Abstract：
:The primary objective of this study was to evaluate the effect of drug loading on the release of leuprolide acetate from an injectable polymeric implant, formed in situ, and efficacy of the released drug in suppressing serum testosterone levels in dogs for at least 90 days. An additional objective was to compare the optimum implant formulation with a commercial microsphere product. Evaluated implant formulations contained 45% w/w 75/25 poly (DL-lactide-co-glycolide) polymer having an intrinsic viscosity of 0.20 dL/g, dissolved in N-methyl-2-pyrrolidone. Irradiated polymer solution was mixed with leuprolide at different drug loads (3%, 4.5%, and 6% w/w) prior to subcutaneous administration to dogs. Dog serum was analyzed for testosterone (RIA) and leuprolide (LC/MS/MS) levels and comparisons within the three implant formulation groups were made. Varying the drug load did not significantly affect the release of leuprolide or efficacy of the implant formulation. Thus, the 6% w/w formulation with the smaller injection volume was selected for comparison with the commercial LUPRON Depot product, which was administered intramuscularly at a similar dosage. These comparisons of serum testosterone and leuprolide levels showed no significant difference in the pharmacologic efficacy even though drug levels were different at a number of points. This was mainly due to associated high standard deviations. Based on these studies, the 6% w/w leuprolide implant formulation was considered to be a suitable candidate for further development. Additional benefits of this system include its simple manufacturing and lower costs.
journal_name
AAPS PharmSciTechjournal_title
AAPS PharmSciTechauthors
Ravivarapu HB,Moyer KL,Dunn RLdoi
10.1208/pt010101keywords:
subject
Has Abstractpub_date
2000-02-28 00:00:00pages
E1issue
1issn
1530-9932journal_volume
1pub_type
杂志文章abstract：:The use of amorphous solid dispersions to improve the bioavailability of active ingredients from the BCS II and IV classifications continues to gain interest in the pharmaceutical industry. Over the last decade, methods for generating amorphous solid dispersions have been well established in commercially available pro...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章,评审
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更新日期：2018-07-01 00:00:00
abstract：:The objective of this study was to evaluate possible usefulness of pectins for direct compression of tablets. The deformation behavior of pectin grades of different degree of methoxylation (DM), namely, 5%, 10%, 25%, 35%, 40%, 50%, and 60% were, examined in terms of yield pressures (YP) derived from Heckel profiles fo...
journal_title：AAPS PharmSciTech
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
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更新日期：2009-01-01 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章,评审
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-012-9790-7
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journal_title：AAPS PharmSciTech
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-019-1420-1
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt050109
更新日期：2004-02-12 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-008-9184-z
更新日期：2009-01-01 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-019-1523-8
更新日期：2020-01-29 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章,评审
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doi：10.1208/s12249-017-0799-9
更新日期：2017-11-01 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-020-01775-0
更新日期：2020-08-13 00:00:00
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journal_title：AAPS PharmSciTech
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更新日期：2011-06-01 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章,评审
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更新日期：2017-02-01 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-020-01712-1
更新日期：2020-07-07 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt020311
更新日期：2001-07-12 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
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更新日期：2011-12-01 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt070110
更新日期：2006-02-03 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-008-9116-y
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-017-0746-9
更新日期：2017-10-01 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
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更新日期：2017-02-01 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt050336
更新日期：2004-04-26 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
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更新日期：2018-01-01 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt050453
更新日期：2004-09-13 00:00:00
