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Tadalafil pharmaceutical composition and preparation method thereof

A technology of tadalafil and composition, applied in the field of tadalafil powder direct compression tablet composition and preparation thereof, can solve the problems of undiscovered tadalafil, easy aggregation of drugs, poor mixing uniformity, etc. Good disintegration effect, high dissolution and bioavailability, good compressibility

Inactive Publication Date: 2016-01-06
SHENZHEN NEPTUNUS PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, micronized drugs have low bulk density and serious electrostatic phenomena, and direct compression has problems such as poor mixing uniformity, poor compressibility, poor formability of tablets, and easy aggregation of drugs due to electrostatic effects during dissolution.
At present, the formulation of tadalafil on the market is prepared by wet granulation, and there is no report on the preparation of tadalafil by direct compression method

Method used

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  • Tadalafil pharmaceutical composition and preparation method thereof
  • Tadalafil pharmaceutical composition and preparation method thereof
  • Tadalafil pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Embodiment 1 Tadalafil powder direct compression tablet formulation and preparation method thereof

[0030] 【prescription】

[0031] Element

Weight per tablet (mg)

Tadalafil

5.0

Spray Dried Mannitol

274.0

Microcrystalline Cellulose (PH102)

90.5

Hydroxypropyl Cellulose (EXF)

28.0

Crospovidone

20.0

Talc

2.5

total

420.0

[0032] 【Preparation】

[0033] (1) spray-dried mannitol, microcrystalline cellulose (PH102), hydroxypropyl cellulose (EXF), crospovidone, talc are respectively crossed with 40 mesh sieves for subsequent use;

[0034] (2) the spray-dried mannitol that crosses 40 mesh sieves in the step (1) of taking by weighing recipe quantity, crosses 60 mesh sieves again, and 60 mesh sieves lower part and tadalafil (particle diameter is D 90 = 7.6 μm) mixed for 5 min, and then passed through a 60-mesh sieve to mix;

[0035] (3) adding in step (2) the spray-dried mannitol of...

Embodiment 2

[0038] Embodiment 2 Tadalafil powder direct compression tablet prescription and preparation method thereof

[0039] 【prescription】

[0040] Element

Weight per tablet (mg)

Tadalafil

10.0

Granular lactose (Tablettose80)

140.07

Microcrystalline Cellulose (PH102)

35.0

Hydroxypropylmethylcellulose

1.5

Sodium Stearyl Fumarate

3.5

total

190.0

[0041] 【Preparation】

[0042] (1) Granular lactose (Tablettose80), microcrystalline cellulose (PH102), hydroxypropyl methylcellulose, croscarmellose sodium, sodium stearyl fumarate are respectively sieved through 40 mesh sieves for subsequent use;

[0043] (2) the granular lactose (Tablettose80) that crossed 40 mesh sieves in the step (1) of taking by weighing recipe quantity, crossed 60 mesh sieves again, and the part under 60 mesh sieves was mixed with tadalafil (particle size is D 90 =53μm) mixed for 5min, and then mixed through a 60 mesh sieve;

[00...

Embodiment 3

[0047] Embodiment 3 Tadalafil powder direct compression tablet prescription and preparation method thereof

[0048] 【prescription】

[0049] Element

Weight per tablet (mg)

Tadalafil

20.0

Lactose-Microcrystalline Cellulose Complex (Cellactose)

321.0

Croscarmellose sodium

7.2

Magnesium stearate

1.8

total

350.0

[0050] 【Preparation】

[0051] (1) Lactose-microcrystalline cellulose composite (Cellactose), croscarmellose sodium, magnesium stearate were respectively sieved through a 40-mesh sieve for subsequent use;

[0052](2) The lactose-microcrystalline cellulose compound (Cellactose) passing through a 40-mesh sieve in the step (1) of weighing the prescription amount is passed through a 60-mesh sieve, and the part under the 60-mesh sieve is mixed with tadalafil (particle size for D 90 =7.6 μm) and mix for 5 minutes, then pass through a 60-mesh sieve and mix;

[0053] (3) Add the remaining lactose-micr...

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Abstract

The invention discloses a tadalafil pharmaceutical composition. The tadalafil pharmaceutical composition comprises, by weight percentage, 1-10% of tadalafil, 80-95% of filler, 0.5-2% of lubricant, not more than 7% of binder and not more than 5% of disintegrating agent. The tadalafil pharmaceutical composition has the advantages that medicine powder direct compression problems are solved by optimizing powder direct compression auxiliary material types, controlling raw material and auxiliary material proportion and optimizing powder direct compression mixing sequence; tadalafil tablets with good compressibility, high medicine content evenness and high dissolution rate can be obtained unexpectedly; disintegrating agent use amount of the tablets can be reduced evidently as compared with that of original trituration while a good disintegrating effect and high dissolution rate and bioavailability are achieved; no wetting agent such as lauryl sodium sulfate needs to be added into the tablets, and the side effects of the tablets on the gastrointestinal tract can be reduced.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a powdered direct tableting composition of insoluble micronized medicine and a preparation method thereof, in particular to a tadalafil powdered direct tableting composition and a preparation method thereof. Background technique [0002] Tadalafil, a reversible and selective inhibitor of phosphodiesterase-5 (PDE5), enhances the release of nitric oxide during sexual stimulation. Eli Lilly is developing the drug for two indications: erectile dysfunction (ED) and pulmonary hypertension, and its trade name is Cialis. A large number of clinical studies have proved that tadalafil can effectively improve the erectile function of patients with various etiologies and degrees of ED, even refractory ED, such as ED after severe spinal cord injury, diabetic ED and ED after prostatectomy. [0003] Cialis is an ordinary film-coated tablet of tadalafil. In addition to the active ingredi...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/4985A61K47/38A61K47/32A61K47/26A61K47/12A61K47/04A61P15/00A61P15/10
Inventor 肖琰王志国杨经安崔婧王丽丽
Owner SHENZHEN NEPTUNUS PHARM CO LTD
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