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Salvia miltiorrhiza effective-component synchronous site-specific drug delivery mini-pill and preparation method thereof

A technology of simultaneous positioning and active ingredients, applied in the field of medicine, to achieve the effects of reducing the dosage of administration, simple and easy-to-control preparation process, and promoting absorption

Inactive Publication Date: 2010-07-14
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no report on the method of making the effective components of Salvia miltiorrhiza into localized drug release preparations.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Example 1 Salvia miltiorrhiza effective fraction extraction

[0043] Extraction of total phenolic acid of salvia miltiorrhiza

[0044] The Danshen medicinal material is pulverized and passed through a 40-mesh sieve as Danshen coarse powder. Take an appropriate amount of Danshen coarse powder, soak overnight with 0.1mol distilled water 10 times the mass of Danshen coarse powder. Then decoct at 100°C for 1.5h, let cool and then filter. The dregs are decocted twice under this condition. The three filtrates were combined and concentrated as the upper column liquid. After the upper column solution was adsorbed on the macroporous resin for 1 hour, it was washed with distilled water with suitable pH until the phthalic acid-aniline color reaction was negative. Put the combined cleaning solution on the AB-8 macroporous resin column, first wash 5 volumes with water, then wash 6 volumes with 20% ethanol, and finally wash 4 volumes with 40% ethanol, combine this part of the elu...

Embodiment 2

[0047] The preparation of embodiment 2 salvia miltiorrhiza active ingredient pellets

[0048] Preparation of salvianolic acid pellets: total salvianolic acid: 20%

[0049] Microcrystalline Cellulose: 80%

[0050] Water: Appropriate amount

[0051] Preparation of total tanshenone pellets: total tanshenone: 20%

[0052] PVPP: 10%

[0053] Lactose: 20%

[0054] SDS: 0.2%

[0055] MCC: 49.8%

[0056] Weigh the extract raw materials and excipients respectively, make a soft material with an appropriate amount of water as a binder, and put it into an extrusion spheronizer. The extrusion speed is 30Hz, the spheronization speed is 50Hz, and the spheronization time is 5min.

[0057] Coating of Danshen Active Component Drug-releasing Pellets

[0058] Preparation of coating solution for intragastric release pellets of salvianolic acid: slowly pour a certain am...

Embodiment 3

[0064] Salvia phenolic acid coated pellets

[0065] Total Salvianolic Acids: 10%

[0066] MCC: 90%

[0067] Binder: water

[0068] The total salvianolic acid and microcrystalline cellulose were evenly mixed, and the water-made soft material was extruded at a speed of 30 Hz and spheronized at a speed of 50 Hz. The rounding time is 5 minutes. Eudragit E 100 10%, talc is equivalent to 50% of the polymer, triethyl citrate is equivalent to 15% of the polymer isopropanol / water (85 / 5) balance.

[0069] The weight gain of the coating is 5%, the heat treatment is 40°C for 4h, and the speed of the dissolution apparatus is 100r·min-1. Take the coated pellets, 200 mg, and use artificial gastric juice as the dissolution medium to carry out the release test. The release of the salvia phenolic acid pellets in the artificial gastric juice can be completely released within 4 hours.

[0070] Preparation of tanshen total ketone localized drug release coated pellets

[0071] Total Tanshinon...

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PUM

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Abstract

The invention discloses a salvia miltiorrhiza effective-component synchronous site-specific drug delivery mini-pill and a preparation method thereof, belonging to the technical field of drugs. The effective salvia miltiorrhiza component synchronous site-specific drug delivery mini-pill is a pill-shaped preparation obtained by the following steps of: respectively adding a right amount of excipients to salvianolic acid and tanshinone to prepare a mini-pill with the diameter being smaller than 2.5 mm; then respectively coating stomachic coating and enteric coating on the mini-pill with the diameter being smaller than 2.5 mm; and mixing according to the ratio of 1:1. The preparation method can adopt an extrusion-spheronization method and a fluidized bed coating method. Compared with the prior art, the invention solves the problem of effective-component synchronous site-specific delivery, can enhance the bioavailability and is beneficial to stabilizing the effective components; the salvia miltiorrhiza effective-component synchronous site-specific drug delivery mini-pill has outstanding curative effect on cardiovascular and cerebrovascular diseases, such as hypertension, cerebral thrombosis, coronary heart disease, and the like; in addition, the preparation method can adopt conventional process equipment and has the advantages of high production efficiency, stable product quality, validity period more than two years and easy industrialized production.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to a synchronously positioned drug-releasing pellet of active ingredients of salvia miltiorrhiza and a preparation method thereof. Background technique [0002] Salvia miltiorrhiza is the dry root and rhizome of Salvia miltiorrhiza Bge., a plant of the genus Salvia in the family Lamiaceae. This product can dispel blood stasis and relieve pain, dissipate blood stasis and relieve pain, and is used to treat chest pain, coronary heart disease, angina pectoris, myocardial infarction, etc. It is widely used clinically, promotes blood circulation, stimulates menstrual flow, clears heart and troubles, has mild effect, has no obvious toxic and side effects, can be taken for a long time, and considers the rhythm of the onset of coronary heart disease, so this prescription is suitable for the research of timed release preparations. [0003] At present, there are many kinds of Danshen prepara...

Claims

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Application Information

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IPC IPC(8): A61K36/537A61K9/20A61K9/48A61K9/16A61K47/32A61P9/10A61K125/00
Inventor 赵秀丽陈大为杨春荣胡晓丹
Owner SHENYANG PHARMA UNIVERSITY
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