US2533066A - Micropulverized therapeutic compositions - Google Patents
Micropulverized therapeutic compositions Download PDFInfo
- Publication number
- US2533066A US2533066A US737724A US73772447A US2533066A US 2533066 A US2533066 A US 2533066A US 737724 A US737724 A US 737724A US 73772447 A US73772447 A US 73772447A US 2533066 A US2533066 A US 2533066A
- Authority
- US
- United States
- Prior art keywords
- penicillin
- mixture
- micropulverized
- therapeutic agent
- streptomycin
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
- 239000000203 mixture Substances 0.000 title claims description 19
- 230000001225 therapeutic effect Effects 0.000 title description 4
- 239000003814 drug Substances 0.000 claims description 24
- UCSJYZPVAKXKNQ-HZYVHMACSA-N streptomycin Chemical compound CN[C@H]1[C@H](O)[C@@H](O)[C@H](CO)O[C@H]1O[C@@H]1[C@](C=O)(O)[C@H](C)O[C@H]1O[C@@H]1[C@@H](NC(N)=N)[C@H](O)[C@@H](NC(N)=N)[C@H](O)[C@H]1O UCSJYZPVAKXKNQ-HZYVHMACSA-N 0.000 claims description 24
- 229940049954 penicillin Drugs 0.000 claims description 19
- 229940124597 therapeutic agent Drugs 0.000 claims description 19
- 229930182555 Penicillin Natural products 0.000 claims description 18
- JGSARLDLIJGVTE-MBNYWOFBSA-N Penicillin G Chemical compound N([C@H]1[C@H]2SC([C@@H](N2C1=O)C(O)=O)(C)C)C(=O)CC1=CC=CC=C1 JGSARLDLIJGVTE-MBNYWOFBSA-N 0.000 claims description 18
- 239000000126 substance Substances 0.000 claims description 13
- 229960005322 streptomycin Drugs 0.000 claims description 12
- 230000001387 anti-histamine Effects 0.000 claims description 10
- 239000000739 antihistaminic agent Substances 0.000 claims description 10
- 230000003115 biocidal effect Effects 0.000 claims description 5
- 238000006243 chemical reaction Methods 0.000 description 10
- 230000035945 sensitivity Effects 0.000 description 8
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 description 5
- 239000003795 chemical substances by application Substances 0.000 description 5
- 238000000034 method Methods 0.000 description 5
- UFLGIAIHIAPJJC-UHFFFAOYSA-N Tripelennamine Chemical compound C=1C=CC=NC=1N(CCN(C)C)CC1=CC=CC=C1 UFLGIAIHIAPJJC-UHFFFAOYSA-N 0.000 description 4
- 229940079593 drug Drugs 0.000 description 4
- 229960001031 glucose Drugs 0.000 description 4
- 229960003223 tripelennamine Drugs 0.000 description 4
- 238000001856 aerosol method Methods 0.000 description 3
- 229940088007 benadryl Drugs 0.000 description 3
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 3
- ZZVUWRFHKOJYTH-UHFFFAOYSA-N diphenhydramine Chemical compound C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 ZZVUWRFHKOJYTH-UHFFFAOYSA-N 0.000 description 3
- 239000008103 glucose Substances 0.000 description 3
- 229940127240 opiate Drugs 0.000 description 3
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 description 2
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 2
- NTYJJOPFIAHURM-UHFFFAOYSA-N Histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 description 2
- 206010024769 Local reaction Diseases 0.000 description 2
- 239000003242 anti bacterial agent Substances 0.000 description 2
- 229940088710 antibiotic agent Drugs 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 238000010348 incorporation Methods 0.000 description 2
- 229910052740 iodine Inorganic materials 0.000 description 2
- 239000011630 iodine Substances 0.000 description 2
- 210000004072 lung Anatomy 0.000 description 2
- BQJCRHHNABKAKU-KBQPJGBKSA-N morphine Chemical compound O([C@H]1[C@H](C=C[C@H]23)O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O BQJCRHHNABKAKU-KBQPJGBKSA-N 0.000 description 2
- 239000007921 spray Substances 0.000 description 2
- 150000003456 sulfonamides Chemical class 0.000 description 2
- 206010061218 Inflammation Diseases 0.000 description 1
- 230000006978 adaptation Effects 0.000 description 1
- 238000003745 diagnosis Methods 0.000 description 1
- 229940039227 diagnostic agent Drugs 0.000 description 1
- 239000000032 diagnostic agent Substances 0.000 description 1
- 229960001340 histamine Drugs 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 229960005181 morphine Drugs 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000000069 prophylactic effect Effects 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
Definitions
- xTh v present invention relates to therapeutic agents and to their administration- More specifically it relates to anti-biotics, such as penicillin and streptomycin and their administration by inhalation.
- Penicillin, streptomycin and others of the recently discovered anti-biotics are wonder drugs. Ithasbeen found, however, that some patients, to whom these aIItiFblOtlCS are administered, develop local reactions 'atithesite of administration ofthe' drug. The part may become inflamed and severe sores may develop. For instance, in the administration of penicillin by the aerosol method, that is, by inhalation of a penicillin solution in the form .of, a spray or vapor, it is known that the incidence of local sensitivity reactions to penicillin. is roughly fifteen percent. The threat and mouth become red, swollen, and painful.
- sensitivity reaction isnot'limited, however, to the anti-'biotics.
- Other therapeutic agents such as the sulphonamides, opiates, and iodine-containing radio opaques frequently cause severe local reactions, thus not only hampering the diagnosis and treatment of a disease but producing troubles with which the patient Was not previously afflicted.
- the accepted theory about sensitivity reactions is that they are caused by release of histamine at the reacting organ or site.
- the primary object of the present invention is to provide a new method and a novel form, by
- Anether form of theinvention is'to provide a new method and a novel form for administration of therapeuticagents of the character described whichwill allow the use of these agents to be extended.
- the presentinvention is predicated upon incorporation. of a small amount of an. anti-histamine substance, such as Benadryl..or Pyribenzamine, with penicillin, streptomycin, or other therapeutic agent, which might cause' a local sensitivity reaction, and administering to the patient the mixture of anti-histamine substance and therapeutic agent.
- an. anti-histamine substance such as Benadryl..or Pyribenzamine
- penicillin, streptomycin, or other therapeutic agent which might cause' a local sensitivity reaction
- the anti-histamine substance not only reduces the incidence of reactions to the therapeutic but permits extension of the use of the primary agent, for it allows the therapeutic to do its work Without being hindered by any other reaction in the body of the patient.
- the antihistamine substance acts as a prophylactic.
- the Benadryl or Pyribenzamine can be mixed, for instance, with penicillin and anhydrous glucose or other Water-soluble sugar in the proportion of about one-part of Benadryl or Pyribenzamine to on hundred parts of the mixture of penicillin and glucose, and the whole is then ground to a powder whose particulate size is one micron or less
- the apparatus shown in application No. 733,280 may be employed.
- the penicillin and glucose may have the proportion of 1:5 to 1:20 as described in said application.
- the invention is not restricted, however, to administration by suspension of a micro-pulverized agent in air. It is applicable also where the therapeutic agent is to be administered by the aerosol method.
- a 2% solution of Pyrbbenzamine may be mixed with a penicillin solution and the mixture inhaled in the form of a spray or vapor.
- the invention may also be used where the penicillin, streptomycin, opiate, or other therapeutic is administered by other methods, as for instance by the hypodermic needle. Incorporation of an anti-histamine substance with the therapeutic agent will inhibit the production of the sores or painful lumps that so often occur at the point where the needle enters the body, when a therapeutic agent is administered hypodermically.
- a therapeutic agent for direct administration to humans by inhalation comprising a dry, micropulverized, powdered mixture of an antihistaminic chemical blocker and a soluble antibiotic substance from the group consisting of penicillin and streptomycin, said mixture having a particulate size in the order of one micron.
- a therapeutic agent for direct administration to humans by inhalation comprising a dry, micropulverized, powdered mixture of an antihistaminic chemical blocker and penicillin, said mixture having a particulate size in the order of one micron.
- a therapeutic agent for direct administration to humans by inhalation comprising a dry, micropulverized, powdered mixture of an antihistaminic chemical blocker and streptomycin, said mixture having a particulate size in the order of one micron.
- a therapeutic agent for direct administration to humans by inhalation comprising a dry, micropulverized, powdered mixture of an antihistaminic chemical blocker and a soluble antibiotic crystalline substance from the group consisting of penicillin and streptomycin, said mixture having a particulate size not exceeding one micron.
Description
Patented Dec. 5, 1950 "UNITED "STATES ears-1W1? orrics George .V. Taplin and Frederick A. Bryan,
1 Brighton, N. Y.
N Drawing. Application March 27, 1947, Serial No. 737,724
4 Claims. (01. "167-965) xTh v present invention .relates to therapeutic agents and to their administration- More specifically it relates to anti-biotics, such as penicillin and streptomycin and their administration by inhalation.
Penicillin, streptomycin and others of the recently discovered anti-biotics are wonder drugs. Ithasbeen found, however, that some patients, to whom these aIItiFblOtlCS are administered, develop local reactions 'atithesite of administration ofthe' drug. The part may become inflamed and severe sores may develop. For instance, in the administration of penicillin by the aerosol method, that is, by inhalation of a penicillin solution in the form .of, a spray or vapor, it is known that the incidence of local sensitivity reactions to penicillin. is roughly fifteen percent. The threat and mouth become red, swollen, and painful.
.This local sensitivity reaction isnot'limited, however, to the anti-'biotics. Other therapeutic agents, such as the sulphonamides, opiates, and iodine-containing radio opaques frequently cause severe local reactions, thus not only hampering the diagnosis and treatment of a disease but producing troubles with which the patient Was not previously afflicted. The accepted theory about sensitivity reactions is that they are caused by release of histamine at the reacting organ or site.
Heretofore, when a patient has reacted to a therapeutic agent, such as penicillin or streptomycin, with local sensitivity, either the treatment with the drug has had to be discontinued and some other treatment prescribed, or the patient has had to be treated for the local sore or inflammation developed, and has had to put up with the inconvenience, discomfort, and oftentimes pain of the local sensitivity reaction until that reaction yields to treatment. This frequently takes more time than the illness or disease which in the first place caused the administration of the therapeutic agent.
In our copending application, Serial No. 733,280, filed March 8, 1947, there is disclosed a new method of administering penicillin, streptomycin and other therapeutic agents by inhalation of these agents in micro-pulverized powdered form, the agent being suspended in air. In both this method and in the aerosol method of administration, the therapeutic agent is supplied directly to the lungs. If the lung of the patient should be locally sensitive and react locally from the penicillin or streptomycin treatment, it would be serious and might even be fatal.
The primary object of the present invention is to provide a new method and a novel form, by
Which-penicillin, streptomycin, the sulphonamides, morphine and other opiates iodine-containing radio Opaques and other diagnostic agents,- and similar therapeutics may be administered, that will inhibitlocal sensitivity reactions to these therapeutic agents.
Anether form of theinvention is'to provide a new method and a novel form for administration of therapeuticagents of the character described whichwill allow the use of these agents to be extended.
Other objects of theinvention will be, apparent hereinafter from the specification and from the recital of the appended claims. I
.The presentinvention is predicated upon incorporation. of a small amount of an. anti-histamine substance, such as Benadryl..or Pyribenzamine, with penicillin, streptomycin, or other therapeutic agent, which might cause' a local sensitivity reaction, and administering to the patient the mixture of anti-histamine substance and therapeutic agent. We have found that when this mixture is used there is a very low incidence of local sensitivity reaction to the therapeutic agent. The anti-histamine substance not only reduces the incidence of reactions to the therapeutic but permits extension of the use of the primary agent, for it allows the therapeutic to do its work Without being hindered by any other reaction in the body of the patient. The antihistamine substance acts as a prophylactic.
We prefer to administer the new mixture by incorporating the Benadry or Pyribenzamine in a micronized therapeutic-glucose mixture such as disclosed in application Serial No. 733,280 above mentioned and causing the micro-pulverized new mixture to be suspended in air and inhaled in the manner disclosed in said application. The Benadryl or Pyribenzamine can be mixed, for instance, with penicillin and anhydrous glucose or other Water-soluble sugar in the proportion of about one-part of Benadryl or Pyribenzamine to on hundred parts of the mixture of penicillin and glucose, and the whole is then ground to a powder whose particulate size is one micron or less For inhaling the mixture, the apparatus shown in application No. 733,280 may be employed. The penicillin and glucose may have the proportion of 1:5 to 1:20 as described in said application.
The invention is not restricted, however, to administration by suspension of a micro-pulverized agent in air. It is applicable also where the therapeutic agent is to be administered by the aerosol method. Thus a 2% solution of Pyrbbenzamine may be mixed with a penicillin solution and the mixture inhaled in the form of a spray or vapor. The invention may also be used where the penicillin, streptomycin, opiate, or other therapeutic is administered by other methods, as for instance by the hypodermic needle. Incorporation of an anti-histamine substance with the therapeutic agent will inhibit the production of the sores or painful lumps that so often occur at the point where the needle enters the body, when a therapeutic agent is administered hypodermically.
It will be obvious, too, that while the invention has been described in connection with particular embodiments and particular uses thereof, it is capable of various further modifications and uses, and that this application is intended to cover any variations, uses, or adaptations of the invention following, in general, the principles of the invention and including such departures from the present disclosure as come within known or customary practice in the art to which the invention pertains and as may be applied to the essential features hereinbefore set forth and as fall within the scope of the invention or the limits of the appended claims.
Having thus described our invention, what we claim is:
1. A therapeutic agent for direct administration to humans by inhalation comprising a dry, micropulverized, powdered mixture of an antihistaminic chemical blocker and a soluble antibiotic substance from the group consisting of penicillin and streptomycin, said mixture having a particulate size in the order of one micron.
2. A therapeutic agent for direct administration to humans by inhalation comprising a dry, micropulverized, powdered mixture of an antihistaminic chemical blocker and penicillin, said mixture having a particulate size in the order of one micron.
3. A therapeutic agent for direct administration to humans by inhalation comprising a dry, micropulverized, powdered mixture of an antihistaminic chemical blocker and streptomycin, said mixture having a particulate size in the order of one micron.
4. A therapeutic agent for direct administration to humans by inhalation comprising a dry, micropulverized, powdered mixture of an antihistaminic chemical blocker and a soluble antibiotic crystalline substance from the group consisting of penicillin and streptomycin, said mixture having a particulate size not exceeding one micron.
GEORGE V. TAPLIN. FREDERICK A. BRYAN.
REFERENCES CITED The following references are of record in the file of this patent:
UNITED STATES PATENTS Number Name Date 2,421,714 Rieveschl June 3, 1947 OTHER REFERENCES Article by Harris et al. in Amer. J. Medical Sciences, vol. 205, pages 1 to 6.
Science, Nov. 29, 1946, pages 498 and 499.
Proc. Staff Meetings Mayo Clinic, Nov. 14, 1945, pages 417 to 429.
The Pharmaceutical Journal (London), Feb. 8,
1941, page 40.
J. A. M. A., Dec. 14, 1946, pages 915 to 919.
J. A. M. A., July 21, 1945, page 910.
J. A. Pharm. Assoc., Scientific Edition, Nov. 1946, pages 326 and '7.
California Medicine, Apr. 1947, pages 242 to 248.
Claims (1)
1. A THERAPEUTIC AGENT FOR DIRECT ADMINISTRATION TO HUMANS BY INHALATION COMPRISING A DRY, MICROPULVERIZED, POWDERED MIXTURE OF AN ANTIHISTAMINIC CHEMICAL BLOCKER AND A SOLUBLE ANTIBIOTIC SUBSTANCE FROM THE GROUP CONSISTING OF PENICILLIN AND STREPTOMYCIN, SAID MIXTURE HAVING A PARTICULATE SIZE IN THE ORDER OF ONE MICRON.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US737724A US2533066A (en) | 1947-03-27 | 1947-03-27 | Micropulverized therapeutic compositions |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US737724A US2533066A (en) | 1947-03-27 | 1947-03-27 | Micropulverized therapeutic compositions |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| US2533066A true US2533066A (en) | 1950-12-05 |
Family
ID=24965046
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| US737724A Expired - Lifetime US2533066A (en) | 1947-03-27 | 1947-03-27 | Micropulverized therapeutic compositions |
Country Status (1)
| Country | Link |
|---|---|
| US (1) | US2533066A (en) |
Cited By (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2585239A (en) * | 1949-12-28 | 1952-02-12 | Bristol Lab Inc | Amine salt of penicillin |
| US2627491A (en) * | 1950-07-15 | 1953-02-03 | Wyeth Corp | Penicillin salts of substituted alkylene diamines |
| US2683711A (en) * | 1950-02-07 | 1954-07-13 | Boots Pure Drug Co Ltd | Penicillin-amine salts |
| US2704270A (en) * | 1951-04-16 | 1955-03-15 | Leo Ab | Antihistaminic injectable X-ray contrast media |
| US2730483A (en) * | 1952-08-12 | 1956-01-10 | Nepera Chemical Co Inc | Therapeutic compositions comprising neomycin, gramicidin and quaternary ammonium salt of thonzylamine |
| US2734846A (en) * | 1956-02-14 | Aqueous suspension of procaine penicil- | ||
| US2741573A (en) * | 1953-12-28 | 1956-04-10 | Abbott Lab | Penicillin compositions for intramuscular injection |
| US2754296A (en) * | 1950-09-01 | 1956-07-10 | Schi Wa Chemisch Pharmazeutisc | Antihistaminic compounds |
| US2768115A (en) * | 1951-11-02 | 1956-10-23 | Bristol Lab Inc | Penicillin-aspirin tablets |
| US2802772A (en) * | 1954-09-09 | 1957-08-13 | Merck & Co Inc | Aerosols compositions; bomb, and process for treating flocks of chickens |
| US2861024A (en) * | 1957-11-12 | 1958-11-18 | Merck & Co Inc | Antibiotic dusts |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2421714A (en) * | 1944-04-18 | 1947-06-03 | Parke Davis & Co | Dialkylaminoalkyl benzhydryl ethers and salts thereof |
-
1947
- 1947-03-27 US US737724A patent/US2533066A/en not_active Expired - Lifetime
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2421714A (en) * | 1944-04-18 | 1947-06-03 | Parke Davis & Co | Dialkylaminoalkyl benzhydryl ethers and salts thereof |
Cited By (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2734846A (en) * | 1956-02-14 | Aqueous suspension of procaine penicil- | ||
| US2585239A (en) * | 1949-12-28 | 1952-02-12 | Bristol Lab Inc | Amine salt of penicillin |
| US2683711A (en) * | 1950-02-07 | 1954-07-13 | Boots Pure Drug Co Ltd | Penicillin-amine salts |
| US2627491A (en) * | 1950-07-15 | 1953-02-03 | Wyeth Corp | Penicillin salts of substituted alkylene diamines |
| US2754296A (en) * | 1950-09-01 | 1956-07-10 | Schi Wa Chemisch Pharmazeutisc | Antihistaminic compounds |
| US2704270A (en) * | 1951-04-16 | 1955-03-15 | Leo Ab | Antihistaminic injectable X-ray contrast media |
| US2768115A (en) * | 1951-11-02 | 1956-10-23 | Bristol Lab Inc | Penicillin-aspirin tablets |
| US2730483A (en) * | 1952-08-12 | 1956-01-10 | Nepera Chemical Co Inc | Therapeutic compositions comprising neomycin, gramicidin and quaternary ammonium salt of thonzylamine |
| US2741573A (en) * | 1953-12-28 | 1956-04-10 | Abbott Lab | Penicillin compositions for intramuscular injection |
| US2802772A (en) * | 1954-09-09 | 1957-08-13 | Merck & Co Inc | Aerosols compositions; bomb, and process for treating flocks of chickens |
| US2861024A (en) * | 1957-11-12 | 1958-11-18 | Merck & Co Inc | Antibiotic dusts |
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