Novel pH-dependent colon-specific drug delivery system

A colon positioning and dependent technology, applied in the field of medicine, can solve the problems of poor potency and limit the range of drug use, and achieve the effect of increasing drug concentration, avoiding the first-pass effect, and improving drug efficacy

Inactive Publication Date: 2008-07-02
TIANJIN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The disadvantage is that the degradable material is only effective against certain bacteria in the colon, but poorly effective against other bacteria in the colon, which limits the scope of use of the drug

Method used

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  • Novel pH-dependent colon-specific drug delivery system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Tablet prescription:

[0046] Salbutamol Sulfate 9.6g

[0047] Hypromellose 70g

[0048] Dextrin 15g

[0049] Povidone K 30 Appropriate amount

[0050] Magnesium Stearate 1%

[0051] Preparation:

[0052] Take salbutamol sulfate, hypromellose, dextrin by recipe quantity, cross 80 mesh sieves, add 5% PVP (K 30 ) an appropriate amount of ethanol solution to prepare soft materials, pass through a 16-mesh sieve to granulate, ventilate and dry at 40°C, pass through a 16-mesh sieve for granulation, add magnesium stearate for tableting, and obtain No. 1 sample, with a tablet weight of 120mg / tablet.

Embodiment 2

[0054] Tablet prescription:

[0055] Salbutamol Sulfate 9.6g

[0056] Hypromellose 60g

[0057] Low Substitution-Hydroxypropyl Cellulose 10g

[0058] 15g powdered sugar

[0059] Povidone K 30 Appropriate amount

[0060] Magnesium Stearate 1%

[0061] Preparation:

[0062] Take albuterol sulfate, hypromellose, powdered sugar, low-substituted-hydroxypropyl cellulose and mix evenly according to the prescription amount, cross an 80 mesh sieve, add 15% PVP (K 30) ethanol solution to make soft material, pass through a 16-mesh sieve to granulate, ventilate and dry at 40°C, pass through a 16-mesh sieve for granulation and add magnesium stearate for tableting to obtain No. 2 sample, with a tablet weight of 120mg / tablet.

Embodiment 3

[0064] Tablet prescription:

[0065] Salbutamol Sulfate 9.6g

[0066] Hypromellose 70g

[0067] Low Substitution-Hydroxypropyl Cellulose 10g

[0068] 15g powdered sugar

[0069] Povidone K 30 Appropriate amount

[0070] Talc powder 6g

[0071] Magnesium Stearate Appropriate amount

[0072] Preparation:

[0073] Take albuterol sulfate, hypromellose, powdered sugar, talcum powder, low-substituted-hydroxypropyl cellulose and mix evenly according to the prescription amount, cross an 80 mesh sieve, add 15% PVP (K 30 ) ethanol solution to make soft material, pass through a 16-mesh sieve to granulate, ventilate and dry at 40°C, pass through a 16-mesh sieve for granulation and add magnesium stearate for tableting to obtain No. 3 sample, with a tablet weight of 120mg / tablet. .

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Abstract

The invention relates to a novel pH-dependent colon-specific drug delivery system, which adopts pH-dependent colon-specific drug delivered polymer thin film coating material as the main coating material, a tablet core forms a hydrophilic gel frame structure, the coating film can be dissolved at specific parts (part is dissolved at the tail end of small intestine and the most is dissolved at the colon part) according to the condition of high pH (pH is more than 7.2) of the tail end of small intestine and the colon part, so as to play the role of colon-specific drug delivery. The invention is based on the principles of chrono-pharmacology and human physiology, which can ensure the pH-dependent colon-specific drug delivered polymer thin film coating material to be released slowly and for 12 hours in a sustained way after the dissolution at least, so as to achieve the oral colon-specific slow release effect.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, and in particular relates to a novel pH-dependent colon-positioned drug delivery system. Background technique: [0002] The time pharmacokinetic data show that most of the physiological functions related to drug transport in the human body, such as cardiac output, liver and kidney blood flow, secretion speed and pH value of various body fluids, gastrointestinal motility, etc., have a circadian rhythm, which makes many One or several pharmacokinetic parameters of a drug thus exhibit diurnal variations. Clinical practice has confirmed that many common diseases such as asthma, hypertension, angina pectoris, and arthritis all show circadian rhythm changes. The best administration time for asthma is at 4:00 in the morning; the best administration time for hypertension is at 3:00 in the morning, etc. However, traditional drug administration methods often result in high blood drug concentrations in ...

Claims

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Application Information

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IPC IPC(8): A61K9/30A61K47/38
Inventor 房志仲王晶晶米莹杨金荣
Owner TIANJIN MEDICAL UNIV
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