CN1049102A - Pharmaceutical preparations and preparation method thereof - Google Patents
Pharmaceutical preparations and preparation method thereof Download PDFInfo
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- CN1049102A CN1049102A CN 90106613 CN90106613A CN1049102A CN 1049102 A CN1049102 A CN 1049102A CN 90106613 CN90106613 CN 90106613 CN 90106613 A CN90106613 A CN 90106613A CN 1049102 A CN1049102 A CN 1049102A
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- pharmaceutical preparation
- podophyllotoxin
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- treatment
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Abstract
The present invention relates to a kind of new medicinal preparation that is used for the treatment of psoriasis and condyloma acuminatum and preparation method thereof, comprise Gui poison is mixed mutually with liquid triglycerides.
Description
The present invention relates to can be used for treating the pharmaceutical preparations of psoriasis and condyloma acuminatum, mainly is the medicament of cream forms, wherein contains podophyllotoxin as active component.The present invention also relates to this preparation is made the emulsifiable paste that is used for the treatment of psoriasis and condyloma acuminatum.
EP-B1-119 852 discloses a kind of podophyllotoxin preparation that is used for the treatment of condyloma acuminatum.These preparations contain podophyllotoxin and at least a dihydroxylic alcohols that is selected from aklylene glycol and poly alkylene glycol.
US-A-4,788,216 disclose the psoriasic method of a kind of treatment, are to carry out administration with podophyllotoxin.Wherein mention the form that can adopt emulsifiable paste, but do not provide concrete medicament.
Existing podophyllotoxin medicament drug effect and stable aspect need be improved.And this improvement is achieved by the present invention.
The purpose of this invention is to provide a kind of preparation that is used for the treatment of psoriasis and condyloma acuminatum with good clinical effectiveness and stability.
According to the present invention, find that unexpectedly the compositions that podophyllotoxin and one or more triglyceride are formed can form stable formulation, it has good curative effect to psoriasis and condyloma acuminatum, and side effect is very little.This preparation is emulsifiable paste or ointment form preferably, wherein together emulsifying of triglyceride and water.
When being used for the treatment of psoriasis, said preparation should contain 0.02-1%(weight) podophyllotoxin, better contain 0.05-0.5%(weight) podophyllotoxin, and preferably contain about 0.1%(weight) podophyllotoxin.Because of needing the very long cycle usually in the treatment psoriasis, it is very important keeping the podophyllotoxin of low concentration, to avoid undesirable side effect.
In this description and claims, except as otherwise noted, all percents all are percetages by weight, and all the gross weight with preparation is a benchmark.
When being used for the treatment of condyloma acuminatum, said preparation should contain 0.02-1%(weight) podophyllotoxin, be preferably contain 0.15-0.5%(weight) podophyllotoxin, preferably contain about 0.3%(weight) podophyllotoxin.
Described preparation contains 3-15%(weight usually) one or more triglyceride, preferably contain about 10%(weight).Preferably has the medium chain liquid triglycerides of (each strand contains 6-14 carbon atom), preferably the triglyceride of suffering/capric acid (fractionated Oleum Cocois).A kind of these commercially available class fractionated coconut oil commodity are called Miglyol.
Except podophyllotoxin and one or more liquid triglycerides, described preparation also contains 50-85%(weight) water, and auxiliary substance, as emulsifying agent, spreading agent, antiseptic, antioxidant and maintenance pH are in the buffer agent of given level.Be used for the treatment of psoriasic preparation and also can contain dihydroxylic alcohols or polyhydric alcohol.
The emulsifying agent that is suitable for comprises the product that following row trade name is sold, Eumlsifier E 2155(Polyethylene Glycol (7) stearyl ether, Polyethylene Glycol (10) stearyl ether and octadecanol), Brij 72(Polyethylene Glycol (2) stearyl ether), Brij 721(Polyethylene Glycol (21) stearyl ether), Arlatone 983 s(Polyethylene Glycol (5) tristerins) and Arlacel 582(Polyethylene Glycol-glycerol-isostearic acid Isosorbide Dinitrate).Certainly be not limited to above-mentionedly enumerate these.Other nonionic emulsifier with similar HLB value (hydrophile-lipophile balance value) also can adopt.The consumption of emulsifying agent is can obtain required emulsifying effectiveness degree of being.Those of ordinary skill in the art just can determine this consumption at an easy rate by simple routine experimentation, and according to the concrete emulsification system that is adopted, the consumption of emulsifying agent is generally between 3-10%(weight) between, this value is not critical.
The effect of spreading agent is to help it to sprawl when preparation being coated onto on skin or the mucosa.A kind of known this class reagent is isopropyl myristate, and other similar agents also is known to those skilled in the art.The consumption of spreading agent can reach about 5%(weight).
Antiseptic and antioxidant are to be used for stablizing said preparation, prevent deleterious external action, as microorganism and oxygen.The antiseptic that is suitable for comprises methyl butex (4-methyl hydroxybenzoate), propylparaben (4-nipasol) and sorbic acid.The consumption of antiseptic can reach about 0.5%(weight usually), preferably be no more than 0.2%(weight).The antioxidant that is suitable for comprises tert-butyl group hydroxyanisol, tert-butyl group hydroxy-methylbenzene, and ascorbic acid and derivant thereof are as ascorbic palmitate.But other suitable antioxidant is also known by the ability technical staff.The consumption of antioxidant seldom is no more than 0.2%(weight usually).
Avoid it that chemical change takes place in order to stablize podophyllotoxin, the pH value of described preparation should be in acidic region, usually between 2-6, is preferably between the 2.6-3.5.Realize this requirement by adding suitable acid or sour buffer agent (as phosphoric acid).Other acid or sour buffer agent that is suitable for also is well known to those skilled in the art.Self-evident, used acid or sour buffer agent must be medicinal acceptable.The consumption of above-mentioned acid or sour buffer agent should make final preparation reach required pH value.
This area other additives known commonly used also can be used in preparation of the present invention.
Above-mentioned preparation is the affected part that topical arrives the psoriatic.When being used for the treatment of condyloma acuminatum, said preparation is part, vagina (tunica vaginalis of testis) or anum administration.Consumption and frequency of administration are decided according to patient's age, health status, distress level and other factor by the doctor.
In clinical trial, prove that pharmaceutical preparation of the present invention has higher activity, does not have or few side effects simultaneously.
For the masculinity and femininity patient who suffers from condyloma acuminatum, Most patients only just can heal entirely through the topical therapeutic of several weeks.In addition, adopt emulsifiable paste of the present invention can reduce treatment cycle.Compare with placebo, the statistics difference is very significant (P=＜0.05).
In treatment psoriasis process, patient's topical application every day with desquamation and scleroma symptom takes an evident turn for the better after several weeks for twice.Each patient all treats in its specific affected part, and other untreated position in contrast.After only around the treatment, emulsifiable paste of the present invention is compared with placebo and is demonstrated excellent effect.This effect says it is very significant (P=＜0.05) from the statistics angle.
In both cases, only observe minimum side effect.
Following example further specifies the present invention, wherein provides some preparations of the present invention.These examples are not construed as limiting the scope of the invention.
In the following emulsifiable paste process of preparation, water and fat are to mix respectively separately and heat mutually.Then water is added to fat mutually in, then add the active component that is suspended in one or more liquid triglycerides.With this mixture homogenization, stir and cooling, obtain required emulsifiable paste.
Example 1 is used for the treatment of the emulsifiable paste of condyloma acuminatum
The fat restriction or checking relation in five elements
Emulgator E-2155 8
Hexadecanol 2
Octadecanol 2
Isopropyl myristate 2
Liquid paraffin 3
Fractionated coconut oil 10
Butylated hydroxyanisole (BHA) 0.008
Water
Water 72.34
Methyl butex 0.10
Propylparaben 0.03
Phosphatase 11 M 0.1
Sorbic acid 0.12
Active component
Podophyllotoxin 0.3
Example 2 is used for the treatment of psoriasic emulsifiable paste
The fat restriction or checking relation in five elements
Protegin WX 22
Fractionated coconut oil 10
Isopropyl myristate 3
Water
Water 59.05
Methyl butex 0.10
Propylparaben 0.03
Propylene glycol 5
Phosphatase 11 M 0.1
MgSO
4·7H
2O 0.5
Sorbic acid 0.12
Active component
Podophyllotoxin 0.1
Protegin WX is the emulsification preparation that is used for emulsifiable paste, and it is the mixture of vaseline, ceresine, castor oil hydrogenated, glyceryl oleate, polyglycereol (4) stearate and tert-butyl group hydroxy-methylbenzene.
Example 3
The fat restriction or checking relation in five elements
Emulsifier W-2155 8
Hexadecanol 2
Octadecanol 2
Fractionated coconut oil 15
Liquid paraffin 2
Butylated hydroxyanisole (BHA) 0.008
Water
Water 69.64
Methyl butex 0.10
Propylparaben 0.03
Phosphatase 11 M 0.1
Sorbic acid 0.12
Active component
Podophyllotoxin 1
Example 4
The fat restriction or checking relation in five elements
Brij 72 3
Brij 721 2
Hexadecanol 2
Stearic acid 1.5
Fractionated coconut oil 9
Butylated hydroxyanisole (BHA) 0.008
Water
Water 81.64
Methyl butex 0.10
Propylparaben 0.03
Phosphatase 11 M 0.1
Sorbic acid 0.12
Active component
Podophyllotoxin 0.5
Example 5 is used for the treatment of the emulsifiable paste of condyloma acuminatum
The fat restriction or checking relation in five elements
Arlatone 983 S 5
Hexadecanol 2
Stearic acid 1.5
Fractionated coconut oil 3
Liquid paraffin 2
Butylated hydroxyanisole (BHA) 0.008
Water
Water 82.10
Methyl butex 0.10
Propylparaben 0.03
Phosphatase 11 M 0.1
Propylene glycol 4
Sorbic acid 0.12
Active component
Podophyllotoxin 0.04
Example 6
The fat restriction or checking relation in five elements
Arlacel 582 10
Isopropyl myristate 3
Liquid paraffin 10
Fractionated coconut oil 12
Butylated hydroxyanisole (BHA) 0.008
Water
Water 59.89
Propylene glycol 4
MgSO
4·7H
2O 0.5
Phosphatase 11 M 0.1
Methyl butex 0.10
Propylparaben 0.03
Sorbic acid 0.12
Active component
Podophyllotoxin 0.25
Claims (12)
1, a kind of pharmaceutical preparation that contains podophyllotoxin is characterized in that described podophyllotoxin is to be suspended in the liquid triglycerides.
2, by the pharmaceutical preparation of claim 1, it is characterized in that it is the form of emulsifiable paste, wherein triglyceride and water are together emulsified.
3, by the pharmaceutical preparation of claim 1 or 2, it has medium chain to it is characterized in that this liquid triglycerides, and each strand contains 6-14 carbon atom.
4, by each pharmaceutical preparation of claim 1-3, it is characterized in that its pH value is 2-6, be preferably 2.6-3.5.
5, by each pharmaceutical preparation of claim 1-4, be used for the treatment of psoriasis.
6,, it is characterized in that it contains 0.02-1%(weight by the pharmaceutical preparation of claim 5), best 0.05-0.5%(weight) podophyllotoxin, and 3-15%(weight) one or more liquid triglycerides.
7,, it is characterized in that it contains 0.1%(weight by the pharmaceutical preparation of claim 6) podophyllotoxin and 10%(weight) fractionated coconut oil.
8, by each pharmaceutical preparation of claim 1-4, be used for the treatment of condyloma acuminatum.
9,, it is characterized in that it contains 0.01-1%(weight by the pharmaceutical preparation of claim 8), best 0.15-0.5%(weight) one or more liquid triglycerides.
10,, it is characterized in that it contains 0.3%(weight by the pharmaceutical preparation of claim 9) podophyllotoxin and 10%(weight) fractionated coconut oil.
11,, it is characterized in that it contains to be no more than 0.2%(weight by each pharmaceutical preparation of claim 1-10) antioxidant.
12, the method for the described pharmaceutical preparation of the above-mentioned arbitrary claim of preparation comprises various components is mixed by a certain percentage mutually.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CH262489 | 1989-07-31 | ||
| SE89026249 | 1989-07-31 | ||
| CH8902624-9 | 1989-07-31 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1049102A true CN1049102A (en) | 1991-02-13 |
| CN1042298C CN1042298C (en) | 1999-03-03 |
Family
ID=4237948
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 90106613 Expired - Lifetime CN1042298C (en) | 1989-07-31 | 1990-07-30 | Pharmaceutical preparations and process for preparing same |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1042298C (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100427082C (en) * | 2005-08-02 | 2008-10-22 | 盛华（广州）医药科技有限公司 | Application of hydroxybenzoate acid and its analogue in the preparing process of medicine for preventing and treating virus infection |
| CN103596528A (en) * | 2011-06-09 | 2014-02-19 | 保罗·哈特曼公司 | Wound dressing containing a non-woven and an ointment base for negative pressure therapy |
-
1990
- 1990-07-30 CN CN 90106613 patent/CN1042298C/en not_active Expired - Lifetime
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100427082C (en) * | 2005-08-02 | 2008-10-22 | 盛华（广州）医药科技有限公司 | Application of hydroxybenzoate acid and its analogue in the preparing process of medicine for preventing and treating virus infection |
| CN103596528A (en) * | 2011-06-09 | 2014-02-19 | 保罗·哈特曼公司 | Wound dressing containing a non-woven and an ointment base for negative pressure therapy |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1042298C (en) | 1999-03-03 |
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| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| C15 | Extension of patent right duration from 15 to 20 years for appl. with date before 31.12.1992 and still valid on 11.12.2001 (patent law change 1993) | ||
| OR01 | Other related matters | ||
| C17 | Cessation of patent right | ||
| CX01 | Expiry of patent term |
Granted publication date: 19990303 |