Segmented intestine targeted drug feeding preparation of brain protein polypeptide and method of preparing the same

A colon-targeted drug delivery and colon-targeted technology, which is applied in pharmaceutical formulations, peptide/protein components, medical preparations of non-active ingredients, etc., to achieve the effects of avoiding pain, improving medication compliance, and avoiding metabolic damage

Inactive Publication Date: 2008-02-27
李立
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, there is no colon-targeted drug delivery preparation of cerebroprotein polypeptide in the domestic market, and there is no research report

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0030]The preparation method for preparing the colon-targeted drug delivery preparation of the cerebroprotein polypeptide of the present invention comprises the following steps: the first step is to prepare the medicinal powder containing the cerebroprotein polypeptide composition; the second step is to place the medicinal powder in a centrifugal coating granulator, Spray sucrose syrup to moisten the drug powder, control the spray flow rate, and dry by blowing air to obtain a 60-80-mesh ball core; the third step is to use the ethanol solution of vidpodone K30 as a binder, and use the powder supply machine to spray the ball core Drug powder, control the feed ratio of binder and drug powder, increase the pellet core to 10-3000um pellets, dry and sieve to obtain the drug-containing pellets; the fourth step, put the drug-containing pellets in a centrifugal bag In the coating granulator, spray the coating solution prepared according to the prescription to the pellets, control the sp...

Embodiment 1

[0033] Take 10,000 grams of fresh pig brain, add 5 times of 0.9% normal saline, homogenate at high speed, add 20,000ml of petroleum ether to degrease three times while stirring, separate the liquid and discard the ether layer, take the degreased solution to adjust to pH 1.5, add appropriate amount of pepsin, 37 Hydrolyze for 6 hours at ℃, adjust to pH 7.5, add appropriate amount of trypsin, hydrolyze for 6 hours at 37℃, centrifuge at high speed, take the supernatant and concentrate it by ultrafiltration, collect the concentrated polypeptide solution with a molecular weight cut-off of 10,000 Daltons, add mannitol as excipient The agent was freeze-dried to obtain 300 grams of off-white polypeptide freeze-dried powder.

[0034] Colon-targeted drug delivery preparation of cerebroprotein polypeptide and its preparation method: Weigh 20 grams of cerebroprotein polypeptide freeze-dried powder, appropriate amount of mannitol excipient and 10 grams of piracetam raw material drug, mix we...

Embodiment 2

[0037] Colon-targeted drug delivery preparation of cerebroprotein polypeptide and its preparation method: Weigh 20 grams of cerebroprotein polypeptide freeze-dried powder, appropriate amount of mannitol excipient and 10 grams of donepezil raw material drug, mix well, put centrifuge and coat to form In the granulator, spray the mass concentration (g / mL) of 50% sucrose syrup to wet the powder, and dry it by blowing at 50°C for 5 hours to obtain 60-80 mesh ball cores, and use the mass concentration (g / mL) of 2% dimension poly The ethanol solution of ketone K30 is used as the binder, and the powder supply machine is used to spray the compound medicine powder on the pellet core, and the feeding ratio of binder and medicine powder is controlled, so that the pellet core is repeatedly enlarged into pellets of 100-400 μm, dried and sieved, that is Get medicated pellets.

[0038] Take by weighing 60 grams of acrylic resin (the mixed resin of acrylic resin EUDRAGIT S100 and acrylic resin...

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Abstract

The invention discloses a colon specific targeting drug-delivery preparation of cerebroprotein polypeptides and its preparing process, wherein the preparation is prepared through coating the drug-containing micro-pellets made from medicinal powder containing cerebroprotein polypeptides components with colon targeting coating layer, or directly loading the drug-containing micro-pellets into the shells of the colon targeting capsule. The process for preparing the colon targeting drug-delivery preparation of the cerebroprotein polypeptides consists of producing drug-containing micro-pellets containing cerebroprotein polypeptides components, then preparing the colon targeting coating liquid, finally coating the drug-containing micro-pellets with the colon targeting coating liquid. The preparation provided by the invention can make the colon release drugs enter blood circulation through colon, thereby avoiding metabolism destruction of the conventional oral preparation peptides drugs on the stomach, as a result, the therapeutic action of the drugs can be sufficiently exploited.

Description

technical field [0001] The invention relates to a colon-targeting preparation, in particular to an active cerebroprotein polypeptide colon-targeting preparation for preventing and treating brain nervous system diseases and a preparation method thereof. Background technique [0002] With the natural increase of population and the change of diet structure, the incidence of aging diseases is becoming more and more serious. Cerebrovascular disease is one of the three main fatal diseases. According to data research, an average of about 10% of the elderly aged 65 to 85 in the world will suffer from suffering from Alzheimer's disease. Animal brain protein hydrolyzate is a specific drug for such diseases. The hydrolyzed cerebroprotein polypeptide is a unique neurotrophic drug for the brain. The peptide has a small molecular weight and can easily pass through the blood-brain barrier. , Cerebral palsy, attention deficit disorder, traumatic brain injury, concussion, cerebral infarcti...

Claims

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Application Information

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IPC IPC(8): A61K38/17A61K47/34A61K47/38A61P25/00A61K31/07A61K31/198A61K31/202A61K31/355A61K31/375A61K31/436A61K31/475A61K31/48A61K31/519A61K31/53A61K31/59A61K31/6615A61K31/7032A61K31/714A61K31/737A61K36/537A61K47/32
Inventor 李立吕应年李延平
Owner 李立
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