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Avanafil effervescent dry suspension and preparation method thereof

A technology of avanafil and dry suspension, which is applied in the direction of medical preparations of non-active ingredients, pharmaceutical formulas, inorganic non-active ingredients, etc., and can solve the problem of not significantly improving the oral bioavailability of insoluble drugs and increasing the insoluble Problems such as drug solubility, large production safety hazards, etc., to achieve the effect of changing pharmacokinetic characteristics, ensuring a highly dispersed state, and fast onset of action

Inactive Publication Date: 2016-12-28
NEW FOUNDER HLDG DEV LLC +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the suspension state, the dispersion of the drug is relatively high, and the dissolution rate is relatively fast, but because the conventional suspension or dry suspension formulation does not focus on increasing the solubility of poorly soluble drugs in aqueous media, it is usually However, conventional suspensions or dry suspensions cannot significantly improve the oral bioavailability of poorly soluble drugs
Due to the poor dissolution rate of many insoluble drugs, the bioavailability after taking the drug is low, which affects the therapeutic effect and causes waste of drug resources.
[0007] Chinese patent application No.02805070.3 discloses a rapidly disintegrating tablet in the mouth containing a phosphodiesterase 5 (PDE5) inhibitor, which requires two-step fluidized bed granulation, using a double-layer or triple-layer rotary press Compressing tablets with a tablet machine, and then treating them with the vapor of an alcohol solvent, is technically difficult, requires high production equipment, and has great potential safety hazards in large-scale production, which is not conducive to industrialized large-scale production, and the residue of alcohol solvent may affect the health of patients
In addition, orally disintegrating tablets will affect the taking of patients with insufficient saliva secretion, and the taste is poor, which affects the compliance of patients taking

Method used

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  • Avanafil effervescent dry suspension and preparation method thereof
  • Avanafil effervescent dry suspension and preparation method thereof
  • Avanafil effervescent dry suspension and preparation method thereof

Examples

Experimental program
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Effect test

preparation example Construction

[0083] (2) Preparation method of avanafil effervescent dry suspension

[0084] method 1:

[0085] The present invention also provides a kind of preparation method of described avanafil effervescent dry suspension, described method comprises:

[0086]1) Fully dry the avanafil, the effervescent disintegrant, the filler, the suspending agent, and optional other pharmaceutical excipients respectively, and pulverize them to 100 mesh Particle size below the sieve; and

[0087] 2) Thoroughly mix the avanafil, effervescent disintegrating agent, filler, suspending agent, and optional other pharmaceutical excipients obtained in step 1), so as to obtain the avanafil effervescent dry mix Suspension.

[0088] Method 2:

[0089] The present invention also provides a kind of preparation method of described avanafil effervescent dry suspension, described method comprises:

[0090] a) Fully dry the avanafil, the effervescent disintegrant, the filler, the suspending agent, and optional oth...

Embodiment 1-3

[0115] See Table 1 for the single dose formulations of Examples 1-3.

[0116] Table 1

[0117] raw material

Embodiment 1

[0118] Example 1 Preparation process: The raw and auxiliary materials were dried and crushed through a 100-mesh sieve, weighed according to the above prescription ratio, and the active ingredient avanafil was mixed with fillers, suspending agents, effervescent disintegrants, and flavoring agents (i.e., sweeteners). Flavor and essence, the same below) and colorant are mixed evenly, and 5% (w / v) povidone k30 absolute ethanol solution is used as a binder to make granules. After the granules are dry, add glidant and mix well. Packed in single doses.

[0119] The preparation process of Example 2: the raw and auxiliary materials were dried and crushed through a 100-mesh sieve, weighed according to the above-mentioned prescription ratio, and the active ingredient avanafil was evenly mixed with the filler, suspending agent, and effervescent disintegrating agent, and then added the correction agent Flavoring agent, glidant and coloring agent are thoroughly mixed and uniformly formed in...

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Abstract

The invention provides an avanafil effervescent dry suspension and a preparation method thereof. The effervescent dry suspension of avanafil of the present invention comprises avanafil, effervescent disintegrant, filler, suspending agent, and optional other pharmaceutical adjuvants, wherein, the other pharmaceutical adjuvants It is one or more of glidants, sweeteners, flavors and coloring agents; the effervescent disintegrant is composed of acidic and alkaline substances; the avanafil and the acidic The weight ratio of the substances is 1:(6-25); and the weight ratio of the acidic substance to the basic substance is greater than or equal to 2.5:1. The avanafil effervescent dry suspension of the invention has rapid dispersion, quick onset of action, high bioavailability and good stability, and the dissolution rate of avanafil can be as high as 89% or more.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an avanafil effervescent dry suspension and a preparation method thereof. Background technique [0002] The molecular formula of avanafil is C 23 h 26 ClN 7 o 3 , a molecular weight of 483.95, is a white crystalline powder, slightly soluble in ethanol, almost insoluble in water; its structural formula is as shown in formula I: [0003] [0004] Formula I [0005] Avanafil is a phosphodiesterase type 5 inhibitor (PDE5-I), which increases blood flow to the penis and is used to treat erectile dysfunction (ED) in men. [0006] In practical application, since avanafil is almost insoluble in water, suspension or dry suspension is one of the more commonly used dosage forms for poorly soluble solid drugs. In the suspension state, the dispersion of the drug is relatively high, and the dissolution rate is relatively fast, but because the conventional suspensi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K31/506A61K47/12A61K47/02A61P15/10
Inventor 易崇勤孟宏涛郑少辉郭欲晓马德君
Owner NEW FOUNDER HLDG DEV LLC
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