Man Hee Rhee graduated in Veterinary Medicine in 1989 and completed his MS degree in 1991 and then PhD degree in 2000 in Neurobiology Department, Weizmann Institute of Science, Israel. He then spent 3 years in the Department of Cell Biology & Physiology, Washington University School of Medicine, USA as a Research Associate. He has joined in Kyungpook National University as Associate Professor. He has published more than 150 papers in reputed journals and has been serving as an Editorial Board Member of repute.

Ginseng, the root of Panax ginseng Meyer, had been used in Easter Asia, including Korea, China and Japan for a thousand of years. The potential benefits of ginseng range from energizing the body to providing the longevity. Ginsenoside Rg3 (Rg3), one of the most effective ginseng saponin, has anti-inflammatory and anti-cancer effects. Numerous previous studies have unraveled the Rg3 Pharmacological effects. One recent study has also revealed its protective cardiovascular effects in hyper sensitive rats. Here we investigated the anti-inflammatory activity of Rg3-enriched red ginseng extract in vitro on murine macrophages RAW 264.7 cells. We found that Rg3-enriched red ginseng extract in dose dependent manner attenuate the expression of proinflammatory cytokines after LPS induction. The MTT assay for dose dependent concentrations of Rg3-enriched red ginseng extract show no cytotoxicity and nitric oxide concentration show a decreasing trend with increase in dose. The mRNA expression of proinflammatory cytokines like IL-1β, IL-6, iNOS, COX-2 and TNF-α show the same trend like that of nitric oxide production. Furthermore, it was found that a remarkable attenuation of inflammation by oral treatment of Rg3-RGE extract in the mice survival study with LPS-induced septic shock. Rg3 enriched gingeng fraction can be hailed as a potent anti-inflammatory therapeutic agent in future.

Presenting author Dr. Namita NaikKhanvte is an Assistant professor at Visveswarapura Institute of Pharmaceutical Sciences, Bangalore-70, India. She is actively involved in research and guiding post-graduate students. She has one Indian patent to her credit.

Helminthiasisis a macroparasitic disease of humans and animals in which a part of the body is infected with parasitic worms (helminthes) like tapeworms, flukes and round worms. There is a need to develop novel herbal formulation with minimum side effects for better patient compliance. Punica granatum L. Family Punicaceae, is an ancient, mystical, unique fruit. It is reported to have anthelmintic activity in previous literature. The objective of the present work was to develop a formulation convenient for administration and appealing to the patient. Difficulty in swallowing is common among geriatrics and pediatrics, hence to avert this problem, soft fruity chews containing a natural anthelmintic extract were formulated. Soft chews are pleasantly chewable dosage forms which offer an enjoyable mouth feel and chewing experience. They mask odors and provide a prolonged contact with mouth thus enhancing product acceptability in children and adults. The prototype jelly base was formulated using a gelling agent, preservative, flavoring agent, novel natural thickening agent, plasticizer, coloring and cooling agent (Ecocool MP). Finally, herbal extract (Punica Granatum) as anthelmintic was incorporated to this jelly base. The developed formulation was evaluated for quality control parameters like appearance, taste, texture and stability. The gummies satisfied the desired physicochemical properties. The formulation was subjected to in vitro anthelmintic activity on Pheretima posthuma and found to exhibit significant level of activity when compared with marketed formulation. Thus, soft fruity chews containing a herbal anthelmintic extract were successfully developed.

Presenting author Dr Rajarajeshwari N is an Assistant professor at Visveswarapura Institute of Pharmaceutical Sciences, Bangalore-70, India. • Presently she is a Principal investigator for two major research project funded: 1. By ICMR entitled “Exploration of medicinal plants from western ghat region of Ramghat for cytotoxic and antiprotozoal potentials with special documentation of Tribal knowledge from the tribal communities located at the base of Ramghat” 2. By RGUHS entitled “Exploration of new medicinal plants of western ghats for their anti-diabetic potentials.

The genus Diospyros is a rich source for napthols and naphthoquinones. During the study, we have chemically examined the roots of three unexplored species of Diospyros crumenata for their chemical profile and biological activities. The plant materials collected from Ramghat of India. On conventional extractions with organic solvents and sequential chromatography yielded seven naphthoquinone derivatives, habibone (1), 8’-Hydroxyisodiospyrin (2), diospyrin (3), 4-Hydroxy-5methoxy-2-naphthaldehyde (4), 5-Hydroxy-4-methoxy-2-naphthaldehyde (5), 4-Hydroxy-3,5-dimethoxy-2-naphthaldehyde (6), and 2-Methyl anthraquinone (7). These isolates were characterized by spectral data (2D NMR, 1H-1H COSY and 13C-1H COSY). In addition, these compounds were evaluated for their potential to inhibit parasitic protozoa belonging to the genera Trypanosoma, Leishmania and Plasmodium using in vitro antiprotozoal assay and anthelmintic activity against adult earth worms, Pheritima posthuma. The study showed that the isolates enjoy significant anthelmintic and antiprotozoal activity and supports its use in folk medicine. Further, three isolates were incorporated into mouth dissolving tablets. The tablets were prepared by wet granulation technique using different ratios of binder, superdisintegrant Florite R, sweeteners, Instacoat® mango flavour. The developed tablets were evaluated for various quality control parameters like appearance, taste, weight variation, thickness, hardness, invitro disintegration time and friability. Results indicated successful formulation of mouth dissolving tablets with pleasant taste and satisfactory mouth feel with optimum physicochemical properties.

The presenting author N.R. Sneha Keerthi is working as research associate under the able guidance of Prof. Dr. Rajarajeshwari N at VISVESWARAPURA INSTITUTE OF PHARMACEUTICAL SCIENCES, Rajiv Gandhi University of Health Science’s. The major research project ICMR, Ad-hok 21/12/17/09HSR dated 24/06/2010. Entitled “Exploration of unexplored medicinal plants from Western Ghat region of Ramghat for their cytotoxic principal and documentation of tribal knowledge from the tribal community located at the base of Ramghat”.

Herbs are staging a comeback and herbal ‘renaissance’ is happening all over the globe. Herbal extracts have been successfully used in dentistry as tooth cleansing and antimicrobial plaque agents. Such dental formulations may lead to improvement in the general dental health of the population. The aim of the present work was to develop medicated toothpaste and dental gel containing natural active with a reported anticaries property. Commercially available toothpastes contain sodium fluoride which is an anticaries agent causing fluorosis and has detrimental effects on the musculoskeletal and nervous systems. They also contain Triclosan which is carcinogenic. Dentifrices were formulated using active Garcinia indica and other excipients. Excipients used for toothpaste included silica as abrasive and thickener, surfactant, humectant, sweetener, preservative and flavor. The dental gel was formulated using active along with Carbopol as gelling agent, sodium saccharin as sweetening agent, glycerin as humectant, triethanolamine as neutralizer and preservative. The dentifrices were evaluated for appearance, taste, odour, pH, foaming character, viscosity and abrasivity. The developed dentifrices satisfied the desired physicochemical properties. They have good commercial value because they are free from fluoride, Triclosan, SLS and synthetic/artificial colors and actives. Hence, they have good potential to be used in pediatrics.

Prof. Anoop Kumar Agarwal completed his PhD in 1988 from Postgraduate Institute of Medical Education and Research, Chandigarh, India. He has 27 years of experience in Pharmacology teaching and research. He is currently the Associate Dean of College of Graduate Studies at Gulf Medical University, Ajman, UAE. He has published more than 50 papers in reputed journals apart from having presented his work in several national and international conferences. He has also been a resource person in several Pharmacology workshops and seminars.

Pharmacogenomics aims to characterize the contribution of genetic polymorphisms to variability in drug response and toxicity. FDA has issued a list of drugs which exhibit polymorphism and relevant sections for providing pharmacogenomic information and their biomarkers to reduce the risk of drug toxicity. The objective of the study was to review the package insert for the presence and extent of pharmacogenomic information as per FDA recommendations. A total of 67 Package inserts of 41 drugs in different therapeutic areas available in UAE under various brand names were thoroughly reviewed for direct and indirect information signifying polymorphism. The description of serious drug-drug interaction and its management was also reviewed for risk assessment. The type of pharmacogenomic biomarker and related toxicity mentioned under different labeling sections was compared. Only 26 package inserts of 17 drugs (41%) prescribed for treating cancer, cardiovascular, CNS and Gastrointestinal disorders provided direct genetic evidence and information on the type of polymorphism influencing drug efficacy and toxicity. Indirect indicators describing genetic variation in metabolizing enzyme activity was present in 20 inserts (30%). Though rare adverse reactions had been mentioned under warning and contraindications, no special reference to genomic cause was identified. The FDA recommended pharmacogenomic information was lacking in 59% package inserts available in UAE. This information needs to be incorporated to enhance patient safety and awareness.

Otávio Pelegrino Rocha, B.Pharm., M.Sc., is a pharmacist and Ph.D. candidate in Toxicology at University of São Paulo. Dr. Danielle Palma de Oliveira is the vice-coordinator of the Toxicology Graduate Program at FCFRP-USP, and president of the Brazilian Society of Toxicology. She has more than 30 papers in reputed journals and has been serving as an editorial board member of repute.

Azo dyes are the most widely used synthetic organic dyes in textile industries. They can be cleaved by skin bacteria or by dermal/systemic metabolism into aromatic amines with undesired toxicological properties. ‘Acid Black 210’ has three azo groups in its chemical structure and is frequently used to dye leather, cotton and woollen. In 2014, this dye was identified as an azo dye which could be cleaved into the non-regulated aromatic amines of toxicological concern 4-nitroaniline and sulfanilic acid. To study the mutagenicity properties of this dye is essential to do a suitable (eco)toxicological risk assessment, specially because there are no information about the toxicological properties of this dye in the scientific literature. The experiments were conducted according to the methods described by Maron and Ames (1983), and Mortelmans and Zeiger (2000), with (+S9) and without (-S9) metabolization using the pre-incubation method in Salmonella typhimurium TA98 and TA100 strains. The number of His+ colonies were counted manually after 66h incubation at 37oC of ‘Acid Black 210’ (range 0.5-5,000 µg/plate). No mutagenic effect was observed for the TA100 strain even after metabolic activation. The mutagenic effect statistically occurred for the TA98 strain only in higher concentrations, increased after S9 treatment, but with very low potency (0.017 and 0.124 revertants/µg for -S9 and +S9, respectively). These new informations corroborate with other tests conducted by our group (data not show), with the conclusion that this dye seems to be sabe from the ecotoxicological point of view in the light of the current knowledge. Financial Support: FAPESP (Process number 2013/09317-7).

Obtaining a diploma of pharmacist in 2006 of the Faculty of Medicine of Algiers. Success in the competitive examination for the specialization in 2007 and integration of the central hospital of the army. Obtaining of diploma of medical specialized study(DEMS) in pharmaceutical chemistry in 2010 Success in the competitive entrance examination of hospitalo-university assistant professor in 2011 2011-until this date hospitalo-university assistant professor to the Faculty of Medicine of Blida and consultant in the center of research and development of the company SAIDAL

The Buprinal generic drug administered by injectable way is an analgesic manufactured by the algerian company SAIDAL. The active ingredient which is Buprinorphine hydrochloride belongs to the class of the strong analgesics and more specially to level II bis which is reserved for the relief of the severe pains. Besides Buprinorphine, Buprinal is constituted by the following excipients: glucose, hydrochloric acid and water for injectable preparations. The appearance during the study of stability of a unknown chromatographic peak(HPLC) ,and non-existent previously, having a time of retention about 2.55 minutes, required the release of a deep investigation. The increase of the area of the peak during the study of stability directed us to the track of a product of degradation which is due either to the degradation of Buprénorphine hydrochloride, or to the degradation of the glucose. Having eliminated the track of the active ingredient, the efforts were concentrated on the glucose which have the 5 HydroxyMéthylFurfural (5HMF) as main product of degradation according to the available literature. By injecting the reference substance (CRS) of 5HMF in the same chromatographic conditions as Buprinal, we deducted that the time of retention of the unknown peak corresponds perfectly to the reference substance 5HMF. Concerning the toxicity of 5 HMF,literature indicates that 5HMF is potentially genotoxic and carcinogenic and that the risk is higher when it is metabolized in SulfoxyMéthylFurfural ( SMF) or ChloroMéthylFurfural ( CMF). Also a study in silico with QSAR Toolbox software of the OECD has confirmed the genotoxic potential of 5 HMF because of his aldehyde group . According to the mixed international committee EXPERTS' FAO/WHO on food additives (JECFA) the maximal quantity tolerated by day and by person should not exceed 540 µg In the 2nd part of our work we looked to determine the concentration of 5HMF in the finished product Buprinal to compare it on one hand with the concentration of 5HMF in the reference drug product and on the other hand to prove the harmlessness by verifying that the limit of JECFA was not exceeded.

Waddah has completed his Master at the age of 25 years from Omdurman Islamic University. He is a pharmacist in Fedral Ministry of Health - Sudan, He has been serving as a member of National Medicine & Poisons Board – Sudan. He has published one paper/poster awarded as a best one in OMICS 2015 /Dubai in October

Gum arabic is a complex, loose aggregate of sugars and hemicelluloses composed of Arabic acid nucleus connected with calcium, magnesium, potassium besides Arabinose, Galactose, and Rhamnose. Gum Arabic is stable flexible material. This study aimed to use gum Arabic in manufacturing of Tablet coating material using water and plasticizer to add elasticity and flexibility. Gum Arabic acacia used in (10%), concentration in a pilot small coating machine with an inlet temperature 400c, and spraying rate 10 mls every 5 minutes on the top of Placebo tablet-bed while continuous drying. Gum : water ratio and plasticizer was determined by trial and error method to obtain the optimum level for the final coat characteristic. Physical tests were done for the tabletsbefore-and after the process. An accelerated stability study for three months was done. The result showed the optimum concentration ratio was 10% Gum arabic with 1% plasticizer. While other ratio variations showed cracking, and roughness in the surface. Physical examination ended to satisfying coat appearance with elegant, smooth picture. Gum Arabic is suitable material for tablets coating. The final property varies with the change in ratio of formula. Colors and anti-transparency additives are required for technological identification & customer’s needs. The ratio of 10:1 is the optimum to be adopted in manufacture film coating.

Pharmacist in 2007 faculty of Medecine Batna. Success in the competitive examination for the specialisation in 2007 and integration of Hussein Dey Hospital Algiers. Obtaning diploma of medical specialized study (DEMS) in pharmaceutical chemistry in 2010. Success in the competitive entrance examination of hospital-university assistant professor in 2011. Today hospital-university assistant professor at faculty of Medecine and consultant at frantz fanon hospital Blida.

A phytochemical and biological study Oleander - Nerium oleander (Apocynaceae) in the region of Larbaa was carried out on a batch harvested in May. The histological analysis of leaf showed the presence of crypts with stomata and trichomes, starch granules, microrosette crystals of calcium oxalate, very thick cuticle and characteristics of plants adapted to drought. The antioxidant power of flavonoid fraction was evaluated by the method diphenylpicrylhydrazyl (DPPH), the ability of extracts to scavenge this radical is measured by spectrophotometry. The results show a percentage of antioxidant activity: - 45% for leaf extracts of the plant -73% for flower extracts. The antibacterial effect was produced by the method of Mueller Hinton agar diffusion (IPA). The antimicrobial potency is estimated by measuring the diameter of inhibition zones of the tested strains. We showed that Nerium oleander possesses an effective antioxidant activity particularly high for flowers extracts. Flowers methanol extracts showed interesting potent antimicrobial activity against S.aureus MRSA 43300 (Resistant strain on standard antibiotics), E.coli, P.aeroginosa. These findings are useful for further research.

Hulya Ozdemir has completed her PhD in Faculty of Medicine, She is working as a Professor at the Medicine Faculty of Yuzuncu Yıl University. She’s the head of department of Pharmacology and Toxicology. She has published more than 70 papers and her research areas are mainly with plant therapy on the diabetes and cancer diseases , antioxidants and behavioural pharmacology

It was researched in this study, the antihyperglycemic effect of the extract prepared from P. harmala L. seeds, harmine and harmaline alkaloids fixed to be present in the extract in the GC-MS analysis of seed’s extract on the streptozotocin diabetic rats. It was given to diabetic rats four different dozes of liquid extract which is prepared from P. harmala L. seeds. It was fixed that there was significant decrease in the rats blood-glucose measure with 1.00 g/kg, 1.25 g/kg and 1.50 g/kg doses. It was observed that harmine 50 mg/kg and harmaline 125 mg/kg doses made fall down the blood glucose measure rihgtly in the first one hour. Glibenclamide and insulin was used as the reference drug in this study and there was no difference between glibenclamide and total extract and the activity of harmine and harmaline. Insulin is found to be more effective than extract and alkaloids. But in the first hour of the study, it was fixed that there was no significant difference between the activities of harmine 50 mg/kg and insulin. If we take these results into consideration, it can be thought that total extract of P. harmala L. and the alkaloids of beta carboline (harmine, harmaline) can be a useful source to develop new oral antidiabetic agent. But it is necessary to do more comprehensive pharmacological and toxicological studies in this subject.

Anne-Laure Pittet completed her PhD in Life Sciences from the University of Lausanne (Switzerland). She completed a Master of Advanced Studies (MAS) in Business Management at the University of Geneva (Switzerland). She is currently an Associate Researcher at the University Institute of the History of Medicine and Public Health (IUHMSP), Lausanne, Switzerland. Her main topic of interest is the interactions between the physicians, the pharmaceutical industry and the health authorities.

Medical representative visits (MRVs) are a means of information and a pharmaceutical strategy that is becoming less common, particularly visits involving generalists, all around Europe. In France, MRVs still remain a predominant pharmaceutical means of information about drugs for physicians, but increasingly the recommendations of drug regulatory authorities are to use representatives of health insurance and to participate in continuing medical education (CME). One of the results of our qualitative study in French-speaking Switzerland is that MRVs are deliberately very limited by generalists but still continue for specialists; participation in CME events is mandatory. Opinion leaders (OLs) are a means of information for physicians and a pharmaceutical strategy that is having an increasing impact. OLs interventions take place during CME events and conferences. The very concept of OLs needs to be clarified. A typology of OLs which was based on the international medical literature has been conducted, in order better to understand their roles and their increasing impacts as a means of information for physicians as well as a strategy for the pharmaceutical industry.

Maral Rashidi is a 25 year-old student at school of pharmacy at Shiraz University of Medical Sciences, Iran. She has finished her BS degree in Biochemistry (cumulative GPA of 3.5) and is currently undertaking pre-registration clinical trainings at designated pharmacies affiliated to Shiraz University. She is also conducting research in the fields of clinical and herbal pharmacology. She has gathered data on 100 rare herbal medicines merely found in Iran and their therapeutic applications (To be published). Considerable part of her work is devoted to clinical pharmacogenetics, chronopharmacology, and approaches to the extrapolation of experimental data to the clinical trials.

Implementing standard treatment guidelines and drug utilization evaluation strategies can be effective in improving the pattern of medications. The this study aimed to evaluate pharmacist interventions in decreasing the cost of albumin as one of the high-cost and overused medications in a teaching oncology hospital in southwest of Iran. A prospective, interventional study was conducted during 9 months from May 2015 to January 2016 in all wards of Amir Oncology Hospital affiliated to Shiraz University of Medical Sciences, Shiraz, Iran. Indication checklist draft of albumin was prepared by clinical pharmacists via reviewing relevant drug information references including Uptodate and Micromedex. These drafts were then revised and validated by the hematology-oncology faculty members. The physician team was requested to fill out this checklist at the time of ordering albumin. Checklists were then examined by the trained pharmacists. They were allowed to reject the orders if there was no indication or rational for giving albumin. Albumin was ordered for 129 patients (77 males and 52 females) aged 33.24 ± 25.75 years during the study period. Among them 10.51% were inappropriate and not approved by the pharmacists. Compared to the pre-intervention period (from August 2014 to April 2015), the total number of administered albumin in the post-intervention period decreased by 42.6% (from 1570 to 901 vials). The total direct cost reduction of albumin was calculated to be around 25,136 USD. Thus pharmacists can be actively involved in improving the utilization pattern and decreasing the cost of high-price medications in hospitalized oncology settings.

Hiwa K Saaed currently the Dean of The School of Pharmacy, Faculty of Medical Sciences at the University of Sulaimani since 2010, where he has been a faculty member since 2007. He is currently a lecturer of Pharmacology, Toxicology, and Communication skills in Pharmacy Practice. Hiwa K Saaed received his B.Sc in pharmacy and a Higher Diploma in Clinical Pharmacy from the College of Pharmacy and M.Sc and Ph.D. (1st Rank) in Clinical Pharmacology and Toxicology from the College of Medicine University of Baghdad. He has over 20 years of experience in Pharmacy Practice/ Hospital and Community settings. He is a director of Joint Higher Diploma (in Clinical Pharmacy) Studies with Ministry of Health KRG-Iraq, since 2010. His academic research explores the different aspects of Pharmacodynamics and –kinetics; permeability of Hydatid (Echinococcus granulosus) Cyst to drugs, GABA Receptor, Apoptotic gene expression in Leukemic patients... etc. He is supervising several postgraduate students in the area of clinical and basic pharmacology leading to MSc in Pharmacology and higher Diploma in Clinical Pharmacy. He is a member of the UniversityCouncil of Sulaimani, Scientific Promotion Committee of Faculty of Medical Sciences, Federal InternationaPharmacist, Royal Pharmaceutical Society, Syndicate of Iraqi Pharmacists and Kurdistan Pharmacists Associations and Faculty Affiliate of College of Pharmacy at Belmont University, Tennessee USA.

The main objective of this study was to optimize the efficacy and minimize the toxicity of long-term oral CsA use, through monitoring of blood CsA trough level, dose adjustment, and evaluation of biomarkers related to organs function, in stable kidney transplant recipients (KTR). Patients and Methodss: A prospective therapeutic drug monitoring (TDM) study was conducted to measure the blood CsA trough level, kidney and liver function test, fasting blood glucose, serum electrolytes for a total of 37 KTR who received immunosuppressant regimen therapy including CsA for more than three months, were offered to participate in this study. Blood CsA trough levels and biomarkers measured at two time points, at starting the study and one month later. Results: Blood CsA trough levels at1st and 2nd visit were within therapeutic range in 11 % : 27 % of the patients, lower in 22% : 25% and higher in 67% : 49% of the patients, respectively. Dose adjusment lead to significant improvement in kidney and liver function test parameters. The number of patients with high Cholesterol, triglyceride, fasting blood glucose, serum potassium and uric acid reduced at 2nd visit, as well. Conclusion: The current study confirmed the correlation between blood CsA trough level and the occurrence of CsA related toxicity that have a negative influence on graft function, morbidity and mortality of the KTR. TDM is the best way to optimize efficacy and minimize the toxicity of the oral CsA post-KT.

Lan Eng Low has completed her MSc from National University of Singapore in Applied Chemistry. She is the Senior Analytical Scientist in the Pharmaceutical Laboratory of Health Sciences Authority, the National Regulatory body in Singapore. She has various experiences in biologics manufacturing and pharmaceutical analysis especially in Quality Management and the use of advanced analytical instrumentation for pharmaceutical analysis.

In this study, an LC-MS/MS EPI method was developed for simultaneous determination of 32 toxic natural substances in herbal products. The analytes include aconite alkaloids, lobelia alkaloids, solanaceous alkaloids, digitalis steroid glycosides, strychnine, tetrahydropalmatine etc. They were commonly used in herbal products. The target analytes were extracted from the samples using the QuEChERS method and analysed using AB SCIEX QTRAP 5500 coupled with Agilent HPLC 1260. The column used was biphenyl reversed phase analytical column. Mobile phase A and B were deionized water and methanol respectively, both containing 5 mM Ammonium Formate and 0.1% formic acid. The MRM-IDA-EPI method enabled quantification and confirmation of the analytes in a single run. The EPI was used for the qualitative analysis while the MRM was used for the quantitative analysis. Limits of detection were determined to be below 10μg/kg for the majority of the analytes. The recoveries for those commonly detected natural substances were in the acceptable range of 70-120%.

Avital is a PhD candidate at the Department of Clinical Pharmacology and the School of Pharmacy, Ben-Gurion University of the Negev in Beer-Sheva, Israel. Avital received her Bachelor degree in Pharmacy from Kazan Medical State University, and Master's degree from Ben-Gurion University of the Negev. Avital's research interest is the interplay between the drug's solubility and permeability when using various solubility-enabling oral formulations for lipophilic drugs. She has published over 14 top-notch Journal papers.

The aim of this work was to assess the efficiency of different rifaximine amorphous solid dispersions (ASDs) in achieving and maintaining supersaturation and to investigate the solubility-permeability interplay when increasing the apparent solubility via ASD formulations. Spray-dried ASDs of rifaximine in different hydrophilic polymers were prepared and their ability to achieve and maintain supersaturation over 24 h was assessed. Then, rifaximine’s apparent intestinal permeability was investigated as a function of increasing supersaturation in-vitro using the parallel artificial membrane permeability assay (PAMPA) model and in-vivo using the single-pass rat intestinal perfusion model. The efficiency of the different ASDs to achieve and maintain supersaturation of rifaximine was found to be highly polymer dependent, and the Copovidone:HPC-SL formulation was found to be superior to the other ASDs, allowing supersaturation of 200× that of the crystalline solubility for over 20 hours. Rifaximine flux across the intestine from supersaturated solutions was increased, and the apparent intestinal permeability was constant, irrespective of the degree of supersaturation. In conclusion, while with other solubility-enabling approaches (e.g., surfactants, cyclodextrins, cosolvents), it is not enough to increase the apparent solubility, but to strike the optimal solubility–permeability balance, which limits the chances for successful drug delivery, the amorphous form emerges as a more advantageous strategy, in which higher apparent solubility (i.e., supersaturation) will be readily translated into higher drug flux and overall absorption.