Isolation and Characterization of Some Solid Phases of Fluprednisolone

Haleblian, John K.; Koda, Robert T.; Biles, John A.

doi:10.1002/jps.2600601008

Cited by 40 publications

(16 citation statements)

References 3 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Kuhnert-Brandstiitter and Gasser (911, in their work with fluocortolone, found dimorphism of the ethanolic solvates. Similarly, polymorphism was also reported for hydratesof fluprednisolone (29) and succinylsulfathiazole (93).…”

Section: Stoichiometric Adducts-solvatesmentioning

confidence: 98%

“…Of all the steroids examined, they found that estradiol formed solvates with all 30 solvents tested, the highest number of solvates so far recorded (92). Other steroids that have been observed to form solvates include hydrocortisone acetate (97), cortisone acetate (98), fluprednisolone (29), the tert-butylacetates of prednisolone and hydrocortisone (99), and fludrocortisone (fluorohydrocortisone) acetate and cholesterol (93).…”

Section: Stoichiometric Adducts-solvatesmentioning

confidence: 99%

See 1 more Smart Citation

Characterization of Habits and Crystalline Modification of Solids and Their Pharmaceutical Applications

Haleblian¹

1975

Journal of Pharmaceutical Sciences

Self Cite

448

202

View full text Add to dashboard Cite

Section: Stoichiometric Adducts-solvatesmentioning

confidence: 98%

Section: Stoichiometric Adducts-solvatesmentioning

confidence: 99%

Characterization of Habits and Crystalline Modification of Solids and Their Pharmaceutical Applications

Haleblian¹

1975

Journal of Pharmaceutical Sciences

Self Cite

448

202

View full text Add to dashboard Cite

“…Polymorphs of a given compound are chemically identical but, in general, different in structure and properties including dissolution rates, melting point, density, hardness, and crystal shape. The choice of the polymorphic form may determine the physical and chemical stability, compressibility, and bioavailability of the drug substance (Haleblian et al, 1971). A compound can exist in a number of polymorphic forms but only one form is thermodynamically stable at a given temperature and pressure, while the others are metastable.…”

Section: Polymorphic Formsmentioning

confidence: 99%

“…Various crystalline solid forms of fluprednisolone have been characterized by using XRPD. In this study, XRPD was used for the identification of (i) anhydrous polymorphic forms; (ii) solvates; and (iii) anhydrous form existing in both crystalline and amorphous states (Haleblian et al, 1971). have evaluated the phase transformations occurring during processing and storage of anhydrous theophylline tablets and its implication of tablet dissolution using XRPD as illustrated in Fig.…”

Section: X-ray Powder Diffractometry (Xrpd)mentioning

confidence: 99%

Physicochemical Characterization of Pharmaceutical Solids

Debnath

2011

Oral Bioavailability

View full text Add to dashboard Cite

“…Among them, some compounds can form different hydrates by incorporating different amounts of water. Hydrates can also form polymorphs in which hydrates with the same chemical composition and molar ratio of water have different crystal packing arrangements [2][3][4][5]. Different hydrates of a particular compound or polymorphs of a hydrate have different physical properties.…”

mentioning

confidence: 99%

Insight into Crystallization Mechanisms of Polymorphic Hydrate Systems

Tian

Louhi-Kultanen

et al. 2010

Chem Eng & Technol

View full text Add to dashboard Cite

Polymorphic anhydrate systems have been well studied but until now little attention has been paid to polymorphic hydrate systems. The incorporation of water molecules can complicate the whole polymorphic system and thus impede the control of the crystallization process. In this work, nitrofurantoin monohydrate polymorphs which have the same chemical composition and molar ratio of water but different crystal packing arrangements, have been investigated. The metastable nitrofurantoin monohydrate was found to be difficult to crystallize, where both evaporative and cooling crystallization failed in its production. The possible phase conversion of the nitrofurantoin hydrate polymorphic system was also investigated in a liquid-assisted ball milling process. High-energy solids, e.g., amorphous and cocrystals, have often been created during high-energy ball milling. Metastable nitrofurantoin monohydrate, however, was again not observed during the whole milling process, in contrast to another polymorphic hydrate system, namely niclosamide. During milling of niclosamide anhydrate in ethyl acetatewater mixture the metastable niclosamide monohydrate was formed immediately upon milling (2 min). Under further milling, the metastable niclosamide hydrate started converting to the stable niclosamide hydrate (from 30 min onwards). IntroductionHydrates are the most common solvates encountered in pharmaceutical compounds, since water and mixtures of water and an organic solvent are frequently used in pharmaceutical processing, e.g., in crystallization and granulation. It has been estimated that approximately one-third of active pharmaceutical ingredients (APIs) are capable of forming a hydrate [1]. Among them, some compounds can form different hydrates by incorporating different amounts of water. Hydrates can also form polymorphs in which hydrates with the same chemical composition and molar ratio of water have different crystal packing arrangements [2][3][4][5]. Different hydrates of a particular compound or polymorphs of a hydrate have different physical properties. In aqueous environment it is unlikely that the most thermodynamically stable hydrate can be overlooked but the formation of stable hydrates may mask the existence of other less stable hydrate forms. Therefore, discovery of a less stable hydrate can be coincidently and sometimes difficult. Several metastable hydrates were only recently discovered [6,7]. This applies similarly to the metastable nitrofurantoin hydrate polymorph. The two nitrofurantoin hydrate polymorphs (monohydrate I and II) have been reported by Pienaar et al. in 1993 [5]. These two hydrates have the same chemical composition and same molar ratio of water in crystalline lattice, differing only in the crystal packing arrangements. Since 1993, a number of studies have investigated nitrofurantoin hydrate [5,[8][9][10][11][12][13][14][15], but only two of them have observed the formation of metastable nitrofurantoin hydrate polymorph (monohydrate I) [14,15]. Crystallization of this metastable nitrofuranto...

show abstract

Isolation and Characterization of Some Solid Phases of Fluprednisolone

Cited by 40 publications

References 3 publications

Characterization of Habits and Crystalline Modification of Solids and Their Pharmaceutical Applications

Characterization of Habits and Crystalline Modification of Solids and Their Pharmaceutical Applications

Physicochemical Characterization of Pharmaceutical Solids

Insight into Crystallization Mechanisms of Polymorphic Hydrate Systems

Contact Info

Product

Resources

About