阅读说明：本技术 一种山庄降脂微丸及其制备方法 (Villa lipid-lowering pellet and preparation method thereof ) 是由 刘景萍 刘全国 陈克领 王家 李党 于 2021-01-29 设计创作，主要内容包括：本发明公开了一种山庄降脂微丸及其制备方法,该微丸由以下重量份原料制成：决明子1240份、山楂620份、荷叶420份、糊精150-320份、蔗糖20-36份、魔芋胶15-32份、羟丙基甲基纤维素18-25份。采用本发明工艺制备的山庄降脂微丸中的有效成分含量较高,大黄酚、橙黄决明素；荷叶的有效成分为荷叶碱是一种生物碱,将其与山楂分开提取避免可能与酸的反应,提高微丸的有效成分；山楂使用离子液体提取,能使山楂中的黄酮类物质等提取更充分完全；采用微丸剂型能缩短药物在人体内的崩解时间,提高药物的利用率。(The invention discloses a villous lipid-lowering pellet and a preparation method thereof, wherein the pellet is prepared from the following raw materials in parts by weight: 1240 parts of cassia seed, 620 parts of hawthorn, 420 parts of lotus leaf, 320 parts of dextrin, 20-36 parts of cane sugar, 15-32 parts of konjac glucomannan and 18-25 parts of hydroxypropyl methyl cellulose. The effective components in the villa lipid-lowering pellet prepared by the process are higher in content, and chrysophanol and aurantio-obtusin; the effective component of the lotus leaf is nuciferine which is an alkaloid, and the nuciferine and the hawthorn are extracted separately to avoid possible reaction with acid, so that the effective component of the pellet is improved; the hawthorn is extracted by using the ionic liquid, so that flavonoids and the like in the hawthorn can be fully and completely extracted; the micro pill can shorten the disintegration time of the medicine in human body and improve the utilization rate of the medicine.)

1. The preparation method of the villous lipid-lowering pellet is characterized in that the pellet is prepared from the following raw materials in parts by weight: 1240 parts of cassia seed, 620 parts of hawthorn, 420 parts of lotus leaf, 320 parts of dextrin, 20-36 parts of cane sugar, 15-32 parts of konjac glucomannan and 18-25 parts of hydroxypropyl methyl cellulose, wherein the preparation method of the pellet comprises the following steps:

r1, respectively selecting semen Cassiae, fructus crataegi and folium Nelumbinis, cleaning, and drying;

r2, weighing the cassia seed, the hawthorn, the lotus leaf, the dextrin, the sucrose, the konjac glucomannan and the hydroxypropyl methyl cellulose according to the parts by weight;

r3, respectively crushing the cassia seeds and the lotus leaves, adding an ethanol water solution A for soaking, ultrasonically extracting, filtering, recovering ethanol from an extracting solution, and concentrating into thick paste;

crushing hawthorn, mixing with ionic liquid, carrying out ultrasonic extraction at 50-60 ℃ for 20-60 min, concentrating and drying filtrate, adding an ethanol water solution B for dissolving, adsorbing by macroporous resin, washing with water, adding an ethanol water solution C for eluting, recovering ethanol, and concentrating into thick paste;

r5. dissolving dextrin in water under stirring, adding the soft extract from step R3, and stirring to obtain mixture;

r6. mixing the thick paste obtained in step R4 with the mixture of R5, adding part of hydroxypropyl methylcellulose, stirring, making into pill, oven drying, and sieving to obtain drug-loaded pellet;

r7. adding water into sucrose, stirring, adding konjac glucomannan, stirring, adding the rest hydroxypropyl methylcellulose, and stirring to obtain coating solution;

r8. and (4) taking the drug-loaded pellets obtained in the step R6, coating the drug-loaded pellets with the coating solution of R7 in a fluidized bed coating machine, and subpackaging to obtain the drug-loaded pellets.

2. The method for preparing the villa lipid-lowering pellet as claimed in claim 1, wherein in the step R3, the volume concentration of the ethanol aqueous solution A is 70-80%, the usage amount is 8-10 times of the weight of the cassia seeds and the lotus leaves, the soaking time is 40-120min, and the ultrasonic extraction time is 45-90 min.

3. The method for preparing the villa lipid-lowering pellet as claimed in claim 1 or 2, wherein in the step R4, the ionic liquid is one or two of 1-butyl-3-methylimidazolium acetate and 1-en-butyl-3-methylimidazolium chloride, and the amount of the ionic liquid is 1.3-1.5 times of the weight of the hawthorn.

4. The method for preparing the villa lipid-lowering pellet as claimed in claim 1, wherein in the step R4, the volume concentration of the ethanol aqueous solution B is 50-65% by weight, and the volume concentration of the ethanol aqueous solution C is 75-85% by weight, and the volume concentration is 10-15% by weight of the hawthorn.

5. The method for preparing the villa lipid-lowering pellet as claimed in claim 1, wherein the hydroxypropyl methylcellulose added in the step R6 is 10-15 parts by weight, the drying temperature is 38-49 ℃, and the drug-loaded pellets collected by screening are 20-35 meshes.

6. A villa lipid-lowering pellet, which is prepared by the preparation method of the villa lipid-lowering pellet of any one of claims 1 to 5.

Technical Field

The invention belongs to the technical field of medicine preparation, and particularly relates to a villous lipid-lowering pellet and a preparation method thereof.

Background

The villa lipid-lowering tablet consists of three medicines of cassia seed, hawthorn, lotus leaf and the like, is used for treating hypertension and hyperlipidemia caused by turbid phlegm and stasis, and has a certain effect on preventing atherosclerosis and the like. In the formula, the active ingredients of the monarch drug cassia seed are anthraquinone compounds, wherein the high content of chrysophanol, aurantio-obtusin and the like. The existing villa lipid-lowering tablet is a sugar-coated tablet, and has the defects of long disintegration time, low utilization rate of active ingredients of the medicine and the like. In addition, the existing villa lipid-lowering tablet is prepared by firstly adding water to decoct cassia seed, hawthorn and lotus leaf to extract effective components, and the effective components of part of the medicines are volatilized and decomposed due to higher temperature during decoction.

Disclosure of Invention

The invention provides a villa lipid-lowering pellet and a preparation method thereof, and aims to solve the technical problems.

In order to solve the technical problems, the invention adopts the following technical scheme:

a preparation method of a villous lipid-lowering pellet comprises the following raw materials in parts by weight: 1240 parts of cassia seed, 620 parts of hawthorn, 420 parts of lotus leaf, 320 parts of dextrin, 20-36 parts of cane sugar, 15-32 parts of konjac glucomannan and 18-25 parts of hydroxypropyl methyl cellulose, wherein the preparation method of the pellet comprises the following steps:

r1, respectively selecting semen Cassiae, fructus crataegi and folium Nelumbinis, cleaning, and drying;

r2, weighing the cassia seed, the hawthorn, the lotus leaf, the dextrin, the sucrose, the konjac glucomannan and the hydroxypropyl methyl cellulose according to the parts by weight;

r3, respectively crushing the cassia seeds and the lotus leaves, adding an ethanol water solution A for soaking, ultrasonically extracting, filtering, recovering ethanol from an extracting solution, and concentrating into thick paste;

crushing hawthorn, mixing with ionic liquid, carrying out ultrasonic extraction at 50-60 ℃ for 20-60 min, concentrating and drying filtrate, adding an ethanol water solution B for dissolving, adsorbing by macroporous resin, washing with water, adding an ethanol water solution C for eluting, recovering ethanol, and concentrating into thick paste;

r5. dissolving dextrin in water under stirring, adding the soft extract from step R3, and stirring to obtain mixture;

r6. mixing the thick paste obtained in step R4 with the mixture of R5, adding part of hydroxypropyl methylcellulose, stirring, making into pill, oven drying, and sieving to obtain drug-loaded pellet;

r7. adding water into sucrose, stirring, adding konjac glucomannan, stirring, adding the rest hydroxypropyl methylcellulose, and stirring to obtain coating solution;

r8. and (4) taking the drug-loaded pellets obtained in the step R6, coating the drug-loaded pellets with the coating solution of R7 in a fluidized bed coating machine, and subpackaging to obtain the drug-loaded pellets.

Further, in the step R3, the volume concentration of the ethanol water solution A is 70-80%, the usage amount is 8-10 times of the weight of the cassia seeds and the lotus leaves, the soaking time is 40-120min, and the ultrasonic extraction time is 45-90 min.

Further, in step R4, the ionic liquid is one or two of 1-butyl-3-methylimidazole acetate and 1-alkene butyl-3-methylimidazole chloride salt, and the usage amount is 1.3-1.5 times of the hawthorn weight.

Further, in the step R4, the volume concentration of the ethanol aqueous solution B is 50-65% and the usage amount is 4-6 times of the weight, and the volume concentration of the ethanol aqueous solution C is 75-85% and the usage amount is 10-15 times of the weight of the hawthorn.

Further, the hydroxypropyl methyl cellulose added in the step R6 accounts for 10-15 parts by weight, the drying temperature is 38-49 ℃, and the drug-loaded pellets collected by screening are 20-35 meshes.

A villa lipid-lowering pellet is prepared by the preparation method of any villa lipid-lowering pellet.

The invention has the beneficial effects that:

the effective component content of the prepared villa lipid-lowering pellet is higher, and comprises chrysophanol, aurantio-obtusin, nuciferine, total flavone, organic acid and the like, the cassia seed and the lotus leaf are ultrasonically extracted by adopting ethanol, the content of the effective components such as chrysophanol, aurantio-obtusin, nuciferine and the like is improved, the hawthorn is extracted by adopting ionic liquid, and then the ethanol is separated and eluted, so that not only can flavonoid substances and the like in the hawthorn be fully and completely extracted, but also the direct reaction of the organic acid of the hawthorn and the nuciferine in the extraction process can be avoided, the loss of the nuciferine is avoided, and the organic acid of the hawthorn is better protected; the dextrin is mixed with the cassia seed and the lotus leaf extract to form an inclusion compound and an isolation layer, so that the reaction of nuciferine and organic acid of hawthorn is further effectively avoided, and the stability of the active ingredients of the pellet is improved; the coating liquid is prepared from konjac glucomannan and hydroxypropyl methyl cellulose, so that the coating liquid is well sprayed on the surfaces of the pellets to form good isolated pellets, effective components such as chrysophanol, aurantio-obtusin and nuciferine are effectively protected, the stability of the pellets is improved, the prepared coating has good water swelling property, the disintegration time of the pellets in a human body can be shortened, and the utilization rate of the medicine is improved. Wherein, the konjac glucomannan not only has the function of isolation, but also has the function of water absorption and expansion of the pellets, and the hydroxypropyl methyl cellulose not only has the function of adhesion, but also has the function of isolation.

Detailed Description

In order to facilitate a better understanding of the invention, the following examples are given to illustrate, but not to limit the scope of the invention.

Example 1

A preparation method of a villous lipid-lowering pellet comprises the following steps:

r1, respectively selecting semen Cassiae, fructus crataegi and folium Nelumbinis, cleaning, and drying;

and R2, weighing the following components in parts by weight: 1240g of cassia seed, 620g of hawthorn, 420g of lotus leaf, 150g of dextrin, 20g of cane sugar, 15g of konjac glucomannan and 18g of hydroxypropyl methyl cellulose;

r3, respectively crushing the cassia seeds and the lotus leaves, adding 80 v/v% ethanol water solution A to soak for 40min, ultrasonically extracting for 45min, wherein the dosage of the ethanol water solution A is 8 times of the total weight of the cassia seeds and the lotus leaves, filtering, recovering ethanol from an extracting solution, and concentrating to obtain thick paste;

r4, crushing the hawthorn, mixing the crushed hawthorn with 1-butyl-3-methylimidazole acetate which is 1.3 times of the weight of the hawthorn, carrying out ultrasonic extraction at 55 ℃ for 45min, concentrating and drying the filtrate, adding 50 v/v% ethanol water solution B for dissolving, wherein the using amount is 4 times of the weight of the hawthorn, adsorbing by macroporous resin, washing with water, adding 75 v/v% ethanol water solution C for eluting, wherein the using amount is 10 times of the weight of the hawthorn, recovering ethanol, and concentrating to obtain thick paste;

r5. dissolving dextrin in water under stirring, adding the soft extract from step R3, and stirring to obtain mixture;

r6., mixing the thick paste obtained in the step R4 with the mixture of R5, adding 10g of hydroxypropyl methylcellulose, stirring uniformly, pelleting, drying and screening to obtain drug-loaded pellets, wherein the drying temperature is 38 ℃, and the drug-loaded pellets collected by screening are 28 meshes;

r7. adding water into sucrose, stirring, adding konjac glucomannan, stirring, adding the rest hydroxypropyl methylcellulose, and stirring to obtain coating solution;

r8. and (4) taking the drug-loaded pellets obtained in the step R6, coating the drug-loaded pellets with the coating solution of R7 in a fluidized bed coating machine, and subpackaging to obtain the drug-loaded pellets.

Example 2

A preparation method of a villous lipid-lowering pellet comprises the following steps:

r1, respectively selecting semen Cassiae, fructus crataegi and folium Nelumbinis, cleaning, and drying;

and R2, weighing the following components in parts by weight: 1240g of cassia seed, 620g of hawthorn, 420g of lotus leaf, 260g of dextrin, 30g of cane sugar, 26g of konjac glucomannan and 23g of hydroxypropyl methyl cellulose;

r3, respectively crushing the cassia seeds and the lotus leaves, adding 70 v/v% ethanol water solution A to soak for 100min, performing ultrasonic extraction for 65min, wherein the dosage of the ethanol water solution A is 9 times of the total weight of the cassia seeds and the lotus leaves, filtering, recovering ethanol from an extracting solution, and concentrating to obtain thick paste;

r4, crushing hawthorn, mixing with 1-butyl-3-methylimidazolium acetate 1.5 times the weight of hawthorn, performing ultrasonic extraction at 50 ℃ for 60min, concentrating and drying filtrate, adding 58 v/v% ethanol water solution B for dissolving, wherein the using amount is 6 times of the weight of hawthorn, adsorbing by macroporous resin, washing with water, adding 80 v/v% ethanol water solution C for eluting, wherein the using amount is 13 times of the weight of hawthorn, recovering ethanol, and concentrating to obtain thick paste;

r5. dissolving dextrin in water under stirring, adding the soft extract from step R3, and stirring to obtain mixture;

r6., mixing the thick paste obtained in the step R4 with the mixture of R5, adding 10g of hydroxypropyl methylcellulose, stirring uniformly, pelleting, drying and screening to obtain drug-loaded pellets, wherein the drying temperature is 45 ℃, and the collected drug-loaded pellets after screening are 20 meshes;

r7. adding water into sucrose, stirring, adding konjac glucomannan, stirring, adding the rest hydroxypropyl methylcellulose, and stirring to obtain coating solution;

r8. and (4) taking the drug-loaded pellets obtained in the step R6, coating the drug-loaded pellets with the coating solution of R7 in a fluidized bed coating machine, and subpackaging to obtain the drug-loaded pellets.

Example 3

A preparation method of a villous lipid-lowering pellet comprises the following steps:

r1, respectively selecting semen Cassiae, fructus crataegi and folium Nelumbinis, cleaning, and drying;

and R2, weighing the following components in parts by weight: 1240g of cassia seed, 620g of hawthorn, 420g of lotus leaf, 320g of dextrin, 36g of sucrose, 32g of konjac glucomannan and 25g of hydroxypropyl methyl cellulose;

r3, respectively crushing the cassia seeds and the lotus leaves, adding 70 v/v% ethanol water solution A to soak for 120min, ultrasonically extracting for 90min, filtering, recovering ethanol from an extracting solution, and concentrating to obtain thick paste, wherein the dosage of the ethanol water solution A is 10 times of the total weight of the cassia seeds and the lotus leaves;

r4, crushing the hawthorn, mixing the crushed hawthorn with 1.5 times of ionic liquid of the weight of the hawthorn, wherein the ionic liquid consists of 1:1 of 1-butyl-3-methylimidazolyl acetate and 1-alkenyl butyl-3-methylimidazolyl chloride, carrying out ultrasonic extraction at 60 ℃ for 30min, concentrating and drying filtrate, adding 65 v/v% ethanol water solution B for dissolving, using the amount of the ethanol water solution B being 6 times of the weight of the hawthorn, adsorbing by macroporous resin, washing by water, adding 85 v/v% ethanol water solution C for eluting, using the amount of the ethanol water solution C being 15 times of the weight of the hawthorn, recovering ethanol, and concentrating to thick paste;

r5. dissolving dextrin in water under stirring, adding the soft extract from step R3, and stirring to obtain mixture;

r6., mixing the thick paste obtained in the step R4 with the mixture of R5, adding 10g of hydroxypropyl methylcellulose, stirring uniformly, pelleting, drying and screening to obtain drug-loaded pellets, wherein the drying temperature is 49 ℃, and the drug-loaded pellets collected by screening are 35 meshes;

r7. adding water into sucrose, stirring, adding konjac glucomannan, stirring, adding the rest hydroxypropyl methylcellulose, and stirring to obtain coating solution;

r8. and (4) taking the drug-loaded pellets obtained in the step R6, coating the drug-loaded pellets with the coating solution of R7 in a fluidized bed coating machine, and subpackaging to obtain the drug-loaded pellets.

Comparative example 1 (conventional method)

1240g of cassia seed, 620g of hawthorn and 420g of lotus leaf, adding water for decocting for three times, filtering, concentrating the filtrate under reduced pressure to obtain thick paste, adding an appropriate amount of auxiliary materials, uniformly mixing, drying under reduced pressure, crushing into fine powder, granulating, drying, pressing into 1000 tablets, and coating sugar.

Comparative example 2

The difference between this comparative example and example 2, step R2, is the following weight ratio of ingredients: 1240g of cassia seed, 620g of hawthorn, 420g of lotus leaf, 260g of dextrin, 30g of cane sugar, 10g of konjac glucomannan and 30g of hydroxypropyl methyl cellulose.

Comparative example 3

This comparative example differs from example 2 in that the same amount of gum arabic is replaced by konjac gum.

Comparative example 4

This comparative example differs from example 2 in that hydroxypropyl methylcellulose is substituted for ethyl cellulose.

Taking a proper amount of the products prepared in the above examples 1-3 and comparative examples 1-4, the contents of chrysophanol, aurantio-obtusin and nuciferine and the disintegration time were measured, and the results were as follows:

TABLE 1 test results

The data show that compared with the comparative example 1, the pellets prepared by the preparation methods of the embodiments 1 to 3 of the invention have higher contents of chrysophanol, aurantio-obtusin, nuciferine, total flavonoids and organic acids, relatively shorten the disintegration time and have indexes which are obviously superior to the indexes of the villa lipid-lowering tablets prepared by the traditional method.

Comparative examples 2-4 show that the addition of a certain amount of konjac gum and hydroxypropyl methylcellulose in the invention can better protect active ingredients, improve the content of active ingredients in the product, and shorten the disintegration time.

The present invention is not limited to the above preferred embodiments, and any modifications, equivalent substitutions and improvements made within the spirit and principle of the present invention should be included in the protection scope of the present invention.