阅读说明：本技术 一种用于治疗痔疮的药物及其制备方法 (Medicine for treating hemorrhoids and preparation method thereof ) 是由 刘泽陆 于 2021-02-04 设计创作，主要内容包括：本发明提供了一种用于治疗痔疮的药物及其制备方法。本发明的用于治疗痔疮的药物包括主药和基质,所述主药包括硝苯吡啶,且硝苯吡啶在药物中的质量含量为1-3％；此外,该药物还可以包括其它用于治疗痔疮的化药原料和/或中药原料。本发明的药物能够良好地治疗内痔、外痔、混合痔、肛瘘、肛裂、肛门囊肿等痔疮疾病。(The invention provides a medicine for treating hemorrhoids and a preparation method thereof. The medicament for treating the haemorrhoids comprises a main medicament and a matrix, wherein the main medicament comprises nifedipine, and the mass content of the nifedipine in the medicament is 1-3%; in addition, the medicine can also comprise other chemical medicine raw materials and/or traditional Chinese medicine raw materials for treating the hemorrhoids. The medicine of the present invention can treat various kinds of piles, including internal pile, external pile, mixed pile, anal fistula, anal fissure, anal cyst, etc.)

1. The medicine for treating the haemorrhoids is characterized by comprising a main medicine and a matrix, wherein the main medicine comprises nifedipine, and the mass content of the nifedipine in the medicine is 1-3%.

2. The medicament as claimed in claim 1, wherein the principal drug further comprises a chemical and/or Chinese medicinal material for treating hemorrhoids.

3. The medicament according to claim 2, wherein the chemical raw material is nitroglycerin, and the mass content of the nitroglycerin in the medicament is 0.1-0.3%.

4. The medicine according to claim 2, wherein the traditional Chinese medicine raw materials comprise the following components in parts by weight: 6-12 parts of garden burnet, 5-10 parts of sophora flower, 4-8 parts of dandelion, 1-5 parts of borneol, 3-6 parts of phellodendron and 2-4 parts of fig.

5. The medicament as claimed in claim 4, wherein the mass content of the Chinese medicinal raw materials in the medicament is 10-15%.

6. The medicament of claim 1, wherein the base is at least one of petrolatum, lanolin, and polyethylene glycol.

7. A process for the preparation of a medicament as claimed in any one of claims 1 to 6, which comprises: mixing the main materials with matrix by grinding, dissolving or emulsifying.

8. The method of claim 7, wherein the developing process comprises: grinding the main medicine with a small amount of matrix into paste, adding the rest matrix, and grinding uniformly.

9. The method of claim 7, wherein the solution polymerization comprises: heating to melt the matrix, adding the main drug, and stirring to condense.

10. The method of claim 7, wherein the emulsification process comprises: heating oil soluble principal drug to melt, dissolving water soluble principal drug in water, mixing and stirring continuously until condensation.

Technical Field

The invention relates to the technical field of medicines, in particular to a medicine for treating hemorrhoids and a preparation method thereof.

Background

Nifedipine (nifedipine) is named as 1, 4-dihydro-2, 6-dimethyl-4- (2-nitrophenyl) -3, 5-pyridinedicarboxylic acid dimethyl ester and nifedipine, is a dihydropyridine calcium antagonist, and is mainly used for preventing and treating angina pectoris caused by coronary heart disease, particularly angina pectoris caused by variant angina pectoris and coronary artery spasm at present. Nifedipine has no adverse effect on respiratory function, and is particularly suitable for angina patients suffering from respiratory tract obstructive diseases, and the curative effect of nifedipine is better than that of beta receptor antagonist. In addition, nifedipine is also suitable for various types of hypertension, and has good curative effect on intractable and severe hypertension.

Hemorrhoids are a chronic disease of one or more soft venous masses formed by varicose of the venous plexus at the bottom of the anorectum and the anal mucosa, and include internal hemorrhoids, external hemorrhoids, and mixed hemorrhoids. The hemorrhoids are caused by a plurality of causes, for example, long-time sitting, standing, fatigue and the like, when a human body is in a fixed position for a long time, blood circulation is affected, so that slow blood flow in a pelvic cavity and congestion of internal organs in an abdomen are caused, and further hemorrhoid veins are excessively filled, varicose, raised and reduced in venous wall tension, which is one of important causes for causing the hemorrhoids. In addition, hypokinesia causes slow intestinal motility, slow descending of feces or habitual constipation, so that veins are pressed, local congestion and blood backflow disorder are caused, internal pressure of hemorrhoidal veins is increased, resistance of vein walls is reduced, and the incidence rate of hemorrhoids is increased.

The conventional treatment methods for hemorrhoids include surgical therapy, ultra-low temperature/ultra-high temperature therapy, ligation/ligation therapy, injection therapy, and the like. The purpose of the surgical therapy is to remove haemorrhoids or embolize or collapse by mechanical methods such as suturing, but the haemorrhoids are easy to recur and may cause sequelae such as fecal incontinence, although the haemorrhoids are quickly taken; the treatment principle of ultra-low temperature and ultra-high temperature therapy is that the ultra-low temperature or ultra-high temperature is utilized to generate cold or heat effect, so that the purposes of curing lesion tissue protein coagulation, vascular embolism closure, electrocautery electrocoagulation hemostasis, cutting, tissue degeneration, necrosis shedding or hardening atrophy and the like are achieved, the treatment effect is general, and the problems of easy recurrence and the like exist; ligation and ligation can block the blood circulation of the anus part, so that extravasated blood edema, pain, difficult defecation and the like are easy to generate; the injection therapy is to inject the medicine into hemorrhoids to treat hemorrhoids, but has the defects of easy mucosal ulceration, mucosal abscess and the like.

In view of this, the invention is particularly proposed.

Disclosure of Invention

The invention aims to provide a medicament for treating hemorrhoids and a preparation method thereof, the medicament can well treat hemorrhoids such as internal hemorrhoids, external hemorrhoids, mixed hemorrhoids, anal fistula, anal fissure, anal cyst and the like, and has the advantages of short treatment course, quick response, good curative effect and the like.

The invention provides a medicament for treating hemorrhoids, which comprises a main medicament and a matrix, wherein the main medicament comprises nifedipine, and the mass content of the nifedipine in the medicament is 1-3%, preferably 2%.

Nifedipine (nifedipine) is also called nifedipine, the name of which is 1, 4-dihydro-2, 6-dimethyl-4- (2-nitrophenyl) -3, 5-pyridinedicarboxylic acid dimethyl ester, the CAS number is 21829-25-4, the molecular weight is 346.335, and the molecular formula is C₁₇H₁₈N₂O₆The structural formula is as follows:

nifedipine is a traditional medicine for preventing and treating coronary heart disease and angina; however, the inventor finds that the traditional Chinese medicine composition has a good treatment effect on the hemorrhoids through research. Based on the above, the invention particularly provides a medicament containing nifedipine for treating hemorrhoids.

Furthermore, in the medicament for treating hemorrhoids of the invention, the main medicament can also comprise chemical medicament raw materials and/or traditional Chinese medicine raw materials for treating hemorrhoids.

In one embodiment, the chemical raw material is nitroglycerin, and the mass content of the nitroglycerin in the medicine is 0.1-0.3%, preferably 0.2%. Researches find that nitroglycerin and nifedipine have good synergistic effect on treating hemorrhoids, can obviously improve the cure rate of hemorrhoids, and simultaneously eliminate the side effect of nifedipine when treating hemorrhoids.

In one embodiment, the traditional Chinese medicine raw materials comprise the following components in parts by weight: 6-12 parts of garden burnet, 5-10 parts of sophora flower, 4-8 parts of dandelion, 1-5 parts of borneol, 3-6 parts of phellodendron and 2-4 parts of fig.

Preferably, the traditional Chinese medicine raw materials comprise the following components in parts by weight: 9 parts of garden burnet root, 8 parts of sophora flower, 6 parts of dandelion, 3 parts of borneol, 5 parts of phellodendron and 3 parts of fig.

The traditional Chinese medicine raw materials have the following effects:

garden burnet root: is dried root of Sanguisorba officinalis L. or Sanguisorba longata L. var. longifolia (Bert.) Yu et Li, which is Rosaceae plant. Has the effects of cooling blood, stopping bleeding, removing toxicity, healing sore, and the like, and is mainly used for hematochezia, hemorrhoidal bleeding, bloody dysentery, metrorrhagia and metrostaxis, water and fire scalds, carbuncle, swelling and sore toxicity.

And (3) flos sophorae: is dried flower and bud of Sophora japonica L.of Leguminosae, has effects of cooling blood, stopping bleeding, clearing liver-fire, etc., and can be used for treating hematochezia, hemorrhoidal bleeding, bloody dysentery, metrorrhagia, hematemesis, epistaxis, liver heat with conjunctival congestion, headache, and giddiness.

Dandelion: is dried whole plant of Taraxacum officinale Kitag of Compositae, Taraxacum alkanna Kitag or plants of the same genus. Bitter, sweet and cold. It is mainly used for furuncle, swelling and toxin, acute mastitis, scrofula, conjunctival congestion, pharyngalgia, pulmonary abscess, intestinal abscess, jaundice due to damp-heat pathogen, stranguria with heat and pain, etc.

Borneol: pungent, bitter and slightly cold in flavor; heart, liver and lung meridians entered; the product has effects of inducing resuscitation, refreshing mind, clearing heat, removing toxic substance, improving eyesight, and removing nebula, and can be used for treating fever, hyperpyrexia, coma, apoplexy, phlegm syncope, convulsion, summer-heat dampness covering resuscitation, pharyngitis, deafness, aphtha, swelling of teeth, skin ulcer, carbuncle, malnutritional hemorrhoid, conjunctival congestion, swelling and pain, nebula, and eye covering.

Phellodendron bark: is dried bark of phellandron chinensis schneid of Rutaceae. Has the effects of clearing heat, eliminating dampness, purging fire, removing steam, removing toxic substance, and treating sore; can be used for treating dysentery due to damp-heat pathogen, jaundice, dark urine, leukorrhagia, pudendal pruritus, pyretic stranguria, pain, tinea pedis, atrophic debility cramped, hectic fever, night sweat, nocturnal emission, pyocutaneous disease, toxic swelling, eczema, and eczema.

Fig: has the effects of clearing heat, promoting fluid production, invigorating spleen, stimulating appetite, removing toxic substance and relieving swelling. Can be used for treating swelling and pain of throat, cough, hoarseness, milk deficiency, constipation due to intestinal heat, anorexia, dyspepsia, diarrhea, dysentery, carbuncle, swelling, and tinea.

Furthermore, the mass content of the traditional Chinese medicine raw materials in the medicine can be 10-15%. The traditional Chinese medicine raw materials and the nifedipine have good synergistic effect on treating the hemorrhoids, can obviously improve the cure rate of the hemorrhoids, and simultaneously reduces the side effect of the nifedipine.

In the drug of the present invention, the matrix is not strictly limited, and an appropriate matrix can be selected depending on the dosage form; for example, when the pharmaceutical dosage form is an ointment, the base may be petrolatum, lanolin, polyethylene glycol, and the like.

The invention also provides a preparation method of the medicine, which comprises the following steps: mixing the main materials with matrix by grinding, dissolving or emulsifying.

Specifically, the developing method may include: grinding the main drug with a small amount of matrix into paste, adding the rest matrix, and grinding uniformly; the solution method may include: heating and melting the matrix, adding the main drug in several times, and continuously stirring until the mixture is condensed; the emulsification process may include: heating the oil-soluble substance to melt, dissolving the water-soluble substance in water, mixing, and continuously stirring until the mixture is condensed. An appropriate blending method can be selected according to the properties of the main drug.

In particular, the traditional Chinese medicine raw materials can be prepared into powder raw materials by stir-frying and crushing, and then are blended with the substrate; the parching process comprises parching with slow fire until the Chinese medicinal materials are dry or substantially dry, and pulverizing.

The medicine can effectively treat internal hemorrhoid, external hemorrhoid, mixed hemorrhoid, anal fistula, anal fissure, anal cyst and other hemorrhoid diseases, and has the advantages of short treatment course, quick response, good curative effect, difficult recurrence and the like.

Detailed Description

It should be noted that the following detailed description is exemplary and is intended to provide further explanation of the disclosure. Unless defined otherwise, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this application belongs.

It is noted that the terminology used herein is for the purpose of describing particular embodiments only and is not intended to be limiting of example embodiments according to the present application. As used herein, the singular forms also include the plural forms unless the context clearly dictates otherwise, and further, it is understood that when the terms "comprises" and/or "comprising" are used in this specification, they specify the presence of the stated features, steps, operations, devices, components, and/or combinations thereof.

The technical solutions of the present invention will be described clearly and completely with reference to the following embodiments, and it should be understood that the described embodiments are some, but not all, embodiments of the present invention. All other embodiments, which can be derived by a person skilled in the art from the embodiments given herein without making any creative effort, shall fall within the protection scope of the present invention.

Example 1

The nifedipine ointment of this example was prepared by blending 0.2g of nifedipine with 9.8g of vaseline.

Example 2

After 9.8g of polyethylene glycol is heated in water bath to be melted, 0.18g of nifedipine and 0.02g of nitroglycerin are added, stirred uniformly and cooled, thus obtaining the nifedipine compound ointment of the embodiment.

Example 3

Parching radix Sangusorbae, flos Sophorae Immaturus, herba Taraxaci, Borneolum Syntheticum, cortex Phellodendri, and fructus fici with slow fire, drying, and pulverizing to obtain powder; the powdery traditional Chinese medicine raw materials are uniformly mixed according to the proportion relation of 9 parts of garden burnet, 8 parts of sophora flower, 6 parts of dandelion, 3 parts of borneol, 5 parts of phellodendron and 3 parts of fig, and the traditional Chinese medicine main material is prepared.

0.1g of nifedipine, 1.4g of the main material of the traditional Chinese medicine and 8.5g of vaseline are evenly blended to obtain the nifedipine traditional Chinese medicine compound ointment of the embodiment.

Comparative example 1

3g of the main material of the traditional Chinese medicine in the embodiment 3 and 7g of vaseline are evenly blended to obtain the nifedipine traditional Chinese medicine compound ointment of the comparative example.

Test examples

Hemorrhoids were treated with the ointments of examples 1-3 and comparative examples 1-2 by: the ointment is applied to hemorrhoid area 2 times per day.

According to the evaluation criteria for hemorrhoid treatment effect, the diagnosis and treatment effect evaluation criteria for hemorrhoid are as follows:

diagnostic criteria: internal hemorrhoid with hematochezia, haemorrhoids prolapse, rectal mucosa congestion, ulcer, and anal discomfort; external hemorrhoid with anal distention, pain, pruritus and foreign body sensation; the mixed hemorrhoids are accompanied by the symptoms of both internal and external hemorrhoids.

The treatment effect evaluation standard is as follows:

the effect is shown: the symptoms of hematochezia, swelling and pain, prolapse, pus discharge, constipation, secretion, haemorrhoids prolapse and the like are completely disappeared;

the method has the following advantages: the times, degree and duration of the attack of symptoms such as hematochezia, swelling and pain, prolapse, pus, constipation, secretion, haemorrhoids prolapse and the like are obviously reduced or basically disappeared;

and (4) invalidation: the symptoms of internal hemorrhoid, external hemorrhoid and mixed hemorrhoid are not changed or all symptoms are aggravated.

The results of treatment of hemorrhoids are shown in Table 1.

TABLE 1 therapeutic results of the ointments on hemorrhoids

The results show that:

1. when the nifedipine ointment is used for treating hemorrhoids, the effect can be achieved within about one week, the total effective rate of treatment can reach 73.3%, and the treatment effect on the hemorrhoids is good; meanwhile, the recurrence rate of hemorrhoids treated by nifedipine ointment is 27.2%, and side effects such as mild headache exist in a few cases.

2. When the compound ointment of the nifedipine and the nitroglycerin is used for treating the hemorrhoids, the total treatment effective rate reaches 95 percent, the treatment effect is greatly improved compared with the nifedipine ointment, and the effective time is faster than that of the nifedipine ointment; in addition, the recurrence rate of the compound ointment is low, only 5.2%, and the side effect is also obviously reduced.

3. When the compound ointment of the nifedipine and the traditional Chinese medicine is used for treating the hemorrhoids, the effect can be achieved within one week, the total effective rate reaches 100%, the treatment effect is obviously improved compared with the nifedipine ointment and the traditional Chinese medicine ointment of the comparison example 1, and the compound ointment of the nifedipine and the traditional Chinese medicine ointment has no recurrence and other adverse side effects.

Finally, it should be noted that: the above embodiments are only used to illustrate the technical solution of the present invention, and not to limit the same; while the invention has been described in detail and with reference to the foregoing embodiments, it will be understood by those skilled in the art that: the technical solutions described in the foregoing embodiments may still be modified, or some or all of the technical features may be equivalently replaced; and the modifications or the substitutions do not make the essence of the corresponding technical solutions depart from the scope of the technical solutions of the embodiments of the present invention.