CN111228247B - Medicine containing benzylidene acetone for treating echinococcosis and preparation method thereof - Google Patents
Medicine containing benzylidene acetone for treating echinococcosis and preparation method thereof Download PDFInfo
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- CN111228247B CN111228247B CN201911236789.XA CN201911236789A CN111228247B CN 111228247 B CN111228247 B CN 111228247B CN 201911236789 A CN201911236789 A CN 201911236789A CN 111228247 B CN111228247 B CN 111228247B
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/12—Ketones
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/10—Anthelmintics
Abstract
The invention relates to a medicine containing benzalacetone for treating echinococcosis and a preparation method thereof. The dosage forms of the medicine comprise emulsion, tablets, powder, pills, granules, capsules and the like. Meanwhile, also relates to a preparation method of the medicine emulsion. The medicament containing the benzylidene acetone can be used for treating echinococcosis, and the medicament active component of the benzylidene acetone is horizontally combined with an echinococcosis animal model in vivo, so that the quantity and the weight of vesicles can be effectively reduced, and the medicament has a good treatment effect on the echinococcosis.
Description
Technical Field
The invention relates to the technical field of medicines for parasitic diseases, in particular to a medicine containing benzalacetone for treating echinococcosis and a preparation method thereof.
Background
Echinococcosis (I)Echinococcosis) Is a parasitic disease of both human and livestock, which is also called echinococcosis disease caused by Taenia infection of echinococcus of Zosteraceae, and is mainly classified as cystic echinococcosis (echinococcosis)Cystic EchinococcosisCE and alveolar echinococcosis (A)Alveolar EchinocococosisAE is Echinococcus granulosus (see below)Echinococus granulosus) And echinococcus multilocularis: (a)Echinocococus multilocularis) Caused by infection. Echinococcus granulosus is usually present in mammals such as cattle, sheep, pigs and the like in the form of larvae, whereas Echinococcus multilocularis is mainly intermediate host in rodents such as mice and the like, and is incidental host in human echinococcus granulosus/multilocularis. The intermediate host/the accidental host is infected by eating eggs, the eggs enter duodenum through stomach and then are hulled under the action of digestive juice to form oncophora, and the oncophora penetrates into intestinal wall, enters portal vein system along with blood circulation, parasitizes in the host and develops into echinococcosis sac (echinococcosis) in organs such as liver and lung. The treatment of the echinococcosis is performed by combining surgical treatment with drug treatment. Albendazole has been used for treating echinococcosis, but has more adverse reactions.
Benzylmethyleneacetone (CAS: 1896-62-4), a commonly used fragrance material, is widely used in food and personal skin care products. The toxicity is small, and the LD50 of the rats is shown to be in the range of 2g/kg-5g/kg in oral acute toxicity experiments. No significant toxicity was shown in the chronic toxicity test. At present, no literature reports exist on killing endoparasites.
Disclosure of Invention
Therefore, it is necessary to provide a therapeutic drug using benzylidene acetone as an active ingredient for solving the problem of poor clinical effect of current echinococcosis drugs.
A medicament containing benzalacetone for treating echinococcosis comprises benzalacetone as active component.
In one embodiment, the benzylidene acetone accounts for 0.1-99% of the total weight of the medicine.
The administration route of the pharmaceutical composition can be gastrointestinal tract or parenteral tract, such as oral, pulmonary, nasal, subcutaneous, sublingual, skin, muscle, rectum, etc., preferably oral administration.
The dose of the pharmaceutical composition to be administered depends on many factors, such as the nature and severity of the disease to be prevented or treated, the sex, age, body weight, character and individual response of the patient or animal, the administration route, the number of administration times, the therapeutic purpose, and thus the therapeutic dose of the present invention may be widely varied. The pharmaceutical composition of the present invention can be taken alone, or combined with other therapeutic or symptomatic drugs and adjusted in dosage.
For the purpose of administration and enhancing the therapeutic effect, the drug of the present invention can be administered by any known administration method.
In one embodiment, the dosage form of the medicament comprises emulsion, tablet, powder, pill, granule, capsule and the like.
The pharmaceutical composition can be prepared into pharmaceutical preparations, and the dosage form of the pharmaceutical preparations can be liquid dosage forms, solid dosage forms or semisolid dosage forms. Wherein, the liquid dosage form can be solution, emulsion, suspension, injection, eye drop, nose drop, lotion, liniment, etc.; the solid dosage form can be tablet (including common tablet, enteric coated tablet, buccal tablet, dispersible tablet, chewable tablet, effervescent tablet, orally disintegrating tablet), powder, pellet, dripping pill, granule, capsule (including hard capsule, soft capsule, enteric coated capsule), suppository, pellicle, patch, aerosol (powder), spray, etc.; semisolid dosage forms can be ointments, gels, pastes, and the like.
The pharmaceutical composition can be prepared into common preparations, sustained release preparations, controlled release preparations, targeting preparations and various microparticle drug delivery systems.
In addition, colorants, preservatives, flavors, flavorings, sweeteners or other materials may also be added to the pharmaceutical preparation, if desired.
The invention also relates to a preparation method of the medicament containing the benzylidene acetone for treating the echinococcosis, the medicament is an emulsion, and the preparation method comprises the following steps:
(1) Preparing raw materials: taking benzylidene acetone;
(2) Preparing an emulsion: dissolving liquid paraffin in benzylidene acetone, adding arabic gum, grinding, adding distilled water, grinding to obtain milky white primary emulsion, adding water, grinding, and diluting to obtain emulsion.
In one embodiment, the content of the benzylidene acetone in the emulsion is 0.1-99% of the total weight.
Drawings
FIG. 1 is a graph showing the results of the dissection of the number and size of vesicles in the abdominal cavity of each group of mice according to the embodiment of the present invention;
FIG. 2 is a graph showing the change of body weight with time of administration in each group of mice according to the example of the present invention;
FIG. 3 is a comparison of the average number of vesicles in the abdominal cavity of mice in each group according to the example of the present invention;
FIG. 4 is a comparison of average vesicle weights in the abdominal cavities of mice in various groups according to the present invention.
Detailed Description
In order to make the aforementioned objects, features and advantages of the present invention comprehensible, embodiments accompanied with figures are described in detail below. In the following description, numerous specific details are set forth in order to provide a thorough understanding of the present invention. This invention may, however, be embodied in many different forms and should not be construed as limited to the embodiments set forth herein.
A medicine containing benzalacetone for treating echinococcosis contains benzalacetone as active component.
Preferably, the benzylidene acetone accounts for 0.1-99% of the total weight of the medicament.
Preferably, the dosage form of the medicament comprises emulsion, tablets, powder, pills, granules, capsules and the like.
A preparation method of a drug containing benzylidene acetone for treating echinococcosis, wherein the dosage form of the drug is emulsion, and the preparation method comprises the following steps:
(1) Preparing raw materials: taking benzylidene acetone;
(2) Preparing an emulsion: dissolving liquid paraffin in benzylidene acetone, adding arabic gum, grinding, adding distilled water, grinding to obtain milky white primary emulsion, adding water, grinding, and diluting to obtain emulsion.
Preferably, the content of the benzalacetone in the emulsion is 0.1-99% of the total weight.
Compared with the prior art, the invention has the following advantages:
the medicament containing the benzylidene acetone can be used for treating echinococcosis, and the medicament active component of the benzylidene acetone is horizontally combined with an echinococcosis animal model in vivo, so that the quantity and the weight of vesicles can be effectively reduced, and the medicament has a good treatment effect on the echinococcosis.
Example (b):
1. experimental materials:
phenylmethylidene acetone (CAS: 1896-62-4) with a purity of >98% was purchased from Chinee chemical industry development Co., ltd.
2. The preparation of the medicament emulsion for treating hydatid disease comprises the following steps:
taking 12mL of liquid paraffin, adding 4 g of benzalacetone for dissolving, adding 4 g of Arabic gum for grinding to uniformly disperse, adding 8 mL of distilled water for continuous grinding to obtain milky white primary emulsion, adding water for grinding while diluting to 30 mL to obtain the emulsion.
3. In vivo experiments investigating agents for treating echinococcosis:
inoculating 1000 per mouse into abdominal cavity, randomly grouping into Model group (Model), albendazole group 75 mg/kg (ABZ), benzalacetone low dose group 75 mg/kg (BZT-L) and benzalacetone high dose group 150 mg/kg (BZT-H) after 4 weeks, perfusing stomach for 10 weeks, measuring body weight each week, collecting blood from eyeball after administration, dissecting and separating mouse abdominal cavity vesicle, counting and weighing.
The results show that: the quantity and the size of the vesicles in the abdominal cavity of the mice in the albendazole group and the benzylidene acetone group are obviously smaller than those in the model group. The results are shown in FIG. 1.
Mice in each group were tested for weight change: the weight change of mice in each experimental group is shown in the figure, the weight of the mice in each experimental group is slowly increased in the experimental period, after 10 weeks of administration, the average weights of the mice in the model group, the albendazole group, the low-drug dose group and the high-drug dose group are respectively 45.78 +/-1.81, 42.38 +/-3.75, 47.56 +/-4.15 and 48.10 +/-3.94 g, the weight average of the drug group is higher than that of the model group and the albendazole group, and the significant difference exists between the high-drug dose group and the albendazole group (the weight average of the drug group is higher than that of the model group and that of the albendazole group)P<0.05). The results are shown in FIG. 2.
Effect of benzylidene acetone on the number of vesicles in the abdominal cavity of mice: the statistical results of the numbers of the vesicles in each group are shown in the table and the figure, the average numbers of the vesicles in the model group, the albendazole group, the benzalacetone low-dose group and the benzalacetone high-dose group are respectively 13.3 +/-3.3, 4.0 +/-5.9, 4.3 +/-4.1 and 6.8 +/-3.4, and compared with the model group, the numbers of the vesicles in the albendazole group, the benzalacetone low-dose group and the benzalacetone high-dose group are all significantly reduced (P is less than 0.05), and compared with the albendazole group, the drug low-dose group, the drug high-dose group and the albendazole group, the statistics of the numbers of the vesicles in the drug low-dose group, the benzylidene acetone low-dose group and the benzalacetone high-dose group are not significantly different. The results are shown in FIG. 3.
Effect of benzylidene acetone on vesicle weight in mouse abdominal cavity: the results of statistics of vesicle weights in abdominal cavities of mice in each group of experiments are shown in the table and the figure, the average vesicle weights in the model group, the albendazole group, the benzylidene acetone low-dose group and the benzylidene acetone high-dose group are respectively 0.39 +/-0.34, 0.04 +/-0.05, 0.07 +/-0.08 and 0.08 +/-0.05 g, and compared with the model group, the vesicle weights in the albendazole group, the benzylidene acetone low-dose group and the benzylidene acetone high-dose group are lower than those in the model group (P is less than 0.05), and compared with the albendazole group, the drug low-dose group, the drug high-dose group and the albendazole group, the statistics are not different. The results are shown in FIG. 4.
The technical features of the embodiments described above may be arbitrarily combined, and for the sake of brevity, all possible combinations of the technical features in the embodiments described above are not described, but should be considered as being within the scope of the present specification as long as there is no contradiction between the combinations of the technical features.
The above-mentioned embodiments only express several embodiments of the present invention, and the description thereof is specific and detailed, but not to be understood as limiting the scope of the invention. It should be noted that, for a person skilled in the art, several variations and modifications can be made without departing from the inventive concept, which falls within the scope of the present invention. Therefore, the protection scope of the present patent shall be subject to the appended claims.
Claims (2)
1. The application of the benzylidene acetone in the preparation of the medicine for treating echinococcosis is characterized in that the active component of the medicine, namely the benzylidene acetone, accounts for 0.1-99% of the total weight of the medicine, the dosage form of the medicine comprises emulsion, tablets, powder, pills, granules and capsules, and the administration route of the medicine is oral administration.
2. The use of benzylidene acetone according to claim 1 for the preparation of a medicament for the treatment of echinococcosis, wherein the medicament is in the form of an emulsion, and the preparation method comprises the steps of:
(1) Preparing raw materials: taking benzylidene acetone;
(2) Preparing an emulsion: dissolving liquid paraffin in benzylidene acetone, adding acacia, grinding to disperse uniformly, adding distilled water, grinding to obtain milky white primary emulsion, adding water while grinding, and diluting to obtain emulsion.
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