RU2730845C1 - Method of producing suppositories with candelabra aloe juice - Google Patents

Abstract

FIELD: pharmaceutics.SUBSTANCE: invention refers to chemical-pharmaceutical industry, in particular to production of a pharmaceutical herbal preparation possessing wound-healing and laxative action, a suppository based on leaves and sprouts of candelabra aloe (Aloe arborescens Mill.). Method of obtaining suppositories with candelabra aloe juice, involving use as raw material of leaves and sprouts of candelabra aloe, in which the juice obtained after holding leaves and sprouts of candelabra aloe for two days in a refrigerator, grinding, triturating, pressing and straining of raw material, introduced into suppositories, for production of which base used is gelatin-glycerol base consisting of gelatin medical – 1 pt., glycerin – 5 pts., water – 2 pts., resulting in suppositories of the following composition: 0.3 g of juice of candelabra aloe leaves and sprouts; 3.43 g of gelatin-glycerol suppository base.EFFECT: invention aims to develop a method for making suppositories with candelabra aloe juice (Aloe arborescens Mill_).1 cl, 1 ex, 2 tbl

Description

The invention relates to the chemical-pharmaceutical industry, in particular to the production of a pharmaceutical herbal medicine with a wound healing and laxative effect (2,3,4), - suppositories based on the juice of leaves and shoots of aloe tree (Aloe arborescens Mill.).

In official medicine, as a source of natural anthraquinones (aloe-emodin and barbaloin) (Table 1), aloe tree juice is used, which has laxative properties in high doses (3,4). In small doses, aloe tree juice is used as a biostimulating, regenerating, adaptogenic and general tonic drug (3,5). The following preparations of aloe tree are registered in the state register of medicines: "Aloe extract liquid" (produced by JSC "DALKHIMFARM", LP-001319; LLC "StatusPharm", LSR-008483/08; CJSC "VIFITEKH, LSR-007787/09)," Aloe juice "(produced by CJSC" VIFITECH ", LSR-000083)," Aloe liniment "(produced by CJSC" VIFITECH ", LSR-002881/09)," Aloe syrup with iron "(produced by CJSC" VIFITEKH ", LSR-008639/08 ), "Alorom" (produced by CJSC "VIFITECH", LSR-010484/08), "Aloe-plus" (produced by LLC "DOCTOR N", R N002797 / 01), "Aloe DN" (produced by LLC "DOCTOR N", P N003706 / 01) (1).

As a prototype of the invention, we have chosen homeopathic suppositories "Aloe DN", recommended for the treatment of chronic constipation obtained by pouring. The composition of one suppository: active ingredients Aloe (aloe) D2 - 0.17 g, Rheym (reum) D2 - 0.17 g, Chamomilla recutita (hamomilla) D2 - 0.17 g; auxiliary components: anhydrous lanolin, cocoa butter (1).

However, the prototype has some disadvantages, namely:

- a small amount of aloe juice contained in one suppository: D2 - 0.17 g (i.e. 0.0017 g), which is insufficient for the development of a therapeutic effect;

- the use of only hydrogenated fats and cocoa butter (hydrophobic base) as the basis for homeopathic suppositories, which are not stable during storage and quickly go rancid, which requires special storage conditions (in a dark place, at a temperature of 5 to 15 ° C).

Thus, the aim of the invention is to provide a method for making suppositories with Aloe arborescens Mill. Juice. The disclosure of the invention consists in the fact that the leaves and shoots of aloe tree were cut off, thoroughly washed with cold water, kept in the refrigerator for 2 days, crushed, placed in a porcelain mortar and ground with a pestle. Then it was transferred into cheesecloth folded in 2-4 layers, the juice was squeezed out, filtered.

As a basis, we used the recipe of a gelatin-glycerin base proposed by us, which consists of: medical gelatin - 1 hour, glycerin 5 hours, water -2 hours. For the manufacture of 5 suppositories, medical gelatin is needed in an amount of 2.14 g, which is filled with water in an amount 4.31 g and allowed to swell for 30-45 minutes, then 10.7 g of glycerin was added and placed in a water bath, stirring until smooth. Then added to the hot solution 1.5 g of aloe juice and cooled the mass to a temperature close to the pour point. The prepared mass was poured into split suppository plastic molds for 5 suppositories, preliminarily lubricated with vaseline oil.

The technical result consists in the fact that a technology has been developed for the manufacture of suppositories with aloe vera juice with a high content of active substances, in which a selected hydrophilic base promotes the rapid absorption of active substances.

Method of making the offer. The goal is achieved by the fact that the leaves and shoots of aloe tree were cut off, thoroughly washed with cold water, kept in the refrigerator for 2 days, crushed, placed in a porcelain mortar and ground with a pestle. Then it was transferred into cheesecloth folded in 2-4 layers, the juice was squeezed out, filtered. As a basis, we used the recipe of a gelatin-glycerin base that we proposed, which consists of: medical gelatin - 1 h, glycerin 5 h, water - 2 h.

To make 5 suppositories, medical gelatin is needed in the amount of 2.14 g, which was poured with water in the amount of 4.31 g and allowed to swell for 30-45 minutes, then glycerin in the amount of 10.7 g was added and placed in a water bath, stirring until smooth ... Then added to the hot solution 1.5 g of aloe juice and cooled the mass to a temperature close to the pour point. The prepared mass was poured into split suppository plastic molds for 5 suppositories, preliminarily lubricated with vaseline oil. Received a suppository of composition: 0.3 g of juice from the leaves and shoots of aloe tree; 3.43 g - gelatin-glycerin suppository base.

For the quantitative determination of the content of the active substance in suppositories, the spectrophotometric method was used.

The 5 g suppository was melted in a water bath and cooled. An exact weighed portion (2 grams) of the resulting mass was placed in a 100 ml flask, added 25 ml of 60% ethyl alcohol, heated in a water bath until the base melted, stirred for 3 minutes, cooled and filtered into a 25 ml volumetric flask. 2 ml of the obtained extract was transferred into a 25 ml volumetric flask and brought up to the mark with water, and 2 ml of the obtained extract was also added to the second flask and brought to the mark with an alkaline ammonia solution.

The optical density of the solution was measured on a spectrophotometer at a wavelength of 380 nm. The calculation of the content of the sum of anthracene derivatives in terms of barbaloin in suppositories with aloe vera juice was carried out according to the formula:

где

Where

E - optical density

- удельный показатель поглощения РСО барбалоина (300)

- specific absorption rate of RSO barbaloin (300)

P is the mass of one suppository

m - mass of exact sample

At the initial stage, the basis for the suppositories was selected:

1) suppositories of aloe tree on a lipophilic basis No. 1 (base composition: emulsifier tween-80 and cocoa butter)

2) suppositories of aloe tree on a hydrophilic basis No. 2 (base composition: gelatin, water and glycerin)

The proposed method is implemented in the following example.

Example. The juice was obtained from the leaves and shoots of aloe tree, after keeping the raw material for 2 days in the refrigerator, crushed, placed in a porcelain mortar and ground with a pestle. Then it was transferred into cheesecloth folded in 2-4 layers, the juice was squeezed out, filtered. As a basis, we used the recipe of a gelatin-glycerin base proposed by us, which consists of: medical gelatin - 1 hour, glycerin 5 hours, water - 2 hours.

To make 5 suppositories, medical gelatin is needed in the amount of 2.14 g, which was poured with water in the amount of 4.31 g and allowed to swell for 30-45 minutes, then glycerin in the amount of 10.7 g was added and placed in a water bath, stirring until smooth ... Then added to the hot solution 1.5 g of aloe juice and cooled the mass to a temperature close to the pour point. The prepared mass was poured into split suppository plastic molds for 5 suppositories, preliminarily lubricated with vaseline oil. Received a suppository composition: - 0.3 g - aloe tree juice - 3.43 g - gelatin-glycerin suppository base.

The content of the sum of anthracene derivatives in one suppository in terms of barbaloin 2.60 ± 0.02 mg (Table 2).

Test results in accordance with the General Pharmacopoeia Monograph "Suppositories" (Table 2).

1. Disintegration. The test was carried out using a pharma test - suppository disintegration tester. Purified water was poured into the tester and heated to 37 ° C, then 3 suppositories were placed and the device was turned on for 30 min for suppositories on a lipophilic basis (cocoa butter), and 60 min for suppositories on a hydrophilic basis (gelatin-glycerol) and the time for which all suppository samples should disintegrate.

Hydrophilic suppositories - 25 min.

Lipophilic suppositories - 10 min.

2. Melting temperature. Samples of suppositories were placed in a melting point apparatus, heated in a water bath with a thermometer, and the temperature at which the samples of suppositories began to melt was recorded. The melting point should not exceed 37 ° C. Melting point of a suppository on a hydrophilic basis - 37 ° С Melting temperature of a suppository on a lipophilic basis - 34 ° С.

3. Quantification was performed using spectrophotometry. The content of the sum of anthracene derivatives in terms of barbaloin in hydrophilic suppositories was 2.60 ± 0.02 mg.

The content of the sum of anthracene derivatives in terms of barbaloin in lipophilic suppositories was 2.36 ± 0.01 mg.

4. The degree of release of active substances.

The determination was carried out by direct diffusion in a 1.5% agar gel containing 10% KOH solution as an indicator. The molten suppository base is placed in the wells of agar plates. The cups are placed in a thermostat with a temperature of 37 ° C. The drug, released from the ointment, diffuses into the agar gel, interacting with the reagent and forming a colored zone. One day later, the diameter of the colored zone was measured using a ruler.

The diameter of the colored zone of the hydrophilic base is 5 mm.

The diameter of the stained zone of the lipophilic base is 3 mm.

The advantages of the developed method of manufacturing and the composition of suppositories with aloe tree juice are as follows:

- the content of juice from the leaves and shoots of aloe tree in the suppositories developed by us is 0.3 g, and in the prototype - 0.0017 g per suppository;

- a hydrophilic base, from which the active substances of aloe tree juice are easily absorbed, allows us to recommend the use of this dosage form as a laxative.

Thus, the proposed method and method for the manufacture of suppositories with aloe juice provides therapeutic benefits due to a higher concentration of active substances in comparison with the prototype and potentially expands the possibilities of application in pharmacy; The proposed suppository base provides a high release of the active substance, which is easily absorbed into the rectal wall and provides a laxative effect.

SOURCES OF INFORMATION

1. State Register of Medicines. - T.1. Official edition. M., 2008 .-- 1398 p.

2. Kurkin V.A. Pharmacognosy: A textbook for students of pharmaceutical universities. - Ed. 2nd, rev. and add. - Samara: OOO "Etching", GOU VPO "SamSMU", 2007. - 1239 p.

3. Kurkin V.A. Fundamentals of herbal medicine: A textbook for students of pharmaceutical universities. - Samara: OOO "Etching", GOU VPO "SamGMU Roszdrav", 2009. 963 p.

4. Muravyova D.A., Samylina I.A., Yakovlev G.P. Pharmacognosy: Textbook. - M .: Medicine, 2002 .-- 656 p.

5. Encyclopedia of medicines. Register of medicines of Russia [Text] / Ch. ed. G.L. Vyshkovsky. - M .: Publishing house of RLS-Media, 2010. - Issue. 18. - 1296 p.

Claims (1)

A method of obtaining suppositories with aloe tree juice, including the use of a gelatin-glycerin base, characterized in that the juice obtained after keeping the leaves and shoots of aloe tree in the refrigerator for two days, crushing, grinding, pressing and filtering raw materials, was introduced into the composition of the suppositories, for the manufacture of which a gelatin-glycerin base was used as a basis, consisting of medical gelatin - 1 tsp, glycerin - 5 tsp, water - 2 tsp, as a result of which suppositories of the following composition were obtained: 0.3 g of juice from the leaves and shoots of aloe tree ; 3.43 g of gelatin-glycerin suppository base.