Preparation method of acetylsalicylic acid colon positioning bioadhesion type sustained release capsules

A technology for acetylsalicylic acid and colon positioning, which is applied in the direction of microcapsules, capsule delivery, medical preparations of non-active ingredients, etc., to achieve the effect of simple and stable preparation technology, stable performance, and good research and development application prospects

Inactive Publication Date: 2018-11-06
QINGDAO UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] It is hard to imagine that a sustained-release drug delivery system that cannot maintain sufficient gastrointestinal residence time and stability can produce satisfactory bioavailability and clinical efficacy, and it is even more difficult to imagine a sustained-release drug delivery system that cannot really solve the problem of burst release of water-soluble drugs It can reduce intestinal mucosal damage, reduce the incidence of gastrointestinal bleeding, and produce satisfactory in vivo effects. Therefore, we believe that the development of ASA colon-localized bioadhesive sustained-release drug delivery system should effectively control the release rate of ASA and overcome the water solubility. While the drug is prone to burst release, it is necessary to ensure the stability of ASA in the intestinal tract and sufficient gastrointestinal residence time

Method used

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  • Preparation method of acetylsalicylic acid colon positioning bioadhesion type sustained release capsules
  • Preparation method of acetylsalicylic acid colon positioning bioadhesion type sustained release capsules
  • Preparation method of acetylsalicylic acid colon positioning bioadhesion type sustained release capsules

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] First fully dissolve β-cyclodextrin and gum arabic respectively, prepare a solution with a concentration of 10% according to a mass ratio of 15:1 between β-cyclodextrin and gum arabic, and mix β-cyclodextrin / gum arabic Glue solution and acetylsalicylic acid crude drug are mixed after being 10:1 by mass ratio, pour into in the dilute hydrochloric acid solution, and add a certain amount of Tween 80 solution wherein, adjust solution pH3, homogeneous pressure is 10MPa, homogeneous The homogenization time is 90s, the homogenization temperature is 45°C, the homogenization is fully emulsified, the vacuum defoaming is 5min, and it is introduced into the spray drying granulator, and the spray drying parameters are adjusted as follows: injection temperature 10°C, injection flow rate 50ml / min, air inlet The temperature is 100°C, and the air outlet temperature is 10°C to obtain acetylsalicylic acid slow-release powder microspheres, which are mixed with hydroxypropyl methylcellulose ...

Embodiment 2

[0033]First fully dissolve the β-cyclodextrin and gelatin respectively, and prepare a solution with a concentration of 15% according to the mass ratio of β-cyclodextrin and gelatin at 1:15, and mix the β-cyclodextrin and gelatin solution with After the acetylsalicylic acid raw material is mixed at a mass ratio of 5:1, it is poured into a deionized aqueous solution, and a certain amount of sodium lauryl sulfate solution is added thereto to adjust the pH to 6, and the homogeneous pressure is 30MPa. The time is 120s, the homogenization temperature is 50°C, the homogenization is fully emulsified, the vacuum defoaming is 8min, and it is introduced into the spray drying granulator, and the spray drying parameters are adjusted as follows: sample injection temperature 20°C, sample flow rate 100ml / min, 150°C and 30°C air outlet temperature to obtain acetylsalicylic acid slow-release powder microspheres, pass through a 100-mesh sieve and mix with hydroxypropyl methylcellulose (HPMC), PVP...

Embodiment 3

[0035] First fully dissolve gum arabic and gelatin respectively, gum arabic and gelatin are made into a solution with a concentration of 8% according to the mass ratio of 3:1, and mix gum arabic and gelatin solution with acetylsalicylic acid raw material drug by mass ratio under stirring condition After mixing 8:1, pour it into the dilute ethanol solution, and add a certain amount of Span solution to it, adjust the pH to 9, the homogenization pressure is 50MPa, the homogenization time is 150s, the homogenization temperature is 40°C, and the homogenization temperature is 40°C. Fully emulsify, vacuum degassing for 10 minutes, import into the spray drying granulator, adjust the spray drying parameters as follows: sample inlet temperature 30°C, sample flow rate 200ml / min, inlet air temperature 200°C, outlet air temperature 60°C, and acetyl water is obtained Salicylic acid slow-release powder microspheres, after passing through 80 mesh sieve, mix with hydroxyethyl cellulose (HEC), c...

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Abstract

The invention discloses a preparation method of acetylsalicylic acid colon positioning bioadhesion type sustained release capsules. The preparation method particularly comprises the following steps: (1) dissolving to obtain a medicine sustained release material solution and mixing the medicine sustained release material solution and ASA; (2) pouring the mixture into a disperse phase solution, adding an emulsifier, and performing high-pressure homogenization, complete emulsification and vacuum defoaming; (3) guiding into a spray drying granulating machine to prepare acetylsalicylic acid sustained release powder microspheres; (4) sieving the prepared acetylsalicylic acid sustained release powder microspheres, mixing the sieved acetylsalicylic acid sustained release powder microspheres, carrier auxiliary materials and filling agents uniformly and preparing granules with ethanol as a wetting agent; and (5) performing granulation and low-temperature vacuum drying on the granules, putting into enterosoluble hollow capsules and packaging to obtain the acetylsalicylic acid colon positioning bioadhesion type sustained release capsules. The preparation method has the advantages of convenience in operation, simple, convenient and stable preparation technology, low manufacturing cost and the like. The prepared product provides a new preparation technology for improving the bioavailabilityof the ASA and the prevention and treatment effect of cardiovascular diseases as well as reducing adverse effect, and has great social benefit and economic benefit.

Description

technical field [0001] The invention belongs to the technical field of new drug research and development, and in particular relates to a preparation method of acetylsalicylic acid colon-localized bioadhesive sustained-release capsules. Background technique [0002] The morbidity and mortality of acute myocardial infarction (AMI) and thromboembolic diseases are very high, and the research on drugs to prevent and treat these diseases has attracted worldwide attention. Since the 1960s, acetylsalicylic acid (ASA) was found to have a significant anti-platelet aggregation effect, and it was used in the treatment and prevention of AMI in the 1970s. Evidence-based medical research has proved that ASA is effective in the prevention and treatment of stroke, angina pectoris, and myocardial infarction. It is an effective drug for diseases such as senile dementia and migraine, which can reduce thrombosis and embolism events in the heart, brain and peripheral blood vessels by 25%. It has...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K47/40A61K47/36A61K47/38A61K47/32A61K47/42A61K31/616A61P7/02A61P9/10A61P25/28A61P25/06
CPCA61K9/5026A61K9/5036A61K9/5047A61K9/5057A61K31/616A61P7/02A61P9/10A61P25/06A61P25/28
Inventor 宋益民张航王慧茹周莉潘爱红满华罗尚邢明霞
Owner QINGDAO UNIV OF SCI & TECH
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