High efficiency dry coating of non-subcoated pellets for sustained drug release formulations using amino methacrylate copolymers.

Dry coating utilizing a fluidized bed was evaluated in order to produce films with sustained drug release using amino methacrylate copolymers as film former. In contrast to other dry coating procedures using amino methacrylate copolymers, the described method enables an appropriate polymer adhesion by the selection of a plasticizer additive mixture in combination with the use of a three-way nozzle for simultaneous application. Well spreading fatty acid esters were found to increase the coating efficiency from 73% to approximately 86%, when they were used in conjunction with the plasticizer.

Solubility parameters of hypromellose acetate succinate and plasticization in dry coating procedures.

Solubility parameters of HPMCAS have not yet been investigated intensively. On this account, total and three-dimensional solubility parameters of HPMCAS were determined by using different experimental as well as computational methods. In addition, solubility properties of HPMCAS in a huge number of solvents were tested and a Teas plot for HPMCAS was created.

Crystallization speed of salbutamol as a function of relative humidity and temperature.

Spray dried salbutamol sulphate and salbutamol base particles are amorphous as a result of spray drying. As there is always the risk of recrystallization of amorphous material, the aim of this work is the evaluation of the temperature and humidity dependent recrystallization of spray dried salbutamol sulphate and base. Therefore in-situ Powder X-ray Diffraction (PXRD) studies of the crystallization process at various temperature (25 and 35 °C) and humidity (60%, 70%, 80%, 90% relative humidity) conditions were performed.

Influence of surface characteristics of modified glass beads as model carriers in dry powder inhalers (DPIs) on the aerosolization performance.

The aim of this work is to investigate the effect of surface characteristics (surface roughness and specific surface area) of surface-modified glass beads as model carriers in dry powder inhalers (DPIs) on the aerosolization, and thus, the in vitro respirable fraction often referred to as fine particle fraction (FPF). By processing glass beads in a ball mill with different grinding materials (quartz and tungsten carbide) and varying grinding time (4 h and 8 h), and by plasma etching for 1 min, glass beads with different shades of surface roughness and increased surface area were prepared. Compared with untreated glass beads, the surface-modified rough glass beads show increased FPFs.

Preparation and characterization of physically modified glass beads used as model carriers in dry powder inhalers.

The aim of this work is the physical modification and characterization of the surface topography of glass beads used as model carriers in dry powder inhalers (DPIs). By surface modification the contact area between drug and carrier and thereby interparticle forces may be modified. Thus the performance of DPIs that relies on interparticle interactions may be improved.

Evaluating the process parameters of the dry coating process using a 2(5-1) factorial design.

Context: A recent development of coating technology is dry coating, where polymer powder and liquid plasticizer are layered on the cores without using organic solvents or water. Several studies evaluating the process were introduced in literature, however, little information about the critical process parameters (CPPs) is given.

Aim: Aim of the study was the investigation and optimization of CPPs with respect to one of the critical quality attributes (CQAs), the coating efficiency of the dry coating process in a rotary fluid bed.

Perfusion calorimetry in the characterization of solvates forming isomorphic desolvates.

In this study, the potential of perfusion calorimetry in the characterization of solvates forming isomorphic desolvates was investigated. Perfusion calorimetry was used to expose different hydrates forming isomorphic desolvates (emodepside hydrates II-IV, erythromycin A dihydrate and spirapril hydrochloride monohydrate) to stepwise increasing relative vapour pressures (RVP) of water and methanol, respectively, while measuring thermal activity. Furthermore, the suitability of perfusion calorimetry to distinguish the transformation of a desolvate into an isomorphic solvate from the adsorption of solvent molecules to crystal surfaces as well as from solvate formation that is accompanied by structural rearrangement was investigated.

Impact of excipients on coating efficiency in dry powder coating.

Dry powder coating is a technique to coat substrates without the use of organic solvent or water. The polymer powder is directly applied to the cores to be coated. Liquid additives are often used to lower the glass transition temperature of the polymer and to enhance the adhesion of the powder to the cores.

Stability of dry coated solid dosage forms.

The dry coating process was evaluated in terms of storage stability investigating drug release and agglomeration tendency of the different coated oral dosage forms; hydroxypropyl methylcellulose acetate succinate (HPMCAS) was used with triethylcitrate (TEC) as plasticizer and acetylated monoglyceride (Myvacet) as wetting agent. Talc or colloidal silicon dioxide (Aerosil) was used as anti-tacking agents. In contrast to coating formulations consisting of HPMCAS and Myvacet all formulations containing TEC showed enteric resistance and no agglomeration tendency after preparation.

The role of capillary force promoters in dry coating procedures--evaluation of acetylated monoglyceride, isopropyl myristate and palmitate.

Previous studies described several dry powder coating procedures. Most of these techniques used polymer powders and plasticizers for attaining film formation. Thermo analytical methods showed that some of the used plasticizers did not reduce the glass transition temperature of the polymer markedly and consequently did not act as a plasticizer in a typical way.

Parameters influencing polymer particle layering of the dry coating process.

The dry coating process is an emerging coating technology using neither organic solvents nor water. In contrast to liquid-borne coatings, coating material application and film formation are divided into two phases, the coating phase where the powdery coating material is applied together with the liquid plasticizer, and the curing phase. In this study the coating phase was characterized with respect to the forces acting between the polymer particles during material application.

Quantifying the degree of disorder in micronized salbutamol sulfate using moisture sorption analysis.

Salbutamol sulfate is often micronized for use in dry powder inhalers. Therefore, it is of high interest to quantify the amorphous amount. It was investigated whether moisture sorption is able to measure the amorphous content of salbutamol sulfate.

Characterization of the film formation of the dry coating process.

As the film formation of the dry coating process differs completely from conventional coating methods it is of certain interest to define a parameter like the minimum film formation temperature (MFT) used for aqueous dispersion based processes in order to describe an efficient film formation. Film formation occurs mainly during the curing step following the coating phase. Therefore, the film formation of the dry coating process was analyzed with regard to the two process parameters influencing film formation, namely curing temperature and time.

Adhesion forces in interactive mixtures for dry powder inhalers--evaluation of a new measuring method.

Dry powder inhalers mostly contain carrier based formulations where micronized drug particles are adhered to coarse carrier particles. The performance of the dry powder inhaler depends on the inhaler device, the inhalation manoeuvre and the formulation. The most important factor influencing the behaviour of the formulation is the adhesion force acting between the active ingredient and the carrier particles, which can be measured using different methods, for example the centrifuge technique or atomic force microscopy.

The influence of povidone K17 on the storage stability of solid dispersions of nimodipine and polyethylene glycol.

Previous studies revealed that solid dispersions containing nimodipine and polyethylene glycol 2000 can be effectively prevented from recrystallization by adding povidone K17. These systems are characterized by a high dissolution rate and a remarkable supersaturation of the drug in the dissolution media. It is still unknown if these characteristics are achievable with all polyethylene glycol and povidone mixtures.

Stabilization of solid dispersions of nimodipine and polyethylene glycol 2000.

Previous investigations revealed that solid dispersions consisting of 20% (m/m) nimodipine and 80% (m/m) polyethylene glycol 2000 prepared by the melting method, represent supersaturated solid solutions of nimodipine recrystallizing upon storage at +25 degrees C. The objective of this study was the improvement of the storage stability by preventing recrystallization. The first approach in order to prevent recrystallization was the development of thermodynamically stable solid solutions by using solvents aiming to enhance the solubility of nimodipine in the carrier material.

Dry coating in a rotary fluid bed.

A highly efficient dry coating process was developed to obtain an enteric film avoiding completely the use of organic solvents and water. Using hydroxypropyl methylcellulose acetate succinate (HPMCAS) an enteric coat should be obtained without adding talc as anti-tacking agent because of problems arising from microbiological contamination. Further on, a method was developed preparing isolated films in order to determine the glass transition temperature (T(g)) and the required process temperature.

Solid dispersions of nimodipine and polyethylene glycol 2000: dissolution properties and physico-chemical characterisation.

The incorporation of a drug in a carrier by melt embedding may either result in a solid solution or in a solid suspension of the active ingredient within the carrier material. As the dispersivity of the drug is of outstanding importance for its dissolution characteristics, parameters which are supposed to influence crystallinity and dispersivity, e.g.