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Bufo bufo gargarizans cantor skin extract gelskeleton sustained-release tablets and preparation method thereof

A technology of gel skeleton and extract, applied in the field of preparation and clinical application, can solve the problems of unreachable, long treatment concentration, slow effect and the like, and achieves the advantages of small fluctuation, reduced medication frequency, and less medication frequency. Effect

Inactive Publication Date: 2013-01-23
LOGISTICS UNIV OF CAPF
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The effect is slow in use, and it takes a long time to obtain an effective therapeutic concentration, which cannot meet the requirements of an ideal sustained-release preparation.

Method used

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  • Bufo bufo gargarizans cantor skin extract gelskeleton sustained-release tablets and preparation method thereof
  • Bufo bufo gargarizans cantor skin extract gelskeleton sustained-release tablets and preparation method thereof
  • Bufo bufo gargarizans cantor skin extract gelskeleton sustained-release tablets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Different models of hypromellose prescription 1, 2, 3 sustained-release tablets (conventional sustained-release tablets):

[0041] Weigh the toad skin extract extract, skeleton material (hypromellose K4M, K15M, K100M three types), filler according to the selected prescription ratio, mix them evenly, and crush them through a 60-mesh sieve. Spraying 95% ethanol aqueous solution into wet granulation, after drying the granules, adding an appropriate amount of lubricant talcum powder to the dry granules, mixing evenly, and pressing into tablets to obtain the product. The specific prescriptions and in vitro release conditions of R1, R2, and R3 are shown in Table 1, figure 1 . figure 1 The results showed that the cumulative release in vitro of toad skin extract sustained-release tablets prepared by different types of hypromellose was different. Among them, the cumulative release of active ingredients (ciobufacin base) in the extract of R1 sustained-release tablets increased ...

Embodiment 2

[0045] Prescription R4, R5, R6 of different types of fillers (microcrystalline cellulose, lactose, starch) and prescription R7 of the same type of filler (microcrystalline cellulose) with different dosages (50%, 45%, 40%, 30%) , R8, R9, the preparation method of R10 sustained-release tablet is the same as embodiment 1. See Table 2 for specific prescriptions of R4, R5, R6, R7, R8, R9, and R10.

[0046] For the in vitro release of R4, R5, and R6 formulations of different fillers, see figure 2 . Among them, prescription R4 and R5 sustained-release tablets with microcrystalline cellulose and lactose as fillers have a 10-hour cumulative release of active ingredients (ciinobufacin base) in the extracts approaching 50%, and prescription R6 sustained-release tablets with starch as fillers for 10 hours The release of active ingredients in the product is too low. figure 2 The results show that different types of fillers have an impact on the cumulative release of sustained-release ...

Embodiment 3

[0051] Preparation process of prescription 11, 12 sustained-release tablets (different granulation methods):

[0052] Blending and granulation method: crush and sieve the toad skin extract extract and all auxiliary materials separately, mix evenly, spray into appropriate amount of ethanol aqueous solution with a concentration of 95% by volume, wet granulate and press into tablets, and the sustained-release tablets obtained are R11.

[0053] The method of the present invention: take toad skin extract extract powder and auxiliary materials according to the selected prescription ratio, and pulverize and pass through a 60-mesh sieve respectively. The toad skin extract extract powder is divided into Part A and Part B, Part A is mixed with the skeleton material, sprayed into an appropriate amount of ethanol aqueous solution with a volume concentration of 85% for wet granulation, and dried; Part B is mixed with the filler After mixing, spray an appropriate amount of ethanol for wet g...

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Abstract

The invention discloses bufo bufo gargarizans cantor skin extract gelskeleton sustained-release tablets and a preparation method thereof. The preparation method comprises the following steps: weighing bufo bufo gargarizans cantor skin extract powder, a skeleton material, a filler and a pore forming agent capable of regulating flavor, sieving with a 60-mesh sieve respectively, dividing the bufo bufo gargarizans cantor skin extract powder into a part A and a part B, uniformly mixing the part A with the skeleton material, spraying a proper amount of ethanol or aqueous solution of ethanol, granulating by a wet process, and drying; uniformly mixing the part B with the filler and the pore forming agent capable of regulating flavor, spraying a proper amount of ethanol or aqueous solution of ethanol, granulating by a wet process and dying; and mixing the two parts of grains, adding a proper amount of lubricating agent, and tabletting to obtain the bufo bufo gargarizans cantor skin extract gelskeleton sustained-release tablets. The in-vitro release curve fitting result of the bufo bufo gargarizans cantor skin extract gelskeleton sustained-release tablets prepared by the method disclosed bythe invention indicates that medicines are released by diffusing and / or skeleton dissolution, that the skeleton material can completely dissolve at last, that the medicinal release is complete, and that the bioavailability is high.

Description

technical field [0001] The invention relates to a gel-skeleton sustained-release tablet of toad skin, in particular to the preparation of a gel-skeleton sustained-release tablet of toad skin extract and its clinical application. Background technique [0002] Toad (toad), also called toad. Amphibians have many bumps on the body surface and poisonous glands inside, commonly known as toads and thorns. In my country, it is divided into two types: Bufo sinensis and Bufo black orbit. It is a kind of medicinal protozoan commonly used in Chinese medicine. It has been recorded in ancient books such as "Shen Nong's Materia Medica", "Chinese Materia Medica", "Bielu of Famous Doctors". Toad is "pungent in taste, cool in nature, and poisonous. Guixin, liver, spleen, and lung meridians" can "detoxify and dissipate stagnation, eliminate accumulated water, kill insects and eliminate malnutrition. It is mainly used to treat carbuncle, furuncle, hair back, scrofula, malignant sore, Abdomin...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K35/56A61K9/22A61K47/38A61K47/32A61P35/00A61P1/16A61P31/20A61K35/65
Inventor 张莉胡霞张磊刘蒙袁园仲博甘学超陈莉张岭
Owner LOGISTICS UNIV OF CAPF
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