A non- surfactant formulation for alfaxalone based on an amorphous cyclodextrin: Activity studies in rats and dogs

Estes, Kerry S.; Brewster, Marcus E.; Webb, Alistair I.; Bodor, Nicholas

doi:10.1016/0378-5173(90)90014-u

Cited by 40 publications

(16 citation statements)

References 12 publications

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“…65 The responses to increasing doses of the anesthetic isoflurane from a HP--CD solution were similar to those after inhalation of the agent. 66 Estes et al 67 evaluated a nonsurfactant formulation that contained HP--CD for administration of alfaxalone (3R-hydroxy-5R-pregnane-11,20-dione, a steroid anesthetic) to rats and dogs. This formulation was compared to a veterinary product containing the surfactant Cremophor-EL.…”

Section: Parenteral Applications Of Cyclodextrinsmentioning

confidence: 99%

Pharmaceutical Applications of Cyclodextrins. 2. In Vivo Drug Delivery

Rajewski¹,

Stella²

1996

Journal of Pharmaceutical Sciences

763

374

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The objective of this Review is to summarize and critique recent findings and applications of both unmodified and modified cyclodextrins for in vivo drug delivery. This review focuses on the use of cyclodextrins for parenteral, oral, ophthalmic, and nasal drug delivery. Other routes including dermal, rectal, and pulmonary delivery are also briefly addressed. This Review primarily focuses on newer findings concerning cyclodextrin derivatives which are likely to receive regulatory acceptance due to improved aqueous solubility and safety profiles as compared to the unmodified cyclodextrins. Many of the applications reviewed involve the use of hydroxypropyl-beta-cyclodextrins (HP-beta-CDs) and sulfobutylether-beta-cyclodextrins (SBE-beta-CDs) which show promise of greater safety while maintaining the ability to form inclusion complexes. The advantages and limitations of HP-beta-CD, SBE-beta-CD, and other cyclodextrins are addressed.

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Section: Parenteral Applications Of Cyclodextrinsmentioning

confidence: 99%

Pharmaceutical Applications of Cyclodextrins. 2. In Vivo Drug Delivery

Rajewski¹,

Stella²

1996

Journal of Pharmaceutical Sciences

763

374

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“…1971) and cat (Dodman 1980). More recently, alfaxalone has been solubilized with 2‐hydroxypropyl beta‐cyclodextrin (Estes et al. 1990).…”

Section: Introductionmentioning

confidence: 99%

“…This preparation found some application in birds (Bailey et al 1999) and in reptiles (Lawrence 1983), but the product was discontinued because Cremophor EL was associated with histamine release in the dog (Child et al 1971) and cat (Dodman 1980). More recently, alfaxalone has been solubilized with 2-hydroxypropyl beta-cyclodextrin (Estes et al 1990). This formulation has been used clinically to induce general anaesthesia in a variety of species including the dog (Maddern et al 2010), cat (Taboada & Murison 2010) and rabbit (Grint et al 2008).…”

Section: Introductionmentioning

confidence: 99%

Alfaxalone anaesthesia in the green iguana (Iguana iguana)

Bertelsen

Sauer

2011

Veterinary Anaesthesia and Analgesia

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“…1993), antimycotic agents (Pedersen et ul., 1993), insulin (Watanabe et ul., 1992a, b), anticancer drugs (Distelmans et ul., 1991) etc. The inclusion complex formation modifies the physicocheniical characteristics of guest molecules; it improves the performance of intravenous formulations (Estes et al, 1990), prolongs the pulmonary absorption of sulbutanol (Cabral et a!., 1991), sustains the release rate of drugs (Uekama et al, 1990) increases the stability of the guest molecule (Djedainipilard et al, 1993) enhances the peak concentration of drugs in blood (Hostetler et al, 1992) and improves bioavailability (Miiller and Albers, 1991). Charge-transfer reversed-phase thin-layer chromatography has been frequently applied to study molecular interactions (Cserhati and Valko, 1993).…”

Section: Introductionmentioning

confidence: 98%

Interaction of carboxymethyl‐γ‐cyclodextrin with anticancer drugs studied by charge‐transfer thin‐layer chromatography

Cserháti

1994

Biomedical Chromatography

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The interaction between 22 anticancer drugs and carboxymethyl-gamma-cyclodextrin (CM-gamma-CD) was studied by reversed-phase charge-transfer thin-layer chromatography and the relative strength of interaction was calculated. CM-gamma-CD formed inclusion complexes with 11 compounds, the complex always being more hydrophilic than the uncomplexed drug. The inclusion forming capacity of drugs differed considerably according to their chemical structure. Both principal component analysis and cluster analysis found a relationship between the inclusion complex forming capacity and hydrophobicity parameters of anticancer drugs. This result suggests that the preponderant role of hydrophobic interactions is in inclusion complex formation.

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A non- surfactant formulation for alfaxalone based on an amorphous cyclodextrin: Activity studies in rats and dogs

Cited by 40 publications

References 12 publications

Pharmaceutical Applications of Cyclodextrins. 2. In Vivo Drug Delivery

Pharmaceutical Applications of Cyclodextrins. 2. In Vivo Drug Delivery

Alfaxalone anaesthesia in the green iguana (Iguana iguana)

Interaction of carboxymethyl‐γ‐cyclodextrin with anticancer drugs studied by charge‐transfer thin‐layer chromatography

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