technology. He then moved to the School of
Environmental Science and Engineering, Kochi University of Technology, in 2009, and he became a Professor in 2011. His research interests comprise synthetic
organic chemistry using nitro compounds, heterocycles (ring transformations, 1,3-dipolar cycloadditions etc.), and pseudo- intramolecular reactions. He has more
than 120 papers and 20 review articles.

Abstract:

Dinitropyridone 1 is an excellent substrate for the nucleophilic type ring transformation to afford heterocyclic compounds
and nitroanilines those are not easily available by alternative methods. When pyridone 1 was reacted with aromatic ketone
in the presence of NH4OAc, 6-arylated 3-nitropyriines 2 were formed besides bicyclic compounds 3. This method was also
applicable to synthesis of cycloalka[b]pyridines 4 and 6-alkynylated/alkenylated pyridines 5, respectively. It was found to be
possible to use aldehydes as the substrate, which leading to 3,5-disubstituted pyridines 6. On the other hand, when aliphatic
ketones were employed as the substrate, two kinds of ring transformation proceeded. Namely, 2,6-disubstituted 4-nitroanilines
8 were formed in addition to nitropyridines 7. It was successful to apply this protocol to synthesis of N,N,2,6-tetrasubstituted
nitroanilines 9 upon treatment of dinitropyridone 1 with ketone and amine in the presence of acetic acid.

Keynote Forum

Christian Luebbert

TU Dortmund University, Germany

Keynote: Long-term stability of pharmaceutical formulations - prediction of recrystallization and amorphousamorphous phase separation

Time : fghhh

Conference Series Formulations 2017 International Conference Keynote Speaker Christian Luebbert photo
Biography:

Christian Luebbert graduated in Chemical Engineering at TU Dortmund University, Germany in 2014. During his work as Research Assistant at the Laboratory of
Thermodynamics, he focuses on the physical long-term stability of amorphous pharmaceutical formulations. With his expertise, he contributes from an engineering
point of view to pharmaceutically highly relevant development of formulation strategies for poorly water-soluble drugs.

Abstract:

Numerous recently-developed Active Pharmaceutical Ingredients (APIs) have a low solubility in water leading to
insufficient absorption and bioavailability. To overcome this solubility limitation, APIs are molecularly dispersed in
hydrophilic polymers. The resulting formulations are denoted as Amorphous Solid Dispersion (ASDs). For the administration
of new pharmaceutical formulations, long-term stability tests are imposed by regulatory authorities at defined conditions
of temperature and humidity (25°C, 60% relative humidity (RH) for 12 months tests and 40°C, 75% RH for accelerated sixmonths
tests). Recrystallization of the amorphous API and/or moisture-induced amorphous-amorphous phase separation
(miAPS) might occur during storage indicating the thermodynamic instability of the ASDs. Long-term stable formulations
are nowadays identified by trial-and-error principles. The aim of this work was to a-priory estimate the long-term stability
of ASDs by applying advanced thermodynamic methods1 and thus to reduce the experimental effort for finding promising
polymeric carriers suitable for formulation development. In order to validate the thermodynamic predictions, ASDs with
different API/polymer compositions were prepared and subjected to two years enduring long-term stability tests at the
aforementioned conditions. Recurring PXRD measurements were performed to detect recrystallization and Raman mapping
was applied to quantify miAPS. Water sorption was observed as function of time using a magnetic suspension balance. Water
sorption and thereby induced phase transitions (recrystallization/ miAPS) could be predicted in quantitative agreement with
the experimental data. This study showed that results of long-term stability tests can be predicted correctly in early stages of
drug development and that promising polymer candidates for long-term stable ASDs can be identified prior to long-term
stability tests by thermodynamic modeling.

Keynote Forum

Shrawan Baghel

Waterford Institute of Technology, Ireland

Keynote: Investigating the dissolution performance of dipyridamole and cinnarizine spray dried amorphous solid dispersion using proton NMR

Time : 14:45-15:05

Conference Series Formulations 2017 International Conference Keynote Speaker Shrawan Baghel photo
Biography:

Shrawan Baghel is currently doing PhD in “Novel technologies and optimized formulations for delivery of solid dispersion of BCS class II drugs” at Pharmaceutical
and Molecular Biotechnology Research Center (PMBRC), Waterford Institute of Technology. He is the winner of Science Foundation Ireland scholarship for this
project in collaboration with Synthesis and Solid State Pharmaceutical Centre. The main aim of this project is to gain an insight into the mechanistic and molecular
aspects of solid dispersion prepared by spray drying, hot melt extrusion and supercritical fluid process using DSC, XRD and NMR. He had also planned, conducted,
interpreted nanotechnology and lipid based formulation approaches to increase the solubility and dissolution of poorly soluble drugs.

Abstract:

Amorphous Solid Dispersions (ASDs) are of great interest as enabling formulations because of their ability to increase
the bioavailability of poorly soluble drugs. However, the dissolution of these ASD based formulations results in highly
supersaturated drug solution that can undergo different types of phase transition. We have investigated the dissolution
performance of amorphous solid dispersions of poorly water-soluble dipyridamole (DPM) and cinnarizine (CNZ) spraydried
amorphous solid dispersions (ASDs) using polyvinyl pyrrolidone (PVP) and polyacrylic acid (PAA) as a carrier matrix.
Dissolution studies were carried out under non sink conditions and solution phase drug-polymer interactions was characterized
using proton NMR. It was found that the dissolution of ASDs led to sustained supersaturation, the duration of which varied
depending on the drug loading and type of polymer used in the formulation. The main mechanism for drug supersaturation
generation and prolongation was found to be anti-plasticization effect of polymers on amorphous drugs within spray dried
ASDs and the ability of polymers to reduce the crystal growth rates of DPM and CNZ. To further understand the molecular
mechanism behind supersaturation stabilization in the presence of polymer, we employed, Solution 1H NMR. The change
in electron densities of proton and the relative intensities of peak shifts indicated the nature of interaction between drug and
polymer in different systems are different. These different effects suggest that DPM and CNZ interacts in a different way with
PVP and PAA in solution which goes some way towards explaining the different polymeric effect, particularly in terms of
inhibition of drug recrystallization and dissolution of DPM and CNZ ASDs. . The overall supersaturation profile observed thus
depended on a complex interplay between dissolution rate, polymer type, drug loading, crystallization mechanism of drugs
and drug-polymer interaction in the solution state.

Keynote Forum

Shahnaz Usman

RAK MHSU, UAE

Keynote: Formulation and in-vitro evaluation of montelukast oral disintegrating (5 mg) tablets: Effects of diluents

Time : affffffffff

Conference Series Formulations 2017 International Conference Keynote Speaker Shahnaz Usman photo
Biography:

Shahnaz Usman has received her PhD in Pharmaceutics from University of Karachi during the period of 2007. Currently, she is working as an Associate Professor
in Department of Pharmaceutics in RAK College of Pharmaceutical Sciences. She is appointed as Reviewer by different international journals. She is a registered
member of Pakistan Pharmacist Association.

Abstract:

Objective: The aim of the present study was to prepare ODT by using relatively a simple direct compression technique with
high mechanical strength while keeping the attributes of fast disintegration and dissolution to improve the bioavailability of
the drug.
Method: Mannitol and microcrystalline cellulose were studied as diluents in the same quantity for manufacture of montelukast
sodium tablet using crospovidone as super disintegrants and sodium bicarbonate as wicking agent. The blend was examined
for angle of repose, bulk and tapped density, compressibility index, and Hausner’s ratio. The drug-excipients interaction was
investigated by FTIR. After compression hardness, friability, disintegration and dissolution, all the formulations batches were
analyzed.
Results: It was found that microcrystalline cellulose was suitable diluent for tablets considering hardness, friability and
disintegration time. Ten formulations F1 to F10 were prepared by central composite methods (two level factorial designs) for
the selection of optimum concentration of disintegrants and diluents.
Conclusions: The overall results showed that crospovidone was the best super-disintegrant for showing the shortest
disintegration time while MCC was the good diluent in preparing montelukast Oro-dispersible tablet and this suggested the
possibility of utilizing the selected best formula (F2) in the preparation of Oro-dispersible tablet as a new dosage form for oral
administration.

Keynote Forum

Tomasz Urbaniak

Wroclaw Medical University, Poland

Keynote: Lamivudine-poly-E-caprolactone conjugate based particles for targeted drug delivery, synthesis and characterization

Time : 15:55 - 16:30

Conference Series Formulations 2017 International Conference Keynote Speaker Tomasz Urbaniak photo
Biography:

Tomasz Urbaniak is a Pharmacist and Research Assistant in Physical Chemistry Department of Faculty of Pharmacy, Wroclaw Medical University. His activity
includes evaluation of polymerization methods, structural analysis of polymeric materials on molecular and bulk level, and examination of drug release from
nanometric and micrometric particles. Also, utilization of quantum chemistry calculations in the field of pharmaceutical science is in scope of his interests.
Interdisciplinary approach is the way he thinks and acts in his work.

Abstract:

Poly-E-caprolactone (PCL) is biodegradable, nontoxic polyester synthesized mainly in ring-opening polymerization
(ROP) of E-caprolactone (CL). PCL alone or in blends was utilized in numerous medical applications, such as scaffolds,
implants, nano- and micro- drug carriers. It is characterized by slow degradation of polyester chains in hydrolytic mechanism.
Lamivudine (LV), as well as other antiretroviral drugs used in HIV-1 treatment, targets infected immune system cells, mainly
CD4+ T helper cells. However, other infected cells like macrophages, monocytes, dendritic cells are found through whole body,
including lungs and central nervous system. This cells halflife, measured in weeks/years, is dramatically longer in comparison
to CD4+ T helper cells, which is counted in hours/days. Such cells are often recognized as reservoirs of retroviruses, especially
these which are found in sites hardly available for drug substances, so called “sanctuaries”. The aim of this study was to design a
process of poly-E-caprolactone-lamivudine conjugate (PCL-LV) synthesis, and forming it into microspheres. Due to extremely
slow hydrolytic degradation, phagocytosis would be main mechanism of intravenously administered particles clearance.
Suggested mechanism of ROP includes formation of bond between initiator and polymer backbone. Drug bound covalently
to oligomeric chain would not be released from polymeric matrix in to plasma, therefore whole administered dose would
eventually achieve phagocytic cells, i.e., HIV-1 infected macrophages, monocytes or dendritics cells. Conjugate structure was
confirmed by the proton nuclear magnetic resonance and electro-spray ionization time of flight mass spectroscopy. Further
stage of study included microsphere forming in a variant of solvent evaporation method. Shape and size of obtained particles
was determined by scanning electron microscopy, light microscopy and dynamic light scattering. Average molecular weight of
obtained polymers was 5400 Da, size of prepared particles varied from nanometric to micrometric dimensions.

Keynote Forum

Supamas Napavichayanun

Chulalongkorn University, Thailand

Keynote: Tolerogenicity, anti-melanogenicity and anti-tyrosinase effects of sericin on melanocyte and dendritic cells: A possibility to alleviate post inflammatory hyperpigmentation

Time : 15:55 - 16:30

Conference Series Formulations 2017 International Conference Keynote Speaker Supamas Napavichayanun photo
Biography:

Supamas Napavichayanun is a PhD student, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Thailand. She earned a BSc from Faculty of
Pharmaceutical Sciences, Chulalongkorn University in 2010. Her research experience has ranged from protein including silk proteins and biomaterials. She also
did clinical researches in the area of dermatology especially materials for wound healing application.

Abstract:

Sericin has been conducted to characterize its immunomodulatory effects especially anti pro-inflammatory activities for
decades. In addition, it is also well known that hyperpigmentation disorders such as post inflammatory hyperpigmentation
(PIH) and melanoma, are a major concern not only in white skin type people, but also raises in darker skin type of Asian
population. Although there are many types of therapeutic products, more effective treatments still need to be evolved. The
important modulators of epidermal innate immune responses are melanocytes and dendritic cells (DCs), which composed of
induction, regulation, and maintenance of inflammatory responses on skin. However, the immunomodulatic role of sericin
on melanocytes and DCs relate to therapeutic effect of hyperpigmentation disorders has not been well established. Moreover,
sericin composes of the anti-tyrosinase property. Although the most prominent target for inhibitors of hyperpigmentation is
tyrosinase, unfortunately, a little is known about its anti-melanogenic property and clinical efficacy. In this study, we conducted
in vitro model and electron microscopic studies (immune-gold labeling) to determine (i) the tolerogenic effect sericin on
melanocytes and DCs indicated by the level of IL-10 and transforming growth factor (TGF)-ß, (ii) the anti-melanogenic
property of sericin characterized by tumor progressive marker (Mtif) and (iii) the anti-tyrosinase effect of sericin using
tyroninase marker. The results showed that sericin (at leat 5 μg/ml) composed of tolerogenicity, anti-tyroninase and antimelanogenicity
effects on melanocytes and DCs as demonstrated by the up-regulation of IL-10 and TGF- ß in association with
the down-regulation of tyrosinase and Mtif, respectively. This study provides the understanding of immunomodulatic role of
silk sericin on melanocytes and DCs underlying hyperpigmentation disorders lead to the applications allowing affected people
to have a better quality of life and their guidelines for therapeutic approaches.

Keynote Forum

Kampanart Huanbutta

Burapha University, Thailand

Keynote: Development and characterization of seed gums from Cassia fistula as disintegrating agent for fast disintegrating Thai cordial tablet

Time : dff

Conference Series Formulations 2017 International Conference Keynote Speaker Kampanart Huanbutta photo
Biography:

Kampanart Huanbutta has his expertise in drug delivery system and application of polymer in pharmaceutical dosage forms. He graduated from Faculty of
Pharmacy, Silpakorn University, Thailand. After that, he received Postdoctoral Scholarship from Erasmus Mundus to conduct research concerning anticancer drug
delivery system in University of Porto, Portugal. Now he is working at Faculty of Pharmaceutical Sciences, Burapha University as an Assistant Dean for academic
affair and post-graduation study. He also works as Secretary General of Pharmaceutical Association of Thailand under Royal Patronage. He has published research
and review articles in international journals for more than 20 articles.

Abstract:

Crude seed gum and their carboxymethyl derivatives from Cassia fistula seed was developed and characterized to apply
as the pharmaceutical disintegrant in fast disintegrating Thai cordial tablet. The chemical structure of crude gum was
chemically modified via carboxymethylation. Degree of substitution (DS) of carboxymethylated gums was determined.
Carboxymethylated gums with minimum and maximum DS values were chosen for further application. IR absorption spectra
of gum samples were observed to verify their chemical structure changes. In physical properties, the intrinsic viscosity and
swelling property of all gum samples were evaluated. The results showed that carboxymethylated gums had higher intrinsic
viscosity than those of crude gum. Moreover, they could swell and be soluble in cold water better than those of crude gums.
In conclusion, the modified gums from both plants could provide higher hardness and be better used than that crude gums
for fast disintegrating Thai cordial tablet. However, this is a preliminary assessment to expressing pharmaceutical application
possibility of these gums as disintegrants, diluents and drug release controlling agents.

  • Pharmaceutical Formulations | Solid Dosage Forms | Novel Drug Delivery Systems | Drug Formulation Procedures | Pharmaceutical Excipients | Regulatory Affairs
Location: Thon Hotel Bristol Stephanie
Speaker

Chair

Nagatoshi Nishiwaki

Kochi University, Japan

Session Introduction

Nagatoshi Nishiwaki

Kochi University of Technology, Japan

Title: Synthesis of versatile aza-heterocyclic compounds by three component ring transformation
Speaker
Biography:

Nagatoshi Nishiwaki received his PhD from Osaka University in 1991. He worked at Osaka Kyoiku University (1991–2008). From 2000 to 2001, he joined Karl Anker Jørgensen’s group at Aarhus University, Denmark. Between 2008 and 2009, he worked at Anan National College of Technology. He then moved to the School of Environmental Science and Engineering, Kochi University of Technology, in 2009, and he became a Professor in 2011. His research interests comprise synthetic organic chemistry using nitro compounds, heterocycles (ring transformations, 1,3-dipolar cycloadditions etc.), and pseudo- intramolecular reactions. He has more than 120 papers and 20 review articles.

Abstract:

Dinitropyridone 1 is an excellent substrate for the nucleophilic type ring transformation to afford heterocyclic compounds and nitroanilines those are not easily available by alternative methods. When pyridone 1 was reacted with aromatic ketone in the presence of NH4OAc, 6-arylated 3-nitropyriines 2 were formed besides bicyclic compounds 3. This method was also applicable to synthesis of cycloalka[b]pyridines 4 and 6-alkynylated/alkenylated pyridines 5, respectively. It was found to be possible to use aldehydes as the substrate, which leading to 3,5-disubstituted pyridines 6. On the other hand, when aliphatic ketones were employed as the substrate, two kinds of ring transformation proceeded. Namely, 2,6-disubstituted 4-nitroanilines 8 were formed in addition to nitropyridines 7. It was successful to apply this protocol to synthesis of N,N,2,6-tetrasubstituted nitroanilines 9 upon treatment of dinitropyridone 1 with ketone and amine in the presence of acetic acid.

Christian Luebbert

TU Dortmund University, Germany

Title: Long-term stability of pharmaceutical formulations - prediction of recrystallization and amorphous-amorphous phase separation
Speaker
Biography:

Christian Luebbert graduated in Chemical Engineering at TU Dortmund University, Germany in 2014. During his work as Research Assistant at the Laboratory of Thermodynamics, he focuses on the physical long-term stability of amorphous pharmaceutical formulations. With his expertise, he contributes from an engineering point of view to pharmaceutically highly relevant development of formulation strategies for poorly water-soluble drugs.

Abstract:

Numerous recently-developed active pharmaceutical ingredients (APIs) have a low solubility in water leading to insufficient absorption and bioavailability. To overcome this solubility limitation, APIs are molecularly dispersed in hydrophilic polymers. The resulting formulations are denoted as amorphous solid dispersion (ASDs). For the administration of new pharmaceutical formulations, long-term stability tests are imposed by regulatory authorities at defined conditions of temperature and humidity (25°C, 60% relative humidity (RH) for 12 months tests and 40°C, 75% RH for accelerated six-months tests). Recrystallization of the amorphous API and/or moisture-induced amorphous-amorphous phase separation (miAPS) might occur during storage indicating the thermodynamic instability of the ASDs. Long-term stable formulations are nowadays identified by trial-and-error principles. The aim of this work was to a-priory estimate the long-term stability of ASDs by applying advanced thermodynamic methods1 and thus to reduce the experimental effort for finding promising polymeric carriers suitable for formulation development. In order to validate the thermodynamic predictions, ASDs with different API/polymer compositions were prepared and subjected to two years enduring long-term stability tests at the aforementioned conditions. Recurring PXRD measurements were performed to detect recrystallization and Raman mapping was applied to quantify miAPS. Water sorption was observed as function of time using a magnetic suspension balance. Water sorption and thereby induced phase transitions (recrystallization/ miAPS) could be predicted in quantitative agreement with the experimental data. This study showed that results of long-term stability tests can be predicted correctly in early stages of drug development and that promising polymer candidates for long-term stable ASDs can be identified prior to long-term stability tests by thermodynamic modeling.

Shrawan Baghel

Waterford Institute of Technology, Ireland

Title: Investigating the dissolution performance of dipyridamole and cinnarizine spray dried amorphous solid dispersion using proton NMR
Speaker
Biography:

Shrawan Baghel is currently doing PhD in “Novel technologies and optimized formulations for delivery of solid dispersion of BCS class II drugs” at Pharmaceutical and Molecular Biotechnology Research Center (PMBRC), Waterford Institute of Technology. He is the winner of Science Foundation Ireland scholarship for this project in collaboration with Synthesis and Solid State Pharmaceutical Centre. The main aim of this project is to gain an insight into the mechanistic and molecular aspects of solid dispersion prepared by spray drying, hot melt extrusion and supercritical fluid process using DSC, XRD and NMR. He had also planned, conducted, interpreted nanotechnology and lipid based formulation approaches to increase the solubility and dissolution of poorly soluble drugs. 

Abstract:

Amorphous solid dispersions (ASDs) are of great interest as enabling formulations because of their ability to increase the bioavailability of poorly soluble drugs. However, the dissolution of these ASD based formulations results in highly supersaturated drug solution that can undergo different types of phase transition. We have investigated the dissolution performance of amorphous solid dispersions of poorly water-soluble dipyridamole (DPM) and cinnarizine (CNZ) spray-dried amorphous solid dispersions (ASDs) using polyvinyl pyrrolidone (PVP) and polyacrylic acid (PAA) as a carrier matrix. Dissolution studies were carried out under non sink conditions and solution phase drug-polymer interactions was characterized using proton NMR. It was found that the dissolution of ASDs led to sustained supersaturation, the duration of which varied depending on the drug loading and type of polymer used in the formulation. The main mechanism for drug supersaturation generation and prolongation was found to be anti-plasticization effect of polymers on amorphous drugs within spray dried ASDs and the ability of polymers to reduce the crystal growth rates of DPM and CNZ. To further understand the molecular mechanism behind supersaturation stabilization in the presence of polymer, we employed, Solution 1H NMR. The change in electron densities of proton and the relative intensities of peak shifts indicated the nature of interaction between drug and polymer in different systems are different. These different effects suggest that DPM and CNZ interacts in a different way with PVP and PAA in solution which goes some way towards explaining the different polymeric effect, particularly in terms of inhibition of drug recrystallization and dissolution of DPM and CNZ ASDs. . The overall supersaturation profile observed thus depended on a complex interplay between dissolution rate, polymer type, drug loading, crystallization mechanism of drugs and drug-polymer interaction in the solution state.

 

Shahnaz Usman

RAK MHSU, UAE

Title: Formulation and in-vitro evaluation of montelukast oral disintegrating (5 mg) tablets: effects of diluents
Speaker
Biography:

Shahnaz Usman has received her PhD in Pharmaceutics from University of Karachi during the period of 2007. Currently, she is working as an Associate Professor in Department of Pharmaceutics in RAK College of Pharmaceutical Sciences. She is appointed as Reviewer by different international journals. She is a registered member of Pakistan Pharmacist Association.

Abstract:

Objective: The aim of the present study was to prepare ODT by using relatively a simple direct compression technique with high mechanical strength while keeping the attributes of fast disintegration and dissolution to improve the bioavailability of the drug.

Method: Mannitol and microcrystalline cellulose were studied as diluents in the same quantity for manufacture of montelukast sodium tablet using crospovidone as super disintegrants and sodium bicarbonate as wicking agent. The blend was examined for angle of repose, bulk and tapped density, compressibility index, and Hausner’s ratio. The drug-excipients interaction was investigated by FTIR. After compression hardness, friability, disintegration and dissolution, all the formulations batches were analyzed.

Results: It was found that microcrystalline cellulose was suitable diluent for tablets considering hardness, friability and disintegration time. Ten formulations F1 to F10 were prepared by central composite methods (two level factorial designs) for the selection of optimum concentration of disintegrants and diluents.

Conclusions: The overall results showed that crospovidone was the best super-disintegrant for showing the shortest disintegration time while MCC was the good diluent in preparing montelukast Oro-dispersible tablet and this suggested the possibility of utilizing the selected best formula (F2) in the preparation of Oro-dispersible tablet as a new dosage form for oral administration.