Modification of Rectal Absorption of Morphine Hollow-Type Suppositories with a Combination of α‐Cyclodextrin and Viscosity-Enhancing Pol ysacc haride

Uekama, Kaneto; Kondo, Takashi; Nakamura, Kiyotomo; Irie, Tetsumi; Arakawa, Katsumasa; Shibuya, Masaoki; Tanaka, Joji

doi:10.1002/jps.2600840106

Cited by 26 publications

(13 citation statements)

References 21 publications

(2 reference statements)

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“…The proposed mechanism of permeation enhancement is supported by a lack of observed interaction (increased chemical activity) between insulin and the cyclodextrins in this study as well as recent studies by Chen and Chien 200 which demonstrated that HP--CD (10%) reduced the degradation rate constant of a protein, methionine enkephalin, in rectal extracts by approximately 3-fold. Uekama et al 237 also reported recently on the use of hollowtype suppositories employing R-CD and polysaccharides to modify the rectal absorption of morphine in rabbits. Generally, R-CD and -CD were found to increase the rate and extent of morphine absorption while γ-CD decreased rectal absorption of morphine.…”

Section: Dermal Rectal and Pulmonary Applications Of Cyclodextrinsmentioning

confidence: 94%

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: Dermal Rectal and Pulmonary Applications Of Cyclodextrinsmentioning

confidence: 94%

Pharmaceutical Applications of Cyclodextrins. 2. In Vivo Drug Delivery

Rajewski¹,

Stella²

1996

Journal of Pharmaceutical Sciences

759

374

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“…7 α-CD enhanced the rectal absorption of morphine and human chorionic gonadotropin by increasing their mucosal permeability and reducing their degradation. 154,155 CDs enhance rectal drug stability either by inhibiting the drug/vehicle interaction (by making the drug insoluble in oleaginous base) or by inhibiting the drug bioconversion in the rectum. α-CD improved the rectal bioavailability of morphine by inhibiting the upward movement of the drug from areas impacted by first pass metabolism.…”

Section: Rectal Drug Deliverymentioning

confidence: 99%

Cyclodextrins in drug delivery: An updated review

et al. 2005

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The purpose of this review is to discuss and summarize some of the interesting findings and applications of cyclodextrins (CDs) and their derivatives in different areas of drug delivery, particularly in protein and peptide drug delivery and gene delivery. The article highlights important CD applications in the design of various novel delivery systems like liposomes, microspheres, microcapsules, and nanoparticles. In addition to their well-known effects on drug solubility and dissolution, bioavailability, safety, and stability, their use as excipients in drug formulation are also discussed in this article. The article also focuses on various factors influencing inclusion complex formation because an understanding of the same is necessary for proper handling of these versatile materials. Some important considerations in selecting CDs in drug formulation such as their commercial availability, regulatory status, and patent status are also summarized. CDs, because of their continuing ability to find several novel applications in drug delivery, are expected to solve many problems associated with the delivery of different novel drugs through different delivery routes.

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“…Hydrogel formulations are now used in a variety of fields, including medicine, where they may be used for topical, 5) oral, 6) and rectal 7) delivery. However, in the application of hydrogels, both the drug release rate in vitro and the in vivo gastric transit profile may affect in vivo usefulness, and it is not always clear whether we have the best gel formulation for the targetted purpose.…”

mentioning

confidence: 99%