Controlled Release Hydrophilic Matrix Tablet Formulations of Isoniazid: Design and In Vitro Studies

Abstract

Abstract. The aim of the present investigation was to develop oral controlled release matrix tablet formulations of isoniazid using hydroxypropyl methylcellulose (HPMC) as a hydrophilic release retardant polymer and to study the influence of various formulation factors like proportion of the polymer, polymer viscosity grade, compression force, and release media on the in vitro release characteristics of the drug. The formulations were developed using wet granulation technology. The in vitro release studies were performed using US Pharmacopoeia type 1 apparatus (basket method) in 900 ml of pH 7.4 phosphate buffer at 100 rpm. The release kinetics was analyzed using KorsmeyerPeppas model. The release profiles were also analyzed using statistical method (one-way analysis of variance) and f 2 metric values. The release profiles found to follow Higuchi's square root kinetics model irrespective of the polymer ratio and the viscosity grade used. The results in the present investigation confirm that the release rate of the drug from the HPMC matrices is highly influenced by the drug/ HPMC ratio and viscosity grade of the HPMC. Also, the effect of compression force and release media was found to be significant on the release profiles of isoniazid from HPMC matrix tablets. The release mechanism was found to be anomalous non-Fickian diffusion in all the cases. In the present investigation, a series of controlled release formulations of isoniazid were developed with different release rates and duration so that these formulations could further be assessed from the in vivo bioavailability studies. The formulations were found to be stable and reproducible.

Inhalable Antitubercular Therapy Mediated by Locust Bean Gum Microparticles

“…In order to establish the experimental setup, it was necessary to determine the solubility of INH and RFB in the specific medium. The solubility of INH in PBS pH 7.4 is reported in the literature as 274˘4.79 mg/mL [57]. In the absence of a value reported in the literature, an experimental determination has defined the maximum solubility of RFB in PBS pH 7.4 + 1% Tween 80 ® as 0.496 mg/mL.…”

QbD-Oriented Development and Characterization of Effervescent Floating-Bioadhesive Tablets of Cefuroxime Axetil

“…The influence of HPMC K100 LV CR, however, was found to be less prominent as compared to the PEO 303 on the bioadhesion strength. However, the bioadhesion characteristics of HPMC K100 LV CR can be attributed owing to its swellable nature by polymer relaxation mechanism, which helps in attachment of the dosage form with the gastric mucosa with the help of entanglement of the polymer chains with mucin chains (33). Overall, the studies revealed maximum bioadhesion strength of the prepared formulation at higher levels of PEO 303 and intermediate levels of HPMC K100 LV CR, where both interact synergistically for exhibiting the optimal bioadhesion.…”

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“…Thus, higher amounts of HPMC and lower amounts of sodium CMC favor the drug release. The amounts of X 1 and X 2 show negative effect on Q 6 . Hence, it can be concluded that both factors show release retardant effect at 6 h. The amounts of X 1 and X 2 show positive effect on SI.…”

“…The drug release pattern is a complex phenomenon at the molecular level, it involves water penetration, polymer swelling as well as drug dissolution, diffusion and polymer erosion process. [3][4][5][6] For drugs with a narrow absorption window in the GI tract, the challenging task was not only to prolong drug release but the retention of the dosage form in the upper GI tract. This results in increase bioavailability, reduced dose, and frequency for drug administration.…”