DE102018111697A1 - A drug for the treatment of osteoporosis and its manufacturing process - Google Patents

Abstract

The present invention discloses a medicament for the treatment of osteoporosis and its method of production. The drug for the treatment of osteoporosis comprises, by weight, Dandelion 10-20, the fruits of Areca catechu 10-15 and Fructus Aurantii Immaturus 3-20, Angelica sinensis 12-18 and Radix Paeoniae Alba 5-10. The medicament for the treatment of osteoporosis according to the invention has different ingredients compared to the medicaments of the prior art and can overcome the shortcomings of the medicaments of the prior art.

Description

Technical area

The present invention relates to the field of medicaments, in particular to a medicament for the treatment of osteoporosis and its method of production.

background

Osteoporosis is the most common disease and a worldwide health problem. Currently, the incidence of osteoporosis in the world has exceeded 25%; and in addition to the common diseases and the common diseases, the incidence of osteoporosis has reached the top 10. China is one of the countries that has one of the largest elderly population in the world. 90 million osteoporosis patients currently live there, corresponding to 7.1% of the total population. It is estimated that the number of osteoporotic patients will increase to 221 million by 2050. Therefore, the study for the prevention and treatment of osteoporosis is of great importance to human health and quality of life.

There are currently two common treatment plans - a "basic treatment" and an "intensive care" - which are used clinically to treat osteoporosis. A basic treatment refers to a treatment with "calcium + vitamin D". In general, a "baseline treatment" with little side effects is relatively safe, but the effects of increasing bone density and reducing the incidence of a fracture are not confirmed. The intensive treatment includes treatment with biphosphonate-based drugs and calcitonin-based drugs. It is generally believed that these drugs can effectively improve bone density, alleviate the symptoms of osteoporosis more quickly, and effectively reduce the possibility of fracture; however, these must be used under the guidance of a specialist to avoid side effects. A "triple therapy" is also clinically common, with the first form of triple therapy using calcium and vitamin D and periodic biphosphonate / calcitonin and being suitable for the treatment of senile osteoporosis in patients and patients who are manifestly suffering from pain. A second form of triple therapy uses calcium and vitamin D and a selective estrogen receptor regulator that can maximize the beneficial effect of estrogen on the bone and also effectively avoids side effects on the breast and uterus, and thus has the potential to replace traditional female hormone replacement therapy.

However, the treatment effects of the above treatment or therapy are not ideal. In addition, the current drugs have different toxicities and unwanted effects. Therefore, there is an urgent need for a new drug for the treatment of osteoporosis in order to overcome the above-mentioned deficiencies.

Summary of the invention

In view of the above problem, the present invention provides a medicament for the treatment of osteoporosis suitable for solving the above-mentioned problems or at least part of the above-mentioned problems for overcoming deficiencies of the medicaments mentioned in the prior art with their weak effects in the treatment.

In a first aspect, the present invention provides a medicament for the treatment of osteoporosis, comprising, by weight, Dandelion 10-20, the fruit of Areca catechu 10-15, Fructus Aurantii Immaturus 3-20, Angelica sinensis 12-18 and Radix Paeoniae Alba 5-10.

The medicament of the present invention for the treatment of osteoporosis has different ingredients as compared to the prior art medicaments and can overcome the deficiencies of the prior art medicaments.

Detailed description of the embodiments

In one embodiment of the present invention, there is provided a medicament for the treatment of osteoporosis, comprising by weight, Dandelion 10-20, the fruit of Areca catechu 10-15, Fructus Aurantii Immaturus 3-20, Angelica sinensis 12-18 and Radix Paeoniae Alba 5-10.

Furthermore, the drug may comprise, by weight, Eucommia ulmoides 20-50.

Furthermore, the drug may comprise by weight the root of Kudzu vine 2-22.

The above Eucommia ulmoides and the root of Kudzu vine are but a few specific examples, but are not intended to be limiting; other materials such as wolfberry fruit, Gynostemma pentaphyllum, 12 Semen Astragali Complanati, Radix Dipsaci, Herba Eclipta, Fructus Ligustri Lucidi, etc. are also possible. Other possible materials are not described in detail.

Optionally, in one embodiment of the present invention, pulmonary vascularization materials may be added, for example, Carcuma longa, Ligusticum chuanxiong Hort, Radix Salviae Miltiorrhizae, and Evening Primrose.

In addition, in one embodiment of the present invention, the medicament may further comprise heat balance materials, such as Fructus Gardeniae, Flos Chrysanthemi, Semen Cassiae, cortex Fraxini, Radix Sophorae Flavescentis, Flos Chrysanthemi Indici, Andrographis Paniculata, etc., to enhance pharmacological effects ,

In addition, the medicament may further comprise moisture balance and urinary excretion promoting materials, such as Herba Sedi, Abrus Herb, etc.

In addition, the medicament may further comprise internal heating materials such as pepper.

In one embodiment of the present invention, the dosage form of the medicament is at least one of film-coated tablet, sugar-coated tablet, enteric-coated tablet, dispersible tablet, capsule, granule, decoction, mixture, syrup, vinum, injection, oral solution and oral cloudy solution.

In one embodiment of the present invention, the medicament, optionally, has a dosage form for oral administration.

In one embodiment of the present invention, the oral dosage form of administration, optionally includes a tablet, capsule, pill, injection, sustained release preparation and controlled release formulation.

The medicament or the medicament composition of the present invention comprising the same may be administered in a dosage unit unit via the intestinal tract, nasal cavity, oral mucosa, eye, lung, respiratory tract, skin, rectum, etc., and by oral administration, intravenous injection, intramuscular injection and subcutaneous Be administered injection.

The dosage form of administration may be a liquid dosage form, a solid dosage form or a semi-solid dosage form. The liquid dosage form may be a solution, emulsion, suspension, injection (including water injection, powder injection and transfusion), eye drops, nasal drops, lotion and liniment; the solid dosage form can be a tablet (including an uncoated tablet, enteric tablet, buccal tablet, dispersible tablet, chewable tablets, effervescent tablets, fast disintegrating tablets), capsule (including hard capsule, soft capsule, enteric capsule), granules, powders, pellets, small, fast dissolving pill, suppositories, film agent, paste, aerosol, spray, etc .; and the semi-solid dosage form may be a balm, gel, paste, etc. The dosage form of the medicament is preferably a tablet, capsule, pill and injection.

The medicament according to one embodiment of the present invention can be prepared in a conventional preparation, a sustained release preparation, a controlled release preparation, a targeting preparation and various granular administration preparations.

In one embodiment of the present invention, various adjuvants such as diluents, binders, humectants, resolving agent, lubricants and lubricants may be used to prepare the medicament of the present invention into a tablet. The diluent may be starch, dextrin, sucrose, lactose, mannitol, sorbitol, xylitol, microcrystalline cellulose, calcium sulfate, calcium hydrogen phosphate, calcium carbonate and the like; the humectant may be water, ethanol, isopropanol and the like; the binder may be starch, powder, dextrin, syrup, honey, glycose solution, microcrystalline cellulose, arabic gum pulp, gelatin pulp, sodium carboxymethylcellulose and methylcellulose; the dissolving agent may be starch pulp, microcrystalline cellulose, low substituted hydroxypropyl cellulose; and the lubricating and lubricating agent may be talc, silica, stearate, liquid paraffin and the like.

Furthermore, the medicament may also be a coated tablet, for example a sugar-coated tablet, a film-coated tablet, an enteric-coated tablet and the like.

When the medicament is prepared in a capsule, the active ingredient may be prepared in granules or pellets with an additive of diluent, binder and a dissolving agent, which are then incorporated in a hard or soft capsule.

When the drug is prepared as an injection, the solvent may be water, ethanol, isopropanol, propylene glycol, or a mixture thereof. Further, an appropriate amount of a dissolution assistant, cosolvent, pH adjusting agent, may be added to the osmotic pressure adjusting agent.

Furthermore, a dye, preservative, perfume, corrigent or other additives can be added to the drug.

• einen ersten Schritt des Wiegens, in Gewichtsanteilen von Dandelion 10-20, die Frucht des Areca catechu 10-15, Fructus Aurantii Immaturus 3-20, Angelica sinensis 12-18 und Radix Paeoniae Alba 5-10;
• einen zweiten Schritt des Pulverisieren von Dandelion, der Frucht des Areca catechu und der Fructus Aurantii Immaturus in Pulver, Sieben des Pulvers insbesondere mit einem 200 Mesh Sieb und gleichmäßiges Mischen, um feines Pulver zu erhalten;
• einen dritten Schritt des zweimaligen Abkochens der Angelica sinensis und Radix Paeoniae Alba mit Wasser für jeweils 30 bis 60 Minuten und Filtern, um zwei Filtrate zu erhalten;
• einen vierten Schritt des Mixens der zwei Filtrate, Stehenlassen um einen Überstand zu erhalten, und den Überstand unter Vakuum zu konzentrieren, um eine dicke Paste zu erhalten; und
• einen fünften Schritt des gleichmäßigen Vermischens der verdickten Paste gegebenenfalls vorab getrocknet und pulverisiert, mit dem oben genannten feinen Pulver und Hilfsstoffen in einem geeigneten Verhältnis, um ein gemischtes Medikament zu erhalten.

In one embodiment of the present invention there is provided a method of making the above medicament, comprising the steps of:

• a first step of weighing, by weight of Dandelion 10-20, the fruit of Areca catechu 10-15, Fructus Aurantii immaturus 3-20, Angelica sinensis 12-18 and Radix Paeoniae Alba 5-10;
• a second step of pulverizing Dandelion, the fruit of the Areca catechu and the Fructus Aurantii Immaturus in powder, sieving the powder, in particular, with a 200 mesh sieve and mixing it uniformly to obtain fine powder;
• a third step of boiling the Angelica sinensis and Radix Paeoniae Alba twice with water for 30 to 60 minutes each and filtering to obtain two filtrates;
• a fourth step of mixing the two filtrates, leaving to leave a supernatant, and concentrating the supernatant under vacuum to obtain a thick paste; and
• optionally, a fifth step of uniformly mixing the thickened paste is preliminarily dried and pulverized with the above fine powder and excipients in an appropriate ratio to obtain a mixed medicament.

The following are some specific examples of the method of producing the medicament for treating osteoporosis.

example 1

First step: Weigh, in parts by weight of Dandelion 10-20, the fruit of Areca catechu 10-15, Fructus Aurantii immaturus 3-20, Angelica sinensis 12-18 and Radix Paeoniae Alba 5-10;
Second step: pulverizing the Dandelion, the fruit of the Areca catechu and the Fructus Aurantii Immaturus in powder, sieving the powder with a 200 mesh sieve, and mixing uniformly to obtain fine powder;
Third step: boil off the Angelica sinensis twice and Radix Paeoniae Alba with water for four hours at 30 ° C by adding 10 ml of water at intervals of 30 minutes each time, and filter to obtain two filtrates;
Fourth step: mixing the two filtrates, leaving for 30 minutes at room temperature to obtain a supernatant and concentrating the supernatant under vacuum to obtain a thickened paste; and
Fifth step: drying the thickened paste and pulverizing and uniformly mixing the pulverized paste with the above-mentioned fine powder and adjuvants in an appropriate ratio to obtain a mixed medicament.

Example 2

First step: mixing the root of Kudzu vine, Dandelion, the fruit of Areca catechu and Fructus Aurantii immaturus;
Second step: pulverizing the root of the kudzu vine, Dandelion, the fruit of the Areca catechu and Fructus Aurantii immaturus into powder, sieving the powder with a 200 mesh sieve and mixing uniformly to obtain fine powder;
Third step: Soak the Angelica sinensis and Radix Paeoniae Alba with water for at least eight hours until completely soaked;
Fourth step: boil off the Angelica sinensis and Radix Paeoniae Alba twice with water for four hours at 30 ° C by adding 10 ml of water every 30 minutes, and filter to obtain two filtrates;
Fifth step: mixing the two filtrates, leaving for 30 minutes at room temperature to obtain a supernatant, and to concentrate the supernatant under vacuum to obtain a thickened paste; and
Sixth step: drying the thickened paste and pulverizing, and uniformly mixing the pulverized thickened paste with the above-mentioned fine powder and adjuvants in a proper ratio to obtain a mixed medicament.

Example 3 (the production of granules)

First step: mixing the root of Kudzu vine, Dandelion, the fruit of Areca catechu and Fructus Aurantii immaturus;
Second step: pulverizing the root of the kudzu vine, Dandelion, the fruit of the Areca catechu and Fructus Aurantii immaturus into powder, sieving the powder with a 200 mesh sieve and mixing uniformly to obtain fine powder;
Third step: Soak the Angelica sinensis and Radix Paeoniae Alba with water for at least eight hours until completely soaked;
Fourth step: boil off Angelica sinensis twice and Radix Paeoniae Alba with water for four hours at 30 ° C by adding 10 ml of water at 30 minute interval each, and filter to obtain two filtrates;
Fifth step: mixing the two filtrates and concentrating the filtrates under vacuum to obtain a relative density extract of 1.25 (60 ° C), mixing the extract with three times the amount of dextrin to obtain a soft material, and preparing Granules with an oscillating granulator with the addition of the fine powder obtained in the second step;
Step Six: Dry the granules at 65 ° C for 30 minutes, finish the granules, sieve to remove small granules and package.

Claims (5)

A medicament for the treatment of osteoporosis, by weight, Dandelion 10-20, the fruit of Areca catechu 10-15, Fructus Aurantii immaturus 3-20, Angelica sinensis 12-18 and Radix Paeoniae Alba 5-10. The drug for the treatment of osteoporosis according to Claim 1 , further comprising, by weight, Eucommia ulmoides 20-50. The drug for the treatment of osteoporosis according to Claim 1 , further comprising, in parts by weight, the root of Kudzu vine 2-22. The drug for the treatment of osteoporosis according to Claim 1 wherein the dosage form of the medicament is at least one of film-coated tablet, sugar-coated tablet, enteric-coated tablet, dispersible tablet, capsule, granule, decoction, mixture, syrup, vinum, injection, oral solution and oral cloudy solution. A method of manufacturing a medicament according to any one of Claims 1 to 4 comprising the following steps: a first step of weighing by weight, Dandelion 10-20, the fruit of Areca catechu 10-15, Fructus Aurantii immaturus 3-20, Angelica sinensis 12-18 and Radix Paeoniae Alba 5-10; a second step of pulverizing the dandelion, the fruit of the Areca catechu and the Fructus Aurantii immaturus into powder, sieving the powder, in particular with a 200 mesh sieve, and uniformly mixing to obtain a fine powder; a third step of boil- ing Angelica sinensis and Radix Paeoniae Alba twice with water, and filtering to obtain two filtrates; a fourth step of mixing the two filtrates, leaving to obtain a supernatant and concentrating the supernatant in vacuo to obtain a thick paste; and a fifth step of uniformly mixing the thick paste, if necessary, after previously drying and pulverizing with the above-mentioned fine powder and excipients in an appropriate ratio to obtain the medicament.