Abstract
Purpose: To develop a pH-controlled two-pulse drug delivery system of amoxicillin in order to overcome the snag of biological tolerance and to improve bactericidal activity.Methods: The core tablets were compressed and coated with hydroxylpropyl methylcellulose (HPMC) of different viscosities with spray-dried lactose (SDL) as a pore former. The final two-pulse release tablet was prepared with the remaining drug fraction (to be released as the first immediate release pulse) with a disintegrant, giving the final tablet. The tablets were evaluated for pharmaceutical properties including disintegration, thickness, hardness, friability and weight variation and by DSC (differential scanning calorimetry) and FTIR (Fourier transform infrared spectroscopy) studies in order to assess drug/polymer compatibility. The tablets further subjected to in vitro dissolution studies and stability studies.Result: The tablet core disintegrated within 30 to 40 s. Drug content ranged from 97.85 to 98.23 %. FTIR and DSC studies showed drug-polymer compatibility. The developed two-pulse release tablets had acceptable thickness, hardness, friability and weight variation. In vitro drug release showed prolongation of lag time as polymer viscosity increased. With 25 % HPMC and 75 % SDL, drug release was 97.5 % by the end of 8th , 9th &10th h and viscosity was 100, 400 and 4000 cps respectively. No significant difference in drug release was found as values were within limits of confidence interval (p < 0.05). The formulation was stable.Conclusion: The developed formulation demonstrates the feasibility of a two-phase release of amoxicillin separated by a well-defined time-controlled lag phase which is desirable for chronotherapeutic drug delivery.Keywords: Two-pulse drug delivery, Chronotherapeutic drug delivery, Bacterial drug resistance, Amoxicillin
Highlights
Controlled-release formulations have several advantages over immediate-release formulations, such as less frequent drug administration, lower plasma peak concentration to avoid adverse effects, and improved patient compliance
The purpose of the present study is to formulate and evaluate a two-pulse drug delivery system for amoxicillin trihydrate using a swellable polymer, such as hydroxylpropyl methylcellulose (HPMC), that would serve as a drug release barrier that results in drug release at two different times in order to minimize development of bacterial resistance as well as improve patient compliance
Drug excipients interaction studies by FT-IR spectroscopy revealed characteristic absorption peaks of formulations as shown in Figure 1 and the results suggested that the drug is compatible with the respective excipients used, under evaluation based on physical observation
Summary
Controlled-release formulations have several advantages over immediate-release formulations, such as less frequent drug administration, lower plasma peak concentration to avoid adverse effects, and improved patient compliance. Principles of delayed release delivery have lately been applied in developing a newer version of drug delivery, popularly known as chronotherapeutic drug delivery system. Such systems are developed based on the concept of biological/circadian rhythm or chronopharmacological behavior of symptom manifestation of specific conditions such as asthma, hypertension and allergic rhinitis [1,2]. Pulsatile drug delivery system (PDDS) is a type of time-controlled DDS (Drug delivery system). It may be classified as a single-unit or multiple-unit system by application of different coating systems. It demonstrates good bioavailability throughout the entire GI tract and has been used to treat a variety of respiratory infections including otitis media, sinusitis, bronchitis and community-acquired pneumonia [4]
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