Ibuprofen-polyvinylpyrrolidone dispersions. Proton nuclear magnetic resonance and infrared studies

El-Hinnawi, Mahmoud A.; Najib, Naji M.

doi:10.1016/0378-5173(87)90024-x

Cited by 24 publications

(11 citation statements)

References 9 publications

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“…Zografi and co-workers 17 have concluded that low levels of poly(vinylpyrrolidone) which inhibit amorphous indomethacin crystallization must act through additional factors not related to glass transition events and molecular mobility but perhaps relate to specific chemical and steric interactions. Thus in a manner similar to the hydrogen bonding complexes known to occur in ibuprofen-poly(vinylpyrrolidone) solid dispersions, 18 specific protein-excipient interactions could inhibit crystallization. It is also possible that the distribution of protein and excipient within a particle is not homogeneous and thus the protein may be preferentially located at sites to inhibit nucleation and growth.…”

Section: Resultsmentioning

confidence: 97%

Water Vapor Sorption Studies on the Physical Stability of a Series of Spray-Dried Protein/Sugar Powders for Inhalation

Forbes

Davis

Hindle

et al. 1998

Journal of Pharmaceutical Sciences

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One theory suggests that by maintaining the protein in an amorphous glassy sugar matrix, the physical hindrance encountered by the protein functions to stabilize it. Thus, the nature of the sugar/protein interaction is important as is the maintenance of the sugar in an amorphous form without any recrystallization. Moisture is known to function as a plasticizer and facilitate crystallization and thus loss of the amorphous state. We report the effect of cospray-drying with different proteins on the physical stability of lactose and mannitol. Particle sizing showed their suitability for inhalation, and the effect of exposure of the spray-dried products to moisture vapor was monitored gravimetrically. Bovine liver catalase, bovine pancreatic insulin, and bovine pancreatic ribonuclease A when individually cospray-dried with lactose showed no extensive initial crystallinity by powder X-ray diffraction, but proteins cospray-dried with mannitol generally showed evidence of mannitol component crystallinity. Catalase appeared to inhibit lactose crystallization from an amorphous matrix to a greater extent than insulin when exposed to short-term elevated humidity, but this difference was a kinetic feature. The hygroscopicities of the cospray-dried materials differed and indicated that each protein/sugar system required individual characterization to identify an optimal formulation.

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Section: Resultsmentioning

confidence: 97%

Water Vapor Sorption Studies on the Physical Stability of a Series of Spray-Dried Protein/Sugar Powders for Inhalation

Forbes

Davis

Hindle

et al. 1998

Journal of Pharmaceutical Sciences

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“…However, carbonyl group is more favorable due to the steric hindrance effect on the nitrogen atom[33]. Thus, any sign of interaction would be reflected by band shifts, broadening, disappearance of peaks or intensity alterations as compared to the spectra of the pure drug and polymers[3435]. …”

Section: Resultsmentioning

confidence: 99%

Formulation development and dissolution rate enhancement of efavirenz by solid dispersion systems

Koh¹,

Chuah²,

Talekar³

et al. 2013

Indian J Pharm Sci

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The aim of this study was to enhance the dissolution rate of efavirenz using solid dispersion systems (binary and ternary). A comparison between solvent and fusion method was also investigated. Solid dispersions of efavirenz were prepared using polyethylene glycol 8000, polyvinylpyrrolidone K30 alone and combination of both. Tween 80 was incorporated to obtain a ternary solid dispersion system. Dissolution tests were conducted and evaluated on the basis of cumulative percentage drug release and dissolution efficiency. Physicochemical characterizations of the solid dispersions were carried out using differential scanning calorimetric, powder X-ray diffraction, Fourier transform infrared spectroscopy, and scanning electron microscopy. Dissolution was remarkably improved in both systems compared to pure efavirenz (P<0.05). An optimum ratio was identified at a drug:polymer of 1:10. Incorporation of Tween 80 to 1:10 formulations formed using solvent method showed further improvement in the dissolution rate. Physicochemical characterization results suggested that efavirenz existed in the amorphous form in all the solid dispersion systems providing evidence of improvement in dissolution. No statistically significant difference (P>0.05) in dissolution was observed between the two methods. Binary and ternary solid dispersion systems both have showed a significant improvement in the dissolution rate of efavirenz. Formulations with only polyvinylpyrrolidone K30 showed best dissolution profile and 1:10 was identified as an optimum drug-polymer weight ratio.

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“…The interactions between the components were studied using infrared spectroscopy and nuclear magnetic resonance (NMR) techniques, and the idea of strong interactions between the two components being important for amorphous formulation performance was introduced ( 15 ). In the same year, El-Hinnawi and Hajib used the same techniques for studying amorphous ibuprofen-PVP ( 16 ). Both these publications indicated that the systems studied were actually “glass solutions”, but in the publications, the authors used the general term “solid dispersion”.…”

Section: Introductionmentioning

confidence: 99%

The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

2017

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The alarming numbers of poorly soluble discovery compounds have centered the efforts towards finding strategies to improve the solubility. One of the attractive approaches to enhance solubility is via amorphization despite the stability issue associated with it. Although the number of amorphous-based research reports has increased tremendously after year 2000, little is known on the current research practice in designing amorphous formulation and how it has changed after the concept of solid dispersion was first introduced decades ago. In this review we try to answer the following questions: What model compounds and excipients have been used in amorphous-based research? How were these two components selected and prepared? What methods have been used to assess the performance of amorphous formulation? What methodology have evolved and/or been standardized since amorphous-based formulation was first introduced and to what extent have we embraced on new methods? Is the extent of research mirrored in the number of marketed amorphous drug products? We have summarized the history and evolution of amorphous formulation and discuss the current status of amorphous formulation-related research practice. We also explore the potential uses of old experimental methods and how they can be used in tandem with computational tools in designing amorphous formulation more efficiently than the traditional trial-and-error approach.

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Ibuprofen-polyvinylpyrrolidone dispersions. Proton nuclear magnetic resonance and infrared studies

Cited by 24 publications

References 9 publications

Water Vapor Sorption Studies on the Physical Stability of a Series of Spray-Dried Protein/Sugar Powders for Inhalation

Water Vapor Sorption Studies on the Physical Stability of a Series of Spray-Dried Protein/Sugar Powders for Inhalation

Formulation development and dissolution rate enhancement of efavirenz by solid dispersion systems

The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

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