Abstract:
:Background: To overcome the rigorous aseptic process widely adopted by commercial long-acting injections, this work aimed to prepare a sterile MPA injection by manipulating the crystal habit through a bottom-up method. Methods: The habit of the precipitated crystals was modified by changing the process conditions. Wherein, the cubic crystal (MPA-C) was obtained by mixing acetonitrile and water at a ratio of 1:4 (v/v) under an ultrasonic condition. Spherical crystal (MPA-S) was prepared with acetonitrile-water mixture (1:20, v/v). The addition of external additives could stop a certain crystal surface growth to obtain rod-like crystal (MPA-R) and branched crystal (MPA-B). Results: All these crystals were proved to be of the same crystal form with different preferential growth orientation by PXRD, DSC, and SEM. The in vitro release of MPA-R microcrystal suspensions is faster than MPA-DP, while that of MPA-C is slightly slower. The relative bioavailability of MPA-C and MPA-R was 103.3% and 68.5%, respectively. The PK profile of MPA-C was most close to the commercial Depo-Provera® (MPA-DP) after intramuscular administration to male SD rats. Conclusions: A cubic crystal of MPA was successfully prepared by anti-solvent precipitation method with the aid of sonication, providing an alternative strategy for the preparation of long-acting injections.
journal_name
Expert Opin Drug Delivjournal_title
Expert opinion on drug deliveryauthors
Sun R,Guo Y,Yin N,Yin J,Yin T,He H,Gou J,Zhang Y,Tang Xdoi
10.1080/17425247.2019.1662394subject
Has Abstractpub_date
2019-10-01 00:00:00pages
1133-1144issue
10eissn
1742-5247issn
1744-7593journal_volume
16pub_type
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journal_title:Expert opinion on drug delivery
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journal_title:Expert opinion on drug delivery
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journal_title:Expert opinion on drug delivery
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journal_title:Expert opinion on drug delivery
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journal_title:Expert opinion on drug delivery
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journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
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journal_title:Expert opinion on drug delivery
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journal_title:Expert opinion on drug delivery
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journal_title:Expert opinion on drug delivery
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journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
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journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
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更新日期:2010-04-01 00:00:00
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journal_title:Expert opinion on drug delivery
pub_type: 杂志文章
doi:10.1517/17425247.2016.1123247
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journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
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journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
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更新日期:2012-04-01 00:00:00
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journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.5.6.641
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journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
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更新日期:2018-07-01 00:00:00
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journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
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journal_title:Expert opinion on drug delivery
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journal_title:Expert opinion on drug delivery
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journal_title:Expert opinion on drug delivery
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journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
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journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
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journal_title:Expert opinion on drug delivery
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journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
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journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
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journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.2014.902048
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abstract:INTRODUCTION:Over the past several decades, liposomes have been used in a variety of applications, from delivery vehicles to cell membrane models. In terms of pharmaceutical use, they can offer control over the release of active agents encapsulated into their lipid bilayer or aqueous core, while providing protection fr...
journal_title:Expert opinion on drug delivery
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abstract:INTRODUCTION:Overexpression of VEGF has been identified to be associated with many pathologic processes such as tumors and retinopathy. Inhibiting uncontrolled growth of VEGF is a promising strategy to treat these diseases. Currently small molecule inhibitors and monoclonal antibodies are the primary treatment. However...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.2014.926886
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journal_title:Expert opinion on drug delivery
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