CH653890A5 - PHARMACEUTICAL COMPOSITIONS WITH ANTINEOPLASTIC ACTIVITY. - Google Patents
PHARMACEUTICAL COMPOSITIONS WITH ANTINEOPLASTIC ACTIVITY. Download PDFInfo
- Publication number
- CH653890A5 CH653890A5 CH2772/83A CH277283A CH653890A5 CH 653890 A5 CH653890 A5 CH 653890A5 CH 2772/83 A CH2772/83 A CH 2772/83A CH 277283 A CH277283 A CH 277283A CH 653890 A5 CH653890 A5 CH 653890A5
- Authority
- CH
- Switzerland
- Prior art keywords
- pharmaceutical compositions
- compositions according
- formula
- cholesterol
- parts
- Prior art date
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C31/00—Saturated compounds having hydroxy or O-metal groups bound to acyclic carbon atoms
- C07C31/34—Halogenated alcohols
- C07C31/38—Halogenated alcohols containing only fluorine as halogen
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
La presente invenzione "riguarda composizioni farmaceutiche ad attività antineoplastica, contenenti come principio attivo (a) almeno un polifluoroalcol di formula I: The present invention "relates to pharmaceutical compositions with antineoplastic activity, containing at least one polyfluoroalcohol of formula I as active ingredient (a):
CHF2-(CF2)„-CH2OH (I) CHF2- (CF2) „- CH2OH (I)
dove n rappresenta i numeri 3, 5, 7 oppure 9. where n represents the numbers 3, 5, 7 or 9.
L'invenzione riguarda inoltre composizioni farmaceutiche ad attività antineoplastica, contenenti oltre al principio attivo (a) anche (b) colesterolo. The invention also relates to pharmaceutical compositions with antineoplastic activity, containing in addition to the active principle (a) also (b) cholesterol.
Di preferenza, le composizioni contengono almeno due dei polifluoroalcoli (I) e colesterolo. Ancor più preferibilmente, tali composizioni contengono (a) tre polifluoroalcoli di formula (I), più (b) colesterolo. Preferably, the compositions contain at least two of the polyfluoroalcohols (I) and cholesterol. Even more preferably, these compositions contain (a) three polyfluoroalcohols of formula (I), plus (b) cholesterol.
Le proporzioni relative dei tre polifluoroalcoli nelle composizioni preferite secondo l'invenzione possono variare entro ampi limiti, per esempio da 12 parti di dodecafluoroeptanolo (I, con n = 5) + 1 parte di ottafluoropentanolo (I, con n = 3) + 1 parte di esadecafluorononanolo (I, con n = 7), al parte di dodecafluoroeptanolo + 12 parti di ottafluoropentanolo + 1 parte di esadecafluorononanolo, a 1 parte di dodecafluoroeptanolo + 1 parte di ottafluoropentanolo + 12 parti di esadecafluorononanolo. The relative proportions of the three polyfluoroalcohols in the preferred compositions according to the invention can vary within wide limits, for example from 12 parts of dodecafluoroeptanol (I, with n = 5) + 1 part of octafluoropentanol (I, with n = 3) + 1 part of hexadecafluorononanol (I, with n = 7), to the part of dodecafluoroeptanol + 12 parts of octafluoropentanol + 1 part of hexadecafluorononanol, to 1 part of dodecafluoroeptanol + 1 part of octafluoropentanol + 12 parts of hexadecafluorononon.
Le proporzioni relative tra i costituenti (a) e (b) possono a loro volta variare da 10:1 a 1:10. The relative proportions between the constituents (a) and (b) can in turn vary from 10: 1 to 1:10.
Le composizioni secondo l'invenzione possono inoltre contenere veicoli lipofili, come olio di sesamo o simili. The compositions according to the invention can also contain lipophilic vehicles, such as sesame oil or the like.
Tutti i costituenti delle composizioni farmaceutiche secondo l'invenzione sono di per sé noti e reperibili in commercio. All the constituents of the pharmaceutical compositions according to the invention are known per se and commercially available.
Gli esempi che seguono illustrano le composizioni secondo l'invenzione, senza tuttavia rivestire alcun carattere limitativo. The following examples illustrate the compositions according to the invention, without however having any limiting character.
Esempio I Example I
In 150 g di olio di sesamo si sciolgono 3 g di ottafluoropentanolo, 5 g fi dodecafluoroeptanolo e 7,5 g di esadecafluorononanolo; quindi, scaldando brevemente a 35-40°C, 2,5 g di colesterolo. 3 g of octafluoropentanol, 5 g of dodecafluoroheptanol and 7.5 g of hexadecafluorononanol are dissolved in 150 g of sesame oil; then, heating briefly at 35-40 ° C, 2.5 g of cholesterol.
Esempio 2 Example 2
A 100 g di olio di sesamo si aggiungono 2,5 g di dodecafluoroeptanolo, 2,5 g di esadecafluorononanolo, 5 g di ottafluoropentanolo e 4 g di colesterolo, agitando sino a dissoluzione completa. To 100 g of sesame oil 2.5 g of dodecafluoroeptanol, 2.5 g of hexadecafluorononanol, 5 g of octafluoropentanol and 4 g of cholesterol are added, stirring until complete dissolution.
Esempio 3 Example 3
A 174 g di olio di sesamo si aggiungono i seguenti componenti, agitando sino a dissoluzione completa: The following components are added to 174 g of sesame oil, stirring until completely dissolved:
dodecafluoroeptanolo (I, con n = 5) g 12 dodecafluoroeptanol (I, with n = 5) g 12
esadecafluorononanolo (I, con n = 7) g 4 hexadecafluorononanol (I, with n = 7) g 4
ottafluoropentanolo (I, con n = 3) g 4 octafluoropentanol (I, with n = 3) g 4
colesterolo g 6 cholesterol g 6
La soluzione ottenuta viene distribuita in fiale da 0,2 mi, 0,3 mi e 0,5 mi. Le fiale vengono sterilizzate a caldo. The obtained solution is distributed in 0.2 ml, 0.3 ml and 0.5 ml ampoules. The vials are heat sterilized.
Esempio 4 Example 4
Si opera come nell'esempio 1, aggiungendo 2 g di eicosa-fluoroundecanolo (I, con n = 9). The procedure is carried out as in example 1, adding 2 g of eicosa-fluoroundecanol (I, with n = 9).
Esempio 5 Example 5
Si opera come nell'esempio 1, sostituendo l'esadecafluoro-nonanolo con una pari quantità di ottafluoropentanolo. One works as in example 1, replacing the hexadecafluoro-nonanol with an equal quantity of octafluoropentanol.
Esempio 6 Example 6
Si opera come nell'esempio 3, trascurando l'aggiunta di colesterolo. One operates as in example 3, neglecting the addition of cholesterol.
Della composizione secondo l'esempio 3 è stata determinata la tossicità acuta, subacuta e cronica. Acute, subacute and chronic toxicity was determined of the composition according to Example 3.
Tossicità acuta. L'iniezione sottocutanea di dosi superiori a 0,5 mi in topi del peso di 30 g provoca, come unico sintomo, un sonno dal quale gli animali si destano dopo qualche ora senza altre manifestazioni anomale. Lo stesso accade a ratti, con dosi superiori a 1,5 ml/100 g. Acute toxicity. The subcutaneous injection of doses greater than 0.5 ml in mice weighing 30 g causes, as the only symptom, a sleep from which the animals wake up after a few hours without other abnormal manifestations. The same happens to rats, with doses higher than 1.5 ml / 100 g.
Tossicità subacuta. La somministrazione per vie sottocutanea in ragione di 0,3 ml/giorno per 5 giorni alla settimana e per tre settimane consecutive, a topi del peso di 30 g, non provoca alcun sintomo di tossicità, né si riscontra alcuna alterazione patologica negli animali sacrificati. Subacute toxicity. Subcutaneous administration at a rate of 0.3 ml / day for 5 days a week and for three consecutive weeks, to mice weighing 30 g, does not cause any symptoms of toxicity, nor is there any pathological alteration in the sacrificed animals.
Tossicità cronica. Topi del peso di 30 g furono sottoposti a iniezione sottocutanea di 0,2 ml/giorno per tre volte alla settimana e per tre mesi consecutivi. Gli animali non presentarono alcuna anomalia rispetto ai controlli, né si osservò alcuna alterazione patologica negli animali sacrificati. Eguali risultati si ebbero per somministrazione di 0,4 ml/100 g a ratti. Nessun fenomeno tossico fu osservato somministrando la composizione in oggetto a topi e ratti per via orale, mediante catetere, in ragione di 0,2 ml/giorno (rispett. 0,4 ml/100 g/ giorno), per prolungati periodi di tempo, né aggiungendo I'I% di composizione al mangime dei suddetti animali, quantunque gli animali stessi Chronic toxicity. Mice weighing 30 g underwent 0.2 ml / day subcutaneous injection three times a week and for three consecutive months. The animals did not show any abnormality with respect to the controls, nor did any pathological alteration in the sacrificed animals be observed. The same results were obtained by administering 0.4 ml / 100 g to rats. No toxic phenomenon was observed by administering the subject composition to mice and rats orally, by catheter, at the rate of 0.2 ml / day (respectively 0.4 ml / 100 g / day), for prolonged periods of time, nor by adding I% of composition to the feed of the aforementioned animals, although the animals themselves
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manifestassero una certa riluttanza a cibarsi del mangime così trattato. showed some reluctance to feed on the feed thus treated.
Da quanto sopra esposto appare evidente che i composti secondo l'invenzione sono praticamente atossici. From the above, it is evident that the compounds according to the invention are practically non-toxic.
Farmacologia. Il concetto di dualismo anabolico-catabolico e relative definizioni, qui sotto ricorrenti, sono ampiamente illustrati — anche da un punto di vista sperimentale (in campo animale e in campo umano) — in E. Revici, Research in Phy-siopathology, ediz. Van Nostrand, Princeton, 1861. Tuttavia, la validità dell'invenzione non deve intendersi comunque legata all'effettiva verifica dei presupposti teorici nel suddetto trattato. Le composizioni secondo l'invenzione, in particolare quella secondo l'esempio 3, svolgono un'influenza molto favorevole sulle lesioni esplicando un effetto catabolico. Tale influenza si è chiaramente dimostrata sulla guarigione di ferite e di ustioni. Sui cancri sperimentali si è notata una netta differenza di comportamento a seconda del carattere anabolico o catabolico dei tumori. 5 Infatti, nel primo caso le composizioni in oggetto ritardano soltanto la morte degli animali, mentre le stesse composizioni esercitano un evidente effetto benefico sui tumori a carattere catabolico (con necrosi, accumulo di fluido, cellule in picknosi). Pharmacology. The concept of anabolic-catabolic dualism and related definitions, recurring below, are amply illustrated - also from an experimental point of view (in the animal and human fields) - in E. Revici, Research in Phy-siopathology, ediz. Van Nostrand, Princeton, 1861. However, the validity of the invention is not to be considered in any case linked to the effective verification of the theoretical assumptions in the aforementioned treatise. The compositions according to the invention, in particular the one according to example 3, have a very favorable influence on the lesions, exhibiting a catabolic effect. This influence has clearly proven itself on the healing of wounds and burns. Experimental cancers showed a marked difference in behavior depending on the anabolic or catabolic character of the tumors. 5 In fact, in the first case the compositions in question only delay the death of the animals, while the compositions themselves have an evident beneficial effect on catabolic tumors (with necrosis, accumulation of fluid, cells in picknosis).
Clinica. Anche nel trattamento di pazienti affetti da tumori io catabolici le composizioni secondo l'invenzione, somministrate • mediante iniezione intramuscolare in dosi di 2-3 mi, svolgono un'azione nettamente favorevole, eliminando o riducendo per molte ore la sofferenza. Clinic. Also in the treatment of patients suffering from catabolic tumors the compositions according to the invention, administered by intramuscular injection in doses of 2-3 ml, perform a clearly favorable action, eliminating or reducing suffering for many hours.
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Claims (11)
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
IT8221553A IT8221553A0 (en) | 1982-05-28 | 1982-05-28 | PHARMACEUTICAL COMPOSITIONS ANTINEOPLASTIC ADAPTIVITY. |
Publications (1)
Publication Number | Publication Date |
---|---|
CH653890A5 true CH653890A5 (en) | 1986-01-31 |
Family
ID=11183507
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CH2772/83A CH653890A5 (en) | 1982-05-28 | 1983-05-20 | PHARMACEUTICAL COMPOSITIONS WITH ANTINEOPLASTIC ACTIVITY. |
Country Status (16)
Country | Link |
---|---|
JP (1) | JPS591414A (en) |
AU (2) | AU552557B2 (en) |
BE (1) | BE896838A (en) |
CH (1) | CH653890A5 (en) |
DE (1) | DE3319304A1 (en) |
FR (1) | FR2527439A1 (en) |
GB (1) | GB2121280B (en) |
IE (1) | IE55137B1 (en) |
IL (1) | IL68796A0 (en) |
IN (1) | IN157042B (en) |
IT (1) | IT8221553A0 (en) |
LU (1) | LU84827A1 (en) |
NL (1) | NL8301899A (en) |
NZ (1) | NZ204393A (en) |
SE (1) | SE8302976L (en) |
ZA (1) | ZA833871B (en) |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE3836971C1 (en) * | 1988-10-31 | 1990-05-17 | Weck, Wolfgang, Dr.Med., 6990 Bad Mergentheim, De |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE3219004C1 (en) * | 1982-05-19 | 1984-03-01 | Philippine Dr. 8000 München Hartmann | Pharmaceutical compositions for the treatment of tumours |
-
1982
- 1982-05-28 IT IT8221553A patent/IT8221553A0/en unknown
-
1983
- 1983-05-20 CH CH2772/83A patent/CH653890A5/en not_active IP Right Cessation
- 1983-05-26 SE SE8302976A patent/SE8302976L/en not_active Application Discontinuation
- 1983-05-26 IL IL68796A patent/IL68796A0/en unknown
- 1983-05-26 JP JP58093889A patent/JPS591414A/en active Pending
- 1983-05-26 AU AU15000/83A patent/AU552557B2/en not_active Expired - Fee Related
- 1983-05-26 GB GB08314540A patent/GB2121280B/en not_active Expired
- 1983-05-26 BE BE2/60100A patent/BE896838A/en not_active IP Right Cessation
- 1983-05-27 DE DE19833319304 patent/DE3319304A1/en not_active Ceased
- 1983-05-27 ZA ZA833871A patent/ZA833871B/en unknown
- 1983-05-27 IN IN673/CAL/83A patent/IN157042B/en unknown
- 1983-05-27 LU LU84827A patent/LU84827A1/en unknown
- 1983-05-27 NL NL8301899A patent/NL8301899A/en not_active Application Discontinuation
- 1983-05-27 IE IE1259/83A patent/IE55137B1/en unknown
- 1983-05-27 NZ NZ204393A patent/NZ204393A/en unknown
- 1983-05-27 FR FR8308776A patent/FR2527439A1/en not_active Withdrawn
-
1988
- 1988-05-04 AU AU15570/88A patent/AU1557088A/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
NZ204393A (en) | 1986-03-14 |
JPS591414A (en) | 1984-01-06 |
LU84827A1 (en) | 1983-11-17 |
IT8221553A0 (en) | 1982-05-28 |
AU1500083A (en) | 1983-12-01 |
FR2527439A1 (en) | 1983-12-02 |
IL68796A0 (en) | 1983-09-30 |
BE896838A (en) | 1983-09-16 |
NL8301899A (en) | 1983-12-16 |
GB8314540D0 (en) | 1983-06-29 |
IN157042B (en) | 1986-01-04 |
SE8302976L (en) | 1983-11-29 |
GB2121280A (en) | 1983-12-21 |
GB2121280B (en) | 1985-08-29 |
ZA833871B (en) | 1984-07-25 |
IE55137B1 (en) | 1990-06-06 |
AU1557088A (en) | 1988-11-10 |
IE831259L (en) | 1983-11-28 |
DE3319304A1 (en) | 1983-12-01 |
AU552557B2 (en) | 1986-06-05 |
SE8302976D0 (en) | 1983-05-26 |
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PL | Patent ceased |