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US3890444A - Drug composition - Google Patents

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Publication number
US3890444A
US3890444A US354558A US35455873A US3890444A US 3890444 A US3890444 A US 3890444A US 354558 A US354558 A US 354558A US 35455873 A US35455873 A US 35455873A US 3890444 A US3890444 A US 3890444A
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Prior art keywords
propoxyphene
dextro
phenyl butazone
butazone
phenyl
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Expired - Lifetime
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US354558A
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Helmuth Wawretschek
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Servomed Arzneimittel GmbH
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Servomed Arzneimittel GmbH
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles

Definitions

  • the present invention relates to a drug compound antirheumatic and analgesic indication.
  • phenyl butazone (1,2-diphenyl- 3,5-dioxo-4-n-butyl-pyrazolidine) has analgesic and antirheumatic effects.
  • phenyl butazone was considered to be the most effective antirheumatic drug, apart from the steroids.
  • the administration of phenyl butazone in effective dosages is accompanied by serious side effects, caused by its inhibiting action on certain enzymatic reactions taking place in the body.
  • the objective underlying the present invention was therefore the discovery of a drug based on phenyl butazone which retains the known antirheumatic effects of phenyl butazone, while having a strong analgesic indication at reduced dosage, so that the known side effects are eliminated, or at least reduced.
  • mice In a series of writhing tests performed on mice it was found that especially favorable results are obtained with a drug compound in which dextro-propoxyphene and phenyl butazone are present in a molar ratio of l to 2. These results are reflected in a table given below in which some of the readings obtained in the tests are listed by way of example. The effectiveness of the different drug compounds is stated as a percentage in relation to the l to 2 molar ratio.
  • the extraordinary analgesic effects achieved are particularly evident in the category of post-traumatic conditions.
  • the treatment results obtained in other typical categories of the rheumatoid group indicates that the antirheumatic effects of phenyl butazone in the disclosed combination fully match previously observed effects of treatment with phenyl butazone in its known large dosage, even though its dosage in the disclosed combination is substantially reduced.
  • Drug composition having an antirheumatic and analgesic indication containing as active ingredients dextropropoxyphene and phenyl butazone in moleratio between 1 to l and l to 8.

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Drug composition having antirheumatic and analgesic indications containing as active ingredients dextro-propoxyphene and phenyl butazone, and treatment comprising administering as active ingredients dextro-propoxyphene and phenyl butazone.

Description

United States Patent 1 1 1111 3,890,444
Wawretschek June 17, 1975 [54] DRUG COMPOSITION 3,749,797 7/1973 Miller 424/308 [75] Inventor: Helmuth Wawretschek, Friesoythe, FOREIGN PATENTS OR APPLICATIONS Germany 1,081,105 8/1967 United Kingdom [73] Assignee: Servomed Arzneimittel Gmbl'l, OTHER PUBLICATIONS Oldenburg, Germany Filed: p 1973 Amer can Drug Index (I972) p. 174. pp 58 Primary Examiner--Stanley J. Friedman Attorney, Agent, or Firm-Robert R. Priddy; Burton [30] Foreign Application Priority Data Amermck 1' Apr. 26, 1972 Germany 2220500 [57] ABSTRACT I [52] US. Cl 424/273; 424/311 Drug composition having antirheumatic and analgesic [51] Int. Cl A6lk 27/00 indications containing as active ingredients dextro [58] Fleld of Search 424/273 propoxyphene and phenyl butazone and treatment comprising administering as active ingredients dextro- [56] References cued propoxyphene and phenyl butazone.
UNITED STATES PATENTS 6 Cl N D 3,482,021 12/1969 Gosling 424/273 'awmgs DRUG COMPOSITION t The present invention relates to a drug compound antirheumatic and analgesic indication.
It has been known, following the synthesis by H. Stenzel in 1946, that phenyl butazone (1,2-diphenyl- 3,5-dioxo-4-n-butyl-pyrazolidine) has analgesic and antirheumatic effects. Until the present time, phenyl butazone was considered to be the most effective antirheumatic drug, apart from the steroids. However, the administration of phenyl butazone in effective dosages is accompanied by serious side effects, caused by its inhibiting action on certain enzymatic reactions taking place in the body.
It is also known that these side effects can be avoided by using a combination of a reduced dosage of phenyl butazone with an analgesic.
From British Pat. No. 1,081,105 is known a drug which has anti-inflammatory and analgesic effects and which consists of a combination of butazone l-phenyl- 3,5-dioxo-4-n-butyl-butazolidine) and d-propoxyphene (1,2diphenyl-2-propionoxy-3-methyl-4- dimethylaminobutazone hydrochloride), the analgesic effect of the d-propoxyphene component being magnified through its combination with butazone. From this patent disclosure it is further known that this kind of magnification effect is not obtainable with combinations of phenyl butazone with propoxyphene, and that these combinations are therefore not suitable for medication. Yet, there has existed a long-standing basic need for such a combination, especially of phenyl butazone because of its very strong antirheumatic indication in comparison to butazone, with analgesic agents in which the magnifying characteristics would be present.
In the past, the magnifying effects of phenyl butazone have been obtained only in combination with such drugs as morphine, codeine, or methadone. However, these combinations have the drawback that they involve the risk of patient addiction, and for this reason they are not very desirable.
The objective underlying the present invention was therefore the discovery of a drug based on phenyl butazone which retains the known antirheumatic effects of phenyl butazone, while having a strong analgesic indication at reduced dosage, so that the known side effects are eliminated, or at least reduced.
In spite of the commonly held belief that combinations of phenyl butazone with propoxyphene are not suitable for medication purposes, the above objective has now been unexpectedly attained by the discovery of a drug compound consisting of phenyl butazone and dextro-propoxyphene.
The simultaneous administration of phenyl butazone and dextro-propoxyphene was found to produce an extraordinar'ily pronounced magnification of the analgesic-effects, in addition to a prolongation of the analgesia itself. It has thus become possible to make the therapeutic dosages of the active ingredients in the drug compound small enough to substantially eliminate the known side'effects. I
In the following the invention will be explained in more detail with reference to several embodiments.
In a series of writhing tests performed on mice it was found that especially favorable results are obtained with a drug compound in which dextro-propoxyphene and phenyl butazone are present in a molar ratio of l to 2. These results are reflected in a table given below in which some of the readings obtained in the tests are listed by way of example. The effectiveness of the different drug compounds is stated as a percentage in relation to the l to 2 molar ratio.
Table l Reciprocal values of ED values of various mixtures of dextro-propoxyphene-HCL with phenyl butazone, given as a percentage of the ED value of a mixture with a molar ratio of l to 2, which is equal to 100 percent (writhing test on mice):
Molar ratio: 45 min 90 min d-propoxyphene to phenyl butazone l to 16 57 l to 8 8l 7c 1 to 4 94 7c 97 l to 2 100 100 70 l to l 74 7b 98 7c tropropoxyphene with phenyl butazone when compared to dextropropoxyphene alone (A), produced an analgesia magnification of up to 4.2-fold, as shown by a comparison between the ED values of (A) and (B), taken 180 minutes after oral administration. The values which correspond to various other times elapsed are listed in Table 2 below:
Table 2 ED values obtained in writhing tests on mice, at times elapsed between 15 and 240 minutes after oral administration of compounds A, C, and B (values for B are computed from readings for C):
Compound 15 30 60 180 240 (A) dextro-propoxyphene 24 23 31 H (B) dextro-propoxyphene l3 1 1 I6 27 32 37 m mixture computed from (C) (C) mixture of dextro- 33 30 53 72 85 97 propoxyphene with phenyl butazone, molar ratio 1 to--2-- (D) phenyl butazone 350 360 390 650 650 900 ED, in mg per kg body weight duration in minutes 3 4 A magnification of effectiveness is evident and can Graph 1 also shows another interesting result with rebe computed from the ED values of Table 2. This spect to therapy: 37 mg of dextro-propoxyphenemagnification is illustrated in Graph I. hydrochloride in pure form are sufficient for an analge- G h I sia lasting approximately 70 minutes, whereas the same rap 5 dosage of dextro-propoxyphene in the mixture dis- Effectiveness magnification factor obtained through closed above assures an equally effective analgesia, mp n of 50 values of and in Table 2 even after 4 hours of elapsed time (see Graph II).
Magnification factor 5.-
l l l l I l I l l l i 15 so 120 1 240 4 minutes Graph ll D-Pro mixt e 1 v I a DProp.-HCL
l l 15 3O 60 v v 240 minute s Table 3 Number of very ineffec-- cases good good fair tive Degenerative spine syndromes, 197 49 1 I with or without radiculitis, I I 19 14 I such as: spondyl-arthrosis morbus Bechterew osteochondrosis HWS-syndrome, occipital syndrome, thoracic syndrome LWS-syndrome, lumbo-sacral syndrome discus prolapse Arthroses 44 9 24 9 2 Arthritides 2 31 l 1 Neuralgias, neuritis 46 14 24 5 I 3 Abdominal rheumatisms 22 8 l2 2 Periarthritides l4 5 5 2 2 Post-traumatic conditions 24 30 l Total 413 111 241 37 24 In 82.2 percent of these cases the results observed by the examining physicians were listed as either very good or good. The extraordinary analgesic effects achieved are particularly evident in the category of post-traumatic conditions. The treatment results obtained in other typical categories of the rheumatoid group indicates that the antirheumatic effects of phenyl butazone in the disclosed combination fully match previously observed effects of treatment with phenyl butazone in its known large dosage, even though its dosage in the disclosed combination is substantially reduced.
It has thus become possible to offer successful antirheumatic therapy, in spite of a reduction of the phenyl butazone dosage to one-third of its previously required dosage.
I claim:
1. Drug composition having an antirheumatic and analgesic indication containing as active ingredients dextropropoxyphene and phenyl butazone in moleratio between 1 to l and l to 8.
2. The drug composition of claim 1 wherein the mole ratio of dextro-propoxyphene to phenyl butazone is between 1 to l and 1 to 4.
3. The drug composition of claim 1 wherein the mole ratio of dextro-propoxyphene to phenyl butazone is l 4. The method of treating rheumatic disorder which

Claims (6)

1. Drug composition having an antirheumatic and analgesic indication containing as active ingredients dextropropoxyphene and phenyl butazone in mole ratio between 1 to 1 and 1 to 8.
2. The drug composition of claim 1 wherein the mole ratio of dextro-propoxyphene to phenyl butazone is between 1 to 1 and 1 to
3. The drug composition of claim 1 wherein the mole ratio of dextro-propoxyphene to phenyl butazone is 1 to 2.
4. THE METHOD OF TREATING RHEUMATIC DISORDER WHICH COMPRISES ADMINISTERING TO A PATIENT SUFERING FROM RHEUMATIC DISORDER AN EFFECTIVE ANTIRHEUMATIC AND ANALGESIC AMOUNT OF DEXTRO-PROPOXYPHENE AND PHENYL BUTAZONE IN MOLE RATIO BETWEEN 1 TO 1 AND 1 TO 8 AS ACTIVE INGREDIENTS.
5. The process of claim 4 wherein the mole ratio of dextro-propoxyphene to phenyl butazone is between 1 to 1 and 1 to 4.
6. The process of claim 4 wherein the mole ratio of dextro-propoxyphene to phenyl butazone is 1 to 2.
US354558A 1972-04-26 1973-04-26 Drug composition Expired - Lifetime US3890444A (en)

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DE2220500A DE2220500C3 (en) 1972-04-26 1972-04-26 analgesic

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US (1) US3890444A (en)
AT (1) AT331967B (en)
AU (1) AU5504873A (en)
BE (1) BE798758A (en)
CA (1) CA1014473A (en)
DD (1) DD102916A1 (en)
DE (1) DE2220500C3 (en)
FR (1) FR2182249B1 (en)
GB (1) GB1431661A (en)
LU (1) LU67498A1 (en)
NL (1) NL160487C (en)
ZA (1) ZA732847B (en)

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3482021A (en) * 1965-07-01 1969-12-02 Geigy Chem Corp Anti-phlogistic and analgesic compositions and methods for relieving inflammatory conditions
US3749797A (en) * 1971-07-02 1973-07-31 Lilly Co Eli Analgesic compositions

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3482021A (en) * 1965-07-01 1969-12-02 Geigy Chem Corp Anti-phlogistic and analgesic compositions and methods for relieving inflammatory conditions
US3749797A (en) * 1971-07-02 1973-07-31 Lilly Co Eli Analgesic compositions

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LU67498A1 (en) 1973-07-13
AU5504873A (en) 1974-11-07
DE2220500B2 (en) 1980-06-19
CA1014473A (en) 1977-07-26
GB1431661A (en) 1976-04-14
ZA732847B (en) 1974-03-27
ATA373873A (en) 1975-12-15
FR2182249B1 (en) 1976-07-02
AT331967B (en) 1976-09-10
NL160487C (en) 1979-11-15
DE2220500A1 (en) 1973-11-08
DD102916A1 (en) 1974-01-05
BE798758A (en) 1973-10-26
NL160487B (en) 1979-06-15
FR2182249A1 (en) 1973-12-07
NL7305850A (en) 1973-10-30
DE2220500C3 (en) 1981-02-26

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