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WO2001064229A1 - A medicine for treating obesity and the method of producing thereof - Google Patents

A medicine for treating obesity and the method of producing thereof Download PDF

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Publication number
WO2001064229A1
WO2001064229A1 PCT/CN2000/000037 CN0000037W WO0164229A1 WO 2001064229 A1 WO2001064229 A1 WO 2001064229A1 CN 0000037 W CN0000037 W CN 0000037W WO 0164229 A1 WO0164229 A1 WO 0164229A1
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WO
WIPO (PCT)
Prior art keywords
servings
medicine
treating obesity
atractylodes
dried
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/CN2000/000037
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English (en)
French (fr)
Inventor
Meibin Fujimoto
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
JUN HO CO Ltd
Original Assignee
JUN HO CO Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by JUN HO CO Ltd filed Critical JUN HO CO Ltd
Priority to AU2000229021A priority Critical patent/AU2000229021A1/en
Priority to PCT/CN2000/000037 priority patent/WO2001064229A1/zh
Priority to CN00819102.6A priority patent/CN1434717A/zh
Priority to HK01101462A priority patent/HK1033066A2/zh
Publication of WO2001064229A1 publication Critical patent/WO2001064229A1/zh
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/70Polygonaceae (Buckwheat family), e.g. spineflower or dock
    • A61K36/708Rheum (rhubarb)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/17Gnetophyta, e.g. Ephedraceae (Mormon-tea family)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/23Apiaceae or Umbelliferae (Carrot family), e.g. dill, chervil, coriander or cumin
    • A61K36/232Angelica
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/23Apiaceae or Umbelliferae (Carrot family), e.g. dill, chervil, coriander or cumin
    • A61K36/234Cnidium (snowparsley)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/25Araliaceae (Ginseng family), e.g. ivy, aralia, schefflera or tetrapanax
    • A61K36/258Panax (ginseng)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/28Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
    • A61K36/284Atractylodes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/31Brassicaceae or Cruciferae (Mustard family), e.g. broccoli, cabbage or kohlrabi
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/53Lamiaceae or Labiatae (Mint family), e.g. thyme, rosemary or lavender
    • A61K36/537Salvia (sage)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/88Liliopsida (monocotyledons)
    • A61K36/884Alismataceae (Water-plantain family)

Definitions

  • the invention relates to a weight-loss medicine, in particular to a weight-loss medicine prepared by using a plant Chinese herbal medicine as a raw material.
  • the invention also relates to a method for preparing and using the slimming medicine. Background technique
  • Obesity refers to excessive calorie intake or excessive changes in the body's physiological and biochemical functions that lead to excessive fat storage in the body, obesity, and a weight that exceeds 10% of the standard weight. It is often accompanied by a series of metabolic disorders or neurological conditions, and is clinically prone to a variety of conditions such as arteriosclerosis, hypertension, diabetes, gout, cholangitis, cholelithiasis, impotence, and irregular menstruation. With the continuous improvement of people's living standards, the phenomenon of obesity is becoming more and more serious. In addition, obesity can also accelerate human aging, and the sudden death is significantly increased, so it should be given clinical attention.
  • the first is to eat low-fat, low-energy foods or alternative foods.
  • the second is edible digestion and absorption inhibitors.
  • the disadvantages of these two treatment methods are: easy rebound, no food satisfaction, heavy mental burden, easy to cause nutritional disorders, and obvious side effects such as abdominal pain and diarrhea.
  • CN94113251-X discloses a slimming drink made of thirteen Chinese herbal medicines and a preparation method thereof.
  • CN94116739- 9 discloses a manufacturing method and a product for slimming medicine containing more than 20 kinds of Chinese herbal medicine for internal administration. The products covered by these two patents are taken internally. Obviously, the disadvantages of the methods for treating obesity described above cannot be avoided.
  • CN94101824. 5 Discloses a natural bath liquid containing multiple flavors of Chinese herbal medicine and its preparation mainly for treating simple obesity.
  • CN93114999-1 Disclosed is a weight-loss fitness bath containing multiple flavors of Chinese herbal medicines for the treatment of obesity with alcohol bath.
  • CN93117263. 2 discloses a double-medicine core health care stomach medicine natural gourd containing 84 flavors of Chinese herbal medicine for treating various diseases.
  • the products disclosed in these patents are for external use and do not have the disadvantages of internal medicine, they are mainly health-care, and some of them are not specifically targeted at obesity.
  • the bath liquid is only used when the patient is taking a bath, the product in the form of a bath liquid has certain use limitations. Therefore, the efficacy of these products must be affected to some extent, and the effects are not always satisfactory.
  • the object of the present invention is to provide a medicine for treating obesity that has no side effects, is simple and easy to implement, is safe and reliable, has significant therapeutic effects, and can be consolidated and stabilized.
  • Another object of the present invention is to provide a method for preparing the medicine for treating obesity.
  • Another object of the present invention is to provide a method for using the medicine for treating obesity.
  • the invention provides a new medicine for treating obesity, which is made of Atractylodes macrocephala, Atractylodes macrocephala, Angelica sinensis, Salvia miltiorrhizae, Alisma orientalis, Snake seed, Mustard seed, Ephedra rhubarb, Rhubarb, Panax notoginseng as raw materials, and according to the prescription of each Chinese medicine Ingredients and properties are prepared by extraction.
  • the invention also provides a method for preparing the new medicine for treating obesity, in which rhubarb is extracted twice with 70% ethanol alone to make a thick paste; after the other drugs in the prescription are water-extracted and alcohol-precipitated, The ethanol was recovered under reduced pressure and concentrated to a thick paste.
  • the above two thick creams are combined, dissolved in a PEG mixed matrix solution, and optionally added an appropriate amount of a transdermal absorption enhancer, a surfactant, a preservative, water, etc. to prepare a salve.
  • the obtained ointment is poured into a plastic mold hole of an appropriate shape, and after appropriately cooling and molding, the plastic mold hole and the plastic mold are covered with a suitable carrier to prepare a patch.
  • the present invention also provides a method for using the medicine for treating obesity, which comprises: directly applying the ointment to the umbilicus (Shenque acupoint) or Guanyuan point (three inches below the umbilical cord), or opening the patch Packing, discarding the plastic mold, and sticking the side of Kelu medicine directly to the umbilicus (Shenxi point) or Guanyuan point (three inches below the umbilicus) according to the shape of the ointment, and then peel off the outer support film. Body temperature will dissolve the drug, apply it once a day, and use it 24 hours a day, stop it for one day a day, or stop for two days after using it.
  • a method for using the medicine for treating obesity comprises: directly applying the ointment to the umbilicus (Shenque acupoint) or Guanyuan point (three inches below the umbilical cord), or opening the patch Packing, discarding the plastic mold, and sticking the side of Kelu medicine directly to the umbilicus (Sh
  • the medicine for treating obesity is based on the theory of "internal disease and external treatment” in Chinese medicine, and adopts a natural therapy called “medicine umbilical method", which is based on the theory of traditional Chinese medicine meridian.
  • medicine umbilical method which is based on the theory of traditional Chinese medicine meridian.
  • the therapeutic yellow diarrhea drug is based on the above theory, and then advanced transdermal slow-release technology is used to make the drug reach the whole body through acupoint absorption. Regulates metabolic function, accelerates lipolysis, and has stable drug effect.
  • the medicine of the present invention is prepared by using traditional Chinese medicine plants as raw materials in combination at a certain ratio.
  • the specific raw materials are Astragalus, Atractylodes, Angelica, Salvia miltiorrhiza, Alisma, Snake Bed, Mustard, Ephedra, Rhubarb, Panax notoginseng and so on.
  • composition of the Chinese herbal medicine in the medicine of the present invention is as follows:
  • Atractylodes 3-12 parts Atractylodes 3-12 parts Huanghuang Angelica 3-15 parts Salvia 5-30 parts Alisma 6-30 parts Snake Bed 3-15 parts mustard 3-12 parts ephedra 2-12 parts rhubarb 3-30 parts Sanqi 2-10 servings
  • composition of the Chinese herbal medicine in the medicine of the present invention is as follows (weight ratio):
  • Atractylodes 5- 10 parts Atractylodes 5- 10 parts Angelica 5- 10 parts Danshen 5- 15 parts Alisma 10-20 parts Snake bed 5- 10 parts mustard 5-10 parts ephedra 5-10 parts rhubarb 5- 15 parts sanqi 2 -6 servings
  • composition of the Chinese herbal medicine in the medicine of the present invention is as follows (weight ratio):
  • the two herbs used in the Chinese herbal formula of the medicine of the present invention are commonly used Chinese herbs, and should first meet the standards of the Pharmacopoeia of the People's Republic of China to ensure the quality of the raw materials for drug use and the safety and effectiveness of the prepared drugs.
  • the topical patch in order to make the topical patch have a better effect, it is better to use authentic medicinal materials.
  • the medicine of the invention is based on the theory of "internal disease and external treatment” in traditional Chinese medicine and the theory of traditional Chinese medicine meridian
  • the traditional black medicinal ointment preparation technology in traditional Chinese medicine is combined with new materials and new processes in modern pharmacy.
  • the drug can play the role of participating in the meridian, removing stasis and removing blood stasis, and stimulate the meridian in the entire prescription of the drug, dredge the meridian, and promote the operation of qi and blood to adjust the function of the viscera.
  • coordinate the body's yin and yang balance so as to achieve the purpose of internal disease and external treatment.
  • the mechanism of the traditional Chinese medicine plaster is consistent with the transdermal drug delivery system in modern medicine.
  • TDS transdermal therapeutic system
  • the medicament for treating obesity of the present invention may be any of the pharmacologically stated dosage forms.
  • the medicament for treating obesity of the present invention may include excipients such as a matrix, a transdermal absorption enhancer, a surfactant, a preservative, water, and other additives commonly used in the art.
  • the medicament for treating obesity of the present invention is preferably used as an external ointment.
  • the content of traditional Chinese medicine generally accounts for 20-40%
  • the content of excipients generally accounts for 60-80%.
  • the bases used in the medicament of the present invention may be those bases commonly used in the field of formulations for external films, ointments, emulsions, patches (including plasters), and the like.
  • Black plaster is a lead plaster made from medicinal materials, edible vegetable oil and red dan.
  • the solvent used in the extraction is vegetable oil, but vegetable oil can only dissolve some non-polar substances, and the effective ingredients such as alkaloids contained in general medicinal materials are often combined with organic acids to form salts in cells, so they are not soluble in oil.
  • ointments are generally used in greasy bases, including greases, lipids and hydrocarbons. Its common features are lubricating, non-irritating, stronger protection and softening effect than other matrices, and can cooperate with more drugs. However, it is greasy and hydrophobic, water-soluble components are not easy to dissolve, and it is not easy to wash away with water. The release and penetration of drugs are smaller than those of other matrices.
  • the emulsion-type matrix is similar to the emulsion, and is a semi-solid state matrix formed by the action of an aqueous phase and an oil phase with the aid of an emulsifier.
  • Water-in-oil and water-in-oil are water-in-oil.
  • the water-in-oil emulsion base looks like an ointment, is easier to apply than a greasy base, has less greasiness, and has a cooling effect when moisture evaporates from the skin surface.
  • the oil-in-water emulsion base looks like vanishing cream, can be mixed with water, is non-greasy and easy to remove.
  • the water-soluble base is non-lipid, and is also called a hydrogel ointment base. It consists of natural or synthetic polymer-soluble substances.
  • the water-soluble matrix can be mixed with aqueous body fluids, absorb tissue fluids, and generally release drugs quickly, without oiliness, and easy to spread and wash away. It is non-irritating to the skin and mucous membranes, and can be used for erosive wounds and luminal mucosa.
  • the disadvantage is that it has poor lubricating effect and is easy to lose water and dry. Therefore, it is necessary to add humectants and preservatives.
  • the matrix in the medicament of the present invention is preferably a polyethylene glycol substance having a different molecular weight, and is formulated according to different formulation ratios.
  • polyethylene glycols are non-toxic and irritating to the human body, have stable chemical properties, are heat resistant, and are not prone to rancidity and mold. Because this product has a wide range of solubility, compatibility, film-forming, plasticizing, dispersibility, etc., this product with a smaller molecular weight is used as a solvent, co-solvent and oil / water emulsion stabilizer, used in water mixing Preparation of suspensions, emulsions, injections, etc. Because they are very stable, non-irritating to the skin and lubricating, they are used as water-soluble ointment bases and suppository bases, for manufacturing creams, suppositories, and the like. For drugs that are not easily dissolved in water, this product can be used for the purpose of solid dispersion, improve the solubility or solubility of drugs and increase pharmacological activity.
  • the preparation is in a near-solid state below, plus its own hypertonic state, it is not easy to grow mold, not easy to spoil, and has good stability.
  • the chemical components contained in it are also relatively stable and difficult to decompose. Deterioration. This is also an excellent advantage of the drugs prepared by the present invention.
  • the substrates that can be specifically mentioned are PEG400, PEG1000, and PEG4000. They are the two varieties contained in the 1995 edition of the Pharmacopoeia of the People's Republic of China, and they are formulated in a certain proportion. Melted at body surface temperature of about 35.
  • the content of PEG400 accounts for 2-8%
  • the content of PEG1000 accounts for 30-50%
  • the content of PEG4000 accounts for 15-45%.
  • the content of the matrix generally accounts for 44.7-78.9%, preferably 60-70%.
  • a transdermal absorption-promoting agent may be optionally used. It is generally believed that when the transdermal absorption agent acts on the skin, by changing the skin permeability, the diffusivity of the active ingredient or the solubility of the drug is increased, resulting in an increase in the permeability of the drug, thereby achieving the ultimate goal of promoting transdermal absorption. .
  • the invention preferably uses a small amount of a transdermal absorption enhancer to enhance the transdermal absorption of the drug and improve its efficacy. Based on the total weight of the finished finished ointment, the transdermal absorption enhancer generally accounts for 0.5 to 10%, preferably 1%.
  • the transdermal absorption agent used in the present invention may be any transdermal absorption agent commonly used in the art for this purpose.
  • the transdermal absorption-promoting agent used in the present invention is preferably Azone, and its chemical name is 1-dodecyl-hexahydro-2H-azapyridin-2-one. It is also included in the second part of the 1995 Pharmacopoeia of the People's Republic of China, so its quality should meet the requirements.
  • a transdermal absorption-promoting agent, azatone, which is added to the medicament of the present invention, is a new type of highly effective and low toxicity penetration enhancer. It is a colorless, almost odorless liquid, insoluble in water, lubricating, non-irritating to human skin, mucous membranes and cavity membranes, and low toxicity.
  • Azone is a non-polar transdermal absorption agent. The mechanism of action is believed to soften the keratin, coagulate tissue proteins, enhance permeability, allow the drug to penetrate the skin barrier, increase local or systemic blood drug concentration, and increase the bioavailability of the preparation, thereby obtaining a more ideal therapeutic effect.
  • a surfactant may be optionally used in the medicament for treating obesity of the present invention.
  • Adding a surfactant to the matrix can increase the solubility of insoluble pharmaceutical ingredients in the water and increase the water absorption of the matrix used, so that the pharmaceutical ingredients have better solubility in the matrix, and also promote the penetration of the drug.
  • Sex agent.
  • the non-ionic active agent Tween-80 is used as the surfactant of the present invention. This product has obvious adaptability to different pH, and also coexists with high concentration of electrolyte. More stable. Very little irritation and toxicity to the skin.
  • the content of the surfactant generally accounts for
  • Preservatives are optionally used in the medicament for treating obesity of the present invention.
  • the present invention can use any preservative commonly used in the art.
  • the matrix used in the medicine of the present invention accounts for a large proportion, its solution is in a hypertonic state, and microorganisms are not easy to grow.
  • the storage temperature of this product is below 25, it is preferable to use a preservative in the medicine of the present invention.
  • the preferred preservative is chlorhexidine, because according to the literature, polyethylene glycols may reduce the bacteriostatic effect of benzoate preservatives, while chlorhexidine is not affected so much, so the amount has not increased.
  • the preservative based on the total weight of the finished ointment, the preservative generally accounts for 0.1 0.3%, preferably 0.1%.
  • the medicine of the present invention may contain an appropriate amount of water. Based on the total weight of the finished ointment of the present invention, the water content generally accounts for 0-30%.
  • the medicament of the present invention may optionally contain other additives commonly used in the art, which is selected according to the specific purpose desired.
  • the invention also provides a method for preparing the novel medicine for treating obesity.
  • rhubarb was extracted twice with 70% ethanol alone to make a thick paste; after the other drugs in the prescription were water-extracted and alcohol-precipitated, ethanol was recovered under reduced pressure and concentrated to a thick paste.
  • the two thick pastes are combined, dissolved in a PEG mixed matrix solution, and optionally added an appropriate amount of a transdermal absorption enhancer, a surfactant, a preservative, water, and other commonly used additives to prepare a salve.
  • the obtained ointment is poured into a plastic mold hole of an appropriate shape, and after being appropriately cooled and formed, the plastic mold hole and the plastic mold are covered with a suitable carrier to prepare a patch,
  • 1 gram of the thick paste is equivalent to 1 gram of crude medicine.
  • the specific situation will be slightly different depending on the location and season of the crude medicine.
  • a transdermal absorption enhancer a surfactant, a preservative and water are preferably added.
  • the obtained ointment is poured into a conical plastic mold hole to prepare a conical patch.
  • the present invention also provides a method for using the medicine for treating obesity, which comprises: directly applying the ointment to the umbilicus (Shenque acupoint) or Guanyuan point (three inches below the umbilical cord), or opening the patch Packing, discarding the plastic mold, sticking the side of Kelu medicine directly to the umbilicus (Shenxi point) or Guanyuan point (three inches below the umbilicus) according to the shape of the ointment, and then peel off the outer support film, about 35 Body temperature will dissolve the drug, apply it once a day, use it 24 hours a day, stop it one day a day or Stop for one day after taking two patches.
  • the cone tip of the above-mentioned tape-shaped patch is aligned with the umbilical cord and depressed into the acupoint or directly stuck to the Guanyuan point.
  • the medicament for treating obesity of the present invention When used externally as an ointment, it can be directly applied.
  • the plaster is applied and supported on a suitable carrier material. All carrier materials commonly used in the art for this purpose are suitable for use in the present invention.
  • the characteristics of the carrier material of the present invention are:
  • the carrier is composed of a sponge pad and a special waterproof and breathable film
  • the special waterproof and breathable film is made of, for example, a synthetic resin and an acrylic adhesive.
  • the medicine for treating obesity of the present invention is used as a topical patch, it is applied to the navel (Shenque Acupoint) or Guanyuan Point (three inches below the umbilical cord), and it is used once every two days, or it is stopped for two days and one day, and each patch uses 24 For those who lose more than 1kg per day, please stop posting for two days.
  • the medicine of the present invention After the medicine of the present invention is applied to the selected part for a period of time as required, the medicine will naturally and slowly melt, and the pharmaceutical ingredients enter the body and function. You can feel the peristalsis in the large intestine, increase the exhaust, no hunger, and love vegetarian food. Individual skin temperature is too low, you can apply a warm patch to the medication site (note that the temperature should be softened to a degree not to soften the drug and improve the efficacy. When using the drug of the present invention, it should be noted that: (1) the navel has The ulcer is disabled, (2) Allergic reactions occur and should be discontinued.
  • the medicine for treating obesity of the present invention is used as a topical medicine, it is a new type of topical health-care weight-loss medicine, which is refined from pure Chinese medicine. It does not contain any harmful ingredients, and is safe and convenient to use. It should be affixed to the navel (Shenxi Acupoint) daily. It can effectively regulate the body's fat metabolism through acupoint administration. The whole body weight loss effect is obvious, especially for waist, abdomen and buttocks. No dieting, no diarrhea, no rebound, long-lasting and stable effect.
  • the medicament of the present invention is applicable to various types of obesity.
  • the Chinese herbal formula in the medicine for treating obesity of the present invention is preferably used in the external plaster of the present invention, but it does not exclude that they are directly or made into any appropriate pharmacy Use on an acceptable dosage form.
  • Example Example 1 illustrates the invention. However, the following examples are merely illustrative, and do not limit the present invention in any respect.
  • Example Example 1 illustrates the invention. However, the following examples are merely illustrative, and do not limit the present invention in any respect.
  • Example Example 1 illustrates the invention. However, the following examples are merely illustrative, and do not limit the present invention in any respect.
  • Example Example 1 illustrates the invention. However, the following examples are merely illustrative, and do not limit the present invention in any respect.
  • Atractylodes 200g Atractylodes 200g, Rhubarb 200g, Ephedra 200g, Angelica 200g, Panax notoginseng 80g, Salvia miltiorrhiza 200g, Mustard 200g, Alisma 400g, Snake bed 200g
  • the two filtrates were combined, the ethanol was recovered under reduced pressure, and concentrated to a non-alcoholic taste, and then used.
  • the other traditional Chinese medicines in the formula were extracted twice with hot reflux using water as a solvent. Add 10 times the amount of water for the first time, soak for 1 hour, heat and extract for 1.5 hours, and filter; add 8 times the amount of water for the second time, heat and extract for 1 hour, and filter.
  • the two filtrates were combined and concentrated under reduced pressure to about 1.2 g of medicinal material per 1 ml of medicinal solution. Add 95% ethanol to an alcohol content of 60% for alcohol precipitation, and let stand for 24 hours.
  • the medicines prepared above were clinically treated in 56 patients according to the above usage and dosage.
  • the basic situation of the patients was: Among the 56 patients, 24 were male patients, aged 18 to 65 years, with an average age of 45.8 years. Weight was 20% above normal weight; 32 female patients, aged 21 to 69 years, with an average age of 48.3 years, and average weight over 25%. After 30 days, the results of clinical observation were that 47 people were significantly effective, and the effective rate was 83.9%; 7 were effective, and the effective rate was 12.5%; and 2 were ineffective, and the invalid rate was 3.6%. After 3 months of treatment, the average monthly weight loss was more than 5% of body weight.
  • Atractylodes 120g Atractylodes 120g, Rhubarb 120g
  • Atractylodes 480g Atractylodes 480g Rhubarb 1200g

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Description

一种减肥药及其制备和应用 发明领域
本发明涉及一种减肥药, 特别是涉及一种以植物中草药为原料制 成的减肥药物。 本发明还涉及所述减肥药物的制备方法和使用方法。 背景技术
肥胖症是指热量摄取超过消耗或由于人体生理生化机能改变而引 起体内脂肪储存过多、 体型肥胖、 体重超过标准重量 10%而言。 它常 常伴随着一系列代谢失调或神经功能病状, 临床上易并发动脉硬化、 高血压、 糖尿病、 痛风、 胆嚢炎、 胆石症、 阳痿、 月经不调等多种疾 患。 随着人们生活水平的不断提高, 肥胖现象越来越严重。 另外, 肥 胖也可加速人的衰老, 而且猝死明显增高, 故临床应当给予重视。
目前, 用于治疗肥胖症的方法大体有两种: 第一种是吃低脂肪, 低能量食品或替代食品。 第二种是食用消化吸收抑制剂. 这两种治疗 方法的缺点是: 易反弹, 没有食物满足感, 精神负担重, 容易造成营 养障碍, 以及腹痛、 下泻等副作用明显等。
此外, 目 前有文献中报道了一些涉及治疗肥胖的药物。
CN94113251- X公开了一种由十三味中草药制成的减肥饮料及其制法。
CN94116739- 9 公开了一种供内服的包含二十多味中草药的减肥药的 制造方法及产品。 这两个专利中涉及的产品是内服的。 显而易见, 避 免不了上面所述的治疗肥胖症方法的缺点。 CN94101824. 5 公开了一 种以治疗单纯性肥胖为主的含有多味中草药的天然浴液及其配制。
CN93114999- 1 公开了一种对肥胖症进行酒浴治疗的含有多味中草药 的减肥健身浴液。 CN93117263. 2 公开了一种用于治疗多种疾病的包 含 84味中草药的双药芯保健兜肚天然药物葫芦。 这些专利中公开的产 品虽然是外用的, 没有内服药的缺点, 但它们主要是保健性质的, 其 中一些产品并非是专门针对肥胖症的。 另外, 由于浴液只有在患者洗 浴时才使用, 所以, 浴液形式的产品有一定的使用局限性。 所以, 这 些产品的疗效必定受到一定的影响, 效果不总是令人满意的。
因此, 随着肥胖症给人们的生活带来越来越多的问题, 治疗肥胖 症越来越受到人们的重视。 又鉴于目前在治疗肥胖症药物方面的上述
- 1 - 确 认 本 状况, 所以一直需要一些没有副作用、 简单易行、 安全可靠、 疗效显 著并稳定的治疗肥胖症的药物。
本发明人针对上述治疗方法及产品的不足之处进行深入研究, 经 过反复的临床验证, 最后终于找到了治疗肥胖症的佳药。 发明目的
本发明的目的是提供一种没有副作用、 简单易行、 安全可靠、 疗 效显著且能巩固和稳定的治疗肥胖症的药物。
本发明的另一个目的是提供该治疗肥胖症的药物的制备方法。
本发明的另一个目的是提供该治疗肥胖症的药物的使用方法。 发明概述
本发明提供了一种新的治疗肥胖症的药物, 它是以白术、 苍术、 当归、 丹参、 泽泻、 蛇床子、 芥子、 麻黄、 大黄、 三七为原料, 并根 据处方中各中药所含成分及性质进行提取制备而成的.
本发明还提供了一种制备所述新的治疗肥胖症的药物的方法, 其 中, 将大黄单独用 70%的乙醇提取两次, 制成稠膏; 处方中其它药物 水提醇沉后, 再减压回收乙醇, 并浓缩至稠膏。 上述两种稠膏合并, 溶入 PEG混合基质溶液中, 任选地加入适量的促透皮吸收剂、 表面活 性剂、 防腐剂、 水等, 制成药膏。 任选地将所得药膏倒入合适形状的 塑料模孔中, 适当冷却成型后, 用合适的载体覆盖于塑料模孔及塑料 模上, 制成贴剂。
本发明还提供了使用所述治疗肥胖症药物的方法, 其中包括: 将 上述药膏直接施于脐部 (神阙穴)或关元穴 (脐下三寸)使用, 或者, 将上 述贴剂打开包装, 弃去塑料模, 将棵露药物的一面直接按药膏的形状 平贴于脐部 (神阙穴)或关元穴 (脐下三寸), 再揭去外层支持膜, 35 左 右的体表温度将药物溶化, 一日一贴, 24 小时使用, 贴一天停一天或 用药两贴后停一曰。 发明详述
医学著作 《医门法律》 有 "肥人多脾弱" 的描述, 指出了其病理。 而 "脾为生痰之源" , 临床治疗多从脾胃、 痰湿入手。 中医的外治内 芥丹三白
参术子七
治理论即是本发明的理论依据所在。
本发明的治疗肥胖症的药物是以中国医学中的 "内病外治" 的理 论为基础, 采用一种中医外治的自然疗法即 "药物敷脐法" , 它是以 中医经络学为理论基础, 通过药物对脐的刺激作用以激发经气, 疏通 经络, 促进气血运行, 以调整脏腑功能并促成人体阴阳平衡, 以达到 治疗目的。 所述治疗术黄泻药物是以上述理论为基础, 再用先进透皮緩释技 术, 使药物通过穴位吸收通达全身。 调节代谢功能, 加速脂肪分解, 药效稳定。
本发明的药物采用中药植物为原料, 按一定比例组合配制而成。 具体原料为白术、 苍术、 当归、 丹参、 泽泻、 蛇床子、 芥子、 麻黄、 大黄、 三七等十味。
本发明药物中的中草药配方组成如下蛇大当(重量配比):
白术 3- 12份 苍术 3- 12份 床黄归 当归 3 - 15份 丹参 5- 30份 泽泻 6- 30份 蛇床子 3- 15份 芥子 3- 12份 麻黄 2 - 12份 大黄 3 - 30份 三七 2- 10份
优选地, 本发明药物中的中草药配方组成如下(重量配比):
白术 5- 10份 苍术 5- 10份 当归 5- 10份 丹参 5- 15份 泽泻 10 - 20份 蛇床子 5- 10份 芥子 5- 10份 麻黄 5- 10份 大黄 5- 15份 三七 2- 6份
最优选地, 本发明药物中的中草药配方组成如下(重量配比):
5份 5份 5份
5份 10份 5份
5份 5份 5份。
2份 本发明药物中的中草药配方中所用的药材均为常用中草药材, 首 先应符合《中华人民共和国药典》 标准, 以确保投料用药原料的质量 以及所制备的药物安全有效。 此外, 为使外用贴剂有更好的效果, 选 用道地药材为佳。
本发明的药物是以中医学中的 "内病外治" 理论及中医经络学理 论为基础和指导, 将中药中古老的外用黑药膏制备技术与现代药剂学 的新材料、 新工艺的方法相结合制备而成。 借助经络穴位和透皮两个 作用途径, 以发挥药物的参经走络, 行滞祛瘀的作用, 实现药物整个 处方中的激发经气, 疏通经络, 促进气血运行, 以调整脏腑功能。 并 协调人体阴阳平衡, 从而达到内病外治的目的。 本中药贴膏的作用机 理除与传统中医药理理论相吻合外, 与现代医药学中的透皮给药系统
(TDS)理论或透皮治疗系统 (TTS)也是不谋而合的。
本发明的治疗肥胖症的药物可以是任何一种药剂学上所说的剂 型。
本发明的治疗肥胖症的药物可以包括辅料如基质、 促透皮吸收剂、 表面活性剂、 防腐剂、 水以及本领域中常用的其它添加剂。
本发明的治疗肥胖症的药物优选地是制成外用药膏使用。 在本发 明的外用药膏中, 基于成品药膏的总重量计, 中药的含量一般占 20〜40 % , 辅料的含量一般占 60~80 % 。
本发明药物中所使用的基质可以是制剂学领域中常用于外用膜 剂、 软膏剂、 乳剂、 贴剂(包括硬膏药类)等的那些基质。
在外贴药中, 黑药膏为古老的传统剂型, 最具代表性。 它是将药 物溶解或混合于粘性基质中, 滩涂于裱背材料上供贴敷使用的外用剂 型。 但在其制备及使用过程中, 存在很多问题。 黑膏药是由药材、 食 用植物油与红丹炼制而成的铅硬膏。 提取所用溶媒是植物油, 但植物 油只能溶解一些非极性物质, 而一般药材中所含的有效成份如生物碱 在细胞中常与有机酸结合成盐而存在, 故不溶解于油。 少数游离的生 物碱、 黄酮甙类、 蒽醌甙类与某些甙元等虽能溶解, 但在高温下亦多 半被破坏。 树脂及挥发性成分遇高温亦易分解和挥发, 一般不能耐受 高温熬炼。 在制备过程中, 也同样存在环境污染, 使用后不易清洗等 问题。
在外用的其它许多剂型如外用乳膏剂、 膜剂等中, 也普遍存在着 载药量少、 不易透皮吸收等缺点。 除此以外, 还有其它许多问题。 如 通常所见的软膏, 一般用油脂性基质, 包括油脂类, 类脂类及烃类等。 其共同的特点是润滑、 无刺激性, 保护及软化作用比其它基质强, 能 与较多的药物配合。 但油腻性及疏水性大, 水溶性成分不易溶解, 也 不易用水洗除, 对药物的释放、 穿透较其它基质小。 乳剂型基质与乳剂相似, 是由水相、 油相借助乳化剂的作用而成 的半固体状态基质。 分水包油与油包水两类。 油包水型乳剂基质外观 似油膏状, 较油脂性基质易涂布, 油膩性小, 且水分从皮肤表面蒸发 时有緩和冷却的作用。 水包油型乳剂基质外观似雪花膏, 能与水混合, 无油膩性, 易清除。 但也易干燥, 发霉, 故常需要加入防腐剂和甘油, 丙二醇或山梨醇等保湿剂, 存在着产品不稳定的问题。 尤其是遇水不 稳定的药物及含大量不明成分的处方, 都是引起制剂产品不稳定的重 要因素, 因而不宜选用。
水溶性基质无脂性, 又称水凝胶软膏基质。 由天然或合成的高分 子水溶性物质所组成。 水溶性基质能与水性体液混合, 吸收组织液, 一般释放药物较快, 无油膩性, 易涂展和洗除。 对皮肤和粘膜无刺激 性, 可用于糜烂的创面和腔道粘膜。 其缺点是润滑作用较差, 易失水 干涸, 故需加保湿剂和防腐剂。
作为基质, 由于制成制剂后直接与皮肤接触, 因此, 除在理化性 能上符合要求外, 对皮肤应没有刺激, 无不良反应。 本发明药物中的 基质优选为具有不同分子量的聚乙二醇类物质, 按不同配比组方。
据研究, 聚乙二醇类物质对人体无毒性和刺激性, 化学性质稳定, 耐热, 不易酸败和发霉。 由于本品有广泛的溶解范围、 兼溶性、 成膜 性、 增塑性、 分散性等, 所以较小分子量的本品用作溶剂、 助溶剂和 油 /水型乳剂的稳定剂, 用于水混悬剂、 乳剂、 注射剂等的制备。 由于 它们很稳定, 对皮肤无刺激性而具有润滑性, 用作水溶性软膏基质和 栓剂基质, 制造乳膏剂、 栓剂等。 对水中不易溶解的药物, 本品可作 固体分散的目的, 提高药物的溶解性或溶解度和增加药理活性。
除易与水溶性物质混溶外, 还能与脂溶性物质混溶。 其吸湿性好, 可吸收分泌液。 外观虽为油性, 但易洗除。 可与多数药物配伍。 基质 本身对药物成分的释放和渗透较快, 可充分发挥作用。 加入适量的表 面活性剂及促透皮吸收剂, 使其对本方中提取的成分大部分都能较好 地溶解, 制剂稳定。 由于水溶性及脂溶性成分的溶解度都大大增加, 从而使药物在制剂中分散非常均匀, 利于药物有效成分通过穴位吸收 而最大程度地发挥其作用。 由于本制剂在 以下处于近固体状态, 加上本身的高渗状态, 因此不易长霉, 不易腐败变质, 具有良好的稳 定性, 其所含的化学成分也相应有较好的稳定性, 不易分解、 变质。 这也是本发明所制备的药物具有的卓越优点。
可以具体提到的基质是 PEG400、 PEG1000, PEG4000. 均为 《中 华人民共和国药典》 一九九五年版二部收载品种, 并按一定比例组方, 该比例应使得得到的本发明的药膏在 35 左右的体表温度下而成熔融 状态。优选地, 基于本发明成品药膏的总重量计, PEG400的含量占 2~8 %, PEG1000的含量占 30~50%, 而 PEG4000的含量占 15~45 %。
基于本发明成品药膏的总重量计, 基质的含量一般占 44.7~78.9 %, 优选占 60~70 %。
在本发明的治疗肥胖症的药物中, 可以任选地使用促透皮吸收剂。 一般认为, 当促透皮吸收剂作用在皮肤上时, 通过改变皮肤渗透率, 提高有效成分的扩散性或药物的溶解度, 导致药物通透性增加, 从而 达到促进透皮吸收的这一最终目的。
本发明优选使用少量的促透皮吸收剂, 以加强药物的透皮吸收性, 提高其疗效。 基于制成的成品药膏总重量计, 促透皮吸收剂含量一般 占 0.5~10 % , 优选占 1%。 本发明中所用的促透皮吸收剂可以是本领域 中常用于此目的的任何促透皮吸收剂。 本发明所选用的促透皮吸收剂 优选是氮酮(Azone), 化学名为 1-十二烷基 -六氢 -2H-氮杂箪 -2-酮。 也 为 《中华人民共和国药典》 一九九五年版二部所收载, 因此, 其质量 应符合规定。
本发明的药物中加入的促透皮吸收剂氮酮, 其是一种新型的高效 低毒穿透促进剂。 为无色、 几乎无味的液体, 不溶于水, 有润滑性, 对人的皮肤、 粘膜和腔膜无刺激, 毒性小。 氮酮为非极性促透皮吸收 剂。 作用机理被认为是使角质软化, 凝固组织蛋白, 增强通透性, 使 药物透过皮肤屏障, 提高局部或全身性血药浓度, 提高制剂的生物利 用度, 从而获得更为理想的治疗效果。
在本发明的治疗肥胖症的药物中可以任选地使用表面活性剂。 在 基质中加入表面活性剂可增加水中不溶性药物成分的溶解度以及增加 所用基质的吸水性, 从而使药物成分在基质中有较好的溶解度, 同时 也促进药物的穿透性。 性剂。 优选地, 使用非离子型 活性剂吐温 -80 作为本发明的表面活 性剂。 本品对不同 pH具有显箸的适应性, 与高浓度的电解质共存时也 较稳定。 对皮肤刺激性和毒性都很小。
按照本发明的成品药膏的总重量计, 表面活性剂的含量一般占
0.5-5 % , 优选占 2 % 。
在本发明的治疗肥胖症的药物中任选地使用防腐剂。 本发明可以 使用常用于本领域中的任何防腐剂。 虽然本发明药物中所用的基质占 比例较大, 其溶液呈高渗状态, 微生物不易生长。 但考虑到本品的储 藏温度为 25 以下, 因而在本发明药物中, 优选使用防腐剂。 优选的 防腐剂是洗必泰, 因为据文献报道, 聚乙二醇类可能会減小苯甲酸酯 类防腐剂的抑菌效果, 而洗必泰所受影响不大, 所以用量并未增加。 在本发明的药物中, 基于成品药膏的总重量计, 防腐剂一般占 0.1 0.3 % , 优选占 0.1%。
在本发明的药物中, 可以含有适量的水。 基于本发明成品药膏的 总重量计, 水的含量一般占 0~30 % .
本发明的药物中还可以任选地含有其它在本领域常用的添加剂, 这要根据希望达到的特定目的来选用。
本发明还提供了制备所述新的治疗肥胖症的药物的方法。 其中, 将大黄单独用 70%的乙醇提取两次, 制成稠膏; 处方中其它药物水提 醇沉后, 再减压回收乙醇, 并浓缩至稠膏。 上述两种稠膏合并, 溶入 PEG混合基质溶液中, 任选地加入适量的促透皮吸收剂、 表面活性剂、 防腐剂、 水和其它常用的添加剂, 制成药膏。 任选地将所得药膏倒入 合适形状的塑料模孔中, 适当冷却成型后, 用合适的载体覆盖于塑料 模孔及塑料模上, 制成贴剂,
在本发明的方法中, 一般而言, 1 克所述稠膏相当于 克的生 药. 具体情况会因采生药的地点和季节多少有些不同。
在本发明的方法中, 优选地加入促透皮吸收剂、 表面活性剂、 防 腐剂和水。 优选地, 将所得到的药膏倒入圓锥形状的塑料模孔中, 制 成圓锥形贴剂。
本发明还提供了使用所述治疗肥胖症药物的方法, 其中包括: 将 上述药膏直接施于脐部 (神阙穴)或关元穴 (脐下三寸)使用, 或者, 将上 述贴剂打开包装, 弃去塑料模, 将棵露药物的一面直接按药膏的形状 平贴于脐部(神阙穴)或关元穴 (脐下三寸), 再揭去外层支持膜, 35 左 右的体表温度将药物溶化, 一日一贴, 24 小时使用, 贴一天停一天或 用药两贴后停一日。
优选地, 将上述圓锥形状的贴剂的锥尖端对准脐部按陷进穴位中 或直接贴在关元穴。
当将本发明的治疗肥胖症的药物作为药膏外用时, 可以直接施用。 但优选地, 将所述膏药贴敷及支持在适当的载体材料上使用。 本领域 常用于此目的的所有载体材料都适用于本发明。 本发明载体材料的特 点是:
• 防水
• 透气, 透湿性高, 而且药剂不溢出
• 伸缩性高
• 超薄, 密合性好
• 安全卫生
• 无副作用, 对皮肤负担少, 老少皆宜
优选地, 载体是由海绵垫團和特殊的防水、 透气薄膜构成, 所述 的特殊的防水、 透气薄膜例如是由合成树脂和丙烯酸类粘合剂制成的。
本发明的治疗肥胖症的药物作为外用贴剂使用时, 贴于肚脐 (神阙 穴)或关元穴 (脐下三寸), 隔曰用一次, 或贴两天停一天, 每贴使用 24 小时, 每天体重减轻 lkg以上者, 请用一日停贴二日。
本发明的药物按要求贴用于所选部位一段时间后, 会自然而緩緩 地融化, 药物成分进入体内并发挥作用。 可感觉大肠里蠕动, 排气增 加, 无饥俄感, 爱吃素菜。 个别皮肤温度过低者, 可对用药部位适当 加温敷贴(注意加温以软化为度, 不要超过 以使药物软化, 提 高疗效。 使用本发明的药物时, 应该注意: (1)肚脐有破溃者禁用, (2) 出现过敏反应, 应停止使用。
本发明的治疗肥胖症的药物作为外用药使用时, 是一种新型外用 保健减肥药品, 由纯正中药精制而成。 不含任何有害成份, 使用安全, 方便. 需每日贴于肚脐 (神阙穴), 通过穴位给药, 可有效调节人体脂肪 代谢。 全身减肥效果明显, 尤其对腰、 腹、 臀部减肥有特效。 不需节 食, 不腹泻, 不反弹, 药效持久稳定。 本发明的药物对各种类型的肥 胖都适用。
本发明的治疗肥胖症的药物中的中草药配方优选是在本发明的外 贴膏药中使用, 但并不排除将它们直接地或制做成任何适当的药剂学 上可接受的剂型使用。
下面通过实施例来说明本发明。 但下面的实施例仅仅是说明性的, 并不在任何方面构成对本发明的限制。 实施例 实施例 1
1. 处方
苍术 200g 白术 200g 大黄 200g 麻黄 200g 当归 200g 三七 80g 丹参 200g 芥子 200g 泽泻 400g 蛇床子 200g
PEG400 50g
PEG1000 450g
PEG4000 200g
吐温 -80 20g
Azone lOg
洗必泰 lg
H20 适量
共制成 lOOOg
2. 制备工艺
2. 1大黄的提取
以 75%乙醇为溶媒热回流提取两次, 第一次加药材 8倍量的溶媒, 加热回流 1 小时, 滤过; 第二次加药材 6倍量的溶媒, 加热回流 1 小 时, 滤过。
合并两次滤液, 减压回收乙醇并浓缩至无醇味, 备用。
2. 2方中其它中药的提取
方中其它中药以水为溶媒热回流提取两次。 第一次加药材 10倍量的 水, 浸泡 1小时, 加热提取 1.5小时, 滤过; 第二次加药材 8倍量的水, 加热提取 1小时, 滤过。
合并两滤液, 减压浓缩至每 lml药液相当于药材 1.2g左右, 加 95% 的乙醇到含醇量为 60%进行醇沉, 静置 24小时。
滤取上清液, 减压回收乙醇, 浓缩至稠膏, 备用。 2.3基质的处理
将 PEG400、 PEG1000, PEG4000 混合, 加热至 左右使之完 全熔融, 溶入 Azone及洗必泰后, 滤过。
2.4成型
取 2. 1及 2. 2提得的稠膏, 加水至总量为 450g, 加入吐温 -80, 混 匀, 再加入上述 2. 3项 PEG等的混合溶液中, 保持 65 :左右, 搅拌, 使提取物完全分散均匀, 倒入塑料模孔中, 冷却, 即得。 每粒重 0.5g, 在 25C以下保存, 密封防潮, 备用。
3.用量及用法
揭去塑料罩膜后, 贴于肚脐 (神阙穴)或关元穴 (脐下三指), 每次 1 粒, 贴 12-24 小时, 隔日一次或贴两天停一次 (每天体重减轻 1kg者, 停贴两天)。
4.效果
将上述制成的药品按照上述用法和用量临床治疗 56 例病人, 其中病人的基本情况是: 56例病人中,男性病人 24例,年龄在 18~65 岁之间, 平均年龄为 45.8岁, 平均体重超过正常体重 20% ; 女性 病人 32例, 年龄在 21~69岁之间, 平均年龄为 48.3岁, 平均体重 超过正常体重 25%。 30 天后, 临床观察的结果是, 明显有效的有 47 人, 明显有效率为 83.9% ; 有效的有 7 人, 有效率为 12.5%; 而无效的有 2人, 无效率为 3.6%。 治疗 3个月后, 平均每月减体 重占体重的 5%以上。
然而, 将先有技术中的类似药物按类似方法临床用于治疗 23例 病人, 其中病人的基本情况是: 23 例病人中, 男性病人 9 例, 年 龄在 23~56 岁之间, 平均年龄为 43.6 岁, 平均体重超过正常体重 20%; 女性病人 14 例, 年龄在 19 65 岁之间, 平均年龄为 47.2 岁, 平均体重超过正常体重 20%。 30 天后, 临床观察的结果是, 明显有效的有 0人, 明显有效率为 0% ; 有效的有 7人, 有效率为 34.7%; 而无效的有 15人, 无效率为 65.3%。
从上面的结果可以清楚地看出, 本发明的药物减肥效果好, 人均减 轻体重多, 维持时间长, 较先有技术的药物减肥效果明显为优。 尤为 突出的是, 上面的结果表明, 使用本发明的药物在三个月后即不再出 现反弹, 药效持久稳定。 实施例 2
按照与上述实施例 1类似的方法步骤对组成如下的本发明的药 物进行配制和临床试验, 得到了类似的结果:
苍术 120g 白术 120g 大黄 120g
麻黄 80g 当归 120g 三七 160g
丹参 400g 芥子 120g 泽泻 240g
蛇床子 120g
PEG400 50g
PEG1000 450g
PEG4000 200g
吐温 -80 20g
Azone 10g
洗必泰 ig
H20 适量
共制成 lOOOg. 实施例 3
按照与上述实施例 1类似的方法步骤对组成如下的本发明的药 物进行配制和临床试验, 得到了类似的结果:
苍术 480g 白术 480g 大黄 1200g
麻黄 480g 当归 600g 三七 400g
丹参 1200g 芥子 480g 泽泻 1200g
蛇床子 600g
PEG400 50g
PEG1000 450g
PEG4000 200g
吐温 -80 20g
Azone lOg
洗必泰 lg H20 适量
共制成 1000g。 以上对本发明进行了详细的描述。 但是, 本领域普通技术人员应该 理解, 可以对本发明进行许多变化和改变, 而不脱离本发明的精神和 范围。 本发明不受这些变化和改变的限制。

Claims

权 利 要 求
1. 一种治疗肥胖症的药物, 其特征在于, 它是由以白术、 苍 术、 当归、 丹参、 泽泻、 蛇床子、 芥子、 麻黄、 大黄、 三七为中草 药原料的配方提取. 配制而成的。
2. 根据权利要求 1 的治疗肥胖症的药物, 其中各中草药原料 的重量配比如下:
白术 3- 12份 苍术 3- 12份 当归 3- 15份
丹参 5- 30份 泽泻 6- 30份 蛇床子 3- 15份
芥子 3- 12份 麻黄 2- 12份 大黄 3 - 30份
三七 2- 10份。
3. 根据权利要求 2 的治疗肥胖症的药物, 其中各中草药原料 的重量配比如下:
白术 5— 10份 苍术 5— 10份 当归 5— 10份
丹参 5- 15份 泽泻 10- 20份 蛇床子 5- 10份
芥子 5- 10份 麻黄 5- 10份 大黄 5- 15份
三七 2- 6份。
4. 根据权利要求 3 的治疗肥胖症的药物, 其中各中草药原料 的重量配比如下:
白术 5份 苍术 5份 当归 5份
丹参 5份 泽泻 10份 蛇床子 5份
芥子 5份 麻黄 5份 大黄 5份
三七 2份。
5. 根据权利要求 1~4 任一项的治疗肥胖症的药物, 其特征在 于, 它还含有辅料。
6. 根据权利要求 5的治疗肥胖症的药物, 其中的辅料是基质、 促透皮吸收剂、 表面活性剂、 防腐剂和水。
7. 根据权利要求 6 的治疗肥胖症的药物, 其中的基质是 PEG400、 PEGIOOO 和 PEG4000, 促透皮吸收剂是氮酮,表面活性剂 为吐温 -80, 以及防腐剂是洗必泰。
8. 根据权利要求 7 的治疗肥胖症的药物, 其中它是承载在载 体上做成外用贴剂。
9. 根据权利要求 8 的治疗肥胖症的药物, 其中的载体是由海 绵垫圈和特殊的防水、 透气薄膜构成, 所述的特殊的防水、 透气薄膜 是由合成树脂和丙烯酸类粘合剂制成的。
10.根据权利要求 9 的治疗肥胖症的药物, 其中它被做成圆锥 状的外用贴剂。
11.制备权利要求 1~10任一项的药物的方法, 其特征在于, 将 采用的大黄单独用 70%的乙醇提取两次, 制成稠膏; 处方中其它药物 水提醇沉后, 再减压回收乙醇, 并浓缩至稠膏。 上述两种稠膏合并, 溶入 PEG混合基质溶液中, 任选地加入适量的促透皮吸收剂、 表面活 性剂、 防腐剂、 水等, 制成药膏。 任选地将所得药膏倒入合适形状的 塑料模孔中, 适当冷却成型后, 用合适的载体覆盖于塑料模孔及塑料 模上, 制成贴剂。
12. 使用权利要求 1~10任一项药物的方法, 其中包括将所述 药物施用于脐部或关元穴部位。
PCT/CN2000/000037 2000-02-29 2000-02-29 A medicine for treating obesity and the method of producing thereof Ceased WO2001064229A1 (en)

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WO2004058284A1 (en) * 2002-12-27 2004-07-15 Korea Institute Of Oriental Medicine Anti-obesity ingretients from medicinal plants and their composittion
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EP1706108A4 (en) * 2003-12-30 2009-08-12 Md Bioalpha Co Ltd TREATMENT OF FAT AND METABOLIC SYNDROME WITH TRANSHINONE DERIVATIVES FOR INCREASING METABOLISM ACTIVITY
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