Comparison of the solubility and pharmacokinetics of sildenafil salts

To develop sildenafil lactate, a salt form of sildenafil with improved solubility and bioavailability of poorly water-soluble sildenafil base, this salt form was prepared using a spray dryer. Its solubility and pharmacokinetics in rabbits were evaluated compared with sildenafil base and sildenafil c...

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Published in:	Archives of pharmacal research Vol. 34; no. 3; pp. 451 - 454
Main Authors:	Jung, Si-Young, Seo, Youn-Gee, Kim, Gun Kook, Woo, Jong Soo, Yong, Chul Soon, Choi, Han-Gon
Format:	Journal Article
Language:	English
Published:	Heidelberg Pharmaceutical Society of Korea 01-03-2011 대한약학회
Subjects:	Administration, Oral Animals Area Under Curve Biological Availability Drug Compounding Erectile Dysfunction - drug therapy Male Medicine Pharmacology/Toxicology Pharmacy Piperazines - blood Piperazines - chemistry Piperazines - pharmacokinetics Piperazines - pharmacology Purines - blood Purines - chemistry Purines - pharmacokinetics Rabbits Sildenafil Citrate Solubility Structure-Activity Relationship Sulfones - blood Sulfones - chemistry Sulfones - pharmacokinetics Sulfones - pharmacology 약학 Sildenafil lactate Pharmacokinetics Solubility
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Abstract	To develop sildenafil lactate, a salt form of sildenafil with improved solubility and bioavailability of poorly water-soluble sildenafil base, this salt form was prepared using a spray dryer. Its solubility and pharmacokinetics in rabbits were evaluated compared with sildenafil base and sildenafil citrate. Sildenafil lactate improved the solubility of sildenafil in various solvents including distilled water compared with sildenafil citrate. It provided higher AUC and C max and, shorter t 1/2 values than did the other materials, indicating that it improved the oral bioavailability of sildenafil in rabbits. Our results suggest that sildenafil lactate would be useful to deliver sildenafil in a pattern that allows fast absorption and late metabolism. Furthermore, the plasma concentration at 0.25 h in sildenafil lactate was similar to the C max value at T max (0.5 h) in sildenafil citrate. Thus, sildenafil lactate might provide a faster onset of action and immediate erection compared with sildenafil citrate, the conventional drug.
AbstractList	To develop sildenafil lactate, a salt form of sildenafil with improved solubility and bioavailability of poorly water-soluble sildenafil base, this salt form was prepared using a spray dryer. Its solubility and pharmacokinetics in rabbits were evaluated compared with sildenafil base and sildenafil citrate. Sildenafil lactate improved the solubility of sildenafil in various solvents including distilled water compared with sildenafil citrate. It provided higher AUC and C max and, shorter t 1/2 values than did the other materials, indicating that it improved the oral bioavailability of sildenafil in rabbits. Our results suggest that sildenafil lactate would be useful to deliver sildenafil in a pattern that allows fast absorption and late metabolism. Furthermore, the plasma concentration at 0.25 h in sildenafil lactate was similar to the C max value at T max (0.5 h) in sildenafil citrate. Thus, sildenafil lactate might provide a faster onset of action and immediate erection compared with sildenafil citrate, the conventional drug. To develop sildenafil lactate, a salt form of sildenafil with improved solubility and bioavailability of poorly water-soluble sildenafil base, this salt form was prepared using a spray dryer. Its solubility and pharmacokinetics in rabbits were evaluated compared with sildenafil base and sildenafil citrate. Sildenafil lactate improved the solubility of sildenafil in various solvents including distilled water compared with sildenafil citrate. It provided higher AUC and C_max and, shorter t_(1/2) values than did the other materials, indicating that it improved the oral bioavailability of sildenafil in rabbits. Our results suggest that sildenafil lactate would be useful to deliver sildenafil in a pattern that allows fast absorption and late metabolism. Furthermore, the plasma concentration at 0.25 h in sildenafil lactate was similar to the C_max value at T_max (0.5 h) in sildenafil citrate. Thus, sildenafil lactate might provide a faster onset of action and immediate erection compared with sildenafil citrate, the conventional drug. KCI Citation Count: 36 To develop sildenafil lactate, a salt form of sildenafil with improved solubility and bioavailability of poorly water-soluble sildenafil base, this salt form was prepared using a spray dryer. Its solubility and pharmacokinetics in rabbits were evaluated compared with sildenafil base and sildenafil citrate. Sildenafil lactate improved the solubility of sildenafil in various solvents including distilled water compared with sildenafil citrate. It provided higher AUC and C(max) and, shorter t(1/2) values than did the other materials, indicating that it improved the oral bioavailability of sildenafil in rabbits. Our results suggest that sildenafil lactate would be useful to deliver sildenafil in a pattern that allows fast absorption and late metabolism. Furthermore, the plasma concentration at 0.25 h in sildenafil lactate was similar to the C(max) value at T(max) (0.5 h) in sildenafil citrate. Thus, sildenafil lactate might provide a faster onset of action and immediate erection compared with sildenafil citrate, the conventional drug.
Author	Jung, Si-Young Choi, Han-Gon Woo, Jong Soo Yong, Chul Soon Seo, Youn-Gee Kim, Gun Kook
Author_xml	– sequence: 1 givenname: Si-Young surname: Jung fullname: Jung, Si-Young organization: College of Pharmacy, Yeungnam University, Pharmaceutical Research Center, Hanmi Pharm. Co., Ltd – sequence: 2 givenname: Youn-Gee surname: Seo fullname: Seo, Youn-Gee organization: College of Pharmacy, Yeungnam University – sequence: 3 givenname: Gun Kook surname: Kim fullname: Kim, Gun Kook organization: College of Pharmacy, Yeungnam University – sequence: 4 givenname: Jong Soo surname: Woo fullname: Woo, Jong Soo organization: Pharmaceutical Research Center, Hanmi Pharm. Co., Ltd – sequence: 5 givenname: Chul Soon surname: Yong fullname: Yong, Chul Soon email: csyong@yumail.ac.kr organization: College of Pharmacy, Yeungnam University – sequence: 6 givenname: Han-Gon surname: Choi fullname: Choi, Han-Gon email: hangon@yumail.ac.kr organization: College of Pharmacy, Yeungnam University, College of Pharmacy, Hanyang University
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SubjectTerms	Administration, Oral Animals Area Under Curve Biological Availability Drug Compounding Erectile Dysfunction - drug therapy Male Medicine Pharmacology/Toxicology Pharmacy Piperazines - blood Piperazines - chemistry Piperazines - pharmacokinetics Piperazines - pharmacology Purines - blood Purines - chemistry Purines - pharmacokinetics Rabbits Sildenafil Citrate Solubility Structure-Activity Relationship Sulfones - blood Sulfones - chemistry Sulfones - pharmacokinetics Sulfones - pharmacology 약학
Title	Comparison of the solubility and pharmacokinetics of sildenafil salts
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