Use of Hydrophilic Natural Gums in Formulation of Sustained-release Matrix Tablets of Tramadol Hydrochloride

Department of Pharmaceutics, School of Pharmacy, Isfahan University of Medical Sciences, Isfahan, Iran.
AAPS PharmSciTech (Impact Factor: 1.64). 02/2006; 7(1):E24. DOI: 10.1208/pt070124
Source: PubMed


The objective of this work was to develop matrix sustained-release tablets of highly water-soluble tramadol HCl using natural gums (xanthan [X gum] and guar [G gum]) as cost-effective, nontoxic, easily available, and suitable hydrophilic matrix systems compared with the extensively investigated hydrophilic matrices (ie, hydroxypropyl methylcellulose [HPMC]/carboxymethyl cellulose [CMC] with respect to in vitro drug release rate) and hydration rate of the polymers. Matrix tablets of tramadol (dose 100 mg) were produced by direct compression method. Different ratios of 100:0, 80:20, 60:40, 20:80, 0:100 of G gum (or X):HPMC, X gum:G gum, and triple mixture of these polymers (G gum, X gum, HPMC) were applied. After evaluation of physical characteristics of tablets, the dissolution test was performed in the phosphate buffer media (pH 7.4) up to 8 hours. Tablets with only X had the highest mean dissolution time (MDT), the least dissolution efficiency (DE(8)%), and released the drug following a zero-order model via swelling, diffusion, and erosion mechanisms. Guar gum alone could not efficiently control the drug release, while X and all combinations of natural gums with HPMC could retard tramadol HCl release. However, according to the similarity factor (f(2) ), pure HPMC and H(8)G(2) were the most similar formulations to Topalgic-LP as the reference standard.

Download full-text


Available from: Naser Tavakoli, Mar 03, 2014
  • Source
    • "Natural gums are a group of polymers now widely used in pharmaceutical dosage forms due to their nontoxic , non-irritant nature, ease of accessibility and relatively lower cost compared to synthetic polymers. The various natural gums used in sustained release drug delivery system include xanthan gum [6], guar gum [7], and okra gum [8]. Cissus gum is obtained from the stem of Cissus populnea Guill. "
    [Show abstract] [Hide abstract]
    ABSTRACT: Natural gums are polymers widely used as excipients in drug formulation. Polymer extraction and formulation processing methods could significantly affect formulation characteristics. To evaluate different methods of gum extraction and the effect of different compression methods on the mechanical and release properties of tramadol hydrochloride matrix tablets incorporating cissus gum as controlled release polymer. Water (CW) and acetone (CA) extracts of cissus gum were obtained from Cissus populea stem and two methods - wet granulation and direct compression - were used to compress the tablet and compare it with xanthan gum (X) formulations. Crushing strength and friability were used to assess mechanical properties while dissolution rate were used to assess release properties. Data were analysed using t-test and ANOVA at p < 0.05. The crushing strength of tramadol tablets has increased together with the increase in polymer concentration in all formulations, while friability has decreased for both methods. Tablets made by wet granulation had higher crushing strength than those made by direct compression method. The release mechanism for both direct compression and wet granulation methods was Fickian and non-Fickian respectively. The rank order for t25, t50 and t75 for all formulations was X > CA > CW. Generally, wet granulation method decreased the rate of tramadol release more than direct compression method, indicating a higher drug retarding ability. Incorporation of cissus gum controlled the release of tramadol hydrochloride from the matrix tablets. Extraction method and formulation variables influenced mechanical and release properties of the tablets. Cissus gum acetone extract had comparable release properties with xanthan gum and could serve as a cheaper alternative in controlled release tablet formulations.
    Polimery w medycynie 10/2014; 44(4):209 - 220.
  • Source
    • "Where, ‘n’ is the number of pull points, wt is an optional weight factor, Rt is the reference profile at time point ‘t’, and Tt is the test profile at the same time point; the value of f2 should be between 50 and 100. An f2 value of 100 suggests that the test and reference profiles are identical and, as the value becomes smaller, the dissimilarity between release profiles increases [15]. The above values are summarized in Table 3. "
    [Show abstract] [Hide abstract]
    ABSTRACT: Natural gums are economical, easily available, and useful as tablet binders. In the present investigation, an attempt was made to formulate Ofloxacin tablets using three natural binders, namely Acacia arabica, Hibiscus esculentus, and xanthan gum. Such six batches of Ofloxacin tablets were prepared by using different types and amounts of the natural binders by the wet granulation method. The tablets were analyzed for their hardness, friability, and weight variation, and in vitro release was performed in a phosphate buffer at pH 6.8. The prepared tablets were also evaluated for their various release kinetics and similarity factors f2. The physical properties of the tablets containing the natural binders showed sufficient hardness, desirable disintegration time, and low friability. Their better percentage of drug release was observed as compared to the marketed formulation showing more than 85% drug release within 45 minutes. The in vitro release data was well-fitted into zero-order and the values of release exponent 'n' were between 0.303 and 0.514. The high similarity factor f2 of 64.50 was achieved with the best batch in comparison to the marketed tablets. The results obtained indicated that the gum Acacia arabica performed as well as gelatin compared to the other binders for the Ofloxacin tablet formulation.
    Scientia Pharmaceutica 06/2014; 82(2):441-8. DOI:10.3797/scipharm.1401-14
  • Source
    • "Locust bean gum (LBG) is a neutral plant galactomannan extracted from the seed (kernels) of the carob tree Ceratonia siliqua L. fabaceae [8]. The okra gum and LBG shows a synergistic gelation in acidic pH [9,10] and in combination with HPMC K4M forms an original gelation which has an excellent buoyancy and useful for oral gastro retentive formulations. "
    [Show abstract] [Hide abstract]
    ABSTRACT: Objective of this study is to show the potential use of natural gums in the development of drug delivery systems. Therefore in this work gastro retentive tablet formulations of ziprasidone HCl were developed using simplex lattice design considering concentration of okra gum, locust bean gum and HPMC K4M as independent variables. A response surface plot and multiple regression equations were used to evaluate the effect of independent variables on hardness, flag time, floating time and drug release for 1 h, 2 h, and 8 h and for 24 h. A checkpoint batch was also prepared by considering the constraints and desirability of optimized formulation to improve its in vitro performance. Significance of result was analyzed using ANOVA and p < 0.05 was considered statistically significant. Formulation chiefly contains locust bean gum found to be favorable for hardness and floatability but combined effect of three variables was responsible for the sustained release of drug. The in vitro drug release data of check point batch (F8) was found to be sustained well compared to the most satisfactory formulation (F7) of 7 runs. The 'n' value was found to be between 0.5 and 1 suggesting that release of drug follows anomalous (non-fickian) diffusion mechanism indicating both diffusion and erosion mechanism from these natural gums. Predicted results were almost similar to the observed experimental values indicating the accuracy of the design. In vivo floatability test indicated non adherence to the gastric mucosa and tablets remain buoyant for more than 24 h. Study showed these eco-friendly natural gums can be considered as promising SR polymers.
    DARU-JOURNAL OF FACULTY OF PHARMACY 10/2012; 20(1):58. DOI:10.1186/2008-2231-20-58 · 1.64 Impact Factor
Show more