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Formulation development, optimization, and evaluation of sustained release tablet of valacyclovir hydrochloride by combined approach of floating and swelling for better gastric retention

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Abstract

The present study is intended to enhance gastric retention of sustained release tablet of valacyclovir hydrochloride by combined approach of floating and swelling. The tablets are prepared by direct compression method. Polyethylene oxide (Polyox WSR 303) is selected as the swelling matrix agent. Sodium starch glycolate (SSG) is used as swelling enhancer, and sodium bicarbonate is used as an effervescent agent for floating. A 32 full factorial design is applied to systematically optimize the formulation. The concentration of Polyox WSR 303 (X 1) and concentration of SSG (X 2) are selected as independent variables. The percentage drug release at 12 h, floating lag time, and maximum percentage swelling are selected as dependent variables. Formulations are evaluated for hardness, friability, floating lag time, total floating time, percentage swelling, in vitro drug release, and in vivo floating study. The results indicated that X 1 and X 2 significantly affected the drug release properties, floating lag times, and maximum percentage swelling. Release rate decreases as the concentration of Polyox increased. Regression analysis and numerical optimization are performed to identify the best formulation. Formulation F5 prepared with Polyox WSR 303 (15 %) and SSG (10 %) is found to be the best formulation. F5 followed zero-order release mechanism. Swelling and floating gastroretentive tablets of valacyclovir HCl are successfully formulated with controlled delivery to stomach with an aim of increasing the mean residence time in the upper part of GIT where the drug has its absorption window.

The main objective is to formulate and evaluate swellable and floating tablets of a model drug valacyclovir HCl for sustained delivery to stomach with an aim of increasing the mean residence time in the stomach from where the drug slowly releases and reaches its absorption site at the upper part of the intestine. Thus, better absorption, improved bioavailability, reduction in side effects, local action, and also patient compliance of the product can enhance the efficiency of the medical treatment.

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Acknowledgments

The authors are thankful to LJK Trust, Ahmedabad, for providing the needed lab facilities. Authors are also thankful to Colorcon Asia Pvt. Ltd, Goa, India, for providing polyethylene oxide for the research work.

Conflict of interest

For the submission of this manuscript, we would like to undertake that Pratik Upadhyay, Kunal Nayak, Kaushika Patel, Jaymin Patel, Dr. Shreeraj Shah, and Prof. Jayant Deshpande declare that they have no conflict of interest. The research has been reviewed and approved by an appropriate human or animal research or ethics review committee ref: LJIP/IAEC/12-13/09. All authors agree that the contents of the manuscript are confidential and will not be copyrighted, submitted, or published elsewhere (including the Internet), in any language, while acceptance by the journal is under consideration.

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Authors and Affiliations

  1. Department of Pharmaceutical Technology, L. J. Institute of Pharmacy, Ahmedabad, Gujarat, 382210, India

    Pratik Upadhyay, Kunal Nayak, Kaushika Patel, Jaymin Patel, Shreeraj Shah & Jayant Deshpande

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  1. Pratik Upadhyay
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  2. Kunal Nayak
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  3. Kaushika Patel
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  4. Jaymin Patel
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  5. Shreeraj Shah
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Correspondence to Pratik Upadhyay.

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This manuscript has been submitted for publication in Drug Delivery and Translational Research. The corresponding author of this manuscript is Pratik H. Upadhyay and other contributors of the exertion are Kunal P. Nayak, Kaushika M. Patel, Jaymin M. Patel, Dr. Shreeraj H. Shah, and Prof. Jayant M. Deshpande with their responsibility in the research.

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Upadhyay, P., Nayak, K., Patel, K. et al. Formulation development, optimization, and evaluation of sustained release tablet of valacyclovir hydrochloride by combined approach of floating and swelling for better gastric retention. Drug Deliv. and Transl. Res. 4, 452–464 (2014). https://doi.org/10.1007/s13346-014-0207-x

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