Studies on the Crystal forms of Pefloxacin: Preparation, Characterization, and Dissolution Profile

Yadav, Mange Ram; Shaikh, Anwar R.; Ganesan, V.; Giridhar, Rajani; Chadha, Renu

doi:10.1002/jps.21178

Cited by 11 publications

(4 citation statements)

References 11 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…A battery of techniques is always desirable for screening of various crystal forms of an active pharmaceutical ingredient (API) (13)(14)(15)(16)(17)(18). Although X-ray powder diffractometry remains the most common technique for identifying and characterizing the various crystalline forms, thermoanalytical methods have emerged as a complementary technique to monitor crystallinity and polymorphism due to its speed and minimal sample preparation (19,20). Driven by the importance of the solid-state properties of API, we performed a comprehensive study on the various crystalline forms of nevirapine (11-cyclopropyl-5,11-dihydro-4-methyl-6H-dipyrido[3,2-b:2′,3′-e] [1,4]diazepin-6-one; Fig.…”

Section: Introductionmentioning

confidence: 99%

Solvated Crystalline Forms of Nevirapine: Thermoanalytical and Spectroscopic Studies

et al. 2010

Self Cite

View full text Add to dashboard Cite

Abstract. The study is aimed at exploring the utility of thermoanalytical methods in the solid-state characterization of various crystalline forms of nevirapine. The different forms obtained by recrystallization of nevirapine from various solvents were identified using differential scanning calorimetry and thermogravimetric analysis (TGA). The appearance of desolvation peak accompanied by weight loss in TGA indicated the formation of solvates: hemi-ethanolate (Form I), hemi-acetonitrilate (Form II), hemichloroformate (Form III), hemi-THF solvate (Form IV), mixed hemi-ethanolate hemi-hydrate (Form V), and hemi-toluenate (Form VI). The higher desolvation temperatures of all the solvates except toluenate than their respective boiling point indicate tighter binding of solvent. Emphasis has been laid on the determination of heat capacity and heat of solution utilizing microreaction calorimeter to further distinguish the various forms. The enthalpy of solution (ΔH sol ), an indirect measure of the lattice energy of a solid, was well correlated with the crystallinity of all the solid forms obtained. The magnitude of ΔH sol was found to be −14.14 kJ/mol for Form I and −2.83 kJ/mol for Form V in phosphate buffer of pH 2, exhibiting maximum ease of molecular release from the lattice in Form I. The heat capacity for solvation (ΔC p ) was found to be positive, providing information about the state of solvent molecules in the host lattice. The solubility and dissolution rate of the forms were also found to be in agreement with their enthalpy of solution. Form (I), being the most exothermic, was found to be the most soluble of all the forms.

show abstract

Section: Introductionmentioning

confidence: 99%

Solvated Crystalline Forms of Nevirapine: Thermoanalytical and Spectroscopic Studies

et al. 2010

Self Cite

View full text Add to dashboard Cite

show abstract

“…Yadav et al studied five different polymorphic forms of pefloxacin reported the crystal forms of pefloxacin. Interestingly, all the forms offered high dissolution behavior within 15 min, which was further stabilized to a constant value after 4 hours [93]. Polymorphic forms are established to alter the biological distribution and efficacy of chloramphenicol palmitate [94], phenylbutazone [95], amobarbitol [27], cimetidine [96], 6-mercaptopurine [26] and chlortetracycline hydrochloride [24]; though established in animal models [97].…”

Section: Importance In Pharmaceutical Sciencesmentioning

confidence: 99%

Polymorphism: The Phenomenon Affecting the Performance of Drugs

Raza¹

2014

SOJPPS

View full text Add to dashboard Cite

Pseudopolymorphs, i.e., co-crystals are also studied along with polymorphism, which are solid crystalline materials comprising two or more molecules or atoms in the same crystal lattice [11]. Co-crystals are also generally characterized as hydrates (solvent trapped), solvates (solvent present), and clathrates (molecules trapped) [12]. The first co-crystals reported were the co-crystals of hydroquinone and quinone in 1844 by Friedrich Wöhle [13]. Co-crystals directly affect the solid-state properties in terms of solubility and bioavailability. Co-crystals are frequently designed

show abstract

“…The particle size and crystal form of a drug also affect pharmacological efficacy, due to their ability to alter the physicochemical properties of solubility, dissolution, and dosage forms. During the crystallization of a drug, different crystal structures can be formed, as the packing of molecules in space change at different temperatures, solutions, and pressures [14][15][16][17]. Generally, the appearance, melting point, dissolution, and other aspects of the same drug are significantly different in diverse crystal forms, which correspondingly affect clinical efficacy [18][19][20][21][22].…”

Section: Introductionmentioning

confidence: 99%

Studies on the Crystal Forms of Istradefylline: Structure, Solubility, and Dissolution Profile

Wang

Zheng

et al. 2022

Crystals

View full text Add to dashboard Cite

Istradefylline as a selective adenosine A2A-receptor antagonist is clinically used to treat Parkinson’s disease and improve dyskinesia in its early stages. However, its crystal form, as an important factor in the efficacy of the drug, is rarely studied. Herein, three kinds of crystal forms of istradefylline prepared from ethanol (form I), methanol (form II), and acetonitrile (form III) are reported by use of a crystal engineering strategy. These three crystal forms were characterized and made into tablets for dissolution testing. Both the solubility and the dissolution rates were also determined. The dissolution rate of form I and form III is significantly higher than form II at pH 1.2 (87.1%, 58.2%, and 87.7% for form I, form II, and form III, respectively), pH 4.5 (88.1%, 58.9%, and 87.1% for form I, form II, and form III, respectively) and pH 6.8 (87.5%, 58.2%, and 86.0% for form I, form II, and form III, respectively) at 60 min. Considering the prepared solution and the proper dissolution profile, form I is anticipated to possess promising absorption for bioavailability.

show abstract

Studies on the Crystal forms of Pefloxacin: Preparation, Characterization, and Dissolution Profile

Cited by 11 publications

References 11 publications

Solvated Crystalline Forms of Nevirapine: Thermoanalytical and Spectroscopic Studies

Solvated Crystalline Forms of Nevirapine: Thermoanalytical and Spectroscopic Studies

Polymorphism: The Phenomenon Affecting the Performance of Drugs

Studies on the Crystal Forms of Istradefylline: Structure, Solubility, and Dissolution Profile

Contact Info

Product

Resources

About