Valaciclovir hydrochloride tablet and preparation method thereof

Abstract

The invention provides a valaciclovir hydrochloride tablet and a preparation method thereof. The valaciclovir hydrochloride tablet is prepared from valaciclovir hydrochloride particles, a filling agent, a disintegrating agent, an adhesive, a lubricant A and a lubricant B, wherein the valaciclovir hydrochloride particles are prepared from valaciclovir, magnesium oxide, the lubricant A and the lubricant B. The preparation method comprises the following steps: preparing the valaciclovir hydrochloride particles by adopting a dry granulation technology; then mixing the valaciclovir hydrochloride particles with other auxiliary materials; and tabletting. The magnesium oxide as an alkaline oxidant is added for preparing the valaciclovir hydrochloride particles, so that the release rate of a medicine can be effectively adjusted, and the in-vitro dissolution behavior of the medicine is enabled to be similar to that of a reference preparation in multi-medium; and in addition, the inter-batch quality and the within-batch quality of the valaciclovir hydrochloride tablet are stabilized.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a valacyclovir hydrochloride tablet and a preparation method thereof. Background technique [0002] Valacyclovir Hydrochloride (Valacyclovir Hydrochloride) is the prodrug of Acyclovir. It is absorbed rapidly after oral administration and is quickly converted into Acyclovir in the body. Its antiviral effect is played by Acyclovir. Acyclovir Wei is an open-chain purine nucleoside, which can inhibit the synthesis of viral deoxyribonucleic acid, but has less effect on the synthesis of host cell DNA. [0003] Valaciclovir hydrochloride tablets have been listed in China. Its original research company is GlaxoSmithKline. Its trade name is Valtrex, and its Chinese trade name is Weidesi. The US manual discloses that the auxiliary materials of this product are: carnauba wax, colloidal silicon dioxide, crospovidone, FD&C Blue No.2 Lake, hypromellose, magnesium stearate, microcrys...

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Problems solved by technology

[0004] Patent CN1313081 describes that valacyclovir hydrochloride has stickiness, and the tablet hardness and friability of high-content valacyclovir hydrochloride are poor. Technical measures such as increasing the tableting pressure, reducing the proportion of lubricants and increasing the proportion of binders did not solve the problem

This patent uses colloidal silicon dioxide as an auxiliary material to solve the problem of poor tablet hardness and friability of high-content valacyclovir hydrochloride, but the preparation method adopted is wet granulation, and wet granulation has many disadvantages. If drying and granulation are required after granulation, the batch production time is long and the cost is high, and valacyclovir hydrochloride has various crystal forms, including anhydrous crystal form and hydrate crystal form, and wet granulation has the possibility of crystal conversion of raw materials potential risks

[0005] Patent US20080167325A1 discloses dry granulation or powder direct compression method to prepare valacyclovir hydrochloride tablets, although the disadvantages of wet granulation process have been avoided, but our research It was found that the tablets prepared according to the disclosed protocol and the reference preparation Valtrex had large differences in in vitro dissolution behavior in multiple dissolution media, especially in the first 10 minutes in pH 1.0 hydrochloric acid medium, and the in vitro dissolution behavior between batches was significantly different. Large variation in dissolution behavior and poor batch-to-batch stability

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