RESUMEN
Purpose: Sildenafil citrate is widely used drug for the treatment of Erectile Dysfunction (ED) and Ginseng is a natural aphrodisiac reported to benefit this condition. The objective of the present study was to develop orodispersible tablets (ODTs) containing combination of Sildenafil citrate and Ginseng extract to improve the bioavailability, reduce the dosing frequency and thereby maintaining the therapeutic efficacy of the drug. Methods: The ODTs were prepared using superdisintegrants such as Croscarmellose sodium (CCS), povidone, and sodium starch glycolate (SSG) at varying concentrations (2%, 4% and 6%) by direct compression. The bitter taste of Sildenafil citrate was masked by Doshion resin. The optimized formulation based on least disintegration time (DT) was chosen to reformulate using sublimating agents such as camphor, menthol or thymol at varying concentrations (1%, 2%, 3%) to further reduce the DT. The compatibility of drug with excipients was investigated and the prepared formulations were evaluated for pre and post-compression parameters. Results: The post-compression parameters such as weight variation, hardness, friability, DT and in-vitro drug release was found within specified limit. The formulation with camphor (2%) had DT of 12 sec and drug release >90% within 5 min hence was considered as optimized formulation. The accelerated stability study and kinetics modelling was performed for optimized formulation. Conclusion: The formulated Sildenafil citrate and Ginseng ODT’s were found to be promising formulation with quicker DT and drug release which will eventually have higher bioavailability and better efficacy along with averting the issues of swallowing and improving patient compliance.
RESUMEN
Oral route is presently the gold standard in the pharmaceutical industry where it is regarded as the safest, most economical and most convenient method of drug delivery resulting in highest patient compliance. Oral delivery of active ingredients include a number of technologies, many of which may be classified as Orodispersible tablets (ODTs). Usually, elderly people experience difficulty in swallowing the conventional dosage forms like tablets, capsules, solutions and suspensions because of tremors of extremities and dysphagia. In some cases such as motion sickness, sudden episodes of allergic attack or coughing, and an unavailability of water, swallowing conventional tablets may be difficult. ODTs systems may offer a solution for these problems. Advancements in the technology arena for manufacturing these systems includes the use of freeze drying, cotton candy, melt extrusion, sublimation, direct compression besides the classical wet granulation processes. This has encnouraged both academia and industry to generate new orally disintegrating formulations and technological approaches in this field. This article attempts at discussing the ideal characteristics, advantages and disadvantages, formulation aspects, formulation technologies and future potential of ODTs.
RESUMEN
The main aim of the study was to develop orodispersible tablets of diethyl carbamazine citrate (an anthelmintic) for improving patient compliance,especially those of paediatric & geriatric categories with difficulties in swallowing. In the wet granulation method mixture of sodium bicarbonate and tartaric acid along with agar were used as disintegrants. The tablet formulation containing 28 mg of agar, 26 mg of sodium bicarbonate and 26 mg of tartaric acid considered as the overall best formulation (with an in vitro dispersion time of approx. 54.39 sec and in vitro drug release of 98.4 %) Short term stability studies (at 40±2ºC/75±5% RH) on the best formulation indicated that there no significant changes in drug content. IR spectroscopic study indicated that there are no drug excipient interactions. The use of mixture of tartaric acid and sodium bicarbonate further assists in taste masking. Undoubtedly the availability of various technologies and the manifold advantages of orodispersible tablets will surely enhance the patient compliance providing rapid onset of action.