Sustained release of buserelin acetate, a luteinizing hormone-releasing hormone agonist, from an injectable oily preparation utilizing ethylated β-cyclodextrin

Uekama, Kaneto; Arima, Hisatomi; Irie, Tetsumi; Matsubara, Kazutaka; Kuriki, Takeo

doi:10.1111/j.2042-7158.1989.tb06393.x

Cited by 39 publications

(10 citation statements)

References 9 publications

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“…Uekama et al 92 and Matsubara et al 93 studied the release after im administration of the LHRH agonist buserelin acetate from oily suspensions in the presence of various cyclodextrins. The effects of HP--CD in altering the activity of a number of opioids and model drugs after intracerebral, intrathecal, and epidural administration have been mixed.…”

Section: Parenteral Applications Of Cyclodextrinsmentioning

confidence: 99%

Pharmaceutical Applications of Cyclodextrins. 2. In Vivo Drug Delivery

Rajewski¹,

Stella²

1996

Journal of Pharmaceutical Sciences

759

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

759

374

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“…One single s.c. injection of the suspension containing busereJin-DE,BCD complex to rats provides an effective continuous plasma level of buserelin lasting for at least one month (Figure 8-19) [103]. One single s.c. injection of the suspension containing busereJin-DE,BCD complex to rats provides an effective continuous plasma level of buserelin lasting for at least one month (Figure 8-19) [103].…”

Section: Sustained Release Formulationsmentioning

confidence: 99%

Cyclodextrins in Pharmacy

Frömming

Szejtli

1994

Topics in Inclusion Science

443

280

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“…[14] Other studies claimed the possible use of hydrophobic cyclodextrins (diethyl beta-cyclodextrin, triacetyl betacyclodextrin, triacetyl gamma-cyclodextrin) as controlledrelease carriers for hydrophilic and highly soluble drugs such as vancomycin. [15,16] The aim of the present work was to investigate the capability of vancomycin (VCM) to complex with three hydrophobic cyclodextrins (TACD) (triacetyl alfa, beta-, or gamma cyclodextrin) and the role played by the manufacturing process in the formation of the resulting VCM-TACD interaction products. The ultimate goal was to identify the most promising VCM-TACD interaction product to be subsequently used in prolonged release formulation (oily suspension or biodegradable multiparticulate systems) intended for site-specific treatment of bone infections.…”

Section: Introductionmentioning

confidence: 99%

Vancomycin–Triacetyl Cyclodextrin Interaction Products for Prolonged Drug Delivery

Ferrari

Sorrenti

Rossi

et al. 2008

Pharmaceutical Development and Technology

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The aim of the present work was to investigate the capability of vancomycin (VCM) to interact with three hydrophobic cyclodextrins (TACD) (triacetyl alfa-, beta-, or gamma cyclodextrin) and the role played by the preparation technique in the formation of interaction products aimed at prolonging drug delivery for site-specific treatment of bone infections. Physical mixtures of VCM with triacetyl α-, β-, or γ-cyclodextrin in a 1:1 molar ratio were subjected to kneading, coevaporation, and spray drying from aqueous suspensions or hydroacetonic solution. Thermal behavior (TG, DSC), percent drug content (HPLC), and drug release (Franz cell) of VCM from the physical mixtures, and the relevant binary systems obtained by the various complexation methods were evaluated. All binary systems were characterized by having a particle size compatible with parenteral site-specific administration and with drug-loading efficiencies close to 100%, thus indicating the stability of vancomycin toward each and every complexation process. In vitro drug release measurements showed that the preparation technique plays a different role depending on the type of cyclodextrin used. In the kneading process, the binary system containing TAαCD is the most efficient in slowing down the VCM release. With the coevaporation technique, the system based on TAβCD was most effective in prolonging drug release. None of the triacetyl-cyclodextrins is suitable in prolonging VCM release upon spray drying from aqueous suspensions, because this preparation technique does not determine drug-cyclodextrin interaction. On the other hand, spray drying from hydroacetonic solutions always results in a reduction in drug release, linked to the formation of VCM-TACD interaction products and is particularly pronounced for the VCM-TAγCD interaction product. The unique properties of prolonging drug release and maintaining the antimicrobial activity of the native drug render such an interaction product the most promising candidate in the development of delivery systems intended for parenteral site-specific administration of VCM.

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Sustained release of buserelin acetate, a luteinizing hormone-releasing hormone agonist, from an injectable oily preparation utilizing ethylated β-cyclodextrin

Cited by 39 publications

References 9 publications

Pharmaceutical Applications of Cyclodextrins. 2. In Vivo Drug Delivery

Pharmaceutical Applications of Cyclodextrins. 2. In Vivo Drug Delivery

Cyclodextrins in Pharmacy

Vancomycin–Triacetyl Cyclodextrin Interaction Products for Prolonged Drug Delivery

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