Physicochemical characterization and dissolution properties of meloxicam–cyclodextrin binary systems

Naidu, N.Buchi; Chowdary, K. P. R.; Murthy, K. Srikanta; Satyanarayana, V.; Hayman, Alan R.; Becket, Gordon

doi:10.1016/j.jpba.2004.01.003

Cited by 99 publications

(46 citation statements)

References 15 publications

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“…The significant improvement in dissolution characteristics of the complexes is justified through the concurrence of several factors: increased particle wettability, and reduction of crystallinity of the product (19)(20)(21). Improved dissolution may be attributed to the high energetic amorphous state and reduction in crystallinity of the PRM following complexation in physical mixture and kneaded system, which was confirmed by XRPD and DSC studies.…”

Section: In Vitro Drug Releasementioning

confidence: 69%

Formulation and Evaluation of Taste Masked Oral Reconstitutable Suspension of Primaquine Phosphate

Shah

Mashru

2008

AAPS PharmSciTech

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Abstract. The purpose of this research was to mask the intensely bitter taste of primaquine phosphate (PRM) and to formulate suspension powder (cachets) of the taste masked drug. Taste masking was done using beta-cyclodextrin. To characterize and formulate taste masked cachets of PRM, the 1:25 M physical mixture was selected based on bitterness score. Phase solubility studies, fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray powder diffraction (XRPD) were performed to identify the physicochemical interaction between drug and carrier, hence its effect on dissolution. Cachets were evaluated for angle of repose, sedimentation characterization and pH. In vitro drug release studies for physical mixture and kneaded system were performed at pH, 1.2 and 6.8. Bitterness score was evaluated using gustatory sensation test. Phase solubility studies showed weak interaction between PRM and CD. The FTIR, DSC and XRPD studies indicated inclusion complexation in physical mixture and kneaded system. In addition, kneaded system and physical mixture exhibited better drug release at pH 1.2 and negligible effect at pH 6.8. Cachets prepared using physical mixture, (DS24), showed complete bitter taste masking and easy redispersibility. Taste evaluation of cachets in human volunteers rated tasteless with a score of 0 to DS24 and 3 to DS25. Thus, results conclusively demonstrated successful taste masking and formulation of cachets with taste masked drug.

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Section: In Vitro Drug Releasementioning

confidence: 69%

Formulation and Evaluation of Taste Masked Oral Reconstitutable Suspension of Primaquine Phosphate

Shah

Mashru

2008

AAPS PharmSciTech

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“…It can be assumed that, in the early stages of the dissolution process, HPbCD molecules will operate locally in the hydrodynamic layer surrounding the drug particles. This action resulted in the in situ inclusion process which produced a rapid increase of the amount of dissolved drug (21).…”

Section: Dissolution Studiesmentioning

confidence: 99%

Characterization of ternary complexes of meloxicam-HPβCD and PVP or L-arginine prepared by the spray-drying technique

Elmaradny¹,

Mortada²,

Kamel³

et al. 2008

Acta Pharmaceutica

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Cyclodextrins and their derivatives play an important role in improving the therapeutic efficacy of drugs with poor solubility and/or stability problems. They are capable of alleviating the undesirable properties of drug molecules through the formation of inclusion complexes (1). Hydroxypropyl-b-cyclodextrin (HPbCD) is mainly selected for its higher solubility than other cyclodextrins and this generally results in more extensive solubilization ability toward lipophilic molecules, with a good safety profile (2). Ternary complexes of meloxicam (ME) (a poorly water soluble anti-inflammatory drug) with hydroxypropyl-b--cyclodextrin (HPbCD) and either a hydrophilic polymer, namely, polyvinyl pyrrolidone (PVP) or a basic amino acid such as L-arginine, were prepared by the spray-drying technique. The solubilizing efficiency, physical properties and dissolution behaviour of each ternary system of ME--HPbCD with either PVP or L-arginine were compared with those of the corresponding binary system of ME--HPbCD. Tablets compressed from the ternary system of ME-HPbCD-L-arginine were compared with plain and commercial tablets. Phase solubility experiments suggested the formation of an inclusion complex of A L type. Ternary system of ME-HPbCD-L-arginine exhibited a stability constant 30.3 times higher than the binary system of ME-HPbCD, while the ternary system of ME-HPbCD--PVP increased the stability constant 2.2 times only. The prepared complexes were characterized by scanning electron microscopy, differential scanning calorimetry and infra red spectroscopy. Ternary solid complexes indicated the presence of strong interactions between the components. The dissolution behaviour of ME from different ternary complexes was higher than its dissolution from the binary system. Tablets compressed from ternary complexes of ME-HPbCD-L-arginine highly improved drug release compared to plain and commercial tablets.

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“…The diffraction pattern of the complex should be clearly distinct from that of the superimposition of each of the components if a true inclusion complex has been formed (31). Power X-ray diffractometry was used to investigate in more depth the differences in the solid state between MCZ and MβCD products prepared by different methods.…”

Section: X-ray Powder Diffractionmentioning

confidence: 99%

Preparation and Solid-State Characterization of Inclusion Complexes Formed Between Miconazole and Methyl-β-Cyclodextrin

et al. 2008

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Abstract. The aim of this study is to confirm the formation of inclusion complexes between miconazole (MCZ) and two derivatives of beta-cyclodextrin, methyl-beta-cyclodextrin (MβCD) and 2-hydroxypropyl-beta-cyclodextrin (HPβCD) in aqueous solution by phase solubility studies. Inclusion complexes with MβCD in the solid state were then prepared by different methods, i.e., kneading, coevaporation (COE), spray-drying (SD), and lyophilization (LPh). The physicochemical properties of these complexes were subsequently studied by means of differential scanning calorimetry, Fourier transform infrared spectroscopy, scanning electron microscopy, and X-ray diffraction techniques. Phase solubility diagrams with MβCD and HPβCD were classified as A P type, indicating the formation of 1:1 and 1:2 stoichiometric inclusion complexes. The apparent stability constants (K S ) calculated from the phase solubility diagram were 145.69 M −1 (K 1:1 ) and 11.11 M −1 (K 1:2 ) for MβCD and 126.94 M −1 (K 1:1 ) and 2.20 M −1 (K 1:2 ) for HPβCD. The method of preparation of the inclusion complexes in the solid state was shown to greatly affect the properties of the formed complex. Hence, the LPh, SD, and COE methods produce true inclusion complexes between MCZ and MβCD. In contrast, crystalline drug was still clearly detectable in the kneaded (KN) product.

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Physicochemical characterization and dissolution properties of meloxicam–cyclodextrin binary systems

Cited by 99 publications

References 15 publications

Formulation and Evaluation of Taste Masked Oral Reconstitutable Suspension of Primaquine Phosphate

Formulation and Evaluation of Taste Masked Oral Reconstitutable Suspension of Primaquine Phosphate

Characterization of ternary complexes of meloxicam-HPβCD and PVP or L-arginine prepared by the spray-drying technique

Preparation and Solid-State Characterization of Inclusion Complexes Formed Between Miconazole and Methyl-β-Cyclodextrin

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