Characterization of Drug Loading in Crospovidone by X-ray Photoelectron Spectroscopy

Carli, F.; Garbassi, F.

doi:10.1002/jps.2600740911

Cited by 27 publications

(16 citation statements)

References 10 publications

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“…Crospovidone is a synthetic, insoluble homopolymer of N-vinyl-2-pyrrolidone, formed by a unique, simultaneous polymerization and cross-linking reaction ("popcorn" polymerization) of vinyl pyrrolidone (12)(13)(14). On scanning electron microscopy, crospovidone particles have a convoluted, spongelike appearance (12,15).…”

Section: Discussionmentioning

confidence: 99%

“…Its cross-linked structure provides a large absorptive surface and tremendous hygroscopicity that imparts a rapid swelling rate, making crospovidone an excellent tablet disintegrant. Swelling of crospovidone by slightly soluble drugs also results in a subsequent high release rate of the drug in aqueous media (14). In its purified form, crospovidone is a white powder that is chemically inert, essentially nontoxic, and not absorbed through the gastrointestinal tract.…”

Section: Discussionmentioning

confidence: 99%

“…However, crospovidone can be differentiated from other forms of PVP in tissue sections by combining the infrared spectrum with the observed histologic and histochemical characteristics. In a study of x-ray photoelectron spectra, there were subtle differences between the spectra of crospovidone and other forms of PVP (14). Additional studies may determine whether minor variations in the infrared spectra obtained from various forms of PVP in tissue can be used to distinguish different PVP polymers.…”

Section: Figurementioning

confidence: 99%

“…We have recently identified, in autopsy-derived lung tissue of three intravenous drug users, a distinctive embolic material, crospovidone (a polyvinylpyrrolidone), that is an important disintegrant in pharmaceutical tablets (12)(13)(14)(15). Crospovidone has not generally been emphasized, or recognized by pathologists, as a cause of pulmonary angiothrombosis and foreign body granulomatosis.…”

mentioning

confidence: 99%

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Embolized Crospovidone (poly[N-vinyl-2-pyrrolidone]) in the Lungs of Intravenous Drug Users

et al. 2003

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Crospovidone is an insoluble polymer of N-vinyl-2-pyrrolidone that is used as a disintegrant in pharmaceutical tablets. It can potentially embolize to the lung when aqueous tablet suspensions are injected intravenously. In this report, we identified embolized crospovidone in autopsy-derived lung tissue from three adult IV drug users, 1 man and 2 women, whose ages respectively were 27, 38, and 40 years. Suspected crospovidone was compared with pharmaceutical-grade crospovidone by means of histochemical stains, transmission electron microscopy, and infrared spectroscopy. Similar particles were also observed by light microscopy in a 4-mg tablet of hydromorphone, a preparation prescribed to two of the patients. Two patients had sickle cell disease and were taking methadone and/or hydromorphone for pain management; the third was receiving parenteral hyperalimentation after small bowel resection. Crospovidone appeared as deeply basophilic, coral-like particles within pulmonary arteries and in extravascular foreign-body granulomas. Intrapulmonary crospovidone stained similarly to the pure substance, including intense staining with mucicarmine, Congo red, and Masson trichrome. With Movat pentachrome stain, both intravascular and purified crospovidone appeared orange-yellow, whereas most interstitial particles associated with giant cells stained blue-green. Alcian blue failed to stain intravascular or purified crospovidone but strongly decorated some phagocytized particles. Ultrastructurally, both purified powder and tissue deposits of crospovidone appeared as irregular, electron dense, laminated, and finely granular material. Intrapulmonary crospovidone was associated with inflammatory cells and exhibited degenerative changes. By infrared spectroscopy, crospovidone in tissue had the same spectral characteristics as pharmaceutical grade crospovidone and the library reference, polyvinylpyrrolidone (PVP). We conclude that crospovidone contributes to pulmonary vascular injury in some persons who illicitly inject pharmaceutical tablets. It is readily identifiable histologically and distinguishable from other tablet constituents, such as cornstarch, talc, and microcrystalline cellulose. Pharmaceutical tablets typically consist of active ingredients and a variety of insoluble filler substances, such as talc, microcrystalline cellulose, and cornstarch, which provide bulk and impart physical properties to tablet preparations (1). Pulmonary foreign body granulomatosis caused by the embolization of these filler materials occurs when aqueous suspensions of tablets intended for oral consumption are injected intravenously (1-3). Some of the agents used in this manner, either alone or in combination, include methadone hydrochloride, tripelennamine hydrochloride (Pyribenzamine), methylphenidate (Ritalin), and pentazocine (Talwin; 3-6). Pulmonary angiothrombotic granulomatosis caused by talc, cornstarch and/or microcrys-

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Figurementioning

confidence: 99%

mentioning

confidence: 99%

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Embolized Crospovidone (poly[N-vinyl-2-pyrrolidone]) in the Lungs of Intravenous Drug Users

et al. 2003

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“…Thermal analysis and particularly microcalorimetric differential techniques are often employed to evidence such interactions [1,2].Cross-linked polyvinylpyrrolidone (PVP-XL)i is an amorphous insoluble polymer widely used as a disintegrating agent and binder for tablets [3,4] and for the preparation of molecular dispersions [5,6].Trimethoprim (TMP), whose thermal and structural properties were extensively investigated by some of us [7,8], is a chemotherapeutic agent commonly used as antifolate drug in combination with sulfonamides [9].A preliminary investigation of the thermal behaviour of mixtures of PVP-XL and TM P evidenced deep changes in thermal profiles of ground mixtures with respect to those of the pure components, which were ascribed to possible interactions between TMP and PVP-XL [10]. For a better understanding and characterization of such interactions a more detailed DSC study has been undertaken on the system PVP-XL/TMP, whose results are here reported.…”

mentioning

confidence: 99%

Thermal analysis of a drug-polymeric excipient solid system

Giordano

Bettinetti

Manna

et al. 1988

Journal of Thermal Analysis

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Differential scanning calorimetry has been applied to the study of the solid system crosslinked polyvinylpyrrolidone/trimethoprim.Different results have been systematically obtained on co-ground and not co-ground mixtures, suggesting some type of interaction to take place between components as a consequence of co-grinding.A simple phenomenological model of the interaction is proposed, which quite satisfactorily agrees with thermal data, It is well-known that drug-excipient interactions can deeply influence the technological and biopharmaceutical properties of solid dosage forms. Thermal analysis and particularly microcalorimetric differential techniques are often employed to evidence such interactions [1,2].Cross-linked polyvinylpyrrolidone (PVP-XL)i is an amorphous insoluble polymer widely used as a disintegrating agent and binder for tablets [3,4] and for the preparation of molecular dispersions [5,6].Trimethoprim (TMP), whose thermal and structural properties were extensively investigated by some of us [7,8], is a chemotherapeutic agent commonly used as antifolate drug in combination with sulfonamides [9].A preliminary investigation of the thermal behaviour of mixtures of PVP-XL and TM P evidenced deep changes in thermal profiles of ground mixtures with respect to those of the pure components, which were ascribed to possible interactions between TMP and PVP-XL [10]. For a better understanding and characterization of such interactions a more detailed DSC study has been undertaken on the system PVP-XL/TMP, whose results are here reported.It will be shown that a simple phenomenological model of the interaction can be proposed which quite satisfactorily agrees with thermal data.

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Solid‐State Characterization of Amorphous Dispersions

Vogt¹

2015

Pharmaceutical Sciences Encyclopedia

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This chapter reviews established and emerging analytical and physical techniques for the characterization of amorphous solid dispersions. The thermal analysis methods used in most reported studies of amorphous solid dispersions include differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), and isothermal microcalorimetry (ITC). Many of the commonly used polymers in amorphous solid dispersions are hydrophilic in nature and contain polar functional groups, and can absorb moisture from the atmosphere. In the pharmaceutical sciences, vibrational spectroscopic methods are generally used to probe molecular vibrations and phonon modes in crystalline substances. Solid‐state nuclear magnetic resonance (SSNMR) analysis of mobility in amorphous solid dispersions is complementary to thermal analysis and dielectric spectroscopy techniques. Scanning electron microscopy (SEM) is widely used in the characterization of amorphous solid dispersions. Effective characterization plays a critical role in the development of pharmaceutical amorphous solid dispersions.

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Characterization of Drug Loading in Crospovidone by X-ray Photoelectron Spectroscopy

Cited by 27 publications

References 10 publications

Embolized Crospovidone (poly[N-vinyl-2-pyrrolidone]) in the Lungs of Intravenous Drug Users

Embolized Crospovidone (poly[N-vinyl-2-pyrrolidone]) in the Lungs of Intravenous Drug Users

Thermal analysis of a drug-polymeric excipient solid system

Solid‐State Characterization of Amorphous Dispersions

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