Temperature-Induced Crystallization and Compactibility of Spray Dried Composite Particles Composed of Amorphous Lactose and Various Types of Water-Soluble Polymer.

Takeuchi, Hirofumi; Yasuji, Takehiko; Yamamoto, Hiromitsu; Kawashima, Yasunaru

doi:10.1248/cpb.48.585

Cited by 13 publications

(6 citation statements)

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“…Minor surface structures are, however, visible which may represent PVP material adsorbed to, or embedded in the crystalline ibuprofen particle. The stabilizing effect of PVP seen on actuation of crystalline ibuprofen particles in the PowderJect device as well as in the previous reports on granules27 and spray‐dried particles28 must be related to reduction of friction at the particles' surfaces during the comminution process, viz. ultrasonic acceleration, ball mill, or compression.…”

Section: Resultsmentioning

confidence: 65%

“…Mehta et al27 found that increasing PVP K29–32 amount in crystalline lactose granules of mean diameter 630 µm reduced their attrition coefficient and decreased their Harwood–Pilpel crushing strength on comminution in a ball mill. The tensile strength of compacted, spray‐dried lactose/PVP particles similarly increased with higher PVP content 28. In the PowderJect device the stabilizing effect of the PVP is strongest with the 53–75 µm size fractions, where also attrition of the pure, unprotected ibuprofen was the greatest.…”

Section: Resultsmentioning

confidence: 96%

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Penetration of Crystalline Powder Particles into Excised Human Skin Membranes and Model Gels from a Supersonic Powder Injector

Lahm

Lee

2006

Journal of Pharmaceutical Sciences

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Section: Resultsmentioning

confidence: 65%

Section: Resultsmentioning

confidence: 96%

Penetration of Crystalline Powder Particles into Excised Human Skin Membranes and Model Gels from a Supersonic Powder Injector

Lahm

Lee

2006

Journal of Pharmaceutical Sciences

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“…Heat and moisture can induce spontaneous phase transformations, including crystallization, with obvious adverse effects on the properties of dosage forms. However, it has been suggested that an amorphous material can be coprocessed with a polymer to produce a more stable amorphous composite material 7–9. The commonest methods used to investigate such heat‐ and moisture‐induced crystallization of amorphous materials are measurements of weight change (gravimetric) or heat evolved (calorimetric).…”

Section: Introductionmentioning

confidence: 99%

Moisture-Induced Surface Crystallization of Spray-Dried Amorphous Lactose Particles Studied by Atomic Force Microscopy

Mahlin

Berggren²,

Alderborn³

et al. 2004

Journal of Pharmaceutical Sciences

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“…2,3) Pikal et al have reported the mutual inhibition of crystallization of mannitol and glycine during lyophilization.…”

mentioning

confidence: 99%

“…2,12,13) The crystallinities of AAS and mannitol in each freeze-dried formulation were obtained from the heat absorption at the melting temperatures and related to the corresponding fully crystalline raw materials. A mathematical program (PeakFit ® ) based on deconvolution curves was used to calculate the enthalpy of fusion.…”

mentioning

confidence: 99%

Characterization of Physical State of Mannitol after Freeze-Drying: Effect of Acetylsalicylic Acid as a Second Crystalline Cosolute.

Torrado¹

2002

CHEMICAL & PHARMACEUTICAL BULLETIN

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When two different substances are mixed in a solution and then freeze-dried, some physical changes can affect the crystallographic characteristics of the final product.2,3) Pikal et al. have reported the mutual inhibition of crystallization of mannitol and glycine during lyophilization.3) However, there are not many articles which study the effect of a crystalline active substance on the physical state of mannitol forms.Mannitol is an excipient broadly used in the freeze-drying process, [4][5][6][7][8] and its crystalline and amorphous forms have been extensively studied. 4,[6][7][8] The freeze-drying process can produce a partially amorphous and partially crystalline material 6) ; the crystallization of mannitol during this process can lead to different anhydrous polymorphs (a, b, and d). The existence of crystalline mannitol hydrate obtained during the freeze-drying process has been confirmed by Yu et al. 7)As a result of these changes to the crystal form of mannitol during freeze-drying there is a difference in the physical and chemical stability of the freeze-dried solid, which can induce adverse effects. Therefore, by studying the physical chemistry of freeze-dried mannitol containing formulations one can anticipate these changes and prevent adverse effects.During the freeze-drying process, samples are subject to different cycles of freeze and vacuum drying. These processes can lead to modifications of the initial crystalline form of the drug. 4,5,8,9) The effects of freezing rate, temperature and mannitol concentration may also induce crystallographic changes producing a previously known mannitol form.6,7) Yu et al. have shown that mixtures of d (major) and b (minor) polymorphs were produced by freeze-drying a 4% w/v pure mannitol solution.7) Nevertheless, other authors when employing a fast freezing process favored the formation of b form when 5% (w/v) mannitol solution was freezedried.6) The difficulties which arise when attending to control these variables (as temperature and cooling rate) during the freeze-drying process are shown by Yu et al.,7) who identify several factors that can contribute to the vial-to-vial variation in the amount and stability of the mannitol hydrate.In the current study, acetylsalicylic acid (AAS) is used as model crystalline drug. Possible changes in crystallinity of AAS can be easily detected because its crystallographic characteristics are well known. 10,11) Therefore, the objectives of this study are to (1) Identify and measure the different crystalline mannitol forms obtained when a second crystallizing solute is present. (2) Determine the effect of a similar to industrial scale freeze-drying process conditions on the physical state of freeze-dried mannitol present as a single component. ExperimentalMaterials AAS USP 23 (Merck, Darmstadt, Germany). b Mannitol NF (ICI Americas Inc., U.S.A.). d-mannitol was obtained using a procedure described by Kim et al. 6) All other ingredients were of reagent grade or better (Merck).Methods. Powder Samples Physical Mixtures: Samples ...

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Temperature-Induced Crystallization and Compactibility of Spray Dried Composite Particles Composed of Amorphous Lactose and Various Types of Water-Soluble Polymer.

Cited by 13 publications

References 0 publications

Penetration of Crystalline Powder Particles into Excised Human Skin Membranes and Model Gels from a Supersonic Powder Injector

Penetration of Crystalline Powder Particles into Excised Human Skin Membranes and Model Gels from a Supersonic Powder Injector

Moisture-Induced Surface Crystallization of Spray-Dried Amorphous Lactose Particles Studied by Atomic Force Microscopy

Characterization of Physical State of Mannitol after Freeze-Drying: Effect of Acetylsalicylic Acid as a Second Crystalline Cosolute.

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