Saccharin Research Articles

FORMULATION AND EVALUATION OF MADHUCA LONGIFOLIA EXTRACT SYRUP FOR LITHIASIS

M. longifolia's natural habitat spans from the southernmost tip of the Konkan peninsula down to the westernmost tip of the Western Ghats. Previous studies suggests that syrup of Madhuca longifolia (mahua) leaves & flower extract has not been formulated yet. Lithiasis is the presence of calculi within the urinary tract. So, present study is focused on the formulation and estimation of Madhuca longifolia syrup for urolithiasis activity. The fresh leaves and flower of Madhuca longifolia were collected from the lucknow region in Uttar Pradesh. It was washed, dried under shade, and sieved for making dust-free and kept at room temperature or shade. Chemicals i.e., propylene glycol, glycerin, sucrose, sorbitol, sodium saccharin, methylparaben, and propylparaben were purchased from the local chemical supplier. The leaves and powder of Madhuca longifolia were weighed and extracted through Soxhlet process using methanol and water, separately. The syrup was formulated by adding mahua extract and different excipients. The parameters including organoleptic features, flavonoid estimation, pH determination, density, viscosity, solubility and stability. In results, both the formulation was observed as optimized in terms of their organoleptic features- greenish colour, pH (6.0), characteristic odour with bitter taste. Appearances were heterogenous. The % yield was 9.8% and 8.2% in methanolic flower extract and aqueous flower extract, respectively. It concludes that both formulation of mahua syrup consisting leaves and flowers have shown a remarkable organoleptic characteristic as well as density, solubility and stability. It also demonstrated the presence flavonoids that might be important constituent for the urolithiasis potential and other pharmacological effects of mahua. It may also be confirmed that its syrup production at bulk level would be reasonable in terms of cost. It will improve the use of herbal syrup of Madhuca longifolia with reduced side effects.

Diols and sugar substitutes in attractive toxic sugar baits targeting Aedes aegypti and Aedes albopictus (Diptera: Culicidae) mosquitoes.

Around the world, mosquitoes continue to transmit disease-causing pathogens and develop resistance to insecticides. We previously discovered that a generally regarded as safe (GRAS) compound, 1,2-propanediol, reduces adult mosquito survivorship when ingested. In this study, we assess and compare 5 more chemically related compounds for mosquito lethality and 8 GRAS sugar substitutes to determine toxicity. We conducted a series of feeding assays to determine if ingesting the compounds influenced mosquito mean survivorship in locally collected lab-reared populations of Aedes aegypti (Diptera, Culicidae, Linnaeus, 1762) and Aedes albopictus (Diptera, Culicidae, Skuse, 1894) mosquitoes. Our results indicate that 1,2-propanediol, 1,3-propanediol, 1,5-pentanediol, 1,6-hexanediol, 2-methyl-1,3-propanediol, DL-dithiothreitol, acesulfame potassium, allulose, erythritol, sodium saccharin, stevia, and sucralose significantly reduced the mean survivorship of one or both species. Short-term trials with the most toxic compounds revealed that they could substantially affect survivorship after 24 h. We also found that there were different responses in the 2 species and that in several experimental conditions, male mosquitoes expired to a greater extent than female mosquitoes. These findings indicate that several of the compounds are toxic to mosquitoes. Further study is required to determine their effectiveness in attractive toxic sugar baits (ATSBs) as a potential component of population control strategies.

Effect of different artificial sweeteners on protein glycation

Glycation refers to the non-enzymatic molecular interaction between carbonyl group of sugars and amino groups of macromolecules viz. proteins, DNA, and lipids leading to the generation of Schiff’s base, Amadori products, and finally converted to deleterious advanced glycation end-products (AGEs). Several diseases such as neurodegenerative or mental disorders, cardiovascular complications, as well as diabetes, and its related complications show glycated product involvement. Hyperglycemia and diabetes are the main diseases in which AGEs formation and its accumulation are enhanced and cause secondary complications. This study was performed to investigate the antiglycation and anti-aggregation potential of Food and Drug Administration-approved artificial sweeteners. The in vitro glycation system (BSA and glucose) was incubated along with artificial sweeteners viz acesulfame potassium, saccharin sodium, sucralose, aspartame, and neotame for 35 days at 37 °C. The conventional analytical methods such as browning, NBT assay, DNPH assay, and assessment of fluorescent AGEs were carried out spectroscopically to check the amount of glycation products. The presence of the mentioned artificial sweeteners in the glycation system showed inhibition of carbonyl content, total AGEs generation, and aggregation of β-amyloid structures. On day 35, acesulfame potassium reduced carbonyl content by 62.63 ± 0.91%, total AGEs generation by 49.39 ± 0.82%, and β-amyloid aggregation observed by Thioflavin-T assay by 43.45 ± 1.14%. The tested artificial sweeteners exhibited potential antiglycation and anti-aggregation activity in vitro in protein, BSA. They may be used as a therapeutic agent for the management of diabetes and its complications.

Solubility Enhancement of Clozapine by Co-crystals

Cocrystallization of drug with coformers is a promising approach to alter the solid state properties of drug substances like solubility and dissolution. The objective of the present work was preparation, formulation and evaluation of the clozapine cocrystal by screening various coformers. Clozapine co-crystals were prepared using different coformers like benzoic acid, fumaric acid, sodium saccharin and sodium acetate. Cocrystals were prepared using solvent evaporation method and solvent drop grinding method. The prepared co-crystals were evaluated for saturation solubility, drug content, dissolution studies, XRD studies and DSC analysis.

Exploration of new solid forms of anti-emetic drug domperidone: Novel salts with enhanced solubility and dissolution

Domperidone (DMP) is an anti-emetic agent used for treatments like dyspepsia, indigestion, epigastric pain, nausea, and vomiting. DMP belongs to BCS class II having poor aqueous solubility and high permeability. In the current work, nine novel salts of DMP with coformers namely acetic acid (ACA), oxalic acid (OXC), Fumaric acid (FMA), Glutaric acid (GLA), Adipic acid (ADA), Saccharin (SAH), Salicylic acid (SAL), 4-Hydroxybenzoic acid (4HBA), and Theophylline-7-acetic acid (THA) have been reported. The crystal structures have been determined by Single-Crystal X-ray Diffraction (SC-XRD). In the SC-XRD study, proton transfer from coformer to piperidine ‘N’ of DMP was observed in all the salts. The prepared salts were further characterized by spectroscopic (FT-IR), thermal (DSC and TGA), and Powder X-ray Diffraction (PXRD) techniques. The solubility study in purified water (pH=6.5) showed 127 and 51-fold enhancement in DMP-GLA and DMP-ACA salts. The salts namely, DMP-ACA, DMP-GLA, and DMP-SAL disintegrate to parent DMP after attaining equilibrium in water medium. In 0.1 N HCl medium, DMP-ACA, DMP-GLA, DMP-ADA, and DMP-4HBA exhibited a two-fold increment in solubility compared to DMP. The in-vitro dissolution study in purified water showed faster drug release in DMP-ACA, DMP-GLA, and DMP-ADA salts.

Levels, consumption, and variations of eight artificial sweeteners in the wastewater treatment plants of Dalian city, China

Artificial sweeteners (ASs) are emerging contaminants in the environment, primarily derived from wastewater treatment plant (WWTP) effluents. In this study, the influents and effluents of three WWTPs in the Dalian urban area, China, were analyzed for the distribution of 8 typical ASs to investigate their seasonal fluctuations in the WWTPs. The results showed that acesulfame (ACE), sucralose (SUC), cyclamate (CYC), and saccharin (SAC) were both detected in the influent and effluent water samples of WWTPs, with concentrations ranging from not detected (ND) to 14.02 μg·L−1. In addition, SUC was the most abundant ASs type, accounting for 40 %–49 % and 78 %–96 % of the total ASs in the influent and effluent water, respectively. The WWTPs revealed high removal efficiencies of CYC, SAC, and ACE, while the SUC removal efficiency was poor (26 % ± 36 %). The ACE and SUC concentrations were higher in spring and summer, and all ASs showed lower levels in winter, which may be caused by the high consumption of ice-cream in warmer months. The per capita ASs loads in the WWTPs were determined in this study based on the wastewater analysis results. The calculated per capita daily mas loads for individual ASs ranged from 0.45 g·d−1·1000p−1 (ACE) to 2.04 g·d−1·1000p−1 (SUC). In addition, the relationship between per capita ASs consumption and socioeconomic status showed no significant correlation.

Sweet Taste Receptor T1R3 Expressed in Leydig Cells Is Closely Related to Homeostasis of the Steroid Hormone Metabolism Profile

Taste receptor type 1 subunit 3 (T1R3) is initially expressed in mammal tongue for recognition and response of sweet/umami tastants and is critical to nutrient absorption, even endocrine. In this study, down-regulation of related steroidogenic enzymes such as StAR, 3β-HSD, CYP17A1, and 17β-HSD with the decrease of T1R3 expression was found in Leydig cells treated by a T1R3 inhibitor (lactisole). The abundances of progesterone, 17a-hydroxyprogesterone, androstenedione, testosterone, and deoxycorticosterone were down-regulated by 2.3, 3.5, 1.4, 1.6, and 2.2 times, respectively, after T1R3 inhibition. In addition, opposite results were found in saccharin sodium treatment. T1R3 activation contributed to intracellular cyclic adenosine monophosphate (cAMP) accumulation (14.41 ± 0.58 vs 20.21 ± 0.65) and increased testosterone (20.31 ± 3.49 vs 50.01 ± 7.44) and steroidogenic metabolite levels. Coadministration of human chorionic gonadotropin and saccharin sodium resulted in elevating the testosterone and cAMP levels and enhancing the expression levels of steroidogenic-related factors. Similarly, intratesticular injection of lactisole and saccharin sodium further confirmed that T1R3 inhibition/activation affected the expression of related steroidogenic enzymes and the testosterone levels in mice. The above findings suggest that T1R3 plays a role in testicular steroidogenesis.

Microhardness and tensile strength of electrochemically synthesized nickel-cobalt binary alloy sheets exfoliated from a dumbbell-shaped titanium cathode

Nanocrystalline nickel–cobalt (Ni–Co) binary alloy sheets were fabricated through electroforming in an acidic aqueous bath using exfoliation from a metallic titanium cathode. Cobalt content in Ni–Co alloy sheets ranged from 28.8 at% to 72.0 at% depending on experimental parameters, such as cathodic overpotential and bath composition. The surface roughness (R a) of the electroformed alloy sheets significantly decreased down to 1.5 μm as saccharin sodium dihydrate was added as an additive to the acidic aqueous solution bath. X-ray diffraction profiles and transmission electron microscopy images indicated that the electroformed Ni–Co alloy sheets have a nanocrystalline structure (grain size ≈ 30 nm). The lattice constant of the electroformed Ni–Co alloy sheets increased with an increase in cobalt content (i.e. solute atom concentration). The mechanical properties were significantly improved because of the synergistic effects of crystal grain refinement and solid solution strengthening. The microhardness and tensile strength of the electroformed Ni–Co alloy sheets reached 609 kgf mm−2 and 1757 MPa (X Co = 49.9 at%), respectively. The tensile strength of the electroformed Ni–Co alloy sheets in this study significantly exceeded that of solidified Ni–Co alloys (approximately 370 MPa). Therefore, this study offers a technique to enhance the mechanical properties of electroformed Ni–Co alloy sheets.

Characterization of Cocoa Bean Husk Extract Particles and its Comparison as a Mouthrinse with Different Vehicles in Children aged 7-12 Years.

Assessing the efficacy of cocoa bean husk extract (CBHE) particles with different vehicles as a mouthrinse in children aged 7-12 years in comparison to chlorhexidine (CHX) and sodium fluoride (NaF) mouthrinse. A total of 80 children aged 7-12 years residing at a residential school/orphanage in Bengaluru city were selected and randomly allocated into five groups-group I: 0.1% CBHE with distilled water (DW); group II: 0.1% CBHE with Ringer's lactate (RL); group III: 0.12% CHX; group IV: 0.1% CBHE with normal saline (NS); and group V: 0.05% NaF. A Simplified Oral Hygiene Index (OHI-S) was recorded, salivary pH was assessed, and unstimulated saliva samples were collected at baseline (BL) after 30 minutes of rinsing on day 7 and day 14. These saliva samples were subjected to microbiological analysis, and all the data from five groups at four different time intervals was tabulated and statistically evaluated. Nearly 0.1% CBHE with NS as vehicle showed maximum antibacterial properties among all the groups at all time intervals. The addition of RL to CBHE provided better anti-plaque efficacy than 0.1% CBHE with DW and 0.12% CHX mouthwash. All three combinations of 0.1% CBHE and 0.12% CHX mouthwash proved to be better anti-plaque agents than 0.05% NaF. Improving the preparation of CBHE mouthwash by using NS, RL, and with the addition of saccharin sodium also improved the patient's compliance. Thus, preparing chocolate/CBHE mouthwash with NS or RL instead of plain DW increased the salivary pH, anti-plaque efficacy, and antibacterial property by reducing Streptococcus mutans growth. Cocoa bean husk extract (CBHE) mouthwash is a better anticariogenic and nonalcoholic mouthwash compared to CHX and NaF, which can be safely used in children as a routine oral rinse and also for those with gingivitis and high-risk of caries. Kibriya S, Srinivasan I, Setty JV, et al. Characterization of Cocoa Bean Husk Extract Particles and its Comparison as a Mouthrinse with Different Vehicles in Children aged 7-12 Years. Int J Clin Pediatr Dent 2023;16(1):54-59.

Effect of Unpalatable Diets, Food Restriction and Saccharin-Adulterated Diet on Tryptic, Chymotryptic, and Amylolytic Activity in Pancreas, Intestine and Feces of Rats

Growing rats were fed either 10 or 17% protein (casein) diets whose taste was changed daily by addition of aversive stimuli. Under these circumstances food intake and body weight gain were reduced compared with controls fed unadulterated diets. More amylolytic activity per gram pancreas was found in rats fed a 10% protein, aversive diet and in their pair-fed controls fed restricted amounts of an unadulterated diet compared with ad libitum controls. More amylolytic activity per gram chyme of small intestine was also found in rats fed less than ad libitum amounts of a 10% protein diet. The chymotrypsin activity in the pancreas of rats fed a 17% protein, aversive diet was greater than in that of control animals or that of the pair-fed animals. The 2- to 10-fold higher proteolytic activity found in the small intestine and especially in the large intestine and feces of rats fed the aversive diet was specificially related to the adulteration of the diet with sodium saccharin. Feeding a diet containing sodium saccharin led to lower cecal pH. Under conditions of the present experiments, changes in digestive enzyme activity are not directly related to the aversive taste of the diet.aversive taste unpalatable diets food restriction saccharin trypsin chymotrypsin amylase

Effect of food additives on key bacterial taxa and the mucosa-associated microbiota in Crohn’s disease. The ENIGMA study

ABSTRACT Food additives have been linked to the pro-inflammatory microbial dysbiosis associated with Crohn’s disease (CD) but the underlying ecological dynamics are unknown. Here, we examine how selection of food additives affects the growth of multiple strains of a key beneficial bacterium (Faecalibacterium prausnitzii), axenic clinical isolates of proinflammatory bacteria from CD patients (Proteus, Morganella, and Klebsiella spp.), and the consortia of mucosa-associated microbiota recovered from multiple Crohn’s disease patients. Bacterial growth of the axenic isolates was evaluated using a habitat-simulating medium supplemented with either sodium sulfite, aluminum silicate, carrageenan, carboxymethylcellulose, polysorbate 80, saccharin, sucralose, or aspartame, intended to approximate concentrations found in food. The microbial consortia recovered from post-operative CD patient mucosal biopsy samples were challenged with either carboxymethylcellulose and/or polysorbate 80, and the bacterial communities compared to unchallenged consortia by 16S rRNA gene amplicon profiling. Growth of all F. prausnitzii strains was arrested when either sodium sulfite or polysorbate 80 was added to cultures at baseline or mid-exponential phase of growth, and the inhibitory effects on the Gram-negative bacteria by sodium sulfite were conditional on oxygen availability. The effects from polysorbate 80, saccharin, carrageenan, and/or carboxymethylcellulose on these bacteria were strain-specific. In addition to their direct effects on bacterial growth, polysorbate 80 and/or carboxymethylcellulose can drive profound changes in the CD mucosa-associated microbiota via niche expansion of Proteus and/or Veillonellaceae – both implicated in early Crohn’s disease recurrence. These studies on the interaction of food additives with the enteric microbiota provide a basis for dietary management in Crohn’s disease.

Occurrence, distribution, and ecological risk assessment of artificial sweeteners in surface and ground waters of the middle and lower reaches of the Yellow River (Henan section, China).

As a new class of water contaminants, artificial sweeteners (ASs) have attracted much attention due to their environmental persistence and potential adverse effects to human and the environment. This study systematically investigated the occurrence and distribution of four commonly used ASs in the effluent of wastewater treatment plants (WWTPs), surface water and groundwater in the middle and lower reaches of the Yellow River (Henan section). Sucralose (SUC) was dominant in WWTP effluents and had the highest mass loading. Acesulfame (ACE), cyclamate (CYC), saccharin (SAC), and SUC were consistently detected in surface water at concentrations ranging from 1.364ng/L (CYC) to 7786ng/L (ACE). Spatial analysis showed that the pollution level of ASs in the trunk stream was lower than that in most tributaries. The total concentrations of ASs detected in surface water ranged between 308.7 and 10,498ng/L, while in groundwater, the total concentration of ASs detected was between ND-4863ng/L. ACE and SUC are the main pollutants in surface water and groundwater within this survey area. The risk assessment showed that the risks of the four target ASs to aquatic organisms were negligible (risk quotient (RQ) values < 0.1), and the maximum risk quotient of the mixtures (MRQ) values of all rivers were all much less than 0.1.

Mechanistic insights into the crystallization of coamorphous drug systems.

In our previous study, the coamorphous formulation of lurasidone hydrochloride (LH) with saccharin (SAC) showed significantly enhanced dissolution and physical stability compared to crystalline/amorphous LH. However, the coamorphous system is still in amorphous state, and has the tendency to recrystallization, which will in turn result in the loss of above advantages. In this study, the crystallization kinetics under isothermal and non-isothermal conditions was investigated. Compared to amorphous LH, coamorphous LH-SAC showed 68.3-361.2 and 2.6-6.1 times lower crystallization rates in glassy state and supercooled liquid state, respectively. After co-amorphization, the addition of SAC changed the crystallization mechanism of amorphous LH from nucleation-controlled to diffusion-controlled manner. Amorphous LH followed the site-saturated nucleation, whereas the coamorphous system exhibited a fixed number of nuclei. The non-isothermal crystallization indicated amorphous LH and coamorphous LH-SAC showed two-dimensional (JMAEK 2) and three-dimensional (JMAEK 3) growth of nuclei, respectively. Furthermore, coamorphous LH-SAC exhibited higher molecular mobility and dynamic fragility (mD) than amorphous LH, which is kinetically unfavorable for its physical stability. However, from thermodynamic perspective, coamorphous LH-SAC had a higher configurational entropy, i.e., a higher entropy barrier for crystallization, which is beneficial to hinder its crystallization. Therefore, it was concluded that the higher configurational entropy rather than the molecular mobility was proposed to be responsible for its improved stability. In addition, molecular dynamics simulations with miscibility, radial distribution function and binding energy calculations suggested coamorphous components exhibited good miscibility and strong intermolecular interactions, which was also conductive to the enhancement in its stability. This study offers an in-depth understanding about the effect of the coformer on the crystallization kinetics of coamorphous systems, and points out the important contribution of the configurational entropy in stabilizing the coamorphous systems.

Development of an Oral Liquid Formulation of Nicardipine Hydrochloride Compounded with Simple Excipients for the Treatment of Pediatric Hypertension

Nicardipine hydrochloride is an anti-hypertensive drug that is used off-label to treat hypertension in children. A previous oral formulation of nicardipine hydrochloride was developed using a commercial vehicle as an excipient. However, ready-to-use vehicles are prone to supply shortages, and their composition may undergo substantial modifications. The aim of this study was to propose a new oral formulation of nicardipine hydrochloride 2 mg/mL using simple excipients. The formulation included hydroxypropylmethylcellulose, simple syrup, polysorbate 80, sodium saccharin, citrate buffer, strawberry flavor and 0.2% potassium sorbate. The uniformity of content was maintained before and after agitation. Nicardipine hydrochloride concentration assessed by HPLC-MS/MS remained above 90% for 365 days before opening and for 28 days after opening. pH and osmolality were maintained throughout the study, and no microbial contamination was observed. The uniformity of mass of the delivered doses was evaluated using four different devices. A new oral formulation of nicardipine hydrochloride 2 mg/mL was developed using simple and safe excipients. Pharmacological and clinical parameters remain to be assessed and compared with those of the previous formulation.

SERS determination of sodium saccharin content on the tipping paper of cigarettes using AgNP substrates prepared with a USB-power supply device.

A novel magnetic agitating heater powered by a USB port has been developed and applied to synthesize silver colloid substrate for surface-enhanced Raman scattering (SERS) detection of sodium saccharin content on the tipping paper of cigarettes. The heater device allows the convenient synthesis of the Ag colloid, and the reaction can be completed on-site in 15 min under mild conditions. The on-site synthesis of SERS substrate effectively avoided the need for storage and concerns regarding the poor stability and short lifespan of colloid substrates. The results demonstrated that the substrate obtained with the device could achieve SERS detection of Rhodamine 6G (R6G) at as low as 10-9 mol L-1 while maintaining a stable intensity with a relative standard deviation (RSD) of 5.52% (n = 5). Using the prepared substrate at the optimal conditions, the limit of detection of sodium saccharin (SS) was 1 mg L-1. By introducing an internal standard KSCN, a linear relationship was observed between the relative intensity at 708 cm-1 and the concentration of the SS in a range of 20-100 mg L-1 (R2 = 0.98). With the developed method, SS was directly extracted from the cigarette paper by immersing it in water, and the extracted solution was subsequently detected. The quantitative spike-recoveries were in the range of 95.5-116.7%, with RSD between 2.3-12.6%. The whole detection procedure including the on-site substrate preparation, took only about 30 min. This work opens new avenues for colloidal synthesis, and the detection method of SS on the cigarette paper also holds great promise in food safety applications.

Safety of a feed additive consisting of sodium saccharin for suckling and weaned piglets, fattening pigs, calves for rearing and for fattening (FEFANA asbl).

Following a request from the European Commission, EFSA was asked to deliver a scientific opinion on the safety of sodium saccharin as a sensory feed additive (flavouring compound) for suckling and weaned piglets, fattening pigs, calves for rearing and for fattening. In a previous assessment, the Panelon Additives and Products or substances used in Animal Feed (FEEDAP Panel) could not conclude on the safety of the additive for the environment because concentrations of the additive or its degradation product 4-hydroxysaccharin in groundwater above 0.1μg/L were likely to occur. In addition, regarding user safety, sodium saccharin was considered to be potentially harmful by inhalation or by contact to skin and eyes. In the current opinion, the applicant restricted the use to suckling and weaned piglets and up to a use level of 5mg/kg complete feed. In relation to the user safety, the additive was neither a skin or eye irritant, nor a dermal sensitiser. In the absence of data, the FEEDAP Panelcould not conclude on the potential of the additive to be toxic by inhalation. Regarding the safety of the additive for the environment, the new conditions of use describe a maximum use level of 5mg sodium saccharin/kg feed. The applicant indicated that a restriction to a lower use level due to environmental safety would be accepted and submitted an environment risk assessment based on a use level of 1.13mg sodium saccharin/kg feed. This use level cannot be considered safe. The estimated use level that would result in a concentration in groundwater below 0.1μg/L is of 0.022mg sodium saccharin/kg feed. The available data do not allow to conclude on the potential effect of the degradation product 4-hydroxysaccharin in ground water.

Different electrochemical techniques for the electrosynthesis of poly methylene blue in sodium saccharin aqueous medium

Different electrochemical techniques for the electrosynthesis of poly methylene blue in sodium saccharin aqueous medium

Elucidation of the powder flow pattern in a twin-screw LIW-feeder for various refill regimes

The importance of residence time distribution modeling is acknowledged as a tool for enabling material tracking and control within a continuous manufacturing line in order to safeguard both product quality and production efficiency. One of the first unit-operations into a continuous direct compression line (i.e. CDC-line) worthwhile doing extensive RTD-analysis upon are the LIW-feeders since they dose the ingredients in a controlled way following the label claim and hence can directly influence critical quality attributes like content uniformity. An NIR measurement method was developed determining the RTD of selected powders at specific feeder settings. Step-change experiments using sodium saccharin as a tracer were conducted. In order to gain and in depth understanding of the material flow, spatial samples throughout the hopper were taken at predefined timepoints during the step change experiments. This revealed the presence of a bypass trajectory along the edges of the agitator, while in the center of the agitator an inner mixing volume in which the tracer concentration lags behind seemed to be present. Finally, a model based on a plug flow and continuous stirred tank reactor was evaluated. The fitted model was not able to capture this complex flow behavior and shows the need for an extended compartmental model distinguishing between a bypass trajectory formed by the agitator and an inner mixing volume.

Design and characterization of fast dissolving buccal film of imipramine HCL

In depressed individuals, Imipramine exerts a positive effect on mood. TCAs are potent inhibitors of serotonin and norepinephrine reuptake. Imipramine hydrochloride having variable bioavailability i.e. ranging from 29-77% due to first pass metabolism, peak plasma concentration is usually attained 2-6 hours. Absorption is unaffected by food. It is freely soluble in water. The objective of this research work is to improve the bioavailability of the drug and fast the onset of action to decrease the depressant activity. The Buccal bioavailability of Imipramine HCL is only 29-77% for this reason drug can be administered into Buccal mucosa using mucoadhesive film. It can be made fast drug release and directly enter into blood circulation through Buccal mucosa and increase the drug bioavailability. Fast dissolving Buccal films were prepared by solvent casting method using various polymers like hydroxyl propyl methyl cellulose E15, PVP, PVA and sodium saccharin, plasticizer and vanillin as flavouring agent. Dissolution profile as studied in USP dissolution apparatus type 1 using pH 6.8 simulated saliva. The influence of variable like polymer type and concentration on Imipramine HCL release profile was studied. The formulation was optimized on the basis of various evaluation parameters like drug content and in vitro drug release. Formulation F3 successfully fast the release of drug within 8 minutes. The IR Spectra revealed the absence of interaction between drug and selected polymer, results of stability studies were as per ICH guide lines and results indicated that the selected formulation was stable.

Formulation and Evaluation of Mouth Dissolving Films of Amlodipine Besylate by using Natural and Synthetic Polymers

The present study was undertaken with an objective of formulating the mouth dissolving films of Amlodipine Besylate to enhance convenience and compliance of the elderly and pediatric patients for better therapeutic efficacy. Various batches of Mouth dissolving Films of Amlodipine besylate were prepared by solvent casting method by using various concentration of gelatin and HPMC E5 with PEG- 400, Sodium starch glycolate, Sodium saccharine, Vanillin and Purified water and evaluated for appearance, weight variation, thickness, folding endurance, drug content, disintegration time and in-vitro drug release. The optimized formulation F4 (1:1 ratio of drug and HPMC E5) exhibited acceptable folding endurance (131±1.00), least disintegration time (26±1.00 seconds), highest drug content (100.01±0.89 %) and highest drug release (99.88±0.12%) in 10 minutes. It can be concluded from the study that the mouth dissolving films of amlodipine besylate, formulation F4 for sublingual administration can be an optimized formulation.