IL34178A

IL34178A - Extracts from plants of the genus hypoxis and medicinal preparations containing them

Info

Publication number: IL34178A
Application number: IL34178A
Authority: IL
Original assignee: Liebenberg R W
Priority date: 1969-04-02
Filing date: 1970-03-26
Publication date: 1973-04-30
Also published as: IL34178A0; DE2015877B2; FR2042297B1; FR2042297A1; ZA701904B; DE2015877A1; DE2015877C3; GB1259503A

Description

34178/2 Extrac a from plants of the genus Hypoxia, and medicinal preparations containin them 34178/2 This invention relates to a medicinal product which, in clinical trials has exhibited remarkable antibiotic, antiinflammatory, hormonal, muscle reactivating and conditioning properties; it also alleviates certain arthritic conditions and conditions due to arteriosclerosis including cholesterosis; as well as having a diuretic effect. The product has found particular efficacy in the treatment of urogenital diseases due to pathological conditions of the prostate g¾.and, bladder and urinary tract* The product of the invention comprises an extract of the corms of plants of the genus Hypoxis (Family Hypoxidaceae) .

Species of this genus specially useful in the invention include Hypoxis nitida, Hypoxis rigida and Hypoxia rooperi, but it will be realised that other species of the genus Hypoxis will also be useful for obtaining the product of the invention.

The corms after suitable comminution (with or without previous . drying) are extracted with water, ethanol or aqueous ethanol. The extract may be used as such or it may be dried and taken u with water or other harmless diluent for use.

The aqueous or aqueous alcohol extract may be evaporated under suitable conditions such as flash-drying or spray draying. The dried, powdered material may be tabletted, encapsulated, brought into solution or otherwise made up into a pharmaceutical dosage unit. ' The extracts or infusion may be administered simply or with the addition of suitable sweetening or flavouring agents or the powder obtained after drying the extract may be tabletted, encapsulated or redissolved.

In clinical trials 738 patients suffering from benign, hypertrophy of the prostate gland were .divided into broad groups as follows: i ; Group 1» Patients where residual urine in the bladder measured 350 ml. to over 400 ml. I Group 21 Patients with urine retention of 250 ml. to 350 ml.

Group 31 Patients where residual urine in the bladder after natural passing of water measured up to 250 ml.

All patients were treated by orally administering 30 drops of extract three times per day. The extract was made by soaking 100 g of dried corms with 50 ml. of an aqueous 60% ethanol mixture to produce an extract containing approximately 6% solids.

Group 1 and group 2 patients were hospitalised and daily checks were made on: (a) Residual urine in the bladder after natural passing of water. (b) Bacterial count, in urine, (cj pH Value of urine. (d) Any sign of toxic effects on the liver..

Tolerance: In comparison with other medicaments used for similar purposes the tolerance of the extract was exceptionally good.

Side Effects: tLes8 than one percent of all 738 treated patients complained about 'slight stomach, irritation. No heart or circulatory disturbances were observed and no allergic or toxic symptons could be detected.

Results of Treatment: A. Subjective: All patients reported a subjective improvement. They claimed an increased ease and a lowered frequency of micturition.

B. Clinical Findings: The treatment seems to have a direct influence on: ' (i) the muscle of the bladder, in that collapsed , bladder muscles were reactivated, (ii) the enlarged prostate gland, in that it was reduced in size to form no noticeable obstruction to the natural passing of urine in most patients* ' (iii) the accompanying infection of the bladder, in that the infection disappeared.

C. Objective Results: (I) A direct evaluation of the therapeutic success of the treatment is to determine the residual amount of urine. After 3-6 weeks treatment it was found that - ' (i) of patients with an original urine retention of 100 ml. none was found to retain urine (100% improvement) ; (ii) of patients with an original urine retention of between 100^250 ml. 90% retained no urine > while 10% retained approximately 20 ml. (such small amounts are of no clinical significance) ; (iii) of patients with an original urine retention of between 250-500 ml. the residual urine returned to zero in 72% of cases; while 8% retained approximately 100 ml. and 20% retained such large amounts that an operation became necessary. (iv) of patients carrying a permanent catheter (Longer treatment was required in these cases) , the catheter could be removed and micturition was resumed.with 84% eventually retaining no urine, while the remainder continued treatment due to small residual amounts of urine.

(II) In 96% of all cases a reduction of the enlarged prostate gland could be evaluated by a rectal digital investigation and by determinating the coliculus distances.

(III) In 98% of all cases a definite improvement of all sediment was found. The accompanying infection had disappeared. Tests showed that of the original bacteria present, the coli-group vanished after 4-6 weeks treatment. In addition, the leucocyte concentration had diminished and the urine pH values decreased from 7.8 and higher to approximately 6.

(IV) It has been established that the treatment removes congestion formed 'in the upper urinary tract.

Three methods -of preparing the compositions of the invention are' described below: - 1. Dried chips of Hypoxia rooperi corms (4000g) are soaked with 60% aq. ethanol (201). The mixture is allowed to stand with , intermittent agitation in a cold room (8°) .until the liquid contains between 5-6% solids. This process requires about ' 14 days. The liquid is then separated from the solids. The extract so obtained is either used as such (see clinical trials with prostata hypertrophy patients) or it is spray dried to provide a powder which can be: (a) redissolved in a suitable pharmaceutically acceptable solvent, (b) encapsulated as such or mixed with suitable diluents and other substances, (c) incorporated into tablets and or. other pharmaceutically I useful preparations.

The Hypoxis extract content will- depend on the desired use or .application of the final' product.

NOTE: (i) In place of Hypoxis rooperi corms the corms of other Hypoxis species may be used, e.g. £· nitida H. rigidula, etc. (ii) The water content of the alcohol is not critical, but it was found that 50-60% aq. alcohol gives the best product. 2. Fresh, whole Hypoxis rooperi corms (3 kilo) are placed in a container in a pressure cooker containing water (1 L) . This is brought to boil at a pressure of 20 lbs. per sq. inch and boiling is continued for 30 minutes. The autoclaved corms are then pulped through a homogeniser with continuous addition of. a total of 6 litres of water. The resulting pulp" and water mixture is boiled for one hour after which it is strained and the so obtained extract is spray dried. The resulting. light brown powder (yield approximately 10% of the fresh corms used) is then used in the preparation of pharmaceutical products as described in 1. 3i Fresh Hypoxis rooperi corms (40 kilo) are pulped rapidly ' directly into boiling water (100 L) . The mixture is kept boiling for 1 hour before it is filtered. The filtered extract is spray dried to usually provide a 9-10% yield of a light brown water-soluble hygroscopic powder consisting essentially of carbohydrates (sucrose, glucose, fructose and polysaccharides)'.

Method 3 is the preferred extraction procedure.

Claims

341 78/$ CLAIMS J

1. An extract of the corms of plants of the genus Hypoxis (family Hypoxidaceae) , prepared by comminuting the corms of the plants and extracting, the comminuted mass with water or ethanol or a mixture thereof. ' i

2. The product obtained by drying the extract of claim 1,

3. A pharmaceutical composition including the extract of claim 1 or the product of claim 2 and a pharmaceutical carrier *