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PubMed2002

Glycine crystallization during spray drying: the pH effect on salt and polymorphic forms.

Spray drying of aqueous solutions of glycine revealed a strong pH effect on the salt and polymorphic forms of the resulting powders. Adjusting pH by aqueous HCl or NaOH between 1.7 and 10.0 caused the glycine solutions to crystallize as two polymorphs (alpha and gamma) of the neutral glycine ((+)H(3)NCH(2)CO(2) (-)) and as three salts (diglycine HCl, (+)H(3)NCH(2)CO(2) (-). (+)H(3)NCH(2)CO(2)H. C1(-); glycine HCl, (+)H(3)NCH(2)CO(2)H. C1(-); and sodium glycinate, H(2)NCH(2)CO(2) (-). Na(+)). Although alpha-glycine crystallized from solutions without pH adjustment (pH 6.2), changing the pH to 4.0 and 8.0 caused gamma-glycine to crystallize as the preferred polymorph. This phenomenon is attributed to the pH effect on the dimeric growth unit of alpha-glycine. The formation of alpha-glycine by spray drying solutions of neutral glycine contrasts the outcome of freeze drying, which yields beta-glycine. Because gamma-glycine is thermodynamically more stable than alpha-glycine, the crystallization of gamma-glycine by pH adjustment provides a way to improve the physical stability of glycine-containing formulations. Spray drying at low pH yielded various mixtures of neutral glycine and its HCl salts: pH 3.0, gamma-glycine and diglycine HCl; pH 2.0, diglycine HCl; and pH 1.7 (the natural pH of glycine HCl), diglycine HCl (major component) and glycine HCl (minor component). Spray drying glycine HCl solutions (pH 1.7) yielded the same diglycine HCl/glycine HCl mixture as did spray drying neutral glycine solutions acidified to pH 1.7. Obtaining diglycine HCl by spray drying glycine HCl solutions indicates a 50% loss of HCl during processing. The extent of HCl loss could be altered by changing the inlet temperature of the spray drier. Spray drying glycine solutions at pH 9.0 and 10.0 gave predominantly gamma-glycine and an additional crystalline product, possibly sodium glycinate. The glycine powders spray dried at different pH had different particle morphologies and sizes, which may influence their suitability for pharmaceutical formulations.

Crystallization↗
PubMed2004

Comparative survival of probiotic lactobacilli spray-dried in the presence of prebiotic substances.

AIMS: Probiotic milk-based formulations were spray-dried with various combinations of prebiotic substances in an effort to generate synbiotic powder products. METHODS AND RESULTS: To examine the effect of growth phase and inclusion of a prebiotic substance in the feed media on probiotic viability during spray-drying, Lactobacillus rhamnosus GG was spray-dried in lag, early log and stationary phases of growth in reconstituted skim milk (RSM) (20% w/v) or RSM (10% w/v), polydextrose (PD) (10% w/v) mixture at an outlet temperature of 85-90 degrees C. Stationary phase cultures survived best (31-50%) in both feed media and were the most stable during powder storage at 4-37 degrees C over 8 weeks, with 30-140-fold reductions in cell viability at 37 degrees C in RSM and PD/RSM powders, respectively. Stationary phase Lact. rhamnosus GG was subsequently spray-dried in the presence of the prebiotic inulin in the feed media, composed of RSM (10% w/v) and inulin (10% w/v), and survival following spray-drying was of the order 7.1-43%, while viability losses of 20,000-90,000-fold occurred in these powders after 8 weeks' storage at 37 degrees C. Survival of the Lactobacillus culture after spray-drying in powders produced using PD (20% w/v) or inulin (20% w/v) as the feed media was only 0.011-0.45%. To compare different probiotic lactobacilli during spray-drying, stationary phase Lact. rhamnosus E800 and Lact. salivarius UCC 500 were spray-dried using the same parameters as for Lact. rhamnosus GG in either RSM (20% w/v) or RSM (10% w/v) and PD (10% w/v). Lact. rhamnosus E800 experienced approx. 25-41% survival, yielding powders containing approximately 10(9) CFU g(-1), while Lact. salivarius UCC 500 performed poorly, experiencing over 99% loss in viability during spray-drying in both feed media. In addition to the superior survival of Lact. rhamnosus GG after spray-drying, both strains experienced higher viability losses (570-700-fold) during storage at 37 degrees C over 8 weeks compared with Lact. rhamnosus GG. CONCLUSIONS: Stationary phase cultures were most suitable for the spray-drying process, while lag phase was most susceptible. The presence of the prebiotics PD and inulin did not enhance viability during spray-drying or powder storage. SIGNIFICANCE AND IMPACT OF THE STUDY: High viability (approximately 10(9) CFU g(-1)) powders containing probiotic lactobacilli in combination with prebiotics were developed, which may be useful as functional food ingredients for the manufacture of probiotic foods.

Animals↗
PubMed2000

Liposomes containing drug and cyclodextrin prepared by the one-step spray-drying method.

The one-step spray-drying method was applied in the preparation of liposomes containing drug and cyclodextrin (CD). Spray-dried lecithin liposomes, entrapping metronidazole or verapamil alone or together with hydroxypropyl-beta-cyclodextrin (HP beta CD), were characterized for morphology, size distribution, and drug entrapment efficiency. The main factor influencing the liposomal size was the volume of aqueous medium used for hydration of the spray-dried product. No differences in size or entrapment between liposomes prepared by immediate hydration of dried powder or by hydration after 1 year of powder storage at 4 degrees C were observed. All liposomes were tested for their serum stability. The most stable liposomes (still retaining about 10% of the originally entrapped drug even after 24 hr incubation with serum) were liposomes prepared by the direct spray-drying of the mixture of lipid, drug, and HP beta CD.

Anti-Infective Agents↗
PubMed2004

Formulation and characterization of spray-dried powders containing nanoparticles for aerosol delivery to the lung.

Spray-drying is a common practice of powder preparation for a wide range of drugs. Spray-dried powders can be used to deliver particles to the lungs via a dry powder inhaler (DPI). The present study investigated the feasibility of developing a platform for aerosol delivery of nanoparticles. Lactose was used as the excipient and spray-dried with two different types of nanoparticles: gelatin and polybutylcyanoacrylate nanoparticles. Results showed that some carrier particles were hollow while others had a continuous matrix. Gelatin nanoparticles were incorporated throughout the matrix and sometimes accumulated at one end of the lactose. Polycyanoacrylate nanoparticles mostly clustered in different spots within the lactose carriers. The mean sizes of both nanoparticle types were characterized at two different times: before they were spray-dried and after they were redissolved from the spray-dried powders. Both nanoparticle types remained in the nano-range size after spray-drying. The mean nanoparticle sizes were increased by approximately 30% after spray-drying, though this increase was statistically significant only for the gelatin nanoparticles. Dispersion of the powder with an in-house passive dry powder inhaler and subsequent cascade impaction measurements showed that incorporation of the nanoparticles did not affect the fine particle fraction (FPF) or mass median aerodynamic diameter (MMAD) of the powders. FPF was approximately 40% while MMAD was 3.0+/-0.2 microm, indicating the present formulations yield aerosols of a suitable particle size for efficient lung delivery of nanoparticles. The present work demonstrates that nanoparticles can be delivered to the lungs via carrier particles that dissolve after coming in contact with the aqueous environment of the lung epithelium. This opens the way for new drug-targeting strategies using nanoparticles for pulmonary delivery of drugs and diagnostics.

Aerosols↗
PubMed2003

Spray-dried chitinosans. Part I: preparation and characterization.

PURPOSE: Physicochemical and micromeritic characterization of chitinosans. METHODS: Chitinosans subjected to N-deacetylation and depolymerization were characterized for degree of N-deacetylation (DD), molecular weight (MW), pK(a), particle size determination and morphology, tap/bulk density measurements, surface area determinations, and determination of flow properties. RESULTS: The chitinosan DDs and MWs were dependent on the processing conditions and ranged from 66 to 89% and 2-522 kDa, respectively. Chitinosan particle sizes and shapes were dependent on drying conditions (range 8-465 microm). Spray-dried chitinosans were spherical and had smaller particle sizes than the non-spray-dried materials which were irregularly shaped particles. Higher density values were obtained for processed materials than those for the raw material. Lower specific surface areas were observed for non-spray-dried chitinosans (0.28-1.59 m(2)/g) than for spray-dried chitinosans (0.74-3.01 m(2)/g). Weight variation of chitinosan tablets indicated that spray-dried chitinosans possessed improved flow characteristics as compared with tray-dried chitinosans. CONCLUSIONS: The effect of drying method employed in chitinosan manufacture, i.e. spray versus tray drying, on the physicochemical and micromeritic properties of the resultant chitinosans were evaluated. Although the drying methods did not significantly influence the physicochemical properties, they affected the micromeritic properties of the resultant chitinosans.

Biopolymers↗
PubMed1997

The effect of operating and formulation variables on the morphology of spray-dried protein particles.

The purpose of this research was to investigate the shape and morphology of various spray-dried protein powders as a function of spray-drying conditions and protein formulations. A benchtop spray dryer was used to spray dry three model proteins in formulation with a sugar or a surfactant. Physical characterizations of the powder included morphology (scanning electron microscopy), particle size, residual moisture, and X-ray powder diffraction analyses. A significant change in particle shape from irregular (e.g., "donut") to spherical was observed as the outlet temperature of the dryer was decreased. The drying air outlet temperature was shown to depend on various operating parameters and was found to correlate with the drying rate of atomized droplets in the drying chamber. The morphology of spray-dried protein particles was also affected by formulation. In protein:sugar formulations, spray-dried particles exhibited a smooth surface regardless of the protein-to-lactose ratio, whereas roughness was observed when mannitol was present at > 30% of total solids, due to recrystallization. Protein particles containing trehalose at concentrations > 50% were highly agglomerated. The presence of surfactant resulted in noticeably smoother, more spherical particles. The shape and the morphology of spray-dried powders are affected by spray drying conditions and protein formulation. This study provides information useful for development of dry proteins for fine powder (e.g., aerosol) applications.

Antibodies, Monoclonal↗
PubMed2004

Evaluation of methods to reduce bacteria concentrations in spray-dried animal plasma and its effects on nursery pig performance.

Four experiments with 1,040 weanling pigs (17 +/- 2 d of age at weaning) were conducted to evaluate the effects of spray-dried animal plasma source, drying technique, and methods of bacterial reduction on nursery pig performance. In Exp. 1, 180 barrows and gilts (initial BW 5.9 +/- 1.8 kg) were used to compare effects of animal plasma, animal plasma source, drying technique (spray-dried or freeze-dried), and plasma irradiation in nursery pig diets. From d 0 to 10, pigs fed diets containing irradiated spray-dried animal plasma had increased ADG and ADFI (P < 0.05) compared with pigs fed diets containing nonirradiated spray-dried animal plasma. Pigs fed irradiated animal plasma Sources 1 and 2 were similar in ADG and ADFI, but pigs fed animal plasma Source 1 had greater ADG (P < 0.05) than pigs fed animal plasma Source 2 and pigs not fed plasma. Pigs fed freeze-dried animal plasma had growth performance similar (P > 0.36) to pigs fed spray-dried animal plasma. Overall (d 0 to 24), pigs fed irradiated spray-dried animal plasma were heavier (P < 0.05) than pigs fed no animal plasma, whereas pigs fed nonirradiated spray-dried plasma were intermediate. In Exp. 2, 325 barrows and gilts (initial BW 5.8 +/- 1.7 kg) were used to compare the effects of irradiation or formaldehyde treatment of animal plasma and formaldehyde treatment of the whole diet. Pigs fed diets containing irradiated animal plasma had greater ADG (P < 0.05) than pigs fed nonirradiated plasma. Pigs fed formaldehyde-treated plasma had greater ADG and ADFI (P < 0.05) than pigs fed diets with either nonirradiated plasma or whole diet treated with formaldehyde. In Exp. 3 (360 barrows and gilts; initial BW 6.3 +/- 2.7 kg) and Exp. 4 (175 barrows and gilts; initial BW 6.1 +/- 1.7 kg), the irradiation of feed (high bacteria) and food-grade (low bacteria) animal plasma in nursery pig diets was examined. Pigs fed irradiated feed-grade plasma Product 2 had increased ADG (P < 0.05) compared with pigs fed nonirradiated plasma Product 2 and pigs fed the control diet without plasma. In Exp. 3 and 4, pigs fed irradiated food-grade plasma had growth performance similar to pigs fed nonirradiated food-grade plasma (P > 0.12). These studies indicate that bacterial reduction of feed-grade, but not food-grade animal plasma, improves nursery pig performance.

Animal Feed↗
PubMedDate not supplied

Controlled release of vancomycin from freeze-dried chitosan salts coated with different fatty acids by spray-drying.

The aim of this study was to describe a controlled drug release system based on chitosan salts for vancomycin hydrochloride delivery. Chitosan aspartate (CH-Asp), chitosan glutamate (CH-Glu) and chitosan hydrochloride (CH-HCl) were prepared by freeze-drying and coated with stearic, palmitic, myristic and lauric acids by spray-drying technique. Vancomycin hydrochloride was used as a peptidic model drug whose sustained release should minimize its inactivation in the upper part of the gastrointestinal tract. This study evaluated, in vitro, the influence of chitosan salts on the release behaviour of vancomycin hydrochloride from the freeze-dried and spray-dried systems at pH 2.0 and 7.4.

Anti-Bacterial Agents↗
PubMed2002

Survival of bifidobacteria after spray-drying.

To investigate the survival of bifidobacteria after spray-drying, Bifidobacterium infantis CCRC 14633, B. infantis CCRC 14661, B. longum ATCC 15708, B. longum CCRC 14634 and B. longum B6 were first spray-dried with different carrier media including 10% (w/w) gelatin, gum arabic and soluble starch. B. infantis CCRC 14633 and B. longum were also determined in skim milk. It was found that survival of bifidobacteria after spray-drying varied with strains and is highly dependent on the carriers used. Among the test organisms, B. longum B6 exhibited the least sensitivity to spray-drying and showed the highest survival of ca. 82.6% after drying with skim milk. Comparisons of the effect of carrier concentrations revealed that spray-drying at 10% (w/w) gelatin, gum arabic or soluble starch resulted in the highest survival of bifidobacteria. In addition, among the various outlet-air temperatures tested, bifidobacteria showed the highest survival after drying at 50 degrees C. Elevation of outlet-air temperature caused increased inactivation of bifidobacteria. However, the inactivation caused by increased outlet-air temperature varied with the carrier used, with the greatest reduction observed using soluble starch and the least with skim milk.

Animals↗
PubMed2005

Crystallization and X-ray diffraction of spray-dried and freeze-dried amorphous lactose.

Crystallization of spray-dried and freeze-dried amorphous lactose over different relative vapor pressures (RVP) and storage times was studied. Crystallization was observed from increasing peak intensities in X-ray diffraction patterns. Lactose was crystallized in the samples stored at RVP of 44.1% and above in both types of dehydrated powders. The rate of crystallization increased with increasing RVP and storage time. Similar crystallization behavior of both spray-dried and freeze-dried lactose was observed. Lactose crystallized as alpha-lactose monohydrate, anhydrous beta-lactose, and the anhydrous form of alpha- and beta-lactose in a molar ratio of 5:3 and 4:1 in both spray-dried and freeze-dried forms. Peak intensities of X-ray diffraction patterns for anhydrous beta-lactose were decreased, and for alpha-lactose monohydrate increased with increasing storage RVP and time. The crystallization data were successfully modeled using Avrami equation at RVP of 54.5% and above. The crystallization data obtained is helpful in understanding and predicting storage stability of lactose-containing food and pharmaceutical products.

Crystallization↗
PubMed2002

Release characteristics of the matrices prepared from co-spray-dried powders of theophylline and ethylcellulose.

Co-spray-dried powders of theophylline and ethylcellulose were prepared using aqueous ethylcellulose dispersion. Co-spray-dried powders were directly compressed into the matrices and the release characteristics of the prepared matrices were investigated. The co-spray-dried powders exhibited good matrix formations with high hardness at rather low compression force. The concentration of ethylcellulose in the matrices was, as expected, the rate-determining factor in controlling the release rate of the drug. Increasing the weight fractions of ethylcellulose resulted in a corresponding decrease in the drug release rates in both 0.1 N HCl and phosphate buffer pH 6.8. However, at the same level of ethylcellulose content, the drug release in acidic conditions was higher than in alkaline medium. To modify release characteristics of the matrices, PVP K30 and lactose were employed as channeling agents. At concentrations of 5 and 10%, PVP K30 was found to slow the drug release when incorporated into the co-spray-dried powder formulations containing 5% ethylcellulose. Lactose at a concentration of 15% provided an increasing effect on drug release when added in the formulations. But an increase in lactose quantity from 15 to 25% did not exert much more influence on release characteristics. Higuchi plots were found to be best applicable to all release data. Scanning electron microscopic examinations on the surface and cross-section of the matrices before and after subjection to release testing revealed the formation of porous networks within the matrices by the ethylcellulose fibers. Such polymeric networks would account for the controlled diffusion of the drug from the matrices.

Bronchodilator Agents↗
PubMed1984

Amorphous spray-dried hydroflumethiazide-polyvinylpyrrolidone systems: physiochemical properties.

Hydroflumethiazide was spray-dried with polyvinylpyrrolidone (PVP) to produce products containing 0-30% PVP. These systems were amorphous and differed from previously prepared coprecipitates of similar composition. Differential scanning calorimetry (DSC) suggested that at low PVP weight fractions both amorphous drug and an amorphous drug-PVP complex can be present in spray-dried systems. The apparent solubility of hydroflumethiazide in spray-dried products increased with increasing PVP content reaching a plateau value approximately four times that of the pure crystalline drug. The estimated free energy and entropy of the spray-dried drug were greater than that of crystalline drug and also increased with increasing PVP content. Dissolution studies with compressed discs supported the apparent solubility data. The results suggest that amorphous phases having different orders of organization are formed in spray-dried systems with increasing PVP content.

Chemical Phenomena↗
PubMedDate not supplied

Development of digoxin dry elixir as a novel dosage form using a spray-drying technique.

A rapidly absorbed new novel oral dosage form for digoxin termed 'digoxin dry elixir' was developed by the spray-drying technique. Digoxin, dextrin and sodium lauryl sulphate were dissolved in a ethanol-water mixture (20:25 w/w) and therefore spray-dried to form the digoxin dry elixir. According to scanning electron micrographs, digoxin dry elixir is spherical in shape with a smooth surface. The geometric mean diameter of dry elixir determined by laser particle size analysis was about 13 microns. The appearance and flow properties were almost unchanged and about 10% of ethanol contents in the dry elixir decreased during 180 days in a sealed bottle at room temperature. Comparative studies on the in vitro dissolution and in vivo absorption of digoxin in the form of digoxin dry elixir, digoxin elixir and digoxin powder were carried out. Digoxin in the dry elixirs was completely dissolved within 2 min. On the other hand, only about 87% of digoxin powder dissolved in 60 min. The initial dissolution rates of digoxin in the dry elixirs markedly increased in distilled water at 37 degrees C, which were over 100 fold higher than that of digoxin powder alone. The maximal plasma concentration of digoxin (Cmax) and area under the digoxin concentration-time curve from zero to 6 h (AUC0-6h) after the oral administration of digoxin dry elixir were almost 3.8 and 5.5 fold increased compared to digoxin powder alone. No significant difference of AUC0-6 h between dry elixir and elixir was observed, but the Cmax of digoxin in the form of dry elixir was significantly reduced compared to the digoxin elixir (0.57 versus 0.83). Digoxin dry elixir might be a useful solid dosage form to improve the dissolution rate and bioavailability of poorly water-soluble digoxin compared to digoxin powder alone. It also indicates that dry elixir might reduce the side effects in oral digitalis glycoside therapy compared to the digoxin elixir due to the reduction of Cmax.

Animals↗
PubMed2005

Spray-dried Amioca starch/Carbopol 974P mixtures as buccal bioadhesive carriers.

In the present study, spray-dried Amioca starch/Carbopol 974P mixtures were evaluated as potential buccal bioadhesive tablets. Carbopol (C 974P) concentrations from 5 to 75% were tested. All spray-dried mixtures showed a comparable or better bioadhesive capacity compared to a reference formulation (DDWM/C 974P 95/5). The bioadhesive capacities of Amioca/Carbopol 974P mixtures were improved by spray-drying. All spray-dried mixtures showed significantly higher work of adhesion values compared to their equivalent physical mixtures. The influence of Carbopol concentration on the in vivo adhesion time of placebo tablets and in vitro miconazole nitrate release was tested. The ratio Amioca/C 974P 70/30 showed the longest in vivo adhesion time (24.5+/-8.5 h). Lower and higher C 974P concentrations had a shorter in vivo adhesion time. The mixtures containing between 15 and 30% C 974P could all sustain the in vitro miconazole nitrate release over 20 h. Again, lower and higher C 974P concentrations showed a faster in vitro miconazole release. The drug loading capacity of a spray-dried mixture containing 20% C 974P was investigated in vivo in dogs using testosterone as model drug. The spray-dried mixture could be loaded with 60% drug without loosing its in vivo bioadhesive and pharmacokinetic properties.

Acrylates↗
PubMed2004

Aerosolisation of beclomethasone dipropionate using spray dried lactose/polyethylene glycol carriers.

The aim of this study was to characterize the physical properties of spray dried lactose in the presence of different polyethylene glycols (PEG 400, PEG 3000 and PEG 6000) and to evaluate their performance as carriers for dry powder inhaler (DPI) formulations. The efficiency of spray dried lactose/PEG carriers in aerosolisation of beclomethasone dipropionate (BD), a model hydrophobic drug, was compared to Pharmatose 325 M (L325), spray dried lactose alone (SDL), and also a sieved (< 38 microm) fraction of alpha-lactose monohydrate (SL). In vitro deposition analysis was performed using a twin stage liquid impinger at a flow rate of 60 l/min through a Spinhaler. The deposition profiles of the drug from binary formulations composed of BD and spray dried lactose/PEG carriers were also compared to ternary formulations containing large and fine lactose carriers. Differential scanning calorimetry and X-ray diffraction data showed the presence of alpha-anhydrous lactose in spray dried lactose/PEG crystalline powders. Spray drying of lactose in the presence of PEG 400 resulted in the production of a powder (SDL-PEG400) with lower alpha-lactose monohydrate content, and also smaller particle size distribution than those obtained in the presence of PEG 3000 (SDL-PEG3000) or PEG 6000 (SDL-PEG6000). All formulations showed different deposition profiles, except those containing SDL-PEG3000 or SDL-PEG6000 which exhibited similar data. The fine particle fraction of aerosolised BD varied from 6.26 +/- 1.07 (for L325) to 25.87 +/- 5.33 (for SDL-PEG3000). All deposition profiles of BD aerosolised from SDL-PEG3000 were significantly higher (P < 0.01) than those produced by binary and ternary formulations containing L325, a coarse lactose commercially available for DPI formulations. The differences observed in deposition data for various carriers were interpreted according to their physical properties. It was concluded that particle size distribution, morphology and specific surface texture of SDL-PEG3000 and SDL-PEG6000 were important factors influencing their efficiency as small carriers for DPI formulations.

Aerosols↗
PubMed2004

Physical stability of salmon calcitonin spray-dried powders for inhalation.

The effects of excipient crystallinity and water content on the physical stability of salmon calcitonin (sCT) in a spray-dried powder for inhalation have been investigated. sCT was dissolved in water with and without mannitol and then spray dried using a Büchi 190 spray dryer. The spray dried powders were stored for 5 days at 0, 29, 51, 58, 69, and 84% relative humidity at ambient temperature. The crystalline content, water content, secondary structure, and aggregation rates were determined for each powder immediately following spray drying and after storage at various relative humidities. In addition, the water sorption isotherms and reactivity to water vapor were determined using DVS and isothermal calorimetry, respectively. No sCT aggregation occurred during the spray drying process. Crystallinity depended on the amount of mannitol in the formulation. Powders containing up to 50% mannitol were fully amorphous, and those containing 70 and 90% mannitol contained some crystalline polyol. The powders remained aggregate free for over 2 years when stored below the critical RH (e.g., <20% for the powder containing 30% mannitol). Above this RH, sCT aggregation increased as a function of time. The amount of aggregate observed correlates with the amount of intermolecular beta-sheet formed, determined by FTIR. The sCT aggregation rate in powders containing 70% mannitol was significantly lower than that in powders containing 30% mannitol at all RH tested, presumably because of a higher ratio of amorphous mannitol to sCT, which inhibits the formation of beta-sheet structure. Moisture-induced crystallization of mannitol was observed in all powders stored at RH >50%. The moisture induced thermal activity trace (MITAT) offers a useful description on the physical stability of the spray dried powders. In conclusion, spray drying sCT and sCT/mannitol mixtures yields dry powders that contain physically intact peptide. In addition, sCT aggregation and mannitol crystallization in spray dried powders can be prevented during long-term storage if stored in low humidity environments, which can be easily assessed by MITAT.

Administration, Inhalation↗
PubMed1999

Hydroxypropyl-beta-cyclodextrin inhibits spray-drying-induced inactivation of beta-galactosidase.

The single-step, fast spray-drying process may represent a valuable alternative to the multistep, time-consuming freeze-drying process in the area of formulation and processing of biopharmaceuticals. In this study, we tested the use of sucrose and hydroxypropyl-beta-cyclodextrin (HP-beta-CD) as stabilizing excipients in the spray-drying of a model protein, beta-galactosidase. The solutions were processed using a Büchi 190 cocurrent Mini Spray Dryer at an outlet temperature of 61 +/- 2 degrees C. The powders were redissolved and analyzed for catalytic activity, aggregation, chemical decomposition, and thermal susceptibility as observed by high-resolution calorimetry. Spray-drying significantly inactivated beta-galactosidase. Spray-drying beta-galactosidase in the presence of sucrose did not prevent inactivation. However, after spray-drying beta-galactosidase in the presence of HP-beta-CD, or HP-beta-CD and sucrose, full catalytic activity was exhibited on reconstitution. Furthermore, the reconstituted product was unchanged in terms of molecular weight, charge, and thermal stability. These findings are consistent with a hypothesis that the change responsible for inactivation of beta-galactosidase was mainly a monomolecular, noncovalent change, i. e., the formation of incorrect structures, that arose from surface denaturation. This study clearly demonstrates that cyclodextrins can be useful stabilizing excipients in the preparation of spray-dried protein pharmaceuticals.

2-Hydroxypropyl-beta-cyclodextrin↗
PubMed1982

Preparations of solid particulates of theophylline--ethylenediamine complex by a spray-drying technique.

Aqueous solutions of ethylenediamine and theophylline were spray dried to obtain solid particulates of theophylline--ethylenediamine complex to improve solubility of theophylline. Packing and flow properties of the spray-dried products were much improved when compared with those of original theophylline particles, due to their spherical shapes which were confirmed by a scanning electron microscope. The solubility of theophylline in the resultant products was found to be three to five times higher than that of original theophylline. The solubilities of the products decreased with increasing drying temperature and rotation speed of the atomizer, which was interpreted in terms of the contents of ethylenediamine in the products. The products were confirmed to be a mixture of aminophylline, alpha-aminophylline, and theophylline by X-ray analysis and NMR spectroscopy. The logarithm of the relative intensity of the X-ray diffraction peak of alpha-aminophylline to that of theophylline decreased linearly with drying temperature and rotation speed of the atomizer. Thermal decomposition of the spray-dried products involved liberations of crystal water at 100 degrees and ethylenediamine between 110 and 127 degrees. Liberation of ethylenediamine occurred via three steps for aminophylline, but with different steps for the spray-dried products.

Aerosols↗