Method for preparing steroid salt for parentheral administration

专利摘要:
A water-soluble salt of dehydroepiandrosterone sulfate is dissolved in an aqueous solution of a compound selected from the group consisting of dextran, macrogol, a neutral amino acid, a basic amino acid, an alkali metal salt of a weak acid, a solid amine, and mixtures thereof and then the resulting mixture is lyophilized.
公开号:SU1072789A3
申请号:SU762395947
申请日:1976-09-03
公开日:1984-02-07
发明作者:Сугимота Исао；Савазе Еко
申请人:Канебо,Лтд (Фирма)；
IPC主号:

专利说明:

The invention relates to a technology for the preparation of drugs and relates to the preparation of stabilized preparations of steroid salts. . A method of obtaining stable solutions of ergothal by using stabilizers of C is known. A method of obtaining a stable preparation of a steroid salt for parenteral administration by dissolving it in a solution of thioglyceride or thioglycolic acid GZ is also known. However, the known methods do not provide the preparation,. giving a fairly good solubility. . The purpose of the invention is to increase the dilution of the drug. The goal is achieved in that according to the method of obtaining a steroid salt for parenteral administration, including its dissolution in an aqueous stabilizer solution, the sodium salt of dihydroepiandrosterone sulfate is used as the steroid salt, which is introduced into an aqueous solution of glycine containing 20-200% by weight of salt the stabilizer and the resulting solution are sterile filtered and lyophilized. Example. In a 2 liter container, 40 g of glycine is dissolved in distilled water. To the solution, 40 g of dihydroepiandrosterone sulfate DHA-C sodium salt are added with heating. The total volume of the solution is adjusted to 2 liters with distilled water. The solution is sterilized by filtration and poured into 5 ml glass ampoules. Then the solution is lyophilized and sealed vials. EXAMPLE 2: 40 g of sodium soda DGA-C is dissolved in a 2.8 l solution containing 8 g of glycine (20 wt.% By weight of the salt DGA-c) obtained by dissolving it in distilled water when heated. . The total volume of the solution is adjusted to 3.2 liters with distilled water. The resulting solution is filtered under sterile conditions and poured into 8 ml ampoules. Then the solution is lyophilized. Each ampoule contains 100 mg of DHA-C sodium salt and 20 mg of glycine. EXAMPLE 3. 40 g of DGA-C sodium salt are dissolved in 1.8 l of a solution containing 44 g of glycine (100% by weight of salt), and the resulting solution is diluted with distilled water to a total of 2 l, then the solution is sterile filtered and lyophilized in ampoules. EXAMPLE 4 40 g of DGA-C sodium salt are dissolved in 1.8 l of a solution containing 80 g of glycine (200% w / w by weight of salt), diluted with distilled water to an ose volume of 2 l. The resulting solution is filtered under sterile conditions and poured into ampoules. Then solution lyophilized. The solubility of the dihydroepiandrosterone sulfate sodium salt is determined in aqueous solutions with different glycine contents at. When this is obtained, the following results are obtained: Solubility Concentration of sodium soglycine, or DGA-C, wt.% Wt.% Thus, the addition of glycine in an amount of 20-200 weight% by weight of salt leads to an increase in its solubility, which allows further preparation of solutions for injection with less water. In addition, the proposed method allows to obtain a preparation that is stable during storage. The stability test is carried out as follows. A preparation is prepared that does not contain glycine, and also contains the latter in quantities of 5, 20, IO, 200, and 250 wt. % by weight of salt DHA-C. 10 test tubes from each group are kept at. After 30 and 60 days, their content is analyzed for the residual amount of DGA-C salt. For each group, an average value is calculated from the content analysis of 5 tubes. The results are shown in the table. The drug is unsuitable for clinical purposes due to its high glycine content. The results show that the addition of glycine in an amount of 20-200 weight. % by weight of salt
3107 27894
 leads to stabilization of the storage time and may be
.when it is stored. Received predla-easily dissolved in sterile water
 the way the drug is formulated is used for intravenous or
stable over a long period of time1L11ech) 1XX injections.

权利要求:
Claims (1)
[1]
, / 57) A METHOD FOR PRODUCING A STEROID SALT FOR PARENTERAL ADMINISTRATION, including its dissolution in an aqueous stabilizer solution, distinguished by the fact that, in order to increase the solubility of the preparation, the dihydroepiandrosterone sulfate sodium salt is introduced into the aqueous solution, which is introduced into the aqueous solution glycine containing 20 - 200% by weight of the salt of the stabilizer, and the resulting solution is sterile filtered and lyophilized.
Priority by signs: 05.09.75 - when using the dihydroepiandrosterone sulfate sodium salt as a steroid salt;
07/06/76 - with the introduction of the steroid salt in an aqueous solution of glycine containing 20-200% by weight of the stabilizer salt, followed by filtration and lyophilization of the resulting solution.
, SU .. 10727 POISON of the volume of 2 l. The resulting solution was filtered under sterile conditions and poured into ampoules. Then the solution is lyophilized.
The solubility of the dihydroepiandrosterone sulfate sodium salt is determined in aqueous * solutions with different glycine contents at 20 ° C. Thus received • theta:

类似技术:

---

公开号 | 公开日 | 专利标题

---

RU2043118C1|1995-09-10|Method for producing erythropoietin forms useable for injections

---

KR920003332B1|1992-04-27|Process for preparing etoposide preparations

---

SU1072789A3|1984-02-07|Method for preparing steroid salt for parentheral administration

---

US3758683A|1973-09-11|Insulin product

---

US4866044A|1989-09-12|Solubilized composition of poorly-soluble pharmaceutical product

---

KR950010158B1|1995-09-11|Aqueous alcaline injectable solution of torasemid

---

JPH10511967A|1998-11-17|Enrofloxacin injection or infusion solution

---

JP3720262B2|2005-11-24|Stabilized carvedilol injection solution

---

US5681573A|1997-10-28|Process to prepare pharmaceutical compositions containing vecuronium bromide and compositions produced thereby

---

DK159376B|1990-10-08|PROCEDURE FOR THE PREPARATION OF A STABLE, SOLID, WATER SOLUBLE PREPARATION FOR WATER RECONSTITUTION OR Aqueous CARRIER AS A STABLE SOLUTION OF 4 '- | METHAN-SULPHONES

---

KR950006218B1|1995-06-12|Freeze-dried pharmaceutical compositions of phenyl quinoline crboxylic acids

---

CA1140048A|1983-01-25|Etomidate-containing compositions

---

US5034397A|1991-07-23|Stable, water soluble salt compositions of M-AMSA in 1-methyl-2-pyrrolidinone

---

US4518606A|1985-05-21|Pharmaceutical compositions

---

PT93991B|1996-11-29|PROCESS FOR THE PREPARATION OF STABLE SOLUTIONS OF REBECAMYCINAL ANALOGS

---

FI80023C|1990-04-10|FOERFARANDE FOER FRAMSTAELLNING AV NYA, THERAPEUTIC ANVAENDBARA KRISTALLINA LACTATACETONATSOLAT AV M-AMSA.

---

CA1062157A|1979-09-11|Stable injection solutions

---

US5955456A|1999-09-21|Injectable pharmaceutical composition comprising ursodesoxycholic acid or tauroursodesoxycholic acid, a strong base and tromethamol

---

US6187818B1|2001-02-13|Prostaglandins formulation and process

---

JP3242924B2|2001-12-25|Pre-prepared azosemide injection

---

US4742082A|1988-05-03|Solution of luprostiol and 1,2,-propanediol and methods of preparation and use

---

KR810001164B1|1981-09-25|Process for preparing stable water-soluble salts of dehydroepiandrosterone sulfate

---

JP2946015B2|1999-09-06|Stable antiviral infusion injection

---

US4416874A|1983-11-22|Injectable compositions of BBM-928A

---

WO2019070169A1|2019-04-11|Method for obtaining a liophilised form of |-|methane) and the obtained liophilised form

同族专利:

---

公开号 | 公开日

---

ES451256A1|1977-09-16|

---

DK153124C|1988-12-19|

---

NL7609833A|1977-03-08|

---

GB1561360A|1980-02-20|

---

SE439586B|1985-06-24|

---

AU498543B2|1979-03-15|

---

AU1748676A|1978-03-16|

---

US4061744A|1977-12-06|

---

DE2639849A1|1977-03-17|

---

NL183385C|1988-10-17|

---

FR2322605A1|1977-04-01|

---

IL50376D0|1976-10-31|

---

DK396576A|1977-03-06|

---

IL50376A|1979-10-31|

---

DE2639849C2|1987-02-12|

---

DK153124B|1988-06-20|

---

CA1047404A|1979-01-30|

---

FR2322605B1|1982-08-20|

---

DD127381A5|1977-09-21|

---

SE7609443L|1977-03-06|

---

CS216160B2|1982-10-29|

---

NL183385B|1988-05-16|

---

HU173475B|1979-05-28|

引用文献:

---

公开号 | 申请日 | 公开日 | 申请人 | 专利标题

---

---

FR2179M|Farmaceutici Italia|Medicinal product based on 16α-hydroxy-steroids with anticancer activity.|

---

DE1767898A1|1967-07-28|1971-09-30|Hoffmann La Roche|Process for the production of a pharmaceutical preparation|

---

US4005200A|1975-07-17|1977-01-25|Kanebo, Ltd.|Method for improving the maturity of the parturient canal and the sensitivity to oxytocin|US4496556A|1982-08-16|1985-01-29|Norman Orentreich|Topical applications for preventing dry skin|

---

JPH0517884B2|1986-10-20|1993-03-10|Kanebo Ltd|

---

NL194728C|1987-04-16|2003-01-07|Hollis Eden Pharmaceuticals|Pharmaceutical preparation suitable for the prophylaxis or therapy of a retroviral infection or a complication or consequence thereof.|

---

JPS6440428A|1987-08-07|1989-02-10|Daiichi Yakuhin Sangyo Kk|Antihyperlipemia|

---

JP2546808B2|1989-01-23|1996-10-23|鐘紡株式会社|Vaginal suppository|

---

US5246704A|1989-01-23|1993-09-21|Kanebo, Ltd.|Vaginal suppository|

---

US5004651A|1989-01-24|1991-04-02|Abbott Laboratories|Stabilizing system for solid dosage forms|

---

CA2013474C|1989-04-20|2000-01-18|Pharmacia Inc.|Cyclophosphamide - alanine lyophilizates|

---

US5268368A|1991-05-17|1993-12-07|Erbamont, Inc.|Cyclophosphamide--amino acid lyophilizates|

---

US5210081A|1992-02-26|1993-05-11|American Home Products Corporation|Alkali metal 8,9-dehydroestrone sulfate esters|

法律状态:

优先权:

---

申请号 | 申请日 | 专利标题

---

JP10819775A|JPS578086B2|1975-09-05|1975-09-05|

---

JP8061376A|JPS5530769B2|1976-07-06|1976-07-06|

---