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PubMed2004

Molecular reactivity of busulfan through its experimental electrostatic properties in the solid state.

PURPOSE: In the route of developing novel liquid phase formulations based on the encapsulation of busulfan into liposomes in nontoxic solvents, drug crystallization inevitably occurs. In order to better understand the reactivity of busulfan, the characterization of its molecular properties was therefore considered as a key point. Also, preliminary attempts to prevent crystallization using cyclodextrins were explored. METHODS: An accurate single-crystal high-resolution X-ray diffraction experiment at 100 K has been carried out. The experimental electron density of busulfan was refined using a multipole model. Busulfan/beta-cyclodextrin coprecipitates were analyzed by powder X-ray diffraction and 1H-NMR spectroscopy. RESULTS: The electrostatic properties of busulfan and the methylsulfonate fragment dipole moment (3.2 D) were determined. The polar moieties play a key role in the crystallization of busulfan, which presents a nucleophilic region surrounding the sulfonate part, whereas the carbon chain displays an electrophilic character. This highlights the subtle busulfan/beta-cyclodextrin association. CONCLUSIONS: Busulfan electrostatic properties were used to quantify its chemical reactivity. This explains the difficulty to formulate busulfan into liposomes due to a strong polar character of the methylsulfonate terminal groups. The complexation with cyclodextrins deserves to be further investigated to allow the formulation of busulfan in nontoxic solvents.

Busulfan↗
PubMed2001

Chemistry-structure-simulation or chemistry-simulation-structure sequences? The case of MIL-34, a new porous aluminophosphate.

A new aluminophosphate, MIL-34, is investigated from its as-synthesized structure to its calcined microporous form. Single-crystal X-ray diffraction measurements on the as-synthesized MIL-34 (Al(4)(PO(4))(4)OH x C(4)H(10)N, space group P-1, a = 8.701(3) A, b = 9.210(3) A, c = 12.385(3) A, alpha = 111.11(2) degrees, beta = 101.42(2) degrees, gamma = 102.08(2) degrees, V = 863.8(4) A(3), Z = 2, R = 3.8%) reveal a 3-D open framework where Al atoms are in both tetrahedral and trigonal bipyramidal coordinations. It contains a 2-D pore system defined by eight rings where channels along [100] cross channels running along [010] and [110]. CBuA molecules are trapped at their intersection. (27)Al, (31)P, and (1)H MAS NMR spectroscopies corroborate these structural features. Calcination treatments of a powder sample of the as-synthesized MIL-34 indicate its transformation into the related template-free structure that is stable up to 1000 degrees C. Lattice energy minimizations are then used in order to anticipate the crystal structure of the calcined MIL-34, starting with the knowledge of the as-synthesized structure exclusively. Energy minimizations predict a new regular zeotype structure (AlPO(4), space group P-1, a = 8.706 A, b = 8.749 A, c = 12.768 A, alpha = 111.17 degrees, beta = 97.70 degrees, gamma = 105.14 degrees, V = 846.75 A(3), Z = 2) together with a thermodynamic stability similar to that of existing zeotype AlPOs. Excellent agreement is observed between the diffraction pattern calculated from the predicted calcined MIL-34 and the experimental X-ray powder diffraction pattern of the calcined sample. Finally, the atomic coordinates and cell parameters of the calcined MIL-34 predicted from the simulations are used to perform the Rietveld refinement of the calcined sample powder pattern, further corroborated by (27)Al and (31)P NMR measurements. This unique combination of experiment and simulation approaches is an interesting and innovative strategy in materials sciences, where simulations articulate the prediction of a possible template-free framework from its as-synthesized templated form. This is especially valuable when straightforward characterizations of the solid of interest with conventional techniques are not easy to carry out.

Journal Article↗
PubMed1988

Biophysical study of bone mineral in biopsies of osteoporotic patients before and after long-term treatment with fluoride.

Crystallographic characteristics of bone mineral were examined in a group of 60 osteoporotic patients before and after 3 to 6 years of fluoride therapy. The age of the mineral was evaluated by means of X-ray absorption, as degree of mineralization of bone tissue (MDBT). Crystallinity was evaluated by measuring both X-ray diffraction line broadening, beta (31.0) and beta (00.2), and the crystallinity index (CI) by infrared spectrometry. The a and c unit-cell parameters were determined by powder X-ray diffraction. Bone fluoride content was measured by specific electrode. Patients were divided in two groups according to MDBT before treatment: one group with MDBT values less than or equal to mean value; another group with MDBT values greater than mean value. In the first group, trabecular bone volume (TBV) did not change significantly during therapy. In the second group, an increase of TBV was observed. Osteoporoses can then be distinguished, on MDBT criterion, between osteoporosis with hypermaturated mineral and osteoporosis with hypomaturated mineral. The MDBT before treatment permits one to predict the effect of fluoride therapy on TBV. In the two groups there was a significant increase in bone fluoride content between the onset and the end of treatment. Bone fluoride content increased linearly during therapy without any plateau effect. Crystallographic modifications induced by fluoride explain the mechanical and chemical improvement of bone.

Adult↗
PubMed2000

Crystalline versus amorphous content of lumaxistrade mark analog XP280 using X-ray and electron diffraction methods.

In the course of the development of Lumaxistrade mark (roxifiban), the physical state of XP280 (the besylate salt of the active metabolites of roxifiban) and SC887 (the mesylate salt of the free base of roxifiban) were characterized. Powder X-ray diffraction patterns of XP280 were ambiguous in that a high degree of background signal was present and potentially indicative of the existence of an amorphous phase. Herein the results of combined synchrotron X-ray diffraction and electron microscopy (diffraction and imaging) studies on XP280 and SC887 are reported. The combination of these two techniques allowed an unambiguous assessment of the crystallinity, as well as determination of four of the unit cell parameters of XP280 and complete determination of the unit cell parameters for SC887.

Amidines↗
PubMed2006

Development of a laser diffraction method for the determination of the particle size of aerosolised powder formulations.

Impactor data are an essential component of marketing authorisation for new dry powder aerosol formulations. However such data are time-consuming to obtain and therefore impede the rapid screening of pilot formulations. In this phase of development it would be of considerable benefit to employ a technique where data acquisition was more rapid, such as laser diffraction, to predict the fine particle fraction. It was the aim of this study to investigate whether this is a feasible premise. Five different formulations were prepared, each containing 1.5% (w/w) micronised salbutamol base (volume median diameter: 2.42 microm) blended with the sieved fraction (63-90 microm) of one of the following sugars: regular crystalline lactose, spray dried lactose "Zeparox", sorbitol, maltose and dextrose monohydrate. A Perspex box was constructed to contain particles released from a glass inhaler and allow the particles to be measured by laser diffraction at different flow rates. After being validated using monodisperse aerosols, this assembly was then employed to measure the particle size distributions of each powder formulation and its respective sugar carrier at flow rates ranging from 28.3 to 100 l min(-1). Aerodynamic particle size distribution of salbutamol base from each formulation was also measured after aerosolisation at 28.3 l min(-1) from the glass inhaler into an Andersen cascade impactor. The flight of monodisperse particles with diameters (2-6 microm) in the desired size range of dry powders for inhalation could be contained and the size distribution determined by laser diffraction using the assembly at all flow rates investigated. Treatment of the particle size distributions measured by laser diffraction, i.e. examining only the aerosol particles with diameter <60 microm, highlighted the fine fraction (<5 microm) and enabled the aerosolisation of different blends to be feasibly compared at a range of different flow rates. The blends containing the following excipients could be placed in the following order of increasing fine fraction: spray-dried lactose<dextrose<<maltose<lactose<sorbitol. At 28.3 l min(-1) a significant linear correlation was found between the fine fractions measured by laser diffraction and the salbutamol fine fractions determined by inertial impaction (R(2)=87.4%, p=0.02, ANOVA). Therefore, the laser diffraction technique could prove to be an important tool for particle size characterisation of dry powder aerosol formulations.

Aerosols↗
PubMed2002

Structure of nanocrystalline anatase solved and refined from electron powder data.

Energy-filtered Debye-Scherrer electron powder data have been successfully employed to determine the structure of nanocrystalline anatase (TiO2). The performed structure analysis includes determining the unit cell, space group, solving the structure via direct methods from extracted intensities and refining the structure using the Rietveld technique. The refined structural parameters for space group I4(1)/amd are a = 3.872 (2), c = 9.616 (5) A with titanium at 0.5,0.75,0.375 and oxygen at 0.5,0.75,0.1618 (6). The obtained structure indicates low internal stress as judged from the almost regular geometry of the TiO6 building blocks. Striking resemblance with the anatase structure determined previously by Burdett, Hughbanks, Miller, Richardson & Smith [J. Am. Chem. Soc. (1987). 109, 3639-3646] from neutron diffraction on coarse-grained material gives strong support for the correctness of the structure determined here. The result of the present study shows that the methods originally developed for determining structures from X-ray powder data work equally well with data from electron powder diffraction. This may open the window for structural investigations on the vast number of nanocrystalline materials and thin films whose structures are difficult to determine by X-ray diffraction since they are frequently only available in small quantities.

Journal Article↗
PubMed1995

Process-induced crystallinity changes in albuterol sulfate and its effect on powder physical stability.

Pharmaceutical powders are often milled to achieve the optimum particle size. These size reduction processes can introduce dislocations and/or defects onto particle surfaces affecting the overall crystallinity of the powder. If enough energy is imparted, amorphous regions on the particle surfaces may be produced. These amorphous regions have the propensity to absorb significant quantities of water. In this study the effect of sorbed water on the physical characteristics of albuterol sulfate is investigated. Physical properties of this compound are studied in both micronized and unmicronized states using scanning electron microscopy, differential scanning calorimetry, powder x-ray diffraction, solution microcalorimetry, laser diffraction particle size analysis and water vapor sorption analysis. Subtle differences in crystallinity induced by air jet micronization are detected by several analytical methods. Amorphous to crystalline conversions are observed, the kinetics of which are found to be both temperature and relative humidity dependent. These experiments show the dynamic nature of micronized albuterol sulfate and aid in the determination of the actual physical state of this pharmaceutical powder.

Albuterol↗
PubMed2005

Preparation and characterization of inclusion complexes of beta-cyclodextrin with ionic liquid.

The solubilities of beta-cyclodextrin (beta-CD), ionic liquid (IL) 1-butyl-3-methylimidazolium hexafluorophosphate (bmimPF6), and their mixture in water were determined, and the conductivity of these aqueous solutions was measured. It was demonstrated that beta-CD and bmimPF6 could enhance the solubility of each other, and the solubility curves of each were linear with gradients of about 1. The conductivity decreased remarkably with increasing beta-CD concentration, and a discernible break in the conductivity curve could be observed when beta-CD and bmimPF6 were equimolar in the solution. The solubility and conductivity results indicated that inclusion complexes (ICs) of 1:1 stoichiometry were formed. The inclusion compounds were further characterized by using powder X-ray diffraction (XRD) analysis, 13C CP/MAS (cross-polarization magic-angle spinning) NMR and 1H NMR spectroscopy, and thermogravimetric analysis (TGA). The results showed that the ICs were a fine crystalline powder. The host-guest system exhibited a channel-type structure and each glucose unit of beta-CD was in a similar environment. The decomposition temperature of the ICs was lower than that of bmimPF6 and beta-CD individually.

Journal Article↗
PubMed2006

Conformational, concomitant polymorphs of 4,4-diphenyl-2,5-cyclohexadienone: conformation and lattice energy compensation in the kinetic and thermodynamic forms.

4,4-Diphenyl-2,5-cyclohexadienone (1) crystallized as four conformational polymorphs and a record number of 19 crystallographically independent molecules have been characterized by low-temperature X-ray diffraction: form A (P2(1), Z'=1), form B (P1, Z'=4), form C (P1, Z'=12), and form D (Pbca, Z'=2). We have now confirmed by variable-temperature powder X-ray diffraction that form A is the thermodynamic polymorph and B is the kinetic form of the enantiotropic system A-D. Differences in the packing of the molecules in these polymorphs result from different acidic C-H donors approaching the C=O acceptor in C-H...O chains and in synthons I-III, depending on the molecular conformation. The strength of the C-HO interaction in a particular structure correlates with the number of symmetry-independent conformations (Z') in that polymorph, that is, a short C-HO interaction leads to a high Z' value. Molecular conformation (Econf) and lattice energy (Ulatt) contributions compensate each other in crystal structures A, B, and D resulting in very similar total energies: Etotal of the stable form A=1.22 kcal mol(-1), the metastable form B=1.49 kcal mol(-1), and form D=1.98 kcal mol(-1). Disappeared polymorph C is postulated as a high-Z', high-energy precursor of kinetic form B. Thermodynamic form A matches with the third lowest energy frame based on the value of Ulatt determined in the crystal structure prediction (Cerius2, COMPASS) by full-body minimization. Re-ranking the calculated frames on consideration of both Econf (Spartan 04) and Ulatt energies gives a perfect match of frame #1 with stable structure A. Diphenylquinone 1 is an experimental benchmark used to validate accurate crystal structure energies of the kinetic and thermodynamic polymorphs separated by <0.3 kcal mol(-1) (approximately 1.3 kJ mol(-1)).

Journal Article↗
PubMed1996

Solid State Dynamics of Tricarbonyl(eta-1,5-cyclohexadienylium)iron Tetrafluoroborate and Tricarbonyl(eta-1,5-cycloheptadienylium)iron Tetrafluoroborate.

The dynamic behavior of [(C(6)H(7))Fe(CO)(3)]BF(4) (I) and [(C(7)H(9))Fe(CO)(3)]BF(4) (II) in the solid state has been investigated principally by NMR spectroscopy. High-resolution variable-temperature (1)H and (13)C NMR spectra indicate that both complexes have a solid state phase transition above which there is rapid reorientation of the cyclodienylium rings and fast exchange of the carbonyl groups. The transition occurs between 253 and 263 K for I and between 329 and 341 K for II. The presence of the phase transition is confirmed by differential scanning calorimetry (DSC). (57)Fe Mössbauer spectroscopy supports the notion that complex I is highly mobile at room temperature, while II is relatively static. The activation energy for the cyclodienylium group rotation in the high-temperature phase of I is estimated from (1)H spin-lattice relaxation time measurements to be 17.5 kJ mol(-)(1). Static (13)C NMR measurements of the solid complexes in the high-temperature phase indicate that the (13)C chemical shift anisotropies are only 20-30 ppm. This is significantly less than that expected to result from motion of individual groups and thus suggests that rotation of the whole molecule is involved. A single-crystal X-ray structural determination of complex II, at 295 K, showed that the complex is tetragonal (space group P4(1), a = 10.610(1) Å, c = 21.761(3) Å, V = 2449.7(5) Å(3), rho(calc) = 1.734 g cm(-)(3)), with eight cycloheptadienyl cations and eight tetrafluoroborate anions per unit cell. In addition, powder X-ray diffraction studies of both I and II confirm that at low temperatures both complexes have a tetragonal unit cell, which transforms to a cubic unit cell above the phase transition. The powder patterns, recorded above the phase transition, support the proposal that the complexes are undergoing whole-molecule tumbling in their dynamic regimes.

Journal Article↗
PubMed2006

Physical and thermal characterisation of chiral omeprazole sodium salts.

The physical properties of drug substances may affect stability, manufacturing, dissolution and bioavailability. Variations in the degree of crystallinity in a pharmaceutical substance may exhibit physicochemical differences that impact at therapeutic, manufacturing, commercial and legal levels, yet no reference has been found on the physical properties of micronised omeprazole. This study reports on the physical and thermal characterisation of the sodium salts of S- and R-omeprazole, using diffuse reflectance infrared Fourier transform spectroscopy (DRIFT), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), microthermal analysis (microTA) and powder X-ray diffraction (XRPD). DSC experiments were performed in order to determine not only their thermal stability, but also the thermal history of both forms. SEM results indicate similar morphology, particle size and shape of powdered drug, while, microTA of processed discs shows different topographical images for S- and R-omeprazole, exhibiting a smoother surface for the S-form, indicative of the smoother particle size not evident in the SEM results. The low level of crystallinity of both enantiomers was confirmed by DRIFT spectroscopy and XRPD. Thermal stability by DSC of S- and R-omeprazole sodium salts was superior to that of the neutral omeprazole. This study has examined the physical and thermal properties of both forms and in highlighting their differences provides an explanation for the potential differences in bioavailability and therapeutic efficacy.

Calorimetry, Differential Scanning↗
PubMed1996

A New Family of Nonstoichiometric Layered Rare-Earth Tin Antimonides, RESn(x)()Sb(2) (RE = La, Ce, Pr, Nd, Sm): Crystal Structure of LaSn(0.75)Sb(2).

A new class of nonstoichiometric layered ternary rare-earth tin antimonides, RESn(x)()Sb(2) (RE = La, Ce, Pr, Nd, Sm), has been synthesized through reaction of the elements at 950 degrees C. In the lanthanum series LaSn(x)()Sb(2), tin can be incorporated from a maximum content of x approximately 0.7 or 0.8 to as low as x approximately 0.10. The structure of lanthanum tin diantimonide with the maximum tin content, LaSn(0.75)Sb(2), has been determined by single-crystal X-ray diffraction methods. It crystallizes in the orthorhombic space group -Cmcm with a = 4.2425(5) Å, b = 23.121(2) Å, c = 4.5053(6) Å, and Z = 4. The isostructural rare-earth analogues were characterized by powder X-ray diffraction. The structure of LaSn(0.75)Sb(2) comprises layers of composition "LaSb(2)" in which La atoms are coordinated by Sb atoms in a square-antiprismatic geometry. Between these layers reside chains of Sn atoms distributed over three crystallographically independent sites, each partially occupied at about 20%. The structure of LaSn(0.75)Sb(2) can be regarded as resulting from the excision of RE-Sb and Sb-Sb bonds in the related structures of binary rare-earth diantimonides, RESb(2), and then intercalation of Sn atoms between layers.

Journal Article↗
PubMed2004

Diruthenium tetraacetate monocation, [RuII/III2(O2CMe)4]+, building blocks for 3-D molecule-based magnets.

Diruthenium tetracarboxylates monocations are utilized as building blocks for cubic 3-D network structured molecule-based magnets. [Ru(II/III)(2)(O(2)CMe)(4)](3)[M(III)(CN)(6)] [M = Cr (1a), Fe (2), Co (3)] were prepared in aqueous solution. Powder X-ray diffraction indicates that they have body-centered cubic structures (space group = Imm, a = 13.34, 13.30, and 13.10 A for 1a, 2, and 3, respectively), which was confirmed for 1a by Reitveld analysis of the synchrotron powder data [a = 13.3756(5) A]. [Ru(2)(O(2)CMe)(4)](3)[M(III)(CN)(6)].xMeCN [M = Cr, x = 1.8 (1b); M = Mn, x = 3.3 (4)] were prepared from acetonitrile. The magnetic ordering of 1a (33 K), 1b (34.5 K), 2 (2.1 K), and 4 (9.6 K) was determined from the temperature dependencies of the in-phase (chi') alternating current (AC) susceptibility. The field dependence of the magnetization, M(H), at 2 K for 1a showed an unusual constricted hysteresis loop with a coercive field, H(cr), of 470 Oe while the M(H) data for 1b, 2, and 4 showed a normal hysteresis loop with a coercive field of 1670, 10, and 990 Oe, respectively. The (57)Fe Mössbauer spectrum of 2 is consistent with the presence of low spin Fe(III) (delta = -0.05 mm/s; DeltaE = 0.33 mm/s) at room temperature, and the onset of 3-D magnetic ordering at lower temperature (<2 K). The effects of M(III) in [M(III)(CN)(6)](3-), and the large zero-field splitting (D) of diruthenium tetracarboxylates are discussed. The increasing critical temperatures T(c), with increasing S could not be accounted for by mean field models without significantly different J values for 1a, 4, and 2. By fitting the T(c) data with mean field models [H = -2JS(Ru).(S(M) - micro(B)(g(Ru)S(Ru) + g(M)S(M))H], J/k(B) are 4.46, 1.90, and 0.70 K for 1a, 4, and 2, respectively.

Journal Article↗
PubMed2003

Modulated structure of solid iodine during its molecular dissociation under high pressure.

The application of pressure to solid iodine forces the molecules in the crystal to approach each other until intermolecular distances become comparable to the bond length of iodine; at this point, the molecules lose their identity and are essentially dissociated. According to room-temperature X-ray diffraction studies, this process involves direct dissociation of iodine molecules at about 21 GPa, whereas spectroscopic observations have identified intermediate molecular phases at pressures ranging from 15 to 30 GPa. Here we present quasi-hydrostatic powder X-ray diffraction measurements that clearly reveal an intermediate phase during the pressure-induced dissociation of solid iodine. We find that, similar to the behaviour seen in uranium, the structure of this intermediate phase is incommensurately modulated, with the nearest interatomic distances continuously distributed over the range 2.86-3.11 A. The shortest of these interatomic distances falls between the bond length of iodine in the molecular crystal (2.75 A) and the nearest interatomic distance in the fully dissociated monatomic crystal (2.89 A), implying that the intermediate phase is a transient state during molecular dissociation. We expect that further measurements at different temperatures will help to elucidate the origin and stability of the incommensurate structure, which might lead to a better understanding of the molecular-level mechanism of the pressure-induced dissociation seen here and in the molecular crystals of hydrogen, oxygen and nitrogen.

Journal Article↗
PubMed1997

[Studies on X-ray diffraction pattern of traditional Chinese medicinal materials].

Traditional Chinese medicine(TCM) as prescribed by Chinese traditional physicians is usually available as "decoction slices" which calls for a ready method for assessment of quantity or even genuineness. Three groups of TCM drugs (radix Rubiae, bulbus Fritillariae and rhizoma Dioscoreae) were selected by using powder X-ray diffraction analysis with complete absorption profile. Topological regularity and characteristic peaks of the absorption profile were obtained as fingerprint in X-ray diffraction diagrams of the pertinent medicinal materials. We have discovered the similarities of 3 radix Rubiae samples gathered from different localities and their differences with Rubia tinctorum, the similarities and differences between 7 species belonging to Fritillaria Genus, the similarities of 2 rhizoma Dioscoreae samples from different localities and their differences with 2 counterfeits. The result points to a promising prospect in achieving an objective assessment of genuineness at TCM drugs.

Drugs, Chinese Herbal↗
PubMed2005

Hydrothermal synthesis and characterization of a layered cobalt phenylphosphonate, Co(PhPO3)(H2O).

We report the hydrothermal synthesis and characterization of a layered cobalt phenylphosphonate. Unlike most metal phosphonates reported to date, the structure was solved by single crystal X-ray diffraction (SC-XRD). Co(ii) centres are hexa-coordinated by oxygen and the octahedra corner-share into a layer. The layers are capped by phenylphosphonate groups, where the phenyl groups define a hydrophobic bilayer region. The material was also characterized by powder X-ray diffraction (PXRD), thermogravimetric analysis (TGA) and SQUID (superconducting quantum interference device) magnetometry. The material undergoes an antiferromagnetic transition at a relatively low Néel temperature of 4.0 K, while the Curie-Weiss temperature of -76.5 K reflects the low-dimensionality of the magnetic structure. The effective magnetic moment of 5.01 micro(B) per Co(2+) verifies a high-spin configuration and an octahedral coordination of the metal centres. This layered material was correctly predicted in the literature from powder data, adds to the structural diversity of the cobalt phosphonates, and may be useful as an intercalation or exfoliation compound.

Journal Article↗
PubMed2002

Improvement of solubility and oral bioavailability of a poorly water-soluble drug, TAS-301, by its melt-adsorption on a porous calcium silicate.

The aim of the present study was to improve the solubility and oral bioavailability of a poorly water-soluble drug, 3-bis(4-methoxyphenyl) methylene-2-indolinone (TAS-301), by its melt-adsorption on a porous calcium silicate, Florite RE (FLR), without any solvents. The melt-adsorbed products were prepared by two methods: the small-scale batch method and the twin screw extruder method. The drug was melted and adsorbed on FLR (i.e., "melt-adsorption"), above its melting point. Crystallinity of the drug in the melt-adsorbed product was estimated by differential scanning calorimetry (DSC) and powder X-ray diffraction analysis. The dissolution test was conducted by the JP XIII paddle method. Oral absorption of the melt-adsorbed product was studied in fasted and fed dogs. The melt-adsorbed products prepared by the two methods were in powder forms. The drug existed in an amorphous state in the product and hardly recrystallized even after storing at a stressed condition (60 degrees C/80% RH for 3 days). The TAS-301 dissolution rate from the melt-adsorbed product was markedly enhanced compared with drug crystals. The area under the plasma concentration-time curve (AUC) and peak concentration (C(max)) values of the drug after dosing the melt-adsorbed product were significantly greater than those after dosing the drug crystals. The solubility and bioavailability of TAS-301 were improved by its melt-adsorption on FLR. The present findings suggest melt-adsorption is a useful technique for improving solubility and bioavailability of poorly water-soluble drugs.

Administration, Oral↗