Dipyridamole solid dispersion, orally disintegrating tablet and preparation method thereof

A technology of pyridamole solid and dispersion, applied in the field of pharmaceutical preparations, can solve the problems of inconvenient medication for patients, storage aging, low bioavailability, etc., achieve good physical and chemical stability, avoid high temperature heating, and simplify preparation The effect of craft

Active Publication Date: 2021-03-16
GUANGZHOU NEWORLD PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are still only a small amount of solid dispersion formulations on the market, and a major factor restricting its development is the physical and chemical stability of solid dispersions: (1) storage aging, from a thermodynamic point of view, due to the highly dispersed drug and carrier state, these systems are in an unstable state, and tend to transform into a stable crystalline state, and are very easy to transform into low-energy crystals during storage, and the drug crystallizes out from the polymer matrix, which reduces the drug dissolution rate and bioavailability. (2) Gastrointestinal crystallization, the amorphous solid dispersion greatly improves the solubility of the drug in the gastrointestinal fluid, making the drug rapidly released in the gastrointestinal tract to form a supersaturated solution
While the curative effect of injections is positive, there are problems such as the need for professional administration, inconvenience for patients, and low compliance; ordinary tablets and sustained-release tablets have problems such as slow absorption, low bioavailability, and large individual differences, which affect the curative effect
For elderly patients with cardiovascular disease, quick-acting drugs are often needed to relieve symptoms quickly, but there is currently no immediate-release oral preparation of dipyridamole in clinical practice

Method used

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  • Dipyridamole solid dispersion, orally disintegrating tablet and preparation method thereof
  • Dipyridamole solid dispersion, orally disintegrating tablet and preparation method thereof
  • Dipyridamole solid dispersion, orally disintegrating tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Weigh 3.75g of dipyridamole, dissolve in 600ml 80%v / v ethanol aqueous solution, obtain drug solution, slowly add 11.25g of the carrier macromolecule as shown in table 1 respectively in drug solution under the action of magnetic stirring The polymer is dissolved until the carrier is completely dissolved to form a uniform drug-containing carrier solution, and the drug-containing carrier solution is spray-dried at a liquid feed rate of 10 mg / min to obtain a dipyridamole solid dispersion. The process parameters of spray drying are as follows: the outlet air temperature is 79℃~80℃, and the wind speed is 0.6m 3 / min, the atomization pressure is 10Mpa.

[0043] Table 1 is used to prepare the carrier of dipyridamole solid dispersion

[0044]

[0045] The dipyridamole solid dispersion prepared from each recipe in this example was subjected to an in vitro supersaturated dissolution test. Precisely weigh the dipyridamole solid dispersion of each prescription to make it contai...

Embodiment 2

[0049] Stability test of dipyridamole solid dispersion: (1) high temperature test, the dipyridamole solid dispersion newly prepared in Example 1 was spread on a watch glass, and sealed with a cover. Place the watch glass in a constant temperature oven at 60°C, and take samples on the 60th day; (2) Accelerated test, take the dipyridamole solid dispersion newly prepared in Example 1 and place it in a constant temperature and constant humidity at 40°C / 75%RH Under box conditions, samples were taken on the 60th day. The samples taken were characterized as follows.

[0050] (1) Observation of crystal changes by polarizing microscope: take an appropriate amount of sample and place it on a glass slide, gently grind the sample with another clean cover glass to spread it in a thin layer on the glass slide, and then observe the sample under a polarizing microscope Whether there is crystal precipitation.

[0051] (2) Determination of drug content: Accurately weigh 5 mg each of the newly...

Embodiment 3

[0057] Take dipyridamole 3.75g, be dissolved in the ethanol aqueous solution of 600ml 60% v / v, obtain drug solution, slowly add 11.25g HPMC in the drug solution under the action of magnetic stirring, until the carrier material is dissolved to form uniform containing drug carrier solution. The drug-containing carrier solution was spray-dried according to the process parameters described in Example 1 to prepare dipyridamole solid dispersion. The dipyridamole solid dispersion prepared in this example was placed under high temperature and accelerated test conditions (same as Example 2) for stability test, and the storage period was 60 days. The newly prepared and stability tested samples were subjected to supersaturated dissolution according to the method of Example 1, to investigate whether the dissolution behavior of the drug changed. In addition, X-ray powder diffractometer (XRD) is used to determine the crystal form of the drug, and to investigate whether the crystal form of ...

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PUM

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Abstract

The invention relates to a dipyridamole solid dispersion, orally disintegrating tablets and a preparation method thereof. The dipyridamole solid dispersion is prepared from dipyridamole, a carrier and a solvent by virtue of a spray drying method, wherein the mass ratio of the dipyridamole to the carrier is 1:(2-5), and the carrier is at least one of hydroxypropyl methyl cellulose, polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer and hydroxypropyl methylcellulose succinate. The dipyridamole solid dispersion not only can significantly improve in vitro dissolution behaviors of dipyridamole, but also has good physical and chemical stability. The solid dispersion can be compacted into orally disintegrating tablets with similar drug release behaviors, and the orally disintegrating tablet preparation meets clinical requirements of patients and has broad market prospects.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a dipyridamole solid dispersion, an orally disintegrating tablet and a preparation method thereof. Background technique [0002] With the significant increase in life expectancy and the decline in the birth rate, China's population has shown typical "senile" characteristics. In 2010, the proportion of China's population aged 65 and above reached 8.9%, the median age reached about 34.6 years, and the ratio of old to young reached 53.4%. The problem of China's population aging is already quite serious. The arrival of an aging society not only brings great pressure to the social security system, but also brings more challenges to the treatment of diseases of the elderly. Due to the decline of physiological functions, the elderly are prone to various diseases represented by cardiovascular diseases, which makes the development of drugs suitable for the elderly an ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K9/20A61K47/38A61K47/32A61K47/26A61K31/519A61P9/10
CPCA61K9/0056A61K9/1641A61K9/1652A61K9/1682A61K9/2018A61K9/2027A61K9/2054A61K31/519
Inventor 李革彭婷婷陈航平佘友俊王心怡
Owner GUANGZHOU NEWORLD PHARMA CO LTD
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