Chronotherapeutic drug delivery for early morning surge in blood pressure: A programmable delivery system

Usha Yogendra Nayak, Gopal Venktesh Shavi, Yogendra Nayak, Ranjith Kumar Averinen, Srinivas Mutalik, Sreenivasa Meka Reddy, Purshottam Das Gupta, Nayanabhirama Udupa

Research output: Contribution to journalArticle

36 Citations (Scopus)

Abstract

The purpose of the study was to develop pulsatile capsule dosage form of valsartan for controlled delivery. In the majority of individuals blood pressure rises in the early morning hours, which lead to serious cardiovascular complications. Formulations with constant/programmable delivery rates make it possible to deliver drug at definite time or controlled rate in chronopharmacokinetic studies. The prepared system contained swellable polymer (l-hydroxypropyl cellulose (L-HPC), xanthan gum, polyethylene oxide or sodium alginate) together with drug tablet and erodible tablet (L-HPC or guar gum) in a pre-coated capsule. Various formulation factors were investigated through series of tests, in vitro dissolution and ex vivo continuous dissolution-absorption studies. We found that the type, amount of polymers and erodible tablet influenced the drug release. The formulation containing 200 mg sodium alginate and erodible tablet (150 mg) containing 50% guar gum and 46% lactose showed 5-6 h lag time and 10 ± 2.1% drug release in initial 6 h following rapid release (99 ± 1.7% release in 12 h) of drug was observed. The continuous dissolution-absorption study conducted using everted rat intestinal segment indicated delay in absorption of drug. Thus this approach can provide a useful means for timed release of valsartan and may be helpful for patients with morning surge.

Original languageEnglish
Pages (from-to)125-131
Number of pages7
JournalJournal of Controlled Release
Volume136
Issue number2
DOIs
Publication statusPublished - 05-06-2009

Fingerprint

guar gum
Valsartan
Tablets
Blood Pressure
Pharmaceutical Preparations
Capsules
Polymers
Dosage Forms
Lactose
Drug Liberation
alginic acid
hydroxypropylcellulose

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

Cite this

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title = "Chronotherapeutic drug delivery for early morning surge in blood pressure: A programmable delivery system",
abstract = "The purpose of the study was to develop pulsatile capsule dosage form of valsartan for controlled delivery. In the majority of individuals blood pressure rises in the early morning hours, which lead to serious cardiovascular complications. Formulations with constant/programmable delivery rates make it possible to deliver drug at definite time or controlled rate in chronopharmacokinetic studies. The prepared system contained swellable polymer (l-hydroxypropyl cellulose (L-HPC), xanthan gum, polyethylene oxide or sodium alginate) together with drug tablet and erodible tablet (L-HPC or guar gum) in a pre-coated capsule. Various formulation factors were investigated through series of tests, in vitro dissolution and ex vivo continuous dissolution-absorption studies. We found that the type, amount of polymers and erodible tablet influenced the drug release. The formulation containing 200 mg sodium alginate and erodible tablet (150 mg) containing 50{\%} guar gum and 46{\%} lactose showed 5-6 h lag time and 10 ± 2.1{\%} drug release in initial 6 h following rapid release (99 ± 1.7{\%} release in 12 h) of drug was observed. The continuous dissolution-absorption study conducted using everted rat intestinal segment indicated delay in absorption of drug. Thus this approach can provide a useful means for timed release of valsartan and may be helpful for patients with morning surge.",
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Chronotherapeutic drug delivery for early morning surge in blood pressure : A programmable delivery system. / Nayak, Usha Yogendra; Shavi, Gopal Venktesh; Nayak, Yogendra; Averinen, Ranjith Kumar; Mutalik, Srinivas; Reddy, Sreenivasa Meka; Gupta, Purshottam Das; Udupa, Nayanabhirama.

In: Journal of Controlled Release, Vol. 136, No. 2, 05.06.2009, p. 125-131.

Research output: Contribution to journalArticle

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T1 - Chronotherapeutic drug delivery for early morning surge in blood pressure

T2 - A programmable delivery system

AU - Nayak, Usha Yogendra

AU - Shavi, Gopal Venktesh

AU - Nayak, Yogendra

AU - Averinen, Ranjith Kumar

AU - Mutalik, Srinivas

AU - Reddy, Sreenivasa Meka

AU - Gupta, Purshottam Das

AU - Udupa, Nayanabhirama

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Y1 - 2009/6/5

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