Disoproxil fumarate, lamivudine and efavirenz tri-combination compound mini-pill tablet and preparation method thereof

Abstract

The invention discloses a tri-combination compound mini-pill tablet co-prepared by disoproxil fumarate DF coated mini-pills, lamivudine coated mini-pills and efavirenz mini-pills and a preparation method thereof. The invention solves the problems that effective component degradation and dissolution delaying phenomena are generated due to interaction among the tri-combination compound components, tabletting is not facilitated during preparation and patient swallowing is not facilitated; and the single-layer tablet having the three component drugs without mutual contact is prepared by a mini-pill tabletting method, so as to obtain good stability and fast dissolving rate.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a triple compound pellet of tenofovir DF, lamivudine and efavirenz and a preparation method thereof. Background technique [0002] The present invention relates to the treatment of viral infections using the known antiviral compounds tenofovir DF (disoproxilfumarate, also known as TDF, trade name Viread), lamivudine (trade name Epivir) and efavirenz (trade name Sustiva) , especially HIV-infected products. [0003] HIV efficacy has been demonstrated to be ideal with tenofovir DF, lamivudine, and efavirenz. However, producing a commercially viable triple product may require that the final product be bioequivalent to the commercial products Viread, Epivir, Sustiva, and that the tablet be of an appropriate size for patients to swallow easily. [0004] Regarding the tenofovir DF, lamivudine and efavirenz triple compound pellets described in the present invention, there is ...

AI Technical Summary

Problems solved by technology

CN101252920A discloses dry granulation about tenofovir DF, emtricitabine and efavirenz triple compound, thinks that tenofovir DF and efavirenz are incompatible with the indicated active agent, both Tenofovir DF is very unstable and rapidly degrades in stability studies due to exposure

However, because the composition, particle size, density and fluidity of powders and granules are far from those of drug-containing pellets, it is impossible to protect the uniformity of mixing in the process of industrial mass production. Due to the vibration of the machine hopper, the ingredients will also be seriously stratified, resulting in the uncontrollable content of each ingredient in the compound formula.

Disclosed in CN101259111A is the method that the medicine-containing micropill of coating and the blank micropill that accounts for 50%-70% of total tablet weight are mixed and compressed to solve the above problems, but because the proportion of blank micropill is too high, it is only applicable to For small doses of drugs, the dosage of such active ingredients as tenofovir DF, lamivudine and efavirenz compound is as high as 1.2g / tablet (each tablet contains 300mg of tenofovir DF, 300mg of lamivudine, efavirenz Waylon 600mg) varieties are obviously not applicable

Lactose and starch are only used as fillers for pellets, and the pellets have poor plasticity and compressibility