Core Tablets Research Articles

Problems of Applying Film Coatings During Scale-up Technology

Introduction. Technology transfer is an integral part of the life cycle of any drug. The coating is a critical step in the production of coated tablets. The transfer of the film coating application process is often accompanied by the rejection of a part of the drug series due to various defects in the target surface.Aim. To classify the types of defects formed at the stage of “Application of the film shell” in the devices of the “Coater” drum type, to identify the causes of occurrence, to develop ways to eliminate these defects.Materials and methods. Film-coated tablets with INN diosmin, sildenafil, dipyridamole, atorvastatin, rosuvastatin as the object of the study were selected. The samples were obtained on a single-punch tablet press EP-1 (ERWEKA GmbH, Germany) and coated with a film shell in a coating unit of the type "copper" BGB-1 (Chongqing Jinggong Pharmaceutical Machinery Co., Ltd., China).Results and discussion. Appearance defects are classified according to the degree of criticality: critical (influx, chipping, recess, rupture, delamination, breaking, rubbing, sticking, pigmentation, discoloration, scratches, crack), significant (build-up, inclusion), minor defect. The main causes of the defect have been established: the property of the core tablet (for example, poor adhesive properties, hydrophobicity), technological parameters of the process (the speed of rotation of the drum, the speed of spraying, the pressure on the spray, the pressure on the formation of the torch, the temperature of the incoming air. The main consequences of the occurrence of each type of defect are considered, among which are insignificant (not affecting the quality) and critical (affecting the quality indicators of "dissolution").Conclusion. In the course of the study, the types of critical and significant defects, the causes of occurrence and ways to eliminate these defects are considered.

Studying the dissolution of immediate release film coating using terahertz pulsed imaging

Coated tablets introduce complexity to the dissolution process, even with readily soluble immediate release coating layers. Therefore, a more detailed understanding of the physical steps involved in the dissolution process can improve the efficiency of formulation and process design. The current study uses terahertz pulsed imaging to visualise the hydration process of microcrystalline cellulose (MCC) tablet cores that were film coated with an immediate release coating formulation upon exposure to the dissolution medium. Film coated tablets that were prepared from three levels of core porosity (10%, 20% and 30%) and with coating thickness in the range of 30μm to 250μm were investigated. It was possible to resolve and quantify the distinct stages of wetting of the coating layer, swelling of the MCC particles at the core surface, and dissolution of the coating layer followed by the ingress of dissolution media into the tablet core. The liquid transport process through the coating layer was highly consistent and scalable. The penetration rate through the coating layer and the tablet core both strongly depended on coating thickness and core porosity.

THE ANTI-INFLAMMATORY TABLET FORMULATION OF COLEUS (PLECTRANTHUS SCUTELLARIODES) LEAVES EXTRACT USING KOLLICOAT®PROTECT COATING

Objective: The purpose of this study was to find the concentration of weight gain on the use of Kollicoat®Protect to produce coleus leaf extract film-coated tablets with good physical properties.
 Methods: Coleus extract was obtained by maceration using 70% ethanol. Tablet cores were prepared using the wet granulation method, then evaluated (uniformity of weight, size, hardness, friability, and disintegration time). Coated tablets were made in four variations of polymer weight gain, i.e. 5, 6, 7, and 8%. To determine the effect of the weight gain concentration of Kollicoat®Protect an evaluation of the coated tablets was carried out, i.e. the uniformity of weight, size, hardness, disintegration time, and physical appearance of the film-coated tablets.
 Results: The four variations (Film Coated Tablet, FCT 5, 6, 7, and 8%) in weight gain of film-coated tablets showed the physical appearance results per the applicable requirements. However, the physical observation test at room temperature showed the instability of the film-coated tablet. The qualitative analysis of thin-layer chromatography showed that the productive substances in the extracts, tablet cores, and film-coated tablets were still contained even though they had undergone several formulation stages.
 Conclusion: Film-coated tablets met the standards of the Indonesian Pharmacopoeia and the United States Pharmacopeia. After two weeks, there was slight instability in film-coated tablets at room temperature storage. The extract, tablet core, and film-coated tablet contain flavonoids.

Formulation and Optimization of 5-Amino Salicylic acid Tablet for Colon Targeting

Objective: The objective of present work was to prepare colon-specific delivery systems for 5-aminosalicylic acid (5-ASA) using fenugreek gum and chitosan as a carrier target to the colon. Methods: Core tablets containing 5-ASA were prepared by wet granulation with using polyvinyl pyrolidone (PVP) as a binder and sodium starch glycolate as a super disintegrant. The prepared granules were evaluated for the angle of repose, compressibility index and Hausner’s ratio. The prepared tablets were evaluated the hardness, friability, weight variation and disintegration studies. The core tablets were coated with the concentration of 2%, 5%, and 7% in the ratio of 50:50, 40:60, 60:40, 70:30 and 30:70 of fenugreek gum and chitosan. The enteric coated tablets were characterized for the in vitro disintegration, and dissolution. The drug polymer compatibility studies were determined by using FT-IR study and found out no interaction between the drug and polymers. Results: The formation of complexes between fenugreek gum and chitosan prevents the drug release in the stomach. The tablets coated with 7% concentration solutions in the ratio 70:30 (Fenugreek gum: Chitosan) shows better swelling property and 89.99% drug releases in the colon. FT-IR, DSC studies showed the absence of interaction between 5-ASA and the excipients on storage accelerated condition at 40°C±2°C, 75%±5% RH for 12 weeks. Conclusion: Thus, it can be concluded that developed fenugreek gum and chitosan coated 5-ASA tablets can be considered as a promising system for targeted delivery to colon for local action.

Design, Development and In vivo Evaluation of Core in Cup Tablets of Budesonide

Budesonide is widely used drug for treatment of active inflammatory bowel disease (IBD). Core in-cup tablets were prepared to achieve a prolonged release of Budesonide and for alleviating the symptoms of inflammatory bowel disease. The objective of this study was to investigate differences in the pharmacokinetic patterns between an optimized core in cup tablet formulation and pure Budesonide suspension. In-vivo evaluation studies were performed based on the uniform and reliable results of in-vitro drug release studies. Various pharmacokinetic parameters were compared to obtain mean plasma drug concentration curve versus time. The pure drug suspension and Core-in-cup tablets formulation of Budesonide were administered to two groups of white New Zealand rabbits (n=6) through the oral route following cross over design pattern. The drug concentration in plasma samples were measured using LC-MS/MS method. Pharmacokinetic parameters were determined for each formulation. The comparison of the plasma time curves of the dosage forms showed that each dosage form caused significant differences in the drug plasma levels. The optimized core in cup tablet formulation shown some lag phase initially before releasing the drug. The mean residence time of core in cup tablet formulation was found to be more than the pure drug suspension formulation. The oral administration of Budesonide resulted in a low and quite variable AUC of 154.1±1.44 ng/ml/hr., whereas the optimized core-in-cup tablets resulted in AUC of 918.2±3.11 ng/ml/hr. The bioavailability of optimized formulation was enhanced six times compared with pure drug suspension. From the above results, it can be concluded that the prepared core in cup tablet can be considered as one of the promising formulation techniques for chronotherapeutic management of inflammatory bowel disease.

Modeling of inter-tablet coating uniformity of electrostatic dry powder coating by discrete element method

The current study aims to apply an innovative mathematical model based on the discrete element method to numerically simulate the electrostatic dry powder coating process and to predict the inter-tablet coating uniformity. The newly developed mathematical model could efficiently handle millions of coating particles and precisely obtain the coating weight gain of individual tablet core online, which was highly consistent with the experimental results. And the newly developed model was applied to fully investigate the influence factors of the inter-tablet coating uniformity of electrostatic powder coating, including coating particle radius, charge intensity of the coating particles, the rotating speed of the pan coater and the feeding time of the coating powders, all of which could be optimized to largely improve the coating uniformity. The study demonstrates that this newly developed model is promising in precisely simulating the electrostatic dry powder coating process for sufficient coating uniformity. • A novel DEM-based mathematical model for electrostatic dry powder coating; • Validation of the newly developed model with optimized simulation settings; • Precise prediction of the inter-tablet coating uniformity by modulating the coating parameters.

Effect of Coating Thickness and Polyethylene Glycol’s Molecular Weight on Diltiazem Hydrochloride Release from Controlled Porosity Osmotic Pump Tablets

The purpose of this research was to design CPOP tablets to achieve controlled delivery of diltiazem hydrochloride (DH) up to 12 hours, which is a water-soluble calcium channel blocker with a short biological half-life. Two batches of osmotic tablet cores were prepared, containing DH with mannitol as an osmotic agent (1: 1.5 ratio). The tablet cores formulation with 10 mm diameter achieved the required technical and mechanical specifications. Direct compression technique was used to prepare the tablet cores which were evaluated in terms of mechanical resistance and uniformity of dosage units, followed by spray film coating using cellulose acetate as a former polymer of the semipermeable membrane and polyethylene glycol (PEG) as a pore forming agent. Several molecular weights of PEG (6000, 1500 and 400) were used and coating thickness levels were obtained. In vitro drug release, morphology of coating surface and the effect of pH change on release rate were investigated. Most of the prepared formulations demonstrated a burst release at the initial stage, which could be controlled by increasing the coating thickness. Formulations with PEG400 as a pore former presented better controlled and less burst release than those containing PEG6000, PEG1500, or a mixture of PEG6000: PEG400 (1: 1), and the pH change did not affect the drug release except in the initial stage.

Formulation development and Evaluation of Colon Specific Delivery System of Anti- amoebic Drug (Tinidazole) using different Polysaccharide carriers

Amoebiasis is an infection of the large intestine caused by Entamoeba histolytica. Tinidazole is the preferred drug used in the treatment of intestinal amoebiasis. The conventional tablet dosage form provides minimal amount of drug in the colon with undesirable adverse effect due to variation in the transit time. Hence, to target the drug directly to the site of action in the colon, there is need to develop colon targeted drug delivery systems that will enhance the therapeutic drug level, increases the bioavailability of active medicament and reduce the dose of drug. The fast disintegrating core tablet of Tinidazole was prepared by direct compression method. The core tablet was evaluated for hardness, thickness, Friability, weight variation, drug content, in vitro disintegration time and in vitro drug release studies. Using the optimized formulation (C3), different formulations (F1-F6) of coated tablet was prepared by using different polymers like chitosan and xanthan gum. The formulated coated tablet were evaluated for various parameters like for hardness, thickness, Friability, weight variation, drug content, swelling study and in vitro dissolution study. The optimized formulation F3 shows 6.24% drug release in Stomach and Small Intestine and maximum drug release up to 96.53% in the colon. The kinetic data analysis of formulations indicated that it fits to Korsmeyer -Peppas Model and follows zero order release kinetics. The mechanism of drug release from the tablet followed non-Fickian (super case-11) transport. The stability studies of the optimized formulation were investigated as per ICH guidelines. There were no significant changes in thickness, hardness, weight variation, friability, drug content and in vitro drug release. These findings suggest that compression coated tablet using polysaccharide carriers provide more site specific delivery, reduced degradation and release of drug in stomach and small intestine.

Formulation and Evaluation of Time-Controlled Pulsatile Release Rosuvastatin Press-Coated Tablets

Rosuvastatin belongs to the HMG-CoA reductase inhibitor class of drugs (statins). The main aim of the present study was to formulate and evaluate time-controlled pulsatile release Rosuvastatin press-coated tablets. The core tablets were formulated by the Direct compression method. Coated tablets were formulated by the Press-coating technique. The drug delivery system was designed to deliver the drug at a specific time for the patient suffering from Hyperlipidemia. The core tablets containing Rosuvastatin, anhydrous lactose, and different ratios of super disintegrants like croscarmellose sodium, and sodium starch glycolate, among six core tablets were formulated, and they were evaluated for post-compression parameters like Weight variation, Thickness, Hardness, Friability, Disintegration, and In-vitro drug release profile, then the core was optimized by using different ratios of polymers such as Eudragit-S100, Eudragit-L100, and HPMC K4M, Ethyl Cellulose (1:2, 2:1 ratios). Totally four coating compositions were fixed and coated to core tablets by press-coating method, then they were evaluated for post-compression parameters like Weight variation, Hardness, Thickness, and In-vitro drug release studies were performed in 0.1 N HCl for 2 hrs, pH 6.8 phosphate buffer for 6 hrs and pH 7.4 phosphate buffer from the dissolution data the coat containing Eudragit-S100, Eudragit-L100 (2:1) combination shown best profile for pulsatile release of Rosuvastatin. The 10 hrs of lag time for the drug release and the drug release were depending on the effects of the composition of the polymers used.

Press coated Bioadhesive Pulsatile Tablet of Lisinopril for Chronotherapy of Cardiac Disorders: in-vitro Evaluation

The purpose of present investigation was to formulate bioadhesive pulsatile release tablet (BPRT) of lisinopril drug belong to antihypertensive category for chronotherapy of cardiac disorder. The concept behind this dosage form development is to investigate effect of coating polymer concentration on lag time and drug release from directly compressed tablet. The core tablets prepared by using various concentrations of disintegrants found suitable for complete release of drug in acidic medium indicating its solubility in gastric fluid. The FT-IR studies indicate that selected polymers are compatible with lisinopril since no interaction found in drug-excipient compatibility studies. The dissolution study clearly indicates that higher concentration of polymers which is HPMC K100M and Carbopol reduces free water volume and increase viscosity of the tablet coat causes reduction in drug release. The prepared Bioadhesive pulsatile release tablets showed desired hardness and good mucoadhesion strength. The obtained results showed capability of formulated bioadhesive pulsatile drug delivery system in a drug release for a programmable period of time to attain drug release after minimum 3 hr of Lag time. A stability results clearly indicate that developed pulsatile product was sufficiently stable under accelerated and controlled conditions. Thus, the developed pulsatile tablet can be considered to be a promising formulation for the relief of early morning surge in blood pressure and other cardiac disorders which follows a circadian rhythm.

Compression Coating Technique and its Formulation in Circadian Rhythm Activity with Chronotherapeutic Drug Delivery System

Background: Circadian rhythms is a natural process that regulates the sleep wake cycle which is associated with several physiological, biochemical, endocrine, behavioural processes in humans and entrainment to light-dark cycle. The activity of Ramelteon is believed to contribute to its sleep-promoting properties and thought to be involved in the maintenance of the circadian rhythm underlying the normal sleep-wake cycle. A tablet can be given before 2 hr of bed time, so the Ramelteon drug shows its effect throughout the night by releasing the active content with lag time followed by sustained action to promote the sleep. Materials and Methods: Chronotherapeutic drug delivery system were prepared by compression coating technology using pH independent, hydrophilic and hydrophobic polymers. Results: Drug excipient compatibility indicated that the Ramelteon Active pharmaceutical ingredient (API) is compatibility with the excipients proposed. The X-ray Diffraction (XRD) studies indicated that the crystalline form of the Ramelteon API existed in the finished formulation. Conclusion: The core tablets containing Eudragit RSPO 10mg/tablet and ratio of Ethyl cellulose: Hydroxy propyl methyl cellulose (HPMC) of 70:30 in the outer coating material yielded a desired lag time of 2 hr and drug release for a period of 4 hr to achieve a chronotherapeutic drug delivery system. Ramelteon is an excellent candidate in designing chronotherapeutic drug delivery systems and further in vivo studies can be explored in the treatment of circadian rhythm with sleep wake cycle disorders.

Compression-coated pulsatile chronomodulated therapeutic system: QbD assisted optimization

Pulsatile drug delivery systems have drawn attention in contemporary research for designing chronotherapeutic systems. The current work aims to design pulsatile ketorolac tromethamine tablets using compression coating for delayed delivery with a lag time suitable for the treatment of morning stiffness in arthritis. Rapidly disintegrating core tablets of ketorolac tromethamine were formulated using super-disintegrants, and the optimized formulation was compression using PEO WSR coagulant and Eudragit RLPO for delaying the release. The central composite design and response surface methodology were employed to optimize the formulation and process parameters namely PEO WSR Coagulant (X1), Eudragit RLPO (X2), and Hardness (X3). The dependent variables optimized were lag time and time required for 95% drug release. Analysis using response surface graphs and mathematical modeling of the results allowed identifying and quantifying the formulation variables active on the selected responses. A polynomial equation fitted to the data was used to predict the composition with optimum responses. Compression-coated pulsatile tablets’ optimized composition exhibited a lag time of 9 h and released 95% of the ketorolac tromethamine in 17.42 h. Validation of the mathematical model assured the reliability of QBD in formulation design. In vivo X-ray imaging and pharmacokinetic studies established a strong relationship between the coated polymers maintaining the desired lag time for delayed delivery of the active to coincide with the chronobiology for enhanced bioavailability at the right time when needed.

RELEASE MODULATED DELIVERY OF DIGESTIVE ENZYME SUPPLEMENT

A combination of proteolytic enzyme pepsin with amylolytic α- amylase serves as an ideal digestive enzyme supplement for the treatment of functional dyspepsia and exocrine pancreatic insufficiency. In the present research work, an attempt was made to develop a release modulated formulation which ensures the enteric delivery of acid liable α- amylase and stomach-specific delivery of pepsin using inlay tablet technology. Eight formulations of inner core layer containing α- amylase (fungal diastase) i.e., F1 to F8, were developed using varying ratios of microcrystalline cellulose and mannitol. The best suit formulation of inner core tablet was chosen and subjected to enteric coating using coating solutions C1 to C6 and evaluated for intactness of enteric coat. The formulations containing pepsin for immediate release outer coat i.e., P1 to P4, were formulated using mannitol, dicalcium phosphate, lactose and calcium carbonate, respectively, and evaluated for pharmaceutical parameters. The inlay tablet was formulated by coating best fit outer coat formulation on enteric coated inner core tablet using compression coating technique. The results of in vitro evaluation studies for formulated inlay tablet revealed that the prepared formulation releases pepsin in stomach, immediately followed by the release of α- amylase in alkaline environment of intestine.

Chronomodulated Mucoadhesive Gastroretentive Drug Delivery System of Famotidine

In the present study, the main objective was to develop and evaluate a novel floating mucoadhesive drug delivery system for famotidine. In order to deliver drugs in accordance with circadian behavior, continuous drug delivery systems were developed. It represents that these systems will deliver the drug when the patient's condition is at most risk. The combination of floating behaviour with the formulation improves the gastric dosage residence. The method adopted for the preparation of tablets was press coating technology. Here it has two layers: a core layer and a coat layer. The core layer consists of active ingredients, and the coat possesses gas-generating agents and polymers like HPMC, Carbopol, and Pectin. The formulations were characterised for weight variation, friability, hardness, disintegration of core tablets, in vitro drug release studies and Ex vivo mucoadhesive studies. All the formulations manifested better results in terms of floating lag time, floating time of more than 8 hours and good adhesion property. The formulation F6 manifested drug release of 99.42% at the end of 7 hours. It was concluded that the formulation F6 is the best formulation which accomplishes the anticipated release with specific lag time and has the ability for off release followed by burst release which can effectively suppress nocturnal histamine level and hence suppress high nocturnal acid release.

Influence of the punch shape on the core and shell structure of press-coated tablets

Press-coated tablets are a key technology to achieve delayed releases in chronotherapeutics. The drug release properties of this kind of tablets are linked to its unique core–shell structure. It is thus important to understand the influence of the process parameters on this structure. As different shapes can be used in the industry, we focused, in this study, on understanding the influence of punch shape on the final structure of a press-coated tablet. Experiments were performed using flat, bevel-edged and concave punches for the coating-compression to study the effect of the punch shape on the final properties of the core but also on the density distribution in the shell. The experiments were supported by numerical simulation to understand the mechanical effects in the powder compression process. It was found that the radial and axial stress state in the shell and in the core during compression is very dependent on the punch shape. The use of concave punches results in a more hydrostatic stress state compared to flat punches. The consequences on the structure are a more homogenous shell and less deformation of the core, which confirms that the tooling shape is a critical parameter to consider for the production of press-coated tablets.

Active coating of immediate-release evogliptin tartrate to prepare fixed dose combination tablet with sustained-release metformin HCl

This study was aimed to develop a fixed dose combination (FDC) tablet containing a low dose of evogliptin tartrate (6.87 mg) for immediate release combined with a high dose (1000 mg) of sustained-release (SR) metformin HCl appropriate for once daily dosing the treatment of type 2 diabetes. To prepare the FDC tablets, an active coating was used in this study, whereby evogliptin tartrate film was layered on a matrix core tablet containing metformin HCl. To overcome the problem caused by a low-dose drug in combination with a relatively large matrix tablet containing high-dose drug, it was also aimed to confirm the formulation and coating operation for satisfactory content uniformity, and to describe the chemical stability during storage of the amorphous active coating layer formulation in relation to molecular mobility. Furthermore, the in vitro release and in vivo pharmacokinetic profiles of metformin HCl and evogliptin tartrate in the FDC active coating tablet were compared to those of the commercially marketed reference drugs, Diabex XR® (Daewoong, Seoul, Korea) containing metformin HCl and Suganon® (Donga ST, Seoul, Korea) containing evogliptin tartrate. In conclusion, the newly developed FDC active coating tablet in this study was confirmed to be bioequivalent to the reference marketed products in beagle dogs, with satisfactory content uniformity and stability.

Development of Enteric-coated Tablets of Sodium 4,4'-(propnadiamido)dibenzoate

Introduction. Enteric coat have a wide range of functions: from protecting the API from the adverse effects of the acidic environment of the stomach to targeted delivery to certain parts of the intestine in order to increase the effectiveness of the drug. When developing such dosage forms, special attention is paid to the type of film-forming polymer in the coating composition, its solubility and ability to withstand passage through the stomach. Aim. Development of enteric-coated tablets based on sodium 4,4'-(prpoandiamido)dibenzoate. Materials and methods. The objects of the study were sodium 4,4'-(propanediamido)dibenzoate 60 mg core tablets and compositions for enteric coatings. The uniformity of distribution of coatings over tablets was determined by the method developed at the Department of Technology of Medicinal Forms of SPCPU on the basis of the Fokker–Planck equation. The dissolution kinetics of enteric-coated tablets was studied using an Erweka DT 626 tablet dissolution tester ( ERWEKA GmbH , Germany). The amount of the substance that passed into the dissolution medium was determined using an SF-2000 spectrophotometer (LLC "OKB Spektr", Russia). Results and discussion. It has been established that all the studied coatings are evenly distributed over the tablets. When studying the kinetics of tablet dissolution, it was found that all coatings are resistant to acidic environments (0.1 M hydrochloric acid solution), however, in a phosphate buffer solution, the highest rate of release of the substance from tablets is achieved using a coating based on a copolymer of methacrylic acid and ethyl acrylate of the type B. Conclusion . Tablets based on sodium 4,4'-(propanediamido)dibenzoate, enteric-coated AquaPolish® P white 712.06E were developed.

Formulation and Development of Aqueous Film Coating for Moisture Protection of Hygroscopic Herniaria glabra L. Tablets

The present study aims to develop a moisture-protective coating solution and use it to film coat hygroscopic Herniaria glabra L. tablets. Five coating formulations were developed and applied on H. glabra core tablets in a fluidized-bed coating. The film-coated tablets were evaluated by appearance, percentage of moisture gain, disintegration time, and percent of drug release. Physicochemical properties and stability during storage of the best obtained coated tablets were studied. The results of this study showed that the film coating F5 containing 25% hydroxypropyl methyl cellulose (HPMC), 20% shellac, 10% polyethylene glycol (PEG) 1500, 29.6% PEG 4000, 5% tween 80, 10% titanium dioxide, and 0.4% acid red 2 offered good protection for coated tablets against moisture. Coated tablets showed physical and dissolution stability during storage. A combination of hydrophilic polymer HPMC and hydrophobic polymer shellac is suitable for balancing moisture-protective properties and attaining the fast release of drugs. This study could make it worthwhile to develop a pharmaceutical moisture barrier film coating system for immediate release tablets. However, more studies will be needed to evaluate the moisture-resistant film further.

MICROSPHERE AND TABLET IN CAPSULE SYSTEM: A NOVEL CHRONOTHERAPEUTIC SYSTEM OF DICLOFENAC SODIUM FOR SITE AND TIME SPECIFIC DELIVERY

The objective of the present study is to develop and evaluate microsphere and tablet in capsule system for the treatment of rheumatoid arthritis as a dual pulse release system. The capsule system contains enteric coated cap filled with microspheres (sustained release) that lock the impermeable capsule body (coated with ethyl cellulose). The capsule body consists of diclofenac sodium loaded core tablet in the bottom (immediate release), which is sealed with swellable hydrogel plug tablet. Formulations selected for capsule system were MP1 due to least particle size (90.44±0.20 μm) and maximum cumulative release (91.49±0.20 %), T3 for least disintegration time (4±0.040 min) and maximum cumulative release (85.50±0.09 %) and HP2 for maintenance of lag phase that was 6 h and in vitro study was Performed. This formulation included two pulses in one system for reduction of dose frequency and better treatment of night pain and morning stiffness in rheumatoid arthritis patients.

Formulation and Evaluation of Chronomodulated Pulsatile Drug Delivery System for Nocturnal Hyperacidity

Introduction: Chronomodulated pulsatile drug delivery system is basically time-controlled drug delivery system in which the release of drug in the body is allowed to match with circadian rhythm with controlled lag time. Aim and Objective: The objective of this work was to develop and evaluate oral pulsatile tablet of Pantoprazole sodium for the treatment of nocturnal hyperacidity. Pulsatile drug delivery system for Pantoprazole sodium was formulated initially as a core tablet followed by press coated. Five different compositions of the core tablet were prepared by using cross carmellose super disintegrant. Base on drug content and dissolution time F5 formulation optimised and proceeds for press coating. Five different compositions of press coating were prepared and evaluated for in vitro drug release. Result: The formulation C4 achieved a maximum of 99.65% cumulative drug release over a period of 3hr. 30 min. Lag time for C4 formulation was found to be 2 hr. It means that the system was found to be satisfactory in terms of drug release after a lag time. Conclusion: Since the developed formulation when taken at bedtime, the tablet would be expected to release the drug at midnight which provides better control with the nocturnal hyperacidity.