Abstract：
:The spherically agglomerated crystals of aminophylline (theophylline-ethylenediamine complex) can be compounded directly into pharmaceutical formulations without further processing, e.g., granulation. Such crystals were prepared by mixing theophylline and ethylenediamine in a partially miscible solvent system, i.e., organic solvent-ethanol-water. The organic solvents used were chloroform, 1-hexanol, isopropyl acetate, isobutyl acetate, isoamyl acetate, benzene, toluene, n-hexane, or n-heptane. Spherical crystallization depended upon the solubility of theophylline in the solvent mixture. The resultant agglomerated crystals were identical with the theophylline-ethylenediamine complex by IR, X-ray, and differential scanning calorimetry analyses, and was the alpha-, beta-, or gamma-form when the water of crystallization was less than or equal to 0.5, 1.0, and 2.5 mol, respectively. When the amount of ethylenediamine used was less than 1.1 mL (0.0165 mol), the resultant agglomerated crystals were converted to anhydrous theophylline by washing with ethanol. When water was added to the system (greater than or equal to 0.3 mL, i.e., 0.0167 mol), water was occluded in the resultant agglomerates as water of crystallization. Ethylenediamine content in the agglomerated crystals could be controlled by changing the amount of ethylenediamine added in the crystallization solvent.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Kawashima Y,Aoki S,Takenaka H,Miyake Ydoi
10.1002/jps.2600731021subject
Has Abstractpub_date
1984-10-01 00:00:00pages
1407-10issue
10eissn
0022-3549issn
1520-6017pii
S0022-3549(15)46373-7journal_volume
73pub_type
杂志文章abstract：:A method to determine drugs having a carbothionamido group using an ammonia gas-sensing electrode is described. To obtain analytical accuracy, the effect of factors that influence the potential is also discussed. Ethionamide or prothionamide was refluxed with 20% HCl to give ammonium chloride, hydrogen sulfide, and a ...
journal_title：Journal of pharmaceutical sciences
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abstract：:The permeability coefficient, Kp, of pure unbranched alkanoic acids (C2-C7) applied to isolated porcine skin, reached a maximum in the solubility parameter (delta 2) range of 9.7-10 cal1 /2/cm3/2. When these and other penetrants were delivered from a solvent vehicle, the following linear relationships could be demonst...
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doi：10.1002/jps.2600730426
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abstract：:Transdermal delivery of fentanyl from various adhesive matrix formulations to achieve a steady-state skin flux was investigated. For this purpose, various pressure-sensitive adhesives selected from the three chemical classes of polymers (polyisobutylene (PIB), acrylate, and silicone adhesives) were characterized with ...
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更新日期：1996-05-01 00:00:00
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doi：10.1002/jps.2600700519
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abstract：:Racemic and homochiral sodium ibuprofen were characterized by thermal analysis and powder X-ray diffractometry. The melting point phase diagram was constructed and thermodynamic calculation was performed. In contrast to racemic ibuprofen, which is a racemic compound, racemic sodium ibuprofen forms both a racemic congl...
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abstract：:Melphalan (30 microgram/ml) is completely hydrolyzed in water at 37 degrees after 8 hr. At lower temperatures, hydrolysis proceeds at slower rates. The presence of bovine serum albumin retards hydrolysis of melphalan (30 microgram/ml) in water. The melphalan hydrolysis rate is directely releated to the bovine serum al...
journal_title：Journal of pharmaceutical sciences
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更新日期：1978-05-01 00:00:00
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更新日期：1986-09-01 00:00:00
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doi：10.1002/jps.2600800113
更新日期：1991-01-01 00:00:00
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abstract：:Die filling is a critical process step during tablet production as it defines the tablet weight. Achieving die fill consistency during production of mini-tablets, tablets with diameters ≤6 mm, is considerably more challenging. Although die filling in rotary presses had been studied in relation to the feed paddle desig...
journal_title：Journal of pharmaceutical sciences
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更新日期：2019-03-01 00:00:00
abstract：:The crystal and molecular structures of 6-methylmercaptopurine trihydrate and of azathioprine dihydrate were determined by the use of three-dimensional, X-ray, diffractometer data and were refined by least squares. Both molecules crystallize in the N(9)-H tautomer form, in contrast to the N(7)-H tautomer form found in...
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doi：10.1002/jps.2600640206
更新日期：1975-02-01 00:00:00
abstract：:A series of 4-substituted aminoquinoline-3-carboxylates was prepared and evaluated for antimicrobial activity. Four of the compounds (VIII, XIII, XV, and XXIII) exhibited low activity against Staphylococcus aureus. ...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600730828
更新日期：1984-08-01 00:00:00
abstract：:Near-infrared spectroscopy was used to monitor the phase conversion for two solvatomorphs of caffeine, an anhydrous form and a nonstoichiometric hydrate, as a function of time, temperature, and relative humidity. The transformation kinetics between these caffeine forms was determined to increase with temperature. The ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20941
更新日期：2007-05-01 00:00:00
abstract：:The preformulation, solubilization and pharmacokinetic evaluation of antalarmin, a stress inhibitor, have been conducted. Antalarmin has a poor water solubility of less than 1 microg/mL and is weakly basic with an experimentally determined pK(a) of 5.0. Multiple solubilization approaches including pH-control either al...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.21421
更新日期：2009-01-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1016/j.xphs.2019.06.006
更新日期：2019-10-01 00:00:00
abstract：:5-aminolevulinic acid (ALA) is used as a precursor of protoporphyrin IX (PpIX) for photodynamic therapy (PDT) of superficial skin cancers and subcutaneous metastases of internal malignancies. The permeability of ALA across intact skin is always low, making it difficult to achieve the desired therapeutic benefits. Henc...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20577
更新日期：2006-04-01 00:00:00
abstract：:The objective of this study was to determine if a high Tg polymer (Eudragit(®) S100) could be used to stabilize amorphous domains of polyethylene oxide (PEO) and hence improve the stability of binary polymer systems containing celecoxib (CX). We propose a novel method of stabilizing the amorphous PEO solid dispersion ...
journal_title：Journal of pharmaceutical sciences
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doi：10.1016/j.xphs.2016.06.004
更新日期：2016-10-01 00:00:00
abstract：:Formulation pH has been reported to be responsible for the incidence of phlebitis. In this study, the effect of pH on injection phlebitis is investigated. Buffers of varying pHs were examined for their ability to produce phlebitis in rabbits. Thermal measurements as well as visual evaluations were used for phlebitis q...
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doi：10.1002/jps.2600840427
更新日期：1995-04-01 00:00:00
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更新日期：2020-11-26 00:00:00
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更新日期：1999-01-01 00:00:00
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更新日期：2021-01-01 00:00:00
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更新日期：1984-07-01 00:00:00
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更新日期：1995-09-01 00:00:00
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更新日期：1992-07-01 00:00:00
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更新日期：1995-01-01 00:00:00
abstract：:Nonionic block copolymers are surfactants synthesized using propylene oxide and ethylene oxide, and they can be designed so that individual copolymers have unique vaccine adjuvant properties. We have designed and produced nonionic block copolymers based on high molecular weight (MW), 9-15 kDA, cores of poly(oxypropyle...
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更新日期：1998-11-01 00:00:00
abstract：:The objectives of this study were to identify the key process parameters during steam granulation of disordered mesoporous silica material Syloid® 244 FP (244) and to compare two different binders: polyvinylpyrrolidone (PVP) K25 and hydroxypropylmethyl cellulose (HPMC). Itraconazole (ITZ) was selected as the model com...
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更新日期：2013-11-01 00:00:00
abstract：:The association efficiency of oxytetracycline (OTC) to pharmaceutical available, ionic oil-in-water nanoemulsions is studied. Theoretical mathematical developments allowed us to differentiate by diafiltration (DF) between thermodynamically and kinetically controlled binding of the drug to the nanoemulsions, and relate...
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