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Zero-Order Release Formulation of Oxprenolol Hydrochloride with Swelling and Erosion Control

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Abstract

Zero-order release of oxprenolol hydrochloride was obtained by controlling the swelling and erosion of the matrix. This formulation involves only mixing of drug, hydroxypropylmethylcellulose (HPMC), and sodium carboxymethylcellulose (Na CMC) at the ratio of 1:0.4:1.6, respectively, and compressing the mixture directly into tablets. The in vitro release pattern from this optimized matrix tablet was reproducible. Accelerated stability studies revealed that the optimized formulation remains stable for an approximately 2-year shelf life. This sustained-release (SR) tablet was evaluated in dogs, and for comparison a conventional (CV) formulation was also given at the same dose level. Plasma oxprenolol levels were monitored by a sensitive and specific high-performance liquid chromatographic (HPLC) method. Significant differences in the pharmacokinetic parameters, i.e., lower C max, higher values of t max, MRT, AUC, and plasma concentration at 24 hr, and nearly constant plasma levels over 12 hr, indicated that the SR matrix tablet is superior to the CV rapid-releasing formulation. The in vitro release parameters and in vivo pharmacokinetics correlated well.

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Authors and Affiliations

  1. Department of Pharmaceutical Sciences, Panjab University, Chandigarh, 160 014, India

    Kanikanti Padmalatha Devi, Kanikanti V. Ranga Rao & Srikrishan Baveja

  2. Central Laboratory for Clinical Chemistry, University Cantonal Hospital, Geneva, Switzerland

    Marc Fathi & Marc Roth

Authors
  1. Kanikanti Padmalatha Devi
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  2. Kanikanti V. Ranga Rao
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  3. Srikrishan Baveja
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  4. Marc Fathi
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  5. Marc Roth
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Devi, K.P., Rao, K.V.R., Baveja, S. et al. Zero-Order Release Formulation of Oxprenolol Hydrochloride with Swelling and Erosion Control. Pharm Res 6, 313–317 (1989). https://doi.org/10.1023/A:1015998424548

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