Factors Influencing the Release of Aminophylline from Tableted Ethylcellulose Microcapsules

Microcapsules containing aminophylline cores in ethylcellulose walls have been prepared and tableted. The mechanical properties and the release characteristics of tablets obtained by direct compression at six different pressures (ranging from 265 to 1060 Kg.cm^-2) were studied. The release rate of the drug from tableted microcapsules increased with the increase of compression force and was higher than from uncompressed microcapsules, indicating that some damage of the polymeric wall occurred during the compression process. Among the various excipients tested as binding and protective agents, paraffined starch (a mixed system appositely set up) gave the best results, producing the slowest drug release rate. No important effect on drug release rate was found by changing the size of the microcapsules.     

Factors Influencing the Release of Aminophylline from Tableted Ethylcellulose Microcapsules

Abstract

Microcapsules containing aminophylline cores in ethylcellulose walls have been prepared and tableted. The mechanical properties and the release characteristics of tablets obtained by direct compression at six different pressures (ranging from 265 to 1060 Kg.cm^?2) were studied. The release rate of the drug from tableted microcapsules increased with the increase of compression force and was higher than from uncompressed microcapsules, indicating that some damage of the polymeric wall occurred during the compression process. Among the various excipients tested as binding and protective agents, paraffined starch (a mixed system appositely set up) gave the best results, producing the slowest drug release rate. No important effect on drug release rate was found by changing the size of the microcapsules.     

Controlled Nifedipine Release from Microcapsules of its Dispersions in PVP-MCC and HPC-MCC

Nifedipine and its solid dispersions in polyvinyl-pyrrolidone-microcrystalline cellulose (PVP-MCC) and hydroxypropyl cellulose - microcrystalline cellulose (HPC-MCC) were microencapsulated with cellulose acetate by an emulsion solvent evaporation method. The microcapsules are spherical, discrete and free flowing. Nifedipine as such and its microcapsules gave very slow release because of its highly crystalline nature and poor solubility. Solid dispersion in PVP-MCC and HPC-MCC gave fast and rapid dissolution of nifedipine. When these solid dispersions were microencapsulated, a slow, controlled and complete release over a period of 12 hours was observed from the resulting microcapsules. Drug release depended on the proportion of PVP-MCC and HPC-MCC in the solid dispersions used as core, coat: core ratio and size of the microcapsules and the release was pH independent. Drug release was governed by diffusion rate and followed first-order kinetics.     

Captopril Floating and/or Bioadhesive Tablets: Design and Release Kinetics

Two viscosity grades of hydroxypropylmethylcellulose (HPMC 4000 and 15000 cps) and Carbopol 934P were used to prepare captopril floating tablets. In vitro dissolution was carried out in simulated gastric fluid (enzyme free) at 37°C ± 0.1°C using the USP apparatus 2 basket method. Compared to conventional tablets, release of captopril from these floating tablets was apparently prolonged; as a result, a 24-hr controlled-release dosage form for captopril was achieved. Drug release best fit both the Higuchi model and the Korsmeyer and Peppas equation, followed by first-order kinetics. While tablet hardness and stirring rate had no or little effect on the release kinetics, tablets hardness was found to be a determining factor with regard to the buoyancy of the tablets.     

Controlled Drug Release from a Compressed Heterogeneous Polymeric Matrix: Kinetics of Release

A physical model of a new matrix-type system is presented where constant drug release can be maintained irrespective of the extent of the tortuosity and receding drug boundary. Theophylline base was dispersed as discrete crystals and fine particles in a matrix formed by the cross-linking of polymeric mixtures consisting of PEG, acrylic resins and ethyl cellulose. DSC analysis was performed to identify any solid state inactivation of the drug. Concave tablets at specified pressures were prepared in order to achieve a wide range of release rates and patterns of release. It was found that the patterns of release could be controlled by the formulation components and the manufacturing procedures. Drug release rates were determined spectrophotometrically under sink conditions and the flux of drug release, dQ/dt, from these matrix-type delivery systems was almost constant over 15 hours, during which time about 85% of the active drug was released. The release rate was devoid of any hydrodynamic boundary effect and environmental pH. The cumulative amount of drug released was found to be in accordance with zero-order kinetics. The system can be modified within broad limits and have flexibility as well as a wide spectrum of applicability with respect to different types of drugs.     

Controlled Drug Release from a Compressed Heterogeneous Polymeric Matrix: Kinetics of Release

A physical model of a new matrix-type system is presented where constant drug release can be maintained irrespective of the extent of the tortuosity and receding drug boundary. Theophylline base was dispersed as discrete crystals and fine particles in a matrix formed by the cross-linking of polymeric mixtures consisting of PEG, acrylic resins and ethyl cellulose. DSC analysis was performed to identify any solid state inactivation of the drug. Concave tablets at specified pressures were prepared in order to achieve a wide range of release rates and patterns of release. It was found that the patterns of release could be controlled by the formulation components and the manufacturing procedures. Drug release rates were determined spectrophotometrically under sink conditions and the flux of drug release, dQ/dt, from these matrix-type delivery systems was almost constant over 15 hours, during which time about 85% of the active drug was released. The release rate was devoid of any hydrodynamic boundary effect and environmental pH. The cumulative amount of drug released was found to be in accordance with zero-order kinetics. The system can be modified within broad limits and have flexibility as well as a wide spectrum of applicability with respect to different types of drugs.     

Controlled Theophylline Release from Microcapsules of Acrylic & Methacrylic Acid Ester Copolymer

The goal of this work was to develop a suitable method for microencapsulation of theophylline using copolymer of acrylate and methacrylate ester (EUDRAGIT) as the coating material. The effect of protective colloids on the process of microencapsulation was evaluated. The in vitro studies revealed significant control of drug release for the developed dosage form. Individually, the polymer coated drug particles of different core: coat ratio and different proportions of protective colloids were found to influence the pharmacokinetic parameters as revealed from the in vivo bioavailability studies in gastric-emptying controlled rabbits. In vivo bioavailability data were compared using Westlake's confidence limit.     

Controlled Intracellular Release of Peptides from Microcapsules Enhances Antigen Presentation on MHC Class I Molecules

To understand the time course of action of any small molecule inside a single cell, one would deposit a defined amount inside the cell and initiate its activity at a defined moment. An elegant way to achieve this is to encapsulate the molecule in a micrometer‐sized reservoir, introduce it into a cell, remotely open its wall by a laser pulse, and then follow the biological response by microscopy. The validity of this approach is validated here using microcapsules with defined walls that are doped with metallic nanoparticles so as to enable them to be opened with an infrared laser. The capsules are loaded with a fluorescent antigenic peptide and introduced into mammalian cultured cells where, upon laser‐induced release, the peptide binds to major histocompatibility complex (MHC) class I proteins and elicits their cell surface transport. The concept of releasing a drug inside a cell and following its action is applicable to many problems in cell biology and medicine.     

25th Anniversary Article: Double Emulsion Templated Solid Microcapsules: Mechanics And Controlled Release

How droplet microfluidics can be used to fabricate solid‐shelled microcapsules having precisely controlled release behavior is described. Glass capillary devices enable the production of monodisperse double emulsion drops, which can then be used as templates for microcapsule formation. The exquisite control afforded by microfluidics can be used to tune the compositions and geometrical characteristics of the microcapsules with exceptional precision. The use of this approach to fabricate microcapsules that only release their contents when exposed to a specific stimulus – such as a change in temperature, exposure to light, a change in the chemical environment, or an external stress – only after a prescribed time delay, and at a prescribed rate is reviewed.     

In-Vitro Release Kinetics of Salbutamolsulphate Microcapsules Coated with Both Eudragit Rs 100 and Eudragit RL 100

Sabutamolsulphate, a bronchodialatory drug for Asthma is encapsulated by Eudragit RS 100 and Eudragit RL 100 of varying ratios (1:1, 3:1, 1:3) using Emulsion-Solvent-Evaporation method. The experimental data obtained from the in-vitro dissolution study have been computed in the light of different kinetic models like Zero Ordr, Higuchi Matrix, First Order, Baker-Lonsdale. An extensive programming in BASIC is performed to determine the co-relation coefficient and slope for each of the functions. The diffusivity rate constant (K_BL) and diffusion coefficient (Da) have been evaluated with the help of Baker-Lonsdale Model.     

Multi‐Drug‐Loaded Microcapsules with Controlled Release for Management of Parkinson's Disease

Parkinson's disease (PD) is a progressive disease of the nervous system, and is currently managed through commercial tablets that do not sufficiently enable controlled, sustained release capabilities. It is hypothesized that a drug delivery system that provides controlled and sustained release of PD drugs would afford better management of PD. Hollow microcapsules composed of poly‐l ‐lactide (PLLA) and poly (caprolactone) (PCL) are prepared through a modified double‐emulsion technique. They are loaded with three PD drugs, i.e., levodopa (LD), carbidopa (CD), and entacapone (ENT), at a ratio of 4:1:8, similar to commercial PD tablets. LD and CD are localized in both the hollow cavity and PLLA/PCL shell, while ENT is localized in the PLLA/PCL shell. Release kinetics of hydrophobic ENT is observed to be relatively slow as compared to the other hydrophilic drugs. It is further hypothesized that encapsulating ENT into PCL as a surface coating onto these microcapsules can aid in accelerating its release. Now, these spray‐coated hollow microcapsules exhibit similar release kinetics, according to Higuchi's rate, for all three drugs. The results suggest that multiple drug encapsulation of LD, CD, and ENT in gastric floating microcapsules could be further developed for in vivo evaluation for the management of PD.     

Clofibrate Microcapsules: III. Mechanism of Release

The mechanism of release of clofibrate from microcapsules prepared in a gelatin-sodium sulfate system has been investigated. A theoretical model was developed to explain the release pattern of the drug from the microcapsules. It was shown that the release of the drug followed four stages giving individual zero-order profiles. The overall release from the thin-walled microcapsules showed greater deviation from the zero-order kinetics but followed the square-root of the time plots. Microcapsules having thicker walla approximated overall zero-order release but deviated from the square-root of time plots. The effect of hardening on the release profiles and possible explanations for the differences observed in the release of clofibrate from the thin-walled and thick-walled microcapsules are discussed.     

Kinetics and Mechanism of Drug Release From Calcium Alginate Membrane Coated Tablets

Compressed tablets containing guaifenesin (model drug), calcium acetate (reactant) and pharmaceutical excipients were prepared. The tablets were coated with calcium alginate hydrogel using a novel, self-correcting membrane coating technique. Effects of coating time, the type of alginate polymer and pH of the dissolution medium on the rate of drug release were evaluated. In distilled water, zero order drug release profiles were obtained from the coated tablets. The release rate decreased with an increase in the coating time (increased coat thickness) and molecular weight of alginate polymer. The release rate constants correlated with model for spherical reservoir system and, were used to calculate permeability of guaifenesin in the calcium alginate coatings. Alginate polymer with higher guluronic acid content provided acid stable coating and higher molecular weight polymer produced membrane with lower permeability for guaifenesin.     

Clofibrate Microcapsules: III. Mechanism of Release

Abstract

The mechanism of release of clofibrate from microcapsules prepared in a gelatin-sodium sulfate system has been investigated. A theoretical model was developed to explain the release pattern of the drug from the microcapsules. It was shown that the release of the drug followed four stages giving individual zero-order profiles. The overall release from the thin-walled microcapsules showed greater deviation from the zero-order kinetics but followed the square-root of the time plots. Microcapsules having thicker walla approximated overall zero-order release but deviated from the square-root of time plots. The effect of hardening on the release profiles and possible explanations for the differences observed in the release of clofibrate from the thin-walled and thick-walled microcapsules are discussed.     

In-Vitro Release and Permeation Kinetics of Pentazociwe From Matrix-Dispersion Type Trawsdwul Drug Delivery Systw

A matrix-dispersion type Transdermal Drug Delivery System (TDS) of Pentazocine (PZ) was fabricated, using combinations of rate controlling polymers, namely Eudragits RS100 (RS), RL100 (RL), Ethylcellulose (EC) and Polyvinyl pyrrolidone (PVP), with the objective of examining the effects of formulation variables on drug-permeation profiles. In depth in-vitro drug release and skin-permeation kinetics with three different loads, and also the effects of combination of isopropyl Myristate (IPM), as permeation enhancer, were studied using male albino mice abdominal skin. The release of PZ over a 12 hour period followed Higuchi kinetics, while in-vitro mice-skin permeation of PZ followed an apparent Zero-order kinetics over a period of 24 hours.     

In-Vitro Release and Permeation Kinetics of Pentazociwe From Matrix-Dispersion Type Trawsdwul Drug Delivery Systw

Abstract

A matrix-dispersion type Transdermal Drug Delivery System (TDS) of Pentazocine (PZ) was fabricated, using combinations of rate controlling polymers, namely Eudragits RS100 (RS), RL100 (RL), Ethylcellulose (EC) and Polyvinyl pyrrolidone (PVP), with the objective of examining the effects of formulation variables on drug-permeation profiles. In depth in-vitro drug release and skin-permeation kinetics with three different loads, and also the effects of combination of isopropyl Myristate (IPM), as permeation enhancer, were studied using male albino mice abdominal skin. The release of PZ over a 12 hour period followed Higuchi kinetics, while in-vitro mice-skin permeation of PZ followed an apparent Zero-order kinetics over a period of 24 hours.     

异噻唑啉酮微胶囊的制备表征及释放行为

以二异氰酸酯(TDI)、聚乙二醇4000(PEG)、二羟甲基丙酸(DMPA)和三乙胺(TEA)为原料,制备可水乳化的聚氨酯(WPU).以合成的WPU为囊壁、以异噻唑啉酮衍生物(Sea-nine 211)为囊芯,通过乳化自组装得到防污剂Sea-nine 211微胶囊,用红外光谱、粒径分布和扫描电镜对胶囊进行表征,并采用分...     

甜玉米芯多糖纳米乳微胶囊制备及释放

目的 改善甜玉米芯多糖(SCP)大分子特性以及稳定性,促进SCP的肠道吸收。方法 将SCP水溶液制备成油包水型(W/O)甜玉米芯多糖纳米乳液(SCP-NE),以复合蛋白为壁材制备成SCP-NE微胶囊,采用单因素试验、Box-Behnken设计和响应面法优化SCP-NE微胶囊制备工艺,以粒径分析、红外光谱分析、热重分析,对SCP-NE微胶囊物化性质进行研究,并进行体外模拟胃肠液释放研究。结果 制备SCP-NE微胶囊最佳条件为麦芽糊精(MD)与大豆分离蛋白(SPI)的质量比为2∶3、芯壁比为1∶2、总体固形物含量为20%,此时包封率达到(87.6±1.3)%。体外模拟胃肠液释放结果表明,SCP-NE微胶囊在2 h的胃液消化中释放率为8.83%,在模拟肠液中1 h的释放量为62.87%。结论 以MD和SPI作为壁材制备的SCP-NE微胶囊在胃肠液释放中具有良好的缓释性能。     

Evaluation of Tableted Microspheres of Dipyridamole

Microspheres of dipyridamole were prepared by solvent evaporation methods. The effect of additives Avicel PH 101, and beta cyclodextrin on the release rate of tableted microspheres were studied. Incorporating Avicel or beta cyclodextrin increased the dipyridamole release rates in tableted microspheres. Beta cyclodextrin was found to be a good additive for microsphere tablets to increase the drug release rates without causing disintegration.