Kollidon SR Research Articles

Investigations on the Impacts of Drugs or Excipients with Different Physicochemical and Compaction Properties on the Disintegration Behavior of Kollidon®SR-Based Binary Controlled Release Matrix Tablets.

The objective of this study was to examine the impact of the physicochemical properties of the loaded drug or excipient, the concentration of Kollidon®SR (KSR), and the mechanical characteristics of KSR compacts on their disintegration times. Using disintegration apparatus, a two-hour constraint was chosen as the process's end point. Lactose-KSR compacts subjected to the highest compression pressure and Microcrystalline cellulose-KSR compacts with KSR concentrations exceeding 30% exhibited disintegration times of less than ten minutes. Likewise, compacts containing Diltiazem HCl-KSR demonstrated brief disintegration times across all tested KSR concentrations and compression pressures. Compacts of Modafinil, Metformin HCl, and Ascorbic acid-KSR displayed disintegration times ranging from fast to moderate, contingent upon the levels of KSR and compression pressure applied. Compacts containing KSR with Aspirin, Salicylic acid, or Ibuprofen did not exhibit significant disintegration even at minimal amounts of KSR (0.5%). Theophylline-KSR tablets also showed prolonged dissolution times, even at very low concentrations of KSR. The disintegration times of Dic-KSR tablets were roughly close to an hour and were predominantly unaffected by varying KSR levels and only marginally influenced by compression pressures. It is possible to draw the conclusion that different drugs or excipients have different minimum KSR requirements to resist compacts' disintegration process. Compounds that demonstrate low solubility in water can result in extended disintegration times for KSR compacts. The melting points of these compounds, in conjunction with the Py values of the compacts and their compaction properties, could affect the disintegration process, although a precise evaluation is necessary.

Impact of Hot-Melt Extrusion on Glibenclamide's Physical and Chemical States and Dissolution Behavior: Case Studies with Three Polymer Blend Matrices.

This research work dives into the complexity of hot-melt extrusion (HME) and its influence on drug stability, focusing on solid dispersions containing 30% of glibenclamide and three 50:50 polymer blends. The polymers used in the study are Ethocel Standard 10 Premium, Kollidon SR and Affinisol HPMC HME 4M. Glibenclamide solid dispersions are characterized using thermal analyses (thermogravimetric analysis (TGA) and differential scanning calorimetry), X-ray diffraction and scanning electron microscopy. This study reveals the transformation of glibenclamide into impurity A during the HME process using mass spectrometry and TGA. Thus, it enables the quantification of the extent of degradation. Furthermore, this work shows how polymer-polymer blend matrices exert an impact on process parameters, the active pharmaceutical ingredient's physical state, and drug release behavior. In vitro dissolution studies show that the polymeric matrices investigated provide extended drug release (over 24 h), mainly dictated by the polymer's chemical nature. This paper highlights how glibenclamide is degraded during HME and how polymer selection crucially affects the sustained release dynamics.

Studying the API Distribution of Controlled Release Formulations Produced via Continuous Twin-Screw Wet Granulation: Influence of Matrix Former, Filler and Process Parameters.

Hydroxypropyl methylcellulose (HPMC) is a preferred hydrophilic matrix former for controlled release formulations produced through continuous twin-screw wet granulation. However, a non-homogeneous API distribution over sieve fractions with underdosing in the fines fraction (<150 µm) was previously reported. This could result in content uniformity issues during downstream processing. Therefore, the current study investigated the root cause of the non-homogeneous theophylline distribution. The effect of process parameters (L/S-ratio and screw configuration) and formulation parameters (matrix former and filler type) on content uniformity was studied. Next, the influence of the formulation parameters on tableting and dissolution behavior was investigated. Altering the L/S-ratio or using a more aggressive screw configuration did not result in a homogeneous API distribution over the granule sieve fractions. Using microcrystalline cellulose (MCC) as filler improved the API distribution due to its similar behavior as HPMC. As excluding HPMC or including a hydrophobic matrix former (Kollidon SR) yielded granules with a homogeneous API distribution, HPMC was identified as the root cause of the non-homogeneous API distribution. This was linked to its fast hydration and swelling (irrespective of the HPMC grade) upon addition of the granulation liquid.

Sketching feasibility of additively manufactured different size gradient conventional hollow capsular shells (HCSs) by selective laser sintering (SLS): From design to applications

Additive manufacturing (AM) is widely used to fabricate 3D printed objects from Computer-aided Design (CAD) prepared using the SolidWorks CAD modelling software. Different printing techniques are used to fabricate desired 3D objects; among all these techniques, it is widely accepted that SLS is one of the most effective methods of 3D printing for fabricating drug-loaded solid oral dosage forms (SODFs) in bulk quantities using the single-step process. Different SODFs, such as pills, miniprintlets, dual miniprintlets, and tablets, were fabricated with different sizes and shapes. In this study, for the first time, we introduce SLS-mediated hollow capsular shells (HCSs) with the help of the SLS 3D printing technique. This work aimed to explore the sinterability and feasibility of sketching HCSs using the SLS-mediated sintering technique with different marketed sizes of capsules ranging from 000 to 5. Here, we have utilized Kolliphor P 188 (KP 188) and Kollidon SR (KSR) in a 1:1 ratio as a matrix-forming agent and 1% charcoal as a laser absorption-enhancing material. In accordance with the CAD models, we have fabricated the gradient conventional different sizes of HCSs ranging from 000 to 5 using the constant printing parameters and composition. Fabricated all biobased HCSs were subjected to the assessment of mechanistic and physicochemical parameters using varied analytical tools. In the current study, tartrazine dye is used to assess the release pattern from HCSs, which resulted in the modified release pattern. The adapted approach will be the futuristic approach to replace animal-based gelatin capsules with pharmaceutical-grade polymer-based HCSs with a modified release with optimum mechanical strength.

Sustained release polymer and surfactant based solid dispersion of andrographolide exhibited improved solubility, dissolution, pharmacokinetics, and pharmacological activity

Andrographolide (AD) is a potent natural product with a wide range of pharmacological activities. However, it has low oral bioavailability due to poor solubility and dissolution rate. Solid dispersion (SD) is a promising technique to improve the solubility and dissolution rate of such molecules. In this study, SD formulation of AD was prepared using Kollidon-SR (KSR) and Poloxamer-407 (P-407) as carriers. SD was prepared using the solvent evaporation method and evaluated for the modulation of solubility of AD. The developed SD formulation was characterized using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and Fourier transform infrared spectroscopy (FTIR). Further, dissolution rate, yield, drug content, stability, flowability, and pharmacokinetic profile of SD were evaluated. The compatibility of SD with the Caco-2 cells and its impact on the P-glycoprotein (P-gp) mediated efflux was also investigated. Furthermore, carrageenan-induced paw edema, and adjuvant-induced arthritic model were used to evaluate the efficacy of SD. The results showed that SD3 (AD + KSR + P-407, 1:6:8) exhibited the highest solubility and dissolution rate, and significantly improved pharmacokinetic profile compared to native AD. SD3 was found to be stable during storage and displayed excellent yield, drug content, and flowability. This formulation was found to be compatible with the Caco-2 cells and retarded the efflux of P-gp substrate. SD3 also demonstrated substantially better efficacy than native AD in terms of paw edema inhibition (carrageenan-induced paw edema, Wistar rats), and overall improvement of disease condition (in terms of paw edema, arthritic score, AST, ALT, cytokines, radiological changes, and histopathology) in arthritic Wistar rats. In conclusion, SD3 exhibited improved solubility, dissolution rate, pharmacokinetic profile, and pharmacological activity than native AD.

Formulation and Characterization Studies of Paclitaxel Incorporated Kollidon® SR and Chitosan Nanoparticles: An In vitro Evaluation for Potential Use for Colorectal Cancer Treatment

Background: Chemotherapy is regarded as first-line therapy in various cancer types besides surgical procedures. However, lack of cell selectivity and poor drug targeting to the cancer zone of the active agents results in accumulation in normal tissues with considerably high severe side effects. Therefore, novel drug delivery systems are required to enhance cancer treatment. Objective: In this study, Paclitaxel (PTX) incorporated Kollidon® SR (KSR) and Chitosan (CS) based polymeric nanoparticles were prepared for potential use for colorectal cancer treatment. Methods: Polymeric nanoparticles were prepared by spray dying method. Physicochemical characterization studies were performed with particle size (PS), polydispersity index (PDI), zeta potential (ZP), drug loading (DL %), encapsulation efficiency (EE %) and structural evaluations using differential scanning calorimetry (DSC), X-ray diffractometry (XRD), Fourier transform infrared spectroscopy (FT-IR) and proton nuclear magnetic resonance (1H-NMR) analyses. Cytotoxicity of the nanoparticles was screened on HT-29 (human colorectal adenocarcinoma) and HTC-15 (Dukes' type C, colorectal adenocarcinoma) cell lines with MTT assay. Results: Analysis revealed the successful incorporation of PTX into the polymeric lattices. Particles showed cytotoxic activity on HT-29 and HTC-15 cell lines, depending on the application dose after 48 hours. Nanoparticles also remained stable at 5°C ± 3°C and 25°C ± 2°C (60% ± 5 Relative Humidity (RH)) during the storage period of 6 months. Conclusion: As a result of the study, KSR and CS-based nanoparticles could be regarded as promising nano-carriers for improved therapeutic efficacy of PTX for colorectal cancer treatment.

Investigations on Compaction Behavior of Kollidon®SR-Based Multi-component Directly Compressed Tablets for Preparation of Controlled Release Diclofenac Sodium.

The physics of tablets mixtures has gained much attention lately. The purpose of this work is to evaluate the compaction properties of Kollidon® SR (KSR) in the presence of different excipients such as Microcrystalline cellulose (MCC), Monohydrous lactose (MH Lactose), Poly (vinyl acetate) (PVA100), and a water-soluble drug Diclofenac sodium (DNa) to prepare once daily formulation. Tablets were prepared using direct compression and were compressed into flat-faced tablets using hydraulic press at various pressures. The combination of MCC and KSR in the tablets showed reduced porosity, and almost constant low Py values as KSR levels increased; also, KSR-DNa tablets had higher percentage porosity and crushing strength values than KSR-MH Lactose tablets. The crushing strengths of KSR-MCC tablets were larger than those of KSR-DNa tablets. Ternary mixture tablets comprised of KSR-MCC-DNa showed decreased porosities and low Py values as the percentage of KSR increased especially at high compression pressures but had higher crushing strengths compared to KSR-DNa or MCC-DNa binary tablets. KSR-MH Lactose-DNa ternary tablets experienced lower porosities and crushing strengths compared to KSR-MCC-DNa tablets. Quaternary tablets of KSR-PVA100-MCC-DNa showed lower porosity and Py values than quaternary tablets obtained using similar proportion of MH Lactose instead of MCC. In conclusion, optimum quaternary tablets were obtained with optimum crushing strengths, relatively low Py, and moderate percentage porosities among all prepared quaternary tablets. The drug release of the optimum quaternary tablets demonstrated similar in vitro release profile compared to that of the marketed product with a mechanism of release that follows Korsmeyer-Peppas model.

Formulation, Development and Investigation of Matrix Type Sustained Release Tablet of Antiulcer Drug by Using Soluble Polymer as a Drug Release Retarding Agent

The main goals of sustained release drug delivery are to modify the medication's biopharmaceutical, pharmacokinetic, and pharmacodynamic properties in order to lessen adverse effects, increase patient compliance, and treat the illness. The current work set out to create sustained release tablets of nizatidine (220 mg) using a wet granulation process and different concentrations of polymers such as chitosan, Kollidon SR, and HPMC K100M. Pre-formulation characteristics were examined, including medication DSC analysis and FTIR research. We assessed a number of post-compression characteristics, including content homogeneity, thickness, hardness, friability, and weight uniformity. This study demonstrated how the post-compression characteristics of the drug formulation are influenced by the concentration of polymers.

Effect of Laser Power Ratios on Sinterability and Physical Properties of 3D Prototypes Sintered Using Selective Laser Sintering

Aim: This study was intended to investigate the effect of laser power ratios (LPRs) on the sinterability and sintering performance of selective laser sintering (SLS) mediated 3D prototypes. Materials &amp; methods: Physical mixtures (PMs) containing Kollidon SR (98.75% w/w) and IR-absorbing dye (1.25% w/w) were evaluated for flow characteristics and particle size. The same PMs were subjected to SLS-mediated prototyping at constant printing temperatures (feed bed temperature 30°C and print bed temperature 40°C) over a range of LPRs. Results &amp; conclusion: With favoured particle size and flow properties, this PMs was found to be suitable for SLS-mediated 3D printing. Sinterability and sintering performance were improved incrementally throughout the range of studied LPRs. The best sintering performance in terms of dimensional accuracy and printing yield was achieved at the highest LPR (3.0). Scanning electron microscopy (SEM) depicted topography of cross-sectioned sintered printlets.

Fabrication and Characterization of Electros Punned Eprosartan Loaded Biocompatible Polyvinyl Acetate/Povidone Based Nanofiber Mat: A Novel Approach as Transdermal Carrier for Therapeutic Actives

Introduction: Nanofiber (NF) represents one of the newest, promising and advanced technologies in transdermal and or mucosal drug delivery due to its unique advantages. The present study aims to explore the feasibility of Kollidon® SR (K-SR) to fabricate sustained release Eprosartan (EPR) loaded nanofiber (NF) by using electrospinning technology for transdermal drug delivery. The EPR-NF mat was prepared with sodium iodide (SI) along the backing membrane and compared with film cast mat. The fabricated NF mechanical and physicochemical properties were assessed. Further, NF evaluated for in-vitro and ex-vivo diffusion study, skin irritation study and for antihypertensive activity.

Enhancing the dissolution rate of poorly soluble drug Febuxostat using spray dried amorphous solid dispersion technique

Introduction: Febuxostat belongs to Biopharmaceutical classification system (BCS) class II drugs, which have low solubility and high permeability. Amorphous solid dispersion is one of the techniques which can be useful to improve solubility and powder characteristics.&#x0D; Objective: To optimize the concentration of hydrophilic and hydrophobic polymers to improve the dissolution rate and solubility of febuxostat tablets.&#x0D; Methods: The amorphous solid dispersion of febuxostat was prepared by spray drying method using Kolliphor P237 (1:2). This amorphous solid dispersion was further used to compress the tablet. To improve solubility and dissolution rate, a full factorial design was applied to optimize the critical concentration of Kollidon SR and hydroxypropyl methyl cellulose (HPMC K4M). The prepared tablets were characterized by pre-compression and post-compression parameters.&#x0D; Result: The rate of drug release was sustained by formulating an amorphous solid dispersion technique. The optimized batch (FSRT-OB) was found to be fit for release average 93.30 % of the drug in sustain release manner up to 12hrs. The release kinetic data suggests that the drug release was controlled by combination of diffusion and chain relaxation mechanism. The optimized concentration for Kollidon SR and HPMC K4Mwas found to be 38.50 % and 7.72 % respectively.&#x0D; Conclusion: Amorphous solid dispersion technique is useful to enhance solubility, dissolution rate, and bioavailability of the Febuxostat tablet.

Monitoring the weight and dimensional expansion of pyridostigmine bromide tablets under dynamic vapor sorption and impact of deliquescence on tablet strength and drug release

Changes of weight and axial expansion of tablets of the deliquescent drug pyridostigmine bromide with Kollidon SR were followed with relative humidity (RH) using dynamic vapor sorption and displacement transducer. The effects of RH on placebo and drug containing (API) tablets prepared at low and high compression were related to tablet strength and molecular changes. Tablet weight and expansion increased with RH, especially above RH 40%. Tablet rigidity and strength decreased linearly with moisture for placebo tablets whereas for API tablets there was decrease up to 50% followed by large drop at 60%. Raman spectra of tablets did not show chemical interactions due to moisture, but decreased intensity of drug peak at 2370 cm−1 indicating solid state changes. Decrease of polymer peak intensities at 805 and 1740 cm−1 occurred only in API tablets implicating drug deliquescence in polymer moisture sorption. X-ray diffraction and thermal analysis of tablets indicated complete drug liquefaction after exposure at 60% RH, which impacted great loss of strength but did not affect the sustained release profile. In conclusion, monitoring of the physical properties of tablets during production of deliquescent drugs is necessary to avoid pitfalls during downstream processes such as coating, packaging and storage.

ENHANCEMENT OF THERAPEUTIC WINDOW OF METFORMIN HYDROCHLORIDE BY FABRICATION OF MICROSPHERES COMPRISING POLYMERIC INCULCATION WITH SEMI-SYNTHETIC AND SYNTHETIC POLYMERS BY IMPLEMENTATION OF BOX-BEHNKEN DESIGN

Objective: Innovative enhancement of therapeutic window of Metformin hydrochloride (MFH) and bioavailability through mucoadhesive microspheres by polymeric inculcation of hydroxypropyl methylcellulose K4M grade (HPMC K4M), hydroxypropyl methylcellulose K100M grade (HPMC K100M) and Kollidon SR grade (KS).&#x0D; Methods: Controlled release system was developed by incorporating semi-synthetic and synthetic polymers by modified solvent evaporation technique. Fabrication of mucoadhesive microspheres was designed by the implementation of experimental designs to obtain most optimum concentration of selected factors. The method was optimized by Box Behnken design (BBD) with selected factors as concentrations of semi-synthetic and synthetic polymer with stirring speed influence for the obtained responses that were mean particle size (Y1) entrapment efficiency of drug (Y2) and percent mucoadhesion (Y3). Microspheres were characterized for particle size, entrapment efficiency of drug, ex-vivo mucoadhesion study, in vitro study, Fourier transform infrared spectroscopy (FTIR), x-ray diffraction (XRD) detection and H1 Nuclear magnetic resonance (NMR) quantification for optimized formulation.&#x0D; Results: Implementation of response surface method software for BBD yielded stable microspheres with mean particle size 274 µm, entrapment efficiency of drug 85.07% and percent mucoadhesion 67.03% for optimized formulation F5.&#x0D; Conclusion: Bridging of MFH with the highly innovative combination of semi-synthetic and synthetic polymers yielded stable, cost-effective microspheres with improved bioavailability with controlled-release effect as till date no literature is available that provide information with selected polymeric combination and analytical characterization.

FORMULATION DEVELOPMENT AND EVALUATION OF HIGHLY WATER-SOLUBLE DRUG-LOADED CONTROLLED RELEASE MATRIX TABLETS

Formulation of controlled release matrix tablets of Itopride hydrochloride (ITP) was done using direct compression method. Different polymers were used to evaluate the influence of different types (HPM, EC, Kollidon® SR), concentration (20-40%) and viscosity grade (HPMC-4000 cps, HPMC-100000 cps, EC-10 cps and Kollidon SR) on drug release. Twelve different tablet formulations were designed with constant amount of ITP in each tablet formulation (150 mg). The dissolution studies of CR matrix formulations were carried out in acidic buffer (pH 1.2) and phosphate buffer (pH 6.8). Drug release kinetics was studied for first order, Zero-order, Higuchi, Korsmeyer-Peppas and Weibull models using DD Solver (an add-in software for MS Excel). Formulation ECF7, ECF8 and ECF9 containing EC (20-40%) greatly controlled the release rate of drug over an extended period of 12 hr. However, drug release from tablets formulations K4F3, K100F5 and ECF8, followed zero-order kinetics with regression coefficient of 0.966-0.999. The release mechanism of tablets formulations K4F2, KK4F3, K4F4, ECF7, KSRF10, KSRF11 and KSRF12 were non-fickian diffusion, whereas the release mechanism from formulations K4F1, K100F5, K100F6, ECF8 and ECF9 were super case-II transport mechanism. It was concluded that HPMC and ethylcellulose (EC-10cps) in the percentage range of 20-30% were excellent release controlling polymers for itopride HCl.

INFLUENCE OF CELLULOSE AND ACETATE-BASED POLYMERS ON THE RELEASE OF CIPROFLOXACIN HCL FROM EXTENDED RELEASE MATRIX TABLETS PREPARED BY DIRECT COMPRESSION TECHNIQUE

The objectives of the current study were to investigate the influence of different types and concentration of polymers on release of ciprofloxacin HCl as well as to formulate an extended release tablets of ciprofloxacin hydrochloride by direct compression method. Twelve formulations (F1–F12) were manually designed using different proportions (10–30%) of Hydroxypropyl methylcellulose (HPMC), Ethylcellulose (EC) and Kollidon SR polymers. Avicel PH101, talc and magnesium stearate were used in a constant quantity of 2% in all the formulations. Multiple point dissolution was carried out in different media. Dissolution profiles indicated that formulations F1, F4, F8 and F11, extended the drug release up to 12 hrs, while, other formulations failed to retard the drug release up to desired period. DDSolver software was used to analyze the dissolution profile data for drug release kinetics such as first order, Zero-order, Korsmeyer–Peppas and Higuchi models. Drug polymers compatibility was assessed using Fourier Transformed Infrared (FTIR) spectroscopy. Selected formulations were placed in the stability chamber at accelerated temperature (40±2°C and RH 75±5%) for six months and re-evaluated after 3 and 6 months as per ICH guidelines. The present study accomplished that ethylcellulose alone or in combination with HPMC was found to be an excellent rate controlling agent for ciprofloxacin and may be used successfully to develop extended release tablet formulations.

Influence of screw configuration and processing parameters on the dissolution of ketoprofen in polymer blends

AbstractThe solubility and dissolution enhancement of the poorly soluble drug ketoprofen (KTO) in polymer blends prepared by hot melt extrusion was studied using two different screw configurations while changing extrusion processing conditions. A number of different Soluplus and Kollidon SR blends were used as solid dispersion excipients. A design of experiments with three melt temperatures, three screw rotation speeds, and three fill factors was performed, and a phase‐gate methodology was implemented. Different characterization techniques such as differential scanning calorimetry, optical and polarized light microscopy, X‐ray diffraction, solid‐state nuclear magnetic resonance, and dissolution testing were used. The results from differential scanning calorimetry and X‐ray diffraction showed an amorphous solid solution. The characterization by solid‐state nuclear magnetic resonance indicated that KTO could interact with the polymer blend by hydrogen bonds and Van der Waals forces. An optimal processing window was found for each screw configuration achieving more than 80% drug release in 8 hr.

INFLUENCE OF CELLULOSE AND ACETATE-BASED POLYMERS ON THE RELEASE OF CIPROFLOXACIN HCL FROM EXTENDED RELEASE MATRIX TABLETS PREPARED BY DIRECT COMPRESSION TECHNIQUE

The objectives of the current study were to investigate the influence of different types and concentration of polymers on release of ciprofloxacin HCl as well as to formulate an extended release tablets of ciprofloxacin hydrochloride by direct compression method. Twelve formulations (F1–F12) were manually designed using different proportions (10–30%) of Hydroxypropyl methylcellulose (HPMC), Ethylcellulose (EC) and Kollidon SR polymers. Avicel PH101, talc and magnesium stearate were used in a constant quantity of 2% in all the formulations. Multiple point dissolution was carried out in different media. Dissolution profiles indicated that formulations F1, F4, F8 and F11, extended the drug release up to 12 hrs, while, other formulations failed to retard the drug release up to desired period. DDSolver software was used to analyze the dissolution profile data for drug release kinetics such as first order, Zero-order, Korsmeyer–Peppas and Higuchi models. Drug polymers compatibility was assessed using Fourier Transformed Infrared (FTIR) spectroscopy. Selected formulations were placed in the stability chamber at accelerated temperature (40±2°C and RH 75±5%) for six months and re-evaluated after 3 and 6 months as per ICH guidelines. The present study accomplished that ethylcellulose alone or in combination with HPMC was found to be an excellent rate controlling agent for ciprofloxacin and may be used successfully to develop extended release tablet formulations.

Formulation and Evaluation of Oral Controlled Release Matrix Tablets of Propranolol Hydrochloride

The aim of the present study was to develop Propranolol Hydrochloride Oral Controlled release tablets to maintain constant therapeutic levels of the drug for over 12 hrs. Locust bean gum, Kollidon SR, Karaya gum were used as polymers. All the formulations were passed various physicochemical evaluation parameters such as Bulk Density, Tapped Density, Carr's Index, Hausner's Ratio, Angle of Repose, Weight Variation, Hardness, Thickness, Friability and Drug Content. From the dissolution studies it was evident that the formulation F7 showed better and desired drug release pattern i.e., 98.56% in 12 hours. It contains the Karaya gum as polymer. It followed Zero order release kinetics mechanism.

Design and In-vitro evaluation of gastro retentive drug delivery systems of metoprolol succinate

Gastro retentive drug delivery is a special approach that remains in the stomach for a prolonged period which helps to increase gastric residence time along with site specific drug delivery especially in the upper gastrointestinal tract (GIT) for local or systemic effects. Metoprolol succinate is a beta1-selective adrenergic receptor antagonist used to treat hypertension, angina and arrhythmia. It has a t1/2 of 3-7hrs and is mainly absorbed from the upper parts of GIT with good stability in the acidic environment. The main objective of the present study was to design a floating formulation having Metoprolol succinate as a model drug by using the polymers like HPMC K100M, HPMC K15M, HPMC K4M, Kollidon SR to increase the bioavailability of drug and reduce the dosing frequency. FTIR studies proved that there was no incompatability in the optimized formulations. All the formulations remained buoyant without any disintegration. The formulations F4, F8, F12 and F15 showed similar drug release to that of marketed formulation for a period of 12 hours. To ascertain the mechanism of drug release, in-vitro data was fitted into various release kinetic models like zero order, first order, Higuchi and Peppas. The values indicated, the non fickian diffusion with slow erosion of polymer matrix followed by drug diffusion and resulted in linear drug release profile over a prolonged period of time.

Characterization of Eudragit types and Kollidon SR inter-polymer complexes and their effects on the drug release

A novel of polymer combination promotes an increase of the ability for controlling the drug release. The objective of this research was to characterize the inter-polymer complexes (IPCs) of Eudragit (Eud) types (Eud RS, Eud L, or Eud E) and Kollidon SR (KSR), and elucidate their effects on the drug release kinetics and mechanism. Different preparation techniques were proposed using spray drying and ultrasonic-assisted anti-solvent techniques. The thermal activity e.g. glass transition temperature (Tg), and fourier transform infrared spectroscopy were used to characterize the molecular interaction of these IPCs. The effect on the drug release kinetics and mechanism was the main concern of this study. Depending on the results, the hydrogen bonding formation between polymers was observed by a shifting of OH and carbonyl group vibrations. In addition, the van der Waals interaction was identified by an alteration in the vibrational band around the 1000-1500 cm-1. Meanwhile, the change of physicochemical characteristic was identified by the Tg of IPCs. Eud E-KSR and Eud E-Eud L IPC was unable to control the drug release. Meanwhile, Eud L-KSR IPC and Eud RS-KSR IPC were success to control the drug release, but it was pH dependent and independent, respectively. This study concluded that the IPCs allowed the drug release in a controlled manner based on the IPC characteristics and their interactions. Either positive or negative interactions on the drug release were observed due to native characteristics of polymers.