Study On Ribavirin Effervescent Tablet

Ribavirin one kind of nucleosides, is broad-spectrum antiviral agent. It is a IMP dehydrogenase inhibitor, and has the broad-spectrum antiviral acitivity. It can be used to treat influenza, parainfluenza, epidemic hemorrhagic fever, herpes simplex, varicella and herpes zoster. In clinic, it is always used to treat influenza, virus bronchopneumonia, virus hepatitis, respiratory syncytial virus infection, acute keratitis, conjunctivities, epidemic hemorrhagic fever and herpes zoster. Effervescent tablet is one kind of tablet which ontains NaHCO3 and organic acid. It will produce vapor and be effervescent in the presence of water. It can be divided into oral effervescent tablet and external one, according to the different administration routes. The oral effervescent tablet will cause acid-base reaction and disintegrate quickly in the water before administration, which can promote the bioavailability. It is suitable for the children, old people and the patients loss of the ability to swallow because the colour, fragrance and taste can be regulated easily. So ribavirin was developed into effervescent tablet to promote the bioavailability in the thesis.First of all, the compatibility of the main drug and adjuvants was studied to lay a foundation for the formula design and process optimization.Secondly, orthogonal experimental design was adopted to screen the formula by setting the disintegrating time limit, hydroscopic property and briquetting ratio as the indexes after the kinds of acid-base and flavouring agent was confirmed. The bondingagent and granulation methods were studied. We also studied the shape of granulation, liquidity and hydroscopic property. The small scale and pilot scale test showed that the process route was reproducible, feasible and adaptable, and the products can meet the requirements.Thirdly, the acidity, disintegrating time limit, related substances examination, content uniformity and methodology of ribavirin effervescent tablet were studied. The related substances examination was studied, by referring to Chinese Pharmacopoeia 2010 volume Ⅱ. The results showed the method was suitable for the related substances examination. The content of ribavirin in the tablet was determined by HPLC and the methodology study showed than the specificity, linearity, precision, reproducibility and recoverty ratio were good and it was stable in 8hs at the room temperature. Quality standards draft was drawed based on the shape, indentification, disintegrating time limit, content determination methodology and related substances study of the preparation.At last, the infulencing factors and stability in 6 months was studied. The accelerating stability test was explored for 6 months under the temperature of 40℃±2℃ and relative humidity of 75%±5%; the long-term stability test was studied under the temperature of 25℃±2℃ and relative humidity of 60%±10% for 6 months. The items including shape of ribavirin effervescent tablet, indentification, disintegrating time limit, acidity and content were studied to confirm the storage condition and validity period.The results that the process is rational; the appearance of tablet is complete, uniform and glossy and well-effervscent; the content determination method is simple,quick, reliable and controllable and it is stable.