Preparation method for tadalafil tablets and tablets prepared by method

A technology of dalafil tablets and tadalafil, which is applied in the directions of medical preparations without active ingredients, medical preparations containing active ingredients, and pill delivery, etc., can solve problems such as poor fluidity and unsmooth feeding. , to achieve the effect of reducing agglomeration, saving time and facilitating processing

Active Publication Date: 2020-01-03
ZHUZHOU QIANJIN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, as the particle size of tadalafil becomes smaller during the pulverization process, the surface energy such as charge, water content, and van der Waals force carried by the particles increases, and the fluidity rapidly deteriorates, resulting in agglomeration and unsmooth feeding. This phenomenon is especially obvious in large-scale industrialized production, even if CN107303284A uses tadalafil and tensio-active agent premixing also can't overcome this problem

Method used

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  • Preparation method for tadalafil tablets and tablets prepared by method
  • Preparation method for tadalafil tablets and tablets prepared by method
  • Preparation method for tadalafil tablets and tablets prepared by method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] Prepare 1000 tadalafil tablets according to the prescription in Table 1.

[0066] Table 1 (1000 single-chip dosage and composition ratio, the measurement unit of each composition is grams)

[0067] Element Dosage (g) Composition ratio (%)) Tadalafil 20 5.37 lactose 180 48.37 microcrystalline cellulose 120 32.25 Low-substituted hydroxypropyl cellulose 10 2.69 Hypromellose 10 2.69 Croscarmellose Sodium 15 4.03 Sodium dodecyl sulfate 1.5 0.40 Magnesium stearate 3.6 0.97 Gastric film coating premix 12 3.22

[0068] The preparation process is as follows:

[0069] Micronization:

[0070] Tadalafil and lactose are mixed through a 60-mesh sieve according to the mass ratio of 1:3, and processed once by jet milling to form a micronized composition containing tadalafil, and observe the micronized composition containing tadalafil obtained after pulverization. The appearance of the composition was rec...

Embodiment 2

[0080] The prescription is the same as that of Example 1, the difference is that during the micronization process, tadalafil and lactose are mixed according to the mass ratio of 1:1 and passed through a 60-mesh sieve, and then processed by jet milling once to form a micronized combination containing tadalafil Object, observe the appearance of the tadalafil-containing micronized composition obtained after pulverization, and record the aggregation situation. The conditions of jet milling are: feed air pressure 0.6MPa, grinding air pressure 0.4MPa, and the mixture of tadalafil and soluble lactose is detected by Malvern particle size detector.

Embodiment 3

[0082] The prescription is the same as that in Example 1, the difference is that during the micronization process, tadalafil and lactose are mixed through a 60-mesh sieve according to a mass ratio of 1:5, and subjected to jet milling once to form a micronized combination containing tadalafil Object, observe the appearance of the tadalafil-containing micronized composition obtained after pulverization, and record the aggregation situation. The conditions of jet milling are: feed air pressure 0.6MPa, grinding air pressure 0.4MPa, and the mixture of tadalafil and soluble lactose is detected by Malvern particle size detector.

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Abstract

The invention provides a preparation method for tadalafil tablets. According to the method, a tadalafil raw material and a partial hydrophilic diluent are mixed, micronization is performed, the micronized composition powder obtained after the micronization does not have agglomeration, maintains better fluidity and facilitates subsequent processing, so that the time is saved, the consumed time forthe overall process of tablet preparation is shortened, and the method is especially suitable for industrial large-scale production; the prepared tadalafil tablets containing the micronized composition have a better dissolution rate, and dissolution performance basically consistent with dissolution performance of original research tablets; and the formula and the process are combined, and the prepared tadalafil tablets have the advantages of small change of a total impurity content and a single impurity content.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and more specifically relates to a preparation method of tadalafil tablet and the tablet prepared by the method. Background technique [0002] Tadalafil (Tadalafil) is a reversible, selective PDE5 inhibitor, developed by Eli Lilly and Company for the treatment of male erectile dysfunction (ED), approved by the FDA on November 23, 2003, the chemical name is (6R- 12aR)-6-(1,3-benzodioxol-5-yl)-2-methyl-2,3,6,7,12,12a-hexahydropyrazino[1',2'- 1,6]-pyrido[3,4-b]indole-1,4-dione, the structure is as follows: [0003] [0004] Tadalafil is considered as a solid that is essentially insoluble in water and only slightly soluble in certain organic solvents such as methanol, ethanol and acetone, compounds with low water solubility have low dissolution rate and low bioavailability, BCS classification II Class or IV, for poorly soluble drugs. [0005] US Pat. No. 6,841,167 discloses that the s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K47/38A61K31/4985A61P15/10
CPCA61K9/2095A61K9/2054A61K31/4985A61P15/10
Inventor 龙世玉宿亮袁秀菊郭伟文琛彭程赵静芝
Owner ZHUZHOU QIANJIN PHARMA
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