Formulation, optimization and in-vitro evaluation of aqueous-based enteric coated doxycycline hyclate tablets
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Date
2018-05
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Addis Ababa Universty
Abstract
Doxycycline Hyclate (DXYH) is a tetracycline-class antimicrobial used to treat infections caused by susceptible Gram-positive and Gram-negative organisms. Due to doxycycline’s antibacterial effects on a wide range of pathogens, it is currently one of the most commonly prescribed antibiotics worldwide for treating infectious diseases. There are some disadvantages associated with the standard formulation of doxycycline such as gastrointestinal upset, anorexia, vomiting, and nausea, limiting its acceptability by patients. Enteric coating is recommended to overcome these problems.
In the present study, different formulations of DXYH core tablets were developed using micro crystalline cellulose as a dry binder and different disintegrants in different proportions. From those formulations, formulation with average Concentration of crospovidone (FCP2) was selected as optimized core tablet for enteric coating formulation as it was mechanically stronger with least friability and disintegrating within 3.50±0.12 min. Further, optimized formulation was coated by varying the concentration of enteric coating polymers i.e. Eudragit-L30-D55® and Kollicot® MAE 100 P with aqueous based enteric coating systems.
A central composite design was chosen by considering factors as polymer percentage, 1,2-propylene glycol percentage, coating level, and dependent variables as disintegration in 0.1 N HCl, dissolution in 0.06 N HCl and dissolution in phthalate buffer of pH 5.5. Linear and curvature regression models were developed for response variables. The model was used to achieve an optimized response characteristic of disintegration in 0.1 N HCl, dissolution in 0.06 N HCl and dissolution in phthalate buffer of pH 5.5 with predicted input variables of polymer percentage, 1,2-propylene glycol percentage, and coating level. With the optimized process parameters, tablets were coated and the suitability of the model determined.
The results revealed that the prepared enteric coated tablets exhibited cumulative release 99.3± 1.89 % of DXYH from those tablets coated with Eudragit-L-30-D-55® and 98.5± 2.58 % of DXYH from Kollicot® MAE 100 P within 30 min at factors set to polymer percentage, 1,2-propylene glycol percentage, coating level as (97 %, 8.5 % and 5.52 %) for FCP2E-14 and (91.7 %, 8.5 % and 12.5 %) for FCP2K-18), respectively. Further, low percentage of DXYH release were observed in acidic media 9± 0.71 % in 0.06 N for FCP2E-14 and 9.5+ 1.58 % for FCP2K-18 over a period of 20 min of dissolution. Furthermore, the results of accelerated stability studies for these optimized batches.showed no significant changes in the physical parameters of the tablets, drug content and in-vitro dissolution data until the end of 3 months from the initial values.
Thus the study fulfilled the objective of developing efficient Doxycycline Hyclate aqueous-based enteric coted tablets.
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Keywords
Aqueous-based enteric coating, Eudragit-L-30-D-55®, Kollicot® MAE 100 P, Doxycycline Hyclate, Optimization