Tenofovir, lamivudine and efavirenz triple compound pellets and preparation method thereof

A technology of lamivudine pellets and tenofovir, which is applied in pill delivery, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve problems such as delamination, poor compressibility, and poor plasticity of pellets. Achieve good mixing uniformity, reduce the amount of auxiliary materials, and good formability

Active Publication Date: 2016-08-24
ANHUI BIOCHEM BIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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 large-scale industrial production. Due to the vibration of the hopper of the machine, the ingredients will also be seriously stratified, resulting in the uncontrollable content of the ingredients of the compound recipe.
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

Method used

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  • Tenofovir, lamivudine and efavirenz triple compound pellets and preparation method thereof
  • Tenofovir, lamivudine and efavirenz triple compound pellets and preparation method thereof
  • Tenofovir, lamivudine and efavirenz triple compound pellets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] (a) preparation of tenofovir DF coated pellets

[0047] Tenofovir DF

30g

microcrystalline cellulose

6g

lactose

2g

Croscarmellose Sodium

2.5g

2% aqueous solution of povidone K30

Q.S.

Commercially available hydroxypropyl methylcellulose coating solution

Q.S.

100 pieces

[0048] Preparation method: Weigh the prescription amount of raw materials and auxiliary materials, mix them evenly, use 2% aqueous solution of povidone K30 as the adhesive to make soft materials, extrude and spheronize to prepare tenofovir DF drug-containing pellet cores, and sieve 30-40 mesh ready to use. Take the above-mentioned drug-containing pellet cores in a fluidized bed, prepare a commercially available finished hydroxypropyl methylcellulose coating solution, and coat an isolation coat. The weight gain of the coating is about 6%, and tenofovir DF coated pellets are prepared.

[0049] (b) preparation of lamivudine co...

Embodiment 2

[0058] (a) preparation of tenofovir DF coated pellets

[0059] Tenofovir DF

30g

microcrystalline cellulose

8g

Croscarmellose Sodium

2.5g

2% aqueous solution of povidone K30

Q.S.

Commercially available hydroxypropyl methylcellulose coating solution

Q.S.

100 pieces

[0060] Preparation method: Weigh the prescription amount of raw materials and auxiliary materials, mix them evenly, use 2% aqueous solution of povidone K30 as the adhesive to make soft materials, extrude and spheronize to prepare tenofovir DF drug-containing pellet cores, and sieve 30-40 mesh ready to use. Take the above-mentioned drug-containing pellet cores in a fluidized bed, prepare a commercially available finished hydroxypropyl methylcellulose coating solution, and coat an isolation coat. The weight gain of the coating is about 6%, and tenofovir DF coated pellets are prepared.

[0061] (b) preparation of lamivudine coated pellets

[0062...

Embodiment 3

[0069] (a) preparation of tenofovir DF coated pellets

[0070] Tenofovir DF

30g

microcrystalline cellulose

6g

lactose

2g

Croscarmellose Sodium

2.5g

2% aqueous solution of povidone K30

Q.S.

Commercially available hydroxypropyl methylcellulose coating solution

Q.S.

100 pieces

[0071] Preparation method: Weigh the prescription amount of raw materials and auxiliary materials, mix them evenly, use 2% aqueous solution of povidone K30 as the adhesive to make soft materials, extrude and spheronize to prepare tenofovir DF drug-containing pellet cores, and sieve 30-40 mesh ready to use. Take the above-mentioned drug-containing pellet cores in a centrifugal granulation coating machine, prepare a commercially available finished hydroxypropyl methylcellulose coating liquid and coat an isolation coat, and the weight of the coating will increase by about 6%, to prepare tenofovir DF coated pellets .

[0072] ...

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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 use of known antiviral compounds tenofovir DF (disoproxil fumarate, also known as TDF, trade name Viread), lamivudine (trade name Epivir) and efavirenz (trade name Sustiva) for the treatment of viruses Infections, 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, th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/675A61K31/536A61K31/513A61K9/20A61P31/12A61P31/18
Inventor 邢怀阳沈蔡月
Owner ANHUI BIOCHEM BIO PHARMA
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