Hot Melt Coating Research Articles

Hot Melt Coating of Pellets for a Water Soluble Drug using Combination of Waxes

Waxes retards drug release from dosage form based on their lipophilic characteristics. In this study, the effect of hot melt spray coated Verapamil pellets with composition of stearic acid, carnauba wax; glyceryl monostearate and polyethylene glycol on drug release and release kinetics were investigated. The verapamil pellets containing 70% microcrystalline cellulose (Avicel PH101) were prepared by extrusion-spheronization technique and spray coated with molten wax at various ratios and thickness in a hot-melt spray coating instrument. In-vitro drug release was studied using test method for Extended Release tablets USP 24. The drug release was decreased with increase in stearic acid concentration and addition of 5% carnauba wax to stearic acid minimized initial burst release but it also retarded drug release. Glyceryl monostearate 30%w/w as release modifier at 20%w/w coating level provided desired drug release while PEG 6000 provided similar results at 2.5%w/w concentration. The plot of log fraction drug unreleased versus time showed a good linear relationship. Glycerol monostearate at 30%w/w as release modifier showed higher release rate in initial hours which declined with time and also R2 value for first order release kinetics was found to be nearest to one indicating drug release was dependent on initial concentration present in pellets. A zero order release profile was obtained from verapamil HCl sustained release pellets prepared by hot melt spray coating of stearic acid with sitable combination of carnuba wax and PEG 6000.

Design of sustained release pellets of ferrous fumarate using cow ghee as hot-melt coating agent.

Introduction:The objective of the present study was to design ferrous fumarate (FF) sustained release (SR) pellets using of cow ghee (CG) as an important hot-melt coating (HMC) agent.Materials and Methods:The pellets were coated by HMC technique using CG and ethyl cellulose composition by conventional coating pan without the use of spray system. FF formulated as pellets and characterized with regard to the drug content and physico-chemical properties. Stability studies were carried out on the optimized formulation for a period of 6 months at 40 ± 2°C and 75 ± 5% relative humidity.Results:Pellets with good surface morphology and smooth texture confirmed by stereo micrographs. HMC is easy, efficient, rapid and simple method since virtually no agglomeration seen during coating. In-vitro release from pellets at a given level of coating and for present pellet size was dependent upon the physico-chemical property of the drug and mostly aqueous solubility of the drug. The selection of optimized FF formulation was confirmed by comparing percent cumulative drug release with theoretical release profile. Formulation F2 had difference factor (f1) and similarity factor (f2) values was found to be 5 and 66 respectively. F2 showed SR of drug for 8 h with cumulative per cent release of 98.03 ± 4.49%. Release kinetics indicates approximately zero order release pattern. HMC pellets were stable during the course of stability study.Conclusions:By means of HMC using CG and ethyl cellulose, SR pellets containing FF were successfully prepared.

Development and evaluation of a hot-melt coating technique for enteric coating

Conventional enteric coating requires the use of organic based polymers which are equally hazardous to the environment and operating personnel. Hot-melt coating avoids the use of solvents and is a safer and time-saving process. The present study was designed to assess the efficacy of hot-melt coating (HMC) as an enteric coating technique. Pellets prepared by extrusion spheronization were selected as the core formulation for a model of the gastric irritant drug diclofenac sodium (DFS) because of their innate advantages over single-unit formulations. Stearic acid (SA) and palmitic acid (PA) were evaluated as enteric hot-melt coating materials. HMC was carried out in a specially modified coating pan by applying SA and PA in molten state onto preheated pellets to achieve a coating level of 5-15 %w/w. Hot-melt coated pellets were evaluated for disintegration pH and in vitro dissolution in the pH range 1.2 to 6.8, along with basic micromeritics. SEM of coated pellets showed a uniform and smooth coating. These results indicated that HMC of both SA and PA exhibited very good enteric coating ability. The coated pellets showed negligible drug release in acidic pH. As the pellets were subsequently transferred to a higher pH level, a gradual increase in release of the drug from the pellets was observed with increasing pH of the dissolution media. The release was dependent upon coating extent, providing sustained enteric release as opposed to abrupt release with mixed release kinetics.

Application of Hot-Melt Coating Process for Designing a Lipid Based Controlled Release Drug Delivery System for Highly Aqueous Soluble Drugs

Hot-melt coating process (HMCP) was applied to develop a lipid based oral controlled release matrix system (tablet) to deliver highly aqueous soluble drugs using paracetamol as a model drug. Granules prepared from paracetamol and particular filler were coated with different levels of lipid and then compressed into tablets to get controlled/sustained delivery of the drug over an optimum period. Process parameters were optimized with particular focus on fluidization pattern during HMCP proposing a 'design space' with 'Quality by Design' (QbD) concept in mind. The results demonstrated that the granule composition influenced the drug release pattern, and the rate of release could be manipulated by varying the amount of lipid in the formulation. The in vitro release profile of the drug was pH-independent and the most promising release profile was obtained from tablets prepared from granules with the water-soluble filler, lactose, and coated at 9% (w/w) level with a lipid, glyceryl behanate. In vivo plasma profiles of the drug were predicted from the in vitro release profile data by convolution analysis which confirmed that the lactose based formulation with 9% (w/w) lipid coating on the granules would be suitable for controlled delivery of the drug over a period of 12 h making the formulation suitable for highly water soluble drug candidates like paracetamol with twice daily dose regimen. Moreover, the dissolution data adequately fitted into Higuchi model suggesting that the drug release occurred predominantly by diffusion.

Hot-Melt Coating: Water Sorption Behavior of Excipient Films

Hot-melt coating allows encapsulation of water-labile, drug-laden substrates to form a barrier that resists moisture ingress. To understand the interaction of water with excipients that can form moisture-protective coatings, sorption behavior of films of lipidic (glyceryl behenate) and polymeric (polyvinyl alcohol) coating excipients was investigated. A simple and rapid method using a new, fully automated instrumental technique to investigate the sorption/desorption behavior of excipient films is reported. Further, the influence of temperature and film thickness on the sorption behavior of films is examined. Both excipient films displayed sorption isotherms that were classified as type III and demonstrated hysteresis during desorption. The sorption data for both films did not follow the Langmuir model, and the BET model could only be used restrictively. The GAB model fitted the sorption data at all conditions and over the entire range of water activity studied. The ability of the Young and Nelson model to explain the hysteresis behavior, from analytical and mechanistic perspectives, is evaluated. Temperature and film thickness were found to profoundly influence the nature of moisture interaction and distribution of moisture in the excipient films. An Arrhenius-type relationship was observed between equilibrium moisture content of excipient films and temperature at constant water activity.

Development of Hot Melt Coating Methods

Development of Hot Melt Coating Methods

Hot-Melt Coating Techniques of the Bema and the Zimmer Machine

Hot-Melt Coating Techniques of the Bema and the Zimmer Machine