CN102579569B - Pharmaceutical composition for treating piles as well as preparation method and application thereof - Google Patents

Pharmaceutical composition for treating piles as well as preparation method and application thereof Download PDF

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CN102579569B
CN102579569B CN 201210045447 CN201210045447A CN102579569B CN 102579569 B CN102579569 B CN 102579569B CN 201210045447 CN201210045447 CN 201210045447 CN 201210045447 A CN201210045447 A CN 201210045447A CN 102579569 B CN102579569 B CN 102579569B
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parts
pharmaceutical composition
hemorrhoid
treatment
hydrocortisone
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CN102579569A (en
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白蕊
卢克捷
张秀
孙冰
师桂英
何金哲
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BEIJING RECTUM HOSPITAL
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BEIJING RECTUM HOSPITAL
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Abstract

The invention provides a pharmaceutical composition for treating piles, which is a suppository. The invention also provides a preparation method and application of the pharmaceutical composition. The pharmaceutical composition is prepared from the following components in parts by weight: 80-120 parts of berberine hydrochloride, 7-20 parts of procaine hydrochloride, 1.5-4.2 parts of hydrocortisone, 7-18 parts of borneol, 3.5-6.5 parts of menthol and 1000 parts of fat-soluble matrix. The pharmaceutical composition can directly reach piles infected part through rectal administration, thus the side effect of enterohepatic circulation due to oral administration is reduced. The pharmaceutical composition for treating piles provided by the invention can be used for solving the defect that oral administration is slow in acting for diseases in intestine, can substitute for the traditional operative treatment, is convenient to use and does not damage organisms.

Description

A kind of pharmaceutical composition for the treatment of hemorrhoid and its preparation method and application
Technical field
The invention belongs to field of medicaments, relate to a kind of pharmaceutical composition for the treatment of hemorrhoid and its preparation method and application.
Background technology
Hemorrhoid are a kind of chronic diseases of the vein group of the venous plexus generation varicose of anal orifice and rectal intestine bottom and anal mucosa and one or more softnesses of forming.Usually continue to exert oneself when defecation, cause herein that intravenous pressure raises repeatedly, vein will enlargement.The women because pelvic veins suffers oppression, hinders blood circulation often hemorrhoid can occur in trimester of pregnancy, and the people of many obesities also can suffer from hemorrhoid.If suffer from hemorrhoid, the wall of vein of anal enlargement distortion will become very thin, so very easily breaks during defecation.Internal hemorrhoid is long hemorrhoid at the anus catheter section start, if the vein that expands is positioned at more below, almost is on the anal canal mouth, and the vein of this varicose just is external hemorrhoid.External hemorrhoid is deviate from sometimes or is appeared suddenly outside the anal canal mouth.But this situation only just can occur when defecation, its original position of can retracting again behind the defecation.No matter thrombosis all may occur in internal hemorrhoid or external hemorrhoid.When thrombosis occurs, the blood clotting in bulk in the hemorrhoid, thus cause pain.
The method for the treatment of hemorrhoid is a lot, the multiplex operation of traditional remedies, drug injection, ligation, laser, radio frequency, freezing etc., but the oral medicine onset is slow, and the means such as operation have increased patient's distress level, this shows that prior art needs further improvement and develops.
Summary of the invention
For overcoming defects, the object of the present invention is to provide a kind of pharmaceutical composition for the treatment of hemorrhoid, its composition by following weight portion is made: 80~120 parts of berberine hydrochloride, 7~20 parts of procaine hydrochlorides, 1.5~4.2 parts of hydrocortisone, 7~18 parts of Borneolum Syntheticums, 3.5~6.5 parts of Mentholums, fat-soluble substrate complement to 1000 parts.
Preferably, described pharmaceutical composition is made by the composition of following weight portion: 90~110 parts of berberine hydrochloride, 9~11 parts of procaine hydrochlorides, 1.8~2.2 parts of hydrocortisone, 9~11 parts of Borneolum Syntheticums, 4.5~5.5 parts of Mentholums, fat-soluble substrate complement to 1000 parts.
More preferably, described pharmaceutical composition is made by the composition of following weight portion: 105 parts of berberine hydrochloride, 10 parts of procaine hydrochlorides, 2.0 parts of hydrocortisone, 10 parts of Borneolum Syntheticums, 5 parts of Mentholums, fat-soluble substrate complement to 1000 parts.
Described fat-soluble substrate is fat-soluble suppository substrate; Described fat-soluble suppository substrate is one or both in semi-synthetic fatty acid ester or the glycerin gelatine.
Described pharmaceutical composition provided by the invention is suppository.
The present invention also provides a kind of method for preparing aforementioned pharmaceutical compositions, and the method comprises the steps:
1) the coarse powder raw medicinal material of berberine hydrochloride, procaine hydrochloride, Borneolum Syntheticum, Mentholum is ground into respectively behind the fine powder for subsequent use;
2) substrate is melted, temperature is controlled at 50~60 ℃, adds fine powder after the above-mentioned pulverizing, adds load weighted hydrocortisone in above-mentioned prescription ratio, and stirring and evenly mixing cools off.
Described step 2) temperature of cooling off behind the stirring and evenly mixing in is 10~15 ℃.
Described step 2) the fine powder fineness in is 40~400 orders.
The present invention also provides the application of described pharmaceutical composition in the medicine of preparation treatment hemorrhoid.
Weight portion of the present invention can be the known unit of weights of field of medicaments such as μ g, mg, g, kg.
Berberine hydrochloride claims again berberine, is present in many plants of 4 sections, 10 genus such as Berberidaceae.Be a kind of isoquinoline alkaloid, its molecular formula is C 20H 18NO 4, it has inhibitory action to dysentery bacterium, escherichia coli, Diplococcus pneumoniae, golden Portugal bacterium, streptococcus, Bacillus typhi and ameba.Clinical intestinal infection and the bacillary dysentery etc. of being mainly used in.Recently find also that this product has the antiarrhythmic effect.
Procaine hydrochloride is white crystals or crystalline powder; Odorless, mildly bitter flavor has the paralysis sense subsequently.This product is easily molten in water, and is slightly molten in ethanol, and slightly soluble in chloroform is almost insoluble in ether, is mainly used in local anaesthesia.
Hydrocortisone has another name called hydrocortisone, and it is natural fugitive Aeroseb-Dex.Antiinflammatory action and immunosuppressant, antitoxin, Antishock function are arranged, be used for the treatment of various adrenal hyperplasia disease and some inflammation disease due to shock that adrenocortical insufficiency, severe infections, autoimmune disease, anaphylactic disease, a variety of causes cause, disease in the blood system, the hormone dyssynthesis.
Borneolum Syntheticum has another name called sheet brain, Fructus Citri tangerinae sheet, Borneolum Syntheticum, MEIHUA BINGPIAN, Dipterocarpus pilosus, Flos Mume brain, Borneolum Syntheticum brain, Mei Bing etc., is that resin and the volatile oil processed goods of Spore density Borneolum Syntheticum extracts the crystallization that obtains, and is near pure dextro Borneolum Syntheticum.Also useful chemical method is synthetic.It can be used for for the excess syndrome of stroke coma, is used for conjunctival congestion and swelling pain, the sore throat aphtha, is used for skin infection and swells and ache, and does not hold back after bursting etc.
Mentholum system by in the leaf of Herba Menthae and the stem extract white crystal, molecular formula C 10H 20O is the main component in Herba Menthae and the lavender quintessence oil.In the world, China and Brazil is main natural Herba Menthae manufacturing country, and the annual production of Oleum menthae all reaches 2000-3000t.Mentholum and racementhol all can be used as toothpaste; Perfume; The odorant of beverage and confection etc.As excitants, act on skin or mucosa pharmaceutically, refrigerant itching-relieving action is arranged; The carminative that can be used as for oral administration is used for headache and nose; Pharynx; Laryngitis etc.
The inventor finds by a large amount of research, berberine hydrochloride, procaine hydrochloride, hydrocortisone, Borneolum Syntheticum, Mentholum are made up when making suppository and being applied to the treatment of hemorrhoid according to a certain ratio, effect with obvious hemostasis, reducing swelling and alleviating pain, loosening bowel to relieve constipation, demonstrated unforeseeable effect, greatly brought into play the synergism between them, effective percentage has reached 100%.
The pharmaceutical composition for the treatment of hemorrhoid provided by the invention is suppository, can treat internal hemorrhoid, external hemorrhoid, mixed hemorrhoid etc.The pharmaceutical composition of described treatment hemorrhoid is the compound preparation of Chinese medicine and western medicine compatibility combination.To be obtained by a large amount of experiments by the inventor, it reduces the side effect that the circulation of oral administration liver sausage absorbs by the rectally hemorrhoid affected part of can going directly, and has solved the slow defective of the general oral medicine onset of enteral illness, alternative traditional operation therapy, and easy to use, do not decrease body.
And have antiinflammatory, detumescence, pain relieving, heat clearing away, antianaphylactic effect.Be used for the treatment of all kinds of hemorrhoid, have the advantages such as evident in efficacy, easy to use, that onset rapid, safety is painless.Effective percentage reaches 100%.
The preparation method of the described pharmaceutical composition of preparation provided by the invention has raw material and obtains easily simple operation and other advantages.
The specific embodiment
Following examples are used for explanation the present invention, but are not used for limiting the scope of the invention.
Embodiment 1: the suppository for the treatment of hemorrhoid
1, prescription: berberine hydrochloride 105g, procaine hydrochloride 10g, hydrocortisone 2.0g, Borneolum Syntheticum 10g, Mentholum 5g, glycerin gelatine complement to 1000g.
2, preparation method
Be ground into respectively behind the fine powder coarse powder raw medicinal material of the berberine hydrochloride of above-mentioned recipe quantity, procaine hydrochloride, Borneolum Syntheticum, Mentholum for subsequent use, described fine powder is crossed 300 mesh sieves, substrate is melted under 55 ℃, add fine powder after the above-mentioned pulverizing, add load weighted hydrocortisone in the prescription ratio, stirring and evenly mixing is annotated in suppository production equipment bucket, cool off, chilling temperature is controlled to be 12 ℃, and get final product.
Embodiment 2: the suppository for the treatment of hemorrhoid
1, prescription: berberine hydrochloride berberine hydrochloride 80g, procaine hydrochloride 6g, hydrocortisone 1.5g, Borneolum Syntheticum 7g, Mentholum 3.5g, semi-synthetic fatty acid ester complements to 1000g.
2, preparation method
Be ground into respectively behind the fine powder coarse powder raw medicinal material of the berberine hydrochloride of above-mentioned recipe quantity, procaine hydrochloride, Borneolum Syntheticum, Mentholum for subsequent use, described fine powder is crossed 40 mesh sieves, substrate is melted under 50 ℃, add fine powder after the above-mentioned pulverizing, add load weighted hydrocortisone in the prescription ratio, stirring and evenly mixing is annotated in suppository production equipment bucket, cool off, chilling temperature is controlled to be 10 ℃, and get final product.
Embodiment 3: the suppository for the treatment of hemorrhoid
1, prescription: berberine hydrochloride berberine hydrochloride 120g, procaine hydrochloride 20g, hydrocortisone 4.2g, Borneolum Syntheticum 18g, Mentholum 6.5g, semi-synthetic fatty acid ester complements to 1000g.。
2, preparation method
Be ground into respectively behind the fine powder coarse powder raw medicinal material of the berberine hydrochloride of above-mentioned recipe quantity, procaine hydrochloride, Borneolum Syntheticum, Mentholum for subsequent use, described fine powder is crossed 400 mesh sieves, substrate is melted under 60 ℃, add fine powder after the above-mentioned pulverizing, add load weighted hydrocortisone in the prescription ratio, stirring and evenly mixing is annotated in suppository production equipment bucket, cool off, chilling temperature is controlled to be 15 ℃, and get final product.
Embodiment 4: the suppository for the treatment of hemorrhoid
1, prescription: berberine hydrochloride berberine hydrochloride 90g, procaine hydrochloride 9g, hydrocortisone 108g, Borneolum Syntheticum 9g, Mentholum 4.5g, semi-synthetic fatty acid ester 300g, glycerin gelatine complements to 1000g.
2, preparation method
Be ground into respectively behind the fine powder coarse powder raw medicinal material of the berberine hydrochloride of above-mentioned recipe quantity, procaine hydrochloride, Borneolum Syntheticum, Mentholum for subsequent use, described fine powder is crossed 100 mesh sieves, substrate is melted under 60 ℃, add fine powder after the above-mentioned pulverizing, add load weighted hydrocortisone in the prescription ratio, stirring and evenly mixing is annotated in suppository production equipment bucket, cool off, chilling temperature is controlled to be 13 ℃, and get final product.
Embodiment 5: the suppository for the treatment of hemorrhoid
1, prescription: berberine hydrochloride berberine hydrochloride 110, procaine hydrochloride 11g, hydrocortisone 2.2g, Borneolum Syntheticum 11g, Mentholum 5.5g, glycerin gelatine complements to 1000g.
2, preparation method
Be ground into respectively behind the fine powder coarse powder raw medicinal material of the berberine hydrochloride of above-mentioned recipe quantity, procaine hydrochloride, Borneolum Syntheticum, Mentholum for subsequent use, described fine powder is crossed 200 mesh sieves, substrate is melted under 60 ℃, add fine powder after the above-mentioned pulverizing, add load weighted hydrocortisone in the prescription ratio, stirring and evenly mixing is annotated in suppository production equipment bucket, cool off, chilling temperature is controlled to be 13 ℃, and get final product.
Comparative example 1: the suppository for the treatment of hemorrhoid
1, prescription: berberine hydrochloride berberine hydrochloride 105g, procaine hydrochloride 10g, glycerin gelatine complement to 1000g.
2, preparation method
Be ground into respectively behind the fine powder coarse powder raw medicinal material of the berberine hydrochloride of above-mentioned recipe quantity, procaine hydrochloride, Borneolum Syntheticum, Mentholum for subsequent use, described fine powder is crossed 200 mesh sieves, substrate is melted under 60 ℃, add fine powder after the above-mentioned pulverizing, add load weighted hydrocortisone in the prescription ratio, stirring and evenly mixing is annotated in suppository production equipment bucket, cool off, chilling temperature is controlled to be 11 ℃, and get final product.
Clinical experiment
1, clinical data:
Filter out 180 routine cases, be divided at random two groups, treatment group and matched group.
Treatment group: the suppository that is made by the prescription among the embodiment 1 and preparation method.
Matched group: the suppository that is made by the prescription in the comparative example 1 and preparation method.
Treatment group is 105 examples, and matched group is 75 examples.
Include the case standard in:
A. Clear consciousness, patient that can the clear expression operating position;
B. the age is at 18-65 between year;
C. the patient knows the inside story and agrees.
The Excluded cases standard:
A. the enteropathy patient who merges malignant tumor;
B. suffers from serious skin disease patient;
C. can't take care of oneself, the slurred speech patient.
The standard of curative effect evaluation:
(version in 2006) efficacy evaluation is as the criterion execution by " up-to-date hospital clinical medical diagnosis on disease foundation and healing improvement manual of standards ".
1. produce effects: patient's proctalgia disappears, edema extinction, and blood stasis disappears or retraction, hemostasis, wound healing.
2. effective: patient's proctalgia alleviates, and edema alleviates, and blood stasis slightly diminishes, and bleeding alleviates.
3. invalid: above-mentioned symptom is without improvement after the treatment.
2, test method
1. treatment group: the suppository according to the method for embodiment 1 prepares, touch the place into anal 1-2cm every day, 1 time on the one, 1 1-2 grain is used in conjunction 7-14 days.
2. matched group: the suppository according to the method for examination comparative example 1 prepares, touch the place into anal 1-2cm every day, 1 time on the one, 1 1-2 grain is used in conjunction 7-14 days.
3, result of the test
Treatment group and matched group Comparison of therapeutic see Table 1, table 2, table 3.
Table 1 treatment group experimental result
Hemorrhoid symptom Example number (n) Obvious effective rate % Example number (n) Effective percentage % Example number (n) Inefficiency % Example number (n) Total effective rate %
All kinds of pain due to hemorrhoids 35 85.7% 30 14.3% 5 0 0 100%
All kinds of bleeding hemorrhoidss 25 76% 19 24% 6 0 0 100%
All kinds of hemorrhoid edema 20 85% 17 15% 3 0 0 100%
Blood stasis disappears 25 72% 18 28% 7 0 0 100%
Table 2 matched group experimental result
Hemorrhoid symptom Example number (n) Obvious effective rate % Example number (n) Effective percentage % Example number (n) Inefficiency % Example number (n) Total effective rate %
All kinds of pain due to hemorrhoids 20 50% 10 50% 10 0 0 100%
All kinds of bleeding hemorrhoidss 15 46.7% 7 53.3% 8 0 0 100%
All kinds of hemorrhoid edema 18 27.8% 5 27.8% 5 16.7% 3 55.6%%
Blood stasis disappears 22 22.7% 5 4.5% 1 72.7% 16 27.3%
Table 3 liang group curative effect comparative result
Group Effectively (n) Invalid (n) Total effective rate (%) Amount to (n)
Treatment group 105 0 100% 105
Matched group 56 19 74.7% 75
Conclusion: shown in table 1, table 2, table 3, treatment group and matched group are in treatment hemorrhoid edema and reduce in the total effective rate on the blood stasis notable difference is arranged, and from clinical observation, treatment group is at hemostasis, short wound healing, antiallergic, detumescence, and all obviously be better than matched group on patient's comfort.
Although, above used general explanation, the specific embodiment and test, the present invention is described in detail, on basis of the present invention, can make some modifications or improvement to it, and this will be apparent to those skilled in the art.Therefore, these modifications or improvements all belong to the scope of protection of present invention without departing from theon the basis of the spirit of the present invention.

Claims (9)

1. pharmaceutical composition for the treatment of hemorrhoid, it is characterized in that its composition by following weight portion is made: 80~120 parts of berberine hydrochloride, 7~20 parts of procaine hydrochlorides, 1.5~4.2 parts of hydrocortisone, 7~18 parts of Borneolum Syntheticums, 3.5~6.5 parts of Mentholums, fat-soluble substrate complement to 1000 parts.
2. the pharmaceutical composition for the treatment of hemorrhoid according to claim 1, it is characterized in that its composition by following weight portion is made: 90~110 parts of berberine hydrochloride, 9~11 parts of procaine hydrochlorides, 1.8~2.2 parts of hydrocortisone, 9~11 parts of Borneolum Syntheticums, 4.5~5.5 parts of Mentholums, fat-soluble substrate complement to 1000 parts.
3. the pharmaceutical composition for the treatment of hemorrhoid according to claim 1, it is characterized in that its composition by following weight portion is made: 105 parts of berberine hydrochloride, 10 parts of procaine hydrochlorides, 2.0 parts of hydrocortisone, 10 parts of Borneolum Syntheticums, 5 parts of Mentholums, fat-soluble substrate complement to 1000 parts.
4. the pharmaceutical composition for the treatment of hemorrhoid according to claim 3 is characterized in that, described fat-soluble substrate is one or both in semi-synthetic fatty acid ester or the glycerin gelatine.
5. the pharmaceutical composition of each described treatment hemorrhoid is characterized in that according to claim 1-4, and this pharmaceutical composition is suppository.
6. method for preparing the pharmaceutical composition of each described treatment hemorrhoid among the claim 1-5, the method comprises the steps:
1) the coarse powder raw medicinal material of berberine hydrochloride, procaine hydrochloride, Borneolum Syntheticum, Mentholum is ground into respectively behind the fine powder for subsequent use;
2) substrate is melted, temperature is controlled at 50~60 ℃, adds fine powder after the above-mentioned pulverizing, adds load weighted hydrocortisone in above-mentioned prescription ratio, and stirring and evenly mixing cools off.
7. method according to claim 6 is characterized in that, the fineness of described fine powder is 40~400 orders.
8. method according to claim 6 is characterized in that, described step 2) in the temperature cooled off behind the stirring and evenly mixing be 10~15 ℃.
9. the application of each described compositions in the medicine of preparation treatment hemorrhoid among the claim 1-5.
CN 201210045447 2012-02-24 2012-02-24 Pharmaceutical composition for treating piles as well as preparation method and application thereof Active CN102579569B (en)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106581020A (en) * 2015-10-14 2017-04-26 深圳澳美制药技术开发有限公司 Pharmaceutical composition and preparation method thereof, and hemorrhoid treating medicine

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1579499A (en) * 2004-05-20 2005-02-16 瞿伟 Medicine for treating piles
CN101138592A (en) * 2006-09-08 2008-03-12 海南优方科技有限公司 Preparation method for treating internal hemorrhoid and Chinese medicine suppository thereof
CN101628045A (en) * 2009-04-30 2010-01-20 北京荣昌药物研究院有限公司 Medicine for treating hemorrhoids and preparation method thereof

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1579499A (en) * 2004-05-20 2005-02-16 瞿伟 Medicine for treating piles
CN101138592A (en) * 2006-09-08 2008-03-12 海南优方科技有限公司 Preparation method for treating internal hemorrhoid and Chinese medicine suppository thereof
CN101628045A (en) * 2009-04-30 2010-01-20 北京荣昌药物研究院有限公司 Medicine for treating hemorrhoids and preparation method thereof

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