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Method for producing oral administration delay-control release verapamil hydrochloride micro balls

A technology of verapamil hydrochloride microspheres and verapamil hydrochloride, applied in the field of medicine, can solve problems such as side effects, peaks and valleys, poisoning, etc., and achieve the effects of controllable delay time, controllable release rate, and simple process

Inactive Publication Date: 2006-03-22
TSINGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, except for the coated osmotic pump, most time-selective drug delivery systems use pulsed drug delivery, that is, after a period of delay, the drug is suddenly released in the form of pulses, and the purpose of controlled drug delivery cannot be achieved after the time lag period. Blood drug concentration fluctuates greatly, with "peak and valley" phenomenon
When the blood drug concentration is high (peak), it may exceed the maximum concentration of the therapeutic window (referring to the blood drug concentration range in which the drug exerts its curative effect), causing side effects and even poisoning; when the blood drug concentration is low (valley), it may be lower than the effective The lowest therapeutic concentration, so that the curative effect cannot be shown, which limits the extensive research and application of this technology in this area
The application of microencapsulation technology to prepare delayed-controlled release pharmaceutical preparations has broad application prospects. At present, there are many studies on the preparation of drug particles, and the research on drug particle coating has also been reported, but there is no oral delay-controlled release drug. Report on the preparation method of microspheres

Method used

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  • Method for producing oral administration delay-control release verapamil hydrochloride micro balls
  • Method for producing oral administration delay-control release verapamil hydrochloride micro balls
  • Method for producing oral administration delay-control release verapamil hydrochloride micro balls

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Chitosan-Eudragit RS100 Microspheres (VPH / CS / RS100) Composition of Verapamil Hydrochloride

[0032] Verapamil hydrochloride 0.2g

[0033] Chitosan 2.0g

[0034] Eudragit RS100 4.4g

[0035] 0.1mol / L acetic acid solution 100ml

[0036] Ethyl acetate 220ml

[0037] craft

[0038] 1. Dissolve verapamil hydrochloride and chitosan in 0.1mol / L acetic acid solution, and make a homogeneous solution as the feed liquid for spray drying. The operating parameters of spray drying are: hot air inlet temperature 140°C, hot air volume 0.7m 3 / min, the outlet temperature is 95°C, the feed rate is 12mL / min, and the spray pressure is 250kPa.

[0039] 2. Dissolve Eudragit RS100 in ethyl acetate to make a 2% solution. Under the condition of high-speed stirring, add the chitosan microspheres of verapamil hydrochloride into the solution, and disperse evenly. The obtained material liquid is spray-dried, and the operating parameters are: hot air inlet temperature 80°C, hot air volume 0....

Embodiment 2

[0047] Verapamil Hydrochloride Cellulose Acetate-Eudragit RS100 Microspheres (VPH / CA / RS100)

[0048] Element

[0049] Verapamil hydrochloride 0.6g

[0050] Cellulose acetate 2.4g

[0051] PEG15000.06g

[0052] Eudragit RS100 6.0g

[0053] Ethyl acetate 50ml

[0054] Ethanol 75ml

[0055] craft

[0056] 1. Dissolve cellulose acetate and PEG1500 in ethyl acetate to make a uniform solution. The verapamil hydrochloride is added to the ethyl acetate solution of cellulose acetate under the condition of high-speed stirring to prepare a spray-dried feed liquid. The operating parameters of spray drying are: hot air inlet temperature 55°C, hot air volume 0.7m 3 / min, the outlet temperature is 45°C, the feed rate is 4mL / min, and the spray pressure is 75kPa.

[0057] 2. Dissolve Eudragit RS100 in ethanol to make an 8% solution. Under the condition of high-speed stirring, add the cellulose acetate microcapsules of verapamil hydrochloride into the solution, and disperse evenly. The...

Embodiment 3

[0065] Chitosan-Eudragit RS100 Microspheres of Verapamil Hydrochloride (VPH / CS / RS100)

[0066] Element

[0067] Verapamil hydrochloride 0.5g

[0068] Chitosan 2.0g

[0069] Eudragit RS100 10.0g

[0070] Triethyl citrate 0.5g

[0071] 0.1mol / L acetic acid solution 50ml

[0072] Acetone 200ml

[0073] craft

[0074] 1. Dissolve verapamil hydrochloride and chitosan in 0.1mol / L acetic acid solution, and make a homogeneous solution as the feed liquid for spray drying. The operating parameters of spray drying are: hot air inlet temperature 140°C, hot air volume 0.7m 3 / min, the outlet temperature is 95°C, the feed rate is 12mL / min, and the spray pressure is 75kPa.

[0075] 2. Dissolve Eudragit RS100 and triethyl citrate in acetone to make a solution containing 5% polymer. The drug-loaded microspheres are placed in a micro fluidized bed, and the bottom spray method is used for coating, the nozzle diameter is 0.5mm, and the fluidization air volume is 150m 3 h -1 , the air i...

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Abstract

The present invention belongs to the field of pharmaceutical technology, and the method of preparing orally taken delayed / controlled releasing medicine micro balls features that medicine material and proper functional are dissolved or suspended in delayed / controlled releasing microcapsule material solution and spray dried to prepare medicine particle, and the medicine particle is coated to prepare delayed / controlled releasing medicine micro balls. Via proper preparation process, the present invention may be prepared into various kinds of orally taken preparation. The present invention has the feature that medicine entering body is not released immediately and after the set time delay, the medicine is released in preset rate smoothly and sustainably to reach controlled medicine administration. The present invention can result in optimized treating effect and minimum side effect.

Description

technical field [0001] The invention relates to the technical field of medicine, specifically, it is a method for preparing oral delay-controlled release verapamil hydrochloride microparticles (microcapsules or microspheres) by using spray drying combined with a coating process. Background technique [0002] In recent years, it has been found that certain diseases show rhythmic characteristics. For example, the onset of dyspnea in asthmatic patients changes from day to night. A large number of clinical observations have found that early morning is the high incidence period of asthma; the incidence of hypertension and myocardial infarction is similar. The time-selective drug delivery system can prevent and treat the attack of asthma and myocardial infarction by controlling the drug to release and take effect at an appropriate time. Timed drug formulations generally do not release the drug immediately after entering the body, but rather after a predetermined period of time (la...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K9/52A61K31/275A61P9/10
Inventor 谭丰苹丁富新蒋国强刘铮
Owner TSINGHUA UNIV